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1.2: Introduction to Pharmacology

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• Carl Rosow, David Standaert, & Gary Strichartz
• Massachusetts Institute of Technology via MIT OpenCourseWare

A drug is a chemical agent which can affect living processes. For purposes of this course we will mainly be talking about small molecules which affect cellular processes. Most of these are Xenobiotics (Gr. xenos - stranger) chemicals that are not synthesized by the body, but introduced into it from outside. There is inevitably a certain amount of ambiguity in this definition: Is oxygen or water a drug? How about Vitamin C in a glass of orange juice? How about an injection of Vitamin C to treat scurvy?

Pharmacology (Gr. pharmakon - a drug or poison, logos - word or discourse) is the science dealing with actions of drugs on the body ( pharmacodynamics ) and the fate of drugs in the body ( pharmacokinetics ). It overlaps with pharmacy , the science of preparation of drugs; much of it deals with therapeutics , the treatment of disease (by whatever means). Toxicology is the branch of pharmacology dealing with the "undesirable" effects of drugs on biological processes (in the case of a nerve gas the bad effect may be a desired one).

In order for a drug to work, it must enter the body and somehow be distributed in such a way that it gets to its site of action. In most cases the site of action is a macromolecular "receptor" located in the target tissue. Most drug effects are temporary, because the body has systems for drug detoxification and elimination. We will consider these issues broadly for now and go into more depth in individual lectures. As you read, refer to the figure below:

Overview of Pharmacokinetics - "What the body does to the drug"

• The drug may enter the body in a variety of ways: as an oral liquid, pill, or capsule; as an inhaled vapor or aerosol; absorbed through intact skin or a mucous membrane; injected into muscle, subcutaneous tissue, spinal fluid, or directly into the bloodstream. As we shall see, the physical properties of the drug and the specific way it is prepared greatly influence the speed of absorption.
• If the drug is given orally and swallowed, it must be absorbed from the GI tract into the portal circulation. If it is absorbed from the skin, mouth, lungs or muscle it will go directly into the systemic circulation. If drug is injected directly into the bloodstream (e.g., intravenous injection), 100% of it is available for distribution to tissues. This is not usually the case for other modes of administration. For example, drug which is absorbed via the portal circulation must first pass through the liver which is the primary site of drug metabolism (biotransformation). Some of the drug may therefore be metabolized before it ever reaches the systemic blood. In this case," first-pass " metabolism reduces the bioavailability to less than 100%.
• Once the drug is in the bloodstream a portion of it may exist as free drug, dissolved in plasma water. Some drug will be reversibly taken up by red cells and some will be reversibly bound to plasma proteins. For many drugs, the bound forms can account for 95-98% of the total. This is important because it is the free drug which traverses cell membranes and produces the effect. It is also important because protein-bound drug can act as a reservoir which releases drug slowly and thus prolongs its action.
• The unbound drug may then follow its concentration gradient and distribute into peripheral tissues. In some cases, the tissue contains the target site and in others the tissue is not affected by the drug. Sites of non-specific binding act as further reservoirs for the drug. This total volume of distribution determines the equilibrium concentration of drug after a specified dose.
• Tissue-bound drug eventually reenters the bloodstream where it perfuses the liver and kidneys. The liver metabolizes most drugs into inactive or less active compounds which are more readily excreted. These metabolites and some of the parent compound may be excreted in the bile and eventually may pass out of the body in the feces. Alternatively, some of the drug may be reabsorbed again, farther down the GI tract (the so-called enterohepatic cycle). Any biotransformed drug which is not excreted in bile passes back into the systemic circulation.
• Parent drug and metabolites in the bloodstream may then be excreted: most are filtered by the kidney, where a portion undergoes reabsorption, and the remainder is excreted in the urine. Some drugs are actively secreted into the renal tubule. Another route of excretion is the lung: Drugs like alcohol and the anesthetic gases are eliminated by this route. Smaller amounts of drug are eliminated in the sweat, tears and breast milk.
• Biotransformation may sometimes produce metabolites with a great deal of activity. Occasionally, we administer a parent drug which is inactive (a pro-drug) and only the metabolite has activity. [How might this be useful?]

Overview of Pharmacodynamics - "What the drug does to the body"

As stated above, the majority of drugs bind to specific receptors on the surface or interior of cells, but there are many other cellular components and non-specific sites which can serve as sites of drug action.

• Water can be a target. Osmotic diuretics like mannitol are not reabsorbed by the kidney, and the osmotic load they create in the renal tubule obligates the loss of water. Laxatives like magnesium sulfate work in the intestine by the same principle.
• Hydrogen ions can be targets. Ammonium chloride is sometimes used to acidify the urine. When it is taken orally, the liver metabolizes ammonium ion to urea, while the chloride is excreted in the urine. The loss of Cl- obligates the loss of H+ in the urine, thus the pH is lowered.
• Metal ions can be targets. Chelating agents like EDTA may be used to bind divalent cations like Pb++. Metal ions are most frequently drug targets in cases of poisoning.
• Enzymes are targets of many therapeutically useful drugs. Drugs may inhibit enzymes by competitive, non-competitive, or irreversible blockade at a substrate or cofactor binding site. Digitalis glycosides increase myocardial contractility by inhibiting the membrane enzyme, Na+-K+ - ATPase. Antimicrobial and antineoplastic drugs commonly work by inhibiting enzymes which are critical to the functioning of the cell. In order to be effective, these drugs must have at least someselective toxicity toward bacterial or tumor cells. This usually means that there is a unique metabolic pathway in these cells or some difference in enzyme selectivity for a common metabolic pathway. An example of this is the inhibition of folate synthesis by sulfonamides. These drugs are effective antibacterial agents because the bacteria depend upon folate synthesis, while the host doesn't. This example will be covered in detail in one of our case discussions.
• Nucleic acids are targets for antimetabolites and some antibiotics. In the case of 5- fluorouracil, the compound acts as a counterfeit substitute for uracil and becomes incorporated into a faulty mRNA. Antisense oligonucleotides are another very specific way to interfere with a restricted part of the genome.
• Some drugs, like general anesthetics, appear to act by non-specific binding to a macromolecular receptor target. These drugs are thought to alter the function of membrane proteins, in part, by disordering the structure of the surrounding lipid membranes. Their lack of specificity is reflected in very low chemical structural requirements. The general anesthetics include compounds as chemically diverse as nitrogen, xenon, halogenated ethers, and steroids. They exhibit very little stereoselectivity, that is, there are not marked differences in anesthetic activity between enantiomers.
• Finally, we have the drugs which act by binding to specific receptors . As you will see in lectures 2 and 6, these drugs have both high structural specificity and stereoselectivity, i.e. relatively small changes in chemical structure can radically alter the activity of these drugs.

Let us finish with some important definitions. These are concepts which we will return to repeatedly throughout the course.

• Agonist is a drug which binds to its "receptor" and produces its characteristic effect. A drug may be a full agonist or partial agonist , depending on the maximal effect it produces. An antagonist binds to the receptor without causing an effect, thereby preventing an active substance from gaining access. Antagonists, like enzyme inhibitors, may be competitive, non-competitive or irreversible.
• Dose-Response . The sine qua non of drug effect. Simply put, as the dose of drug increases, the response should increase. [What if the response increases, then decreases as the dose is raised?] The curve generated is usually sigmoidal when effect is plotted against log dose (Dr. Strichartz will discuss the theoretical basis for this). Effect may be measured as a graded variable (change in blood pressure, force of contraction) or as a quantal variable (number dead/alive). The slope of the curve is characteristic of the particular drug-receptor interaction. When two drugs act by the same receptor mechanism, we expect to see two parallel log-dose response curves.
• ED 50 . The median effective dose, or the dose which produces a response in 50% of subjects. If the response is death (lethality) we call it the LD 50 . The EC50 refers to concentration rather than dose. Similar abbreviations are used for other response levels: ED 99 , LD 1 , etc.
• Potency . A terribly misused word – the lay public uses it to mean “effectiveness.” The potency of a drug refers to the dose (actually the molar concentration) required to produce a specific intensity of effect. [We usually specify the ED50, why?] If the ED50of drug A and B are 5 and 10 mg, respectively, the Relative Potency of A is twice that of B. Relative potency specifically applies to the comparison of drugs which act by the same mechanism, and therefore have parallel dose-response curves.
• Efficacy . Also called Maximal Efficacy or Intrinsic Activity . This is the maximum effect of which the drug is capable. A potent drug may have a low efficacy, and a highly efficacious drug may have a low potency. For the clinician, efficacy is much more important than potency (within limits). Who cares if the pill contains 5 or 10 mg of drug?
• Affinity . This refers to the strength of binding between drug and receptor. It is quantified by the dissociation constant kD (covered in the next lecture).
• Selectivity . This refers to the separation between desired and undesired effects of a drug. In the ideal case, a drug is completely specific , and an effective dose does not elicit any undesired effect. Penicillin is an example of a highly selective drug, since it works specifically by inhibiting cell wall synthesis, and (other than allergic responses) it has very little effect on human cells at normal doses. Unfortunately, many therapeutic agents, like digoxin and theophylline, produce dose-related side effects near their therapeutic dose range. For some drugs like cancer chemotherapeutic agents, their selectivity is their dose-limiting property, i.e., they are given to kill tumor cells until they produce toxicity in normal cells as well.
• Therapeutic Window . For every drug, there exists some concentration which is just barely effective (the Effective Concentration ) and some dose which is just barely toxic (the Toxic Concentration ). Between them is the therapeutic window where most safe and effective treatment will occur.
• Therapeutic Index . This is the ratio of toxic to effective doses at the level of 50% response: TD 50 /ED 50 . In animal toxicology studies, it is usually the LD 50 /ED 50 . Another measure sometimes utilized is the Certain Safety Factor , which is TD 1 /ED 99.

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1. Introduction to Pharmacology

Pharmacology: the study of interaction of drugs with living systems.

Sub-Disciplines of Pharmacology

• Drug-Receptor Interactions
• Dose-Response Relationships
• Signal Transduction
• A bsorption
• D istribution
• M etabolism
• Rate of Drug Metabolism
• Drug-Induced Toxicity
• Drug-Induced Allergies

Pharmacology and the Pharmacist

Key Questions you should be asking as a Pharmacist :

• Where is the molecular site of action ?
• What are the body function changes caused by a drug (pharmacodynamics)?
• What is the relationship between the Dose vs. Effect ?
• How does a drug produce its effect ?
• What is the fate of the drug once it enters the body (pharmacokinetics)?
• What is the interplay between genetic makeup and drug response ?

Example: Beta 1 Blocker: Metoprolol Succinate (oral)

Drug Action: selective binding to cardiac muscle beta 1 adrenergic receptors that respond to norepinephrine (at higher doses, also inhibits bronchial and vascular smooth muscle by acting on beta 2 adrenergic receptors) to inhibit the binding of norepinephrine.

Drug Effect: reduced inotropic effect (contractility) and chronotropic effect (heart rate)

Fate of the Drug (pharmacokinetics): 12% protein binding and distribution 5.6 L/kg: hepatic metabolism (CYP2D6 mainly): <5% renal excretion: t 1/2 3-7 hours

Principles of Pharmacology - Study Guide Copyright © by Edited by Dr. Esam El-Fakahany and Becky Merkey, MEd is licensed under a Creative Commons Attribution-NonCommercial 4.0 International License , except where otherwise noted.

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1.1 Introduction

1.2 origins and antecedents, 1.3 the emergence of pharmacology as a science, 1.3.1 chemistry makes its entry, 1.3.2 pathology and physiology lay important foundations, 1.3.3 the receptor concept is established, 1.3.4 many chemical mediators are identified, 1.4 receptors and drug targets, 1.5 pharmacology in drug discovery, 1.6 pharmacology today, 1: what is pharmacology.

• Published: 25 Oct 2017
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H. Rang, in Pharmacology for Chemists: Drug Discovery in Context, ed. R. Hill, T. Kenakin, and T. Blackburn, The Royal Society of Chemistry, 2017, pp. 1-13.

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Pharmacology is the study of the action of drugs on living systems – neatly paraphrased as the chemical control of physiology and pathology. It lies at the interface of chemistry and biology. Drugs , in this context, are chemicals of known structure that are administered as external agents – whether deliberately or accidentally – to the organism, and produce an observable effect on its function. This chapter provides an introduction to pharmacology, describing a brief history of the discipline.

Pharmacology is the study of the action of drugs on living systems – neatly paraphrased as the chemical control of physiology and pathology. It lies at the interface of chemistry and biology. Drugs , in this context, are chemicals of known structure that are administered as external agents – whether deliberately or accidentally – to the organism, and produce an observable effect on its function. Living organisms are, of course, complex chemical machines, which produce and use many of their own chemicals as a means of controlling their own functions. Not surprisingly, exposure to other chemicals ( i.e. drugs) from the outside world is liable to confuse and subvert the internal signals, and that in essence is what pharmacology is all about. An understanding of pharmacology plays an essential role in the discovery and application of drugs as therapeutic agents, where the aim is to provide benefit to individuals by the alleviation of symptoms and disabilities, improved prognosis, prolongation of life, or disease prevention. A drug that does none of these things, even though it has been exquisitely engineered to interrupt what was thought to be a key step in the pathogenesis of the disorder, is of no use as therapy, though it may prove to be a valuable research tool.

Pharmacology comprises two main components, namely pharmacodynamics , which is concerned with the effects that drugs produce on living systems ( i.e. what the drug does to the body), and pharmacokinetics , which describes the mechanisms by which the drug is absorbed, distributed, metabolised and excreted ( i.e. what the body does to the drug). To explain fully the effects of a drug in an intact organism, both need to be understood.

Given the extreme chemical complexity of living organisms, and the delicately balanced regulatory mechanisms that have evolved over millions of years to allow organisms to survive environmental threats, it is not surprising that the intrusion of a foreign chemical is, in general, more likely to do harm than good. † The aim of drug discovery research is to find those few compounds that – against all odds – can deliver benefit to individuals affected by disease. Therapeutic benefit depends not only on choosing the right compound, but delivering it in the right dose, to the right patient, by the best route, at the right time and under the right circumstances. These important aspects are the concern of the subdiscipline of clinical pharmacology.

When developed as therapeutic agents, drugs are incorporated into medicines , which normally include other substances to enable them to be administered as pills, solutions for injection, skin patches, aerosols or other dosage forms ( Box 1.1 ).

Pharmacology. The study of the action of drugs on living systems. Clinical pharmacology is a branch of pharmacology concerned with the action of drugs used clinically to treat patients.

Drug. A substance of known chemical structure that produces a functional effect when added exogenously to a living system. Many endogenous chemical mediators that regulate normal physiological functions in higher animals can also be administered as drugs, but most drugs are synthetic chemicals or natural products not found in higher animals.

Medicine. A preparation containing one or more drugs, designed for therapeutic use. Medicines usually contain additional materials to improve their suitability for clinical use, for example as an injectable solution, a pill to be swallowed, or an ointment for topical application.

Therapeutic efficacy. The disease-related benefit to humans that a medicine produces. The benefit may be:

relief of symptoms or disabilities associated with disease;

improved prognosis, i.e. slowing or reversal of the progress of the disease;

prolongation of life;

prevention of disease.

The word “pharmakon” in ancient Greek, could mean a medicine or a poison; in the ancient world there was little distinction. Attempts to heal the sick by the use of “medicines” – largely herbal and mineral in origin, and based on spiritualist dogma rather than science – was in the hands of spiritual healers, and the tradition survives to the present day, carried on by “medicine men” and “witch doctors”, whose stock-in-trade is not only to heal the sick, but also to inflict harm on enemies. Compilations of such remedies go back thousands of years and it was the task of healers to produce them according to closely guarded recipes. Such traditional practices, based on dogma rather than science, remain popular to this day, despite the fact that evidence that they deliver benefit is generally weak or nonexistent. Prior to the 19th century, even though “medicines” based on traditional dogma had been catalogued and used for thousands of years, the understanding of drug action in terms of scientific principles – in other words, the emergence of pharmacology – was impossible. Chemistry had not yet advanced to the point of defining compounds in terms of their structure; physiology and pathology could not yet describe the functioning and malfunctioning of the body; traditional teaching emphasised the importance of esoteric procedures for concocting herbal preparations as a prerequisite for their clinical use. There were, however, a few earlier breaks with tradition – discoveries that found application in modern medicine. For example, Thomas Sydenham (1624–89) described in 1666 the use of opium (containing morphine) to control pain and “Jesuit's bark” (containing quinine) to control “intermittent fever” ( i.e. malaria); William Withering (1741–99) described the use of foxglove (digitalis) to treat “dropsy” (heart failure) in 1785. But until the nineteenth century these preparations were generally assumed to owe their properties to the vital forces possessed by “organic” substances. Chemistry did not come into it, nor did any understanding of biological mechanism.

Materia medica – the description of natural products and their medicinal uses, based on beliefs passed from generation to generation down the ages – began to be commercialised in the mid-17th century by the apothecary's trade, the forerunner of the modern pharmaceutical industry, its aim being to satisfy the demand for medicines containing ingredients that were difficult to obtain, and prepared in an approved manner. At the same time, the “Age of Enlightenment”, a gradual shift from dogma to science in the practice of medicine began to grow, when luminaries such as Robert Boyle (in chemistry) and William Harvey (in physiology) started to use evidence based on careful observation and experiment, as opposed to received wisdom, as a basis for understanding the natural world. The idea of living organisms as machines governed by the same physical laws as everything else in the material world, and of chemistry as the underlying basis of every substance and structure, slowly took root over the next two centuries, and dogmatic beliefs began to be challenged by discoveries based on empirical observations, many of which have stood the test of time.

Pharmacology as a distinct biomedical discipline began in 1847, when Buchheim (1820–1879) established the first university department with that name in Dorpat. His was a bold vision, for at that time the medicines in use were mainly plant extracts of unknown composition and a few, mostly poisonous, inorganic compounds, such as salts of mercury and arsenic. Complicated mixtures were recommended, prepared and administered in accordance with elaborate rituals. Vomiting, sweating, diarrhoea and fever commonly resulted, and were regarded as evidence of the treatment's effectiveness in ridding the body of harmful “toxins”. A famous quotation from an eminent contemporary physician, Oliver Wendell Holmes in 1860 dismissed them thus: “If all the materia medica, as currently used, could be thrown into the sea, it would be the better for mankind, and the worse for the fishes”. 1   It is certainly true that the “remedies” in use at that time were not based on any understanding of how they produced their effects, or of the underlying pathological dysfunction that needed to be corrected (beyond the “toxins” notion mentioned above), and the idea of testing their therapeutic efficacy rarely surfaced. Nevertheless, Buchheim saw that the challenge, then as now, was to understand better the mechanisms by which they produced their effects in order to put their medicinal uses on a rational, and hopefully effective, basis. Even though organic chemistry had hardly come into being, he had the vision to see that physiology, pathology and chemistry were all advancing rapidly in the very fertile scientific environment of the mid-nineteenth century, to a point where a new interdisciplinary science could emerge.

One of the essential foundations of pharmacology – the use of structural formulae to define chemical compounds – did not exist until the middle of the nineteenth century. A key figure was August Kekule, a German chemist who described both the tetravalent nature of carbon and the aromatic ring structure of benzene, two essential principles that allowed accurate structural formulae of organic molecules to be produced for the first time. The idea that the biological effects of plant extracts was likely to result from their chemical constituents rather than mysterious vital forces was implicit in the work of Buchheim and other pharmacological pioneers in the nineteenth century, but it was not until 1905 that a German pharmacist, Serturner, isolated crystals of morphine from opium poppies, tested it on himself and nearly died – the first irrefutable evidence that opium worked by chemistry, not by magic. Serturner's achievement was followed quickly by others who similarly extracted and purified chemical compounds from medicinal plants and showed them to possess distinctive pharmacological properties. Studying how such plant-derived substances as nicotine, atropine, curare, strychnine and ergot alkaloids, produce their effects, and relating them to the emerging knowledge of physiology and pathology, gave pharmacology the scientific foundations that it needed. But still, at this time, synthetic compounds, as opposed to natural products, played only a very minor part.

The other essential foundations of pharmacology, namely physiology and pathology, also flourished in the nineteenth century. Some key milestones are worth noting. The cell theory, proposed by the German pathologist Rudolf Virchow (1821–1902), identified the cell as the fundamental unit of all living organisms, and proposed that cellular dysfunction – cells dying, dividing, migrating, or otherwise functioning incorrectly – was the basic cause of disease. Louis Pasteur (1822–1896), a French chemist, proposed the germ theory of infection in 1878, having famously demonstrated the role of air-borne micro-organisms in fermentation. He showed that cholera could be transferred from chicken to chicken by inoculation with fresh, but not “stale” material. In fact, inoculation with stale material actually protected against future infection, so Pasteur inadvertently discovered the phenomenon of immunisation.

The first physiological studies aimed at pinning down the site of action of poisons were performed by Francois Magendie (1783–1855) in Paris, who showed that the convulsant action of strychnine was due to its action on the spinal cord, rather than elsewhere in the brain, nerves or muscles. His pupil, Claude Bernard (1813–1878) used a similar anatomical approach to pinpoint the paralysing effect of the arrow-poison curare to the junction between motor nerve and muscle fibre.

The realisation that drugs act very specifically at precise anatomical sites led in later years to the search for cellular components and actual molecules involved. A particularly important stage in the development of modern pharmacology was the emergence of the receptor concept, pharmacology's Big Idea (reviewed by Rang, 2006 2   ) of a “lock and key” mechanism by which drug molecules act on specific cellular molecules to produce their effects. This idea had been expressed, in a philosophical way, centuries earlier: “Did we but know the mechanical affections of the particles of rhubarb, hemlock, opium and a man……we should be able to tell beforehand that rhubarb will purge, hemlock kill and opium make a man sleep…….” 3     (John Locke, 1690, Essay concerning human understanding). These “mechanical affections”, which we would today call chemical interactions, are what pharmacology is all about. The Cambridge physiologist, J. N. Langley (1852–1925), first used the term “receptive substance” in 1878 to describe the hypothetical endogenous substance in salivary glands with which pilocarpine (which causes salivary secretion) and atropine (which blocks pilocarpine's action) combine and compete with each other for binding. A. V. Hill (1886–1977), a student in Langley's laboratory, applied the Law of Mass Action to describe quantitatively the interaction of drug and receptor molecules, and this quantitative approach was further developed by later pharmacologists. We now know that specific receptors exist in all cells and tissues, and are key players in the numerous chemical signalling pathways used by all living organisms to control their physiological functions. The subversion of these signalling pathways by introducing alien chemicals is the basis is modern pharmacology. Understanding pharmacology in this mechanistic way, underpinned now through the application of molecular biological approaches and by detailed knowledge of the structure and function of receptor molecules, has become crucial for the discovery of new therapeutic drugs.

Receptors form one important class of targets for therapeutic drugs. Enzymes, transporter molecules, ion channels, etc . are other types of target, described elsewhere in this book. Identifying such drug targets, and explaining how drugs are able to act on them to influence the function of the cells and tissues that express them, is a central theme in modern pharmacology, and an important starting point for drug discovery and therapeutic innovation.

The idea that internal secretions – chemical substances liberated into the bloodstream by organs such as the thyroid gland, testis and liver – play an important physiological role, emerged in the 17th century, and slowly gained ground over the next 200 years. The term “hormone” was coined in 1905 by Bayliss and Starling, who showed that the duodenum, in response to gastric acid production, produced a substance “secretin” that caused the pancreas to release digestive enzymes. Around the same time, many physiologists described the effects of removing individual glands – adrenal, thyroid, pituitary, pancreas, etc. – and of injecting various gland extracts, on different physiological functions, though chemical techniques for isolating and identifying the mediators involved were not yet available. The realisation that the release of chemical transmitters is the mechanism by which nerve cells communicate with each other, and with other cells and tissues came initially from work by Dale and Loewi, who identified acetylcholine as the transmitter released by parasympathetic nerve endings (winning the Nobel Prize in 1936), and the identification of other chemical mediators became – and remains – a major focus of pharmacology. Many large families of mediators are now recognised. These include:

low molecular weight amines, such as acetylcholine, noradrenaline, histamine, dopamine, 5-hydroxytryptamine;

peptides, such as insulin, oxytocin and angiotensin;

protein mediators, such as growth hormone, interferon and a wide variety of cytokines;

lipid mediators, such as prostaglandins and leukotrienes;

steroids, such as oestrogens and adrenocortical hormones;

amino acids, such as glutamate, glycine and γ-amino butyric acid (GABA);

purines, such as adenosine, ADP and ATP;

small molecules such as nitric oxide, carbon monoxide and hydrogen sulfide.

New members of each of these groups of mediators are still being discovered, particularly in the protein group, where modern techniques in molecular biology, cell biology and genomics have made a big impact in recent years.

From a pharmacological perspective, this profusion of mediators gives rise to many potential drug targets. Each mediator acts by binding to a specific recognition site located on a protein – the receptor – through which it produces its physiological effects. The four main types of receptor are:

G-protein coupled receptors (GPCRs);

ligand-gated ion channels;

kinase-linked receptors;

nuclear receptors.

Apart from nuclear receptors, most receptors are proteins that span cell membranes, accessible to mediators acting on the extracellular surface, and controlling events within the cell.

Most mediators act on more than one receptor, producing different effects on different cells. GPCRs are a particularly large and important type; approximately 350 GPCRs for endogenous mediators have been identified in the human genome, and roughly half the drugs in clinical use target GPCRs. Ligand-gated ion channels, activated by transmitters such as acetylcholine and glutamate, are important mainly in mediating fast synaptic neurotransmission. Kinase-linked receptors, located on the cell surface, respond to mediators such as growth factors, cytokines and insulin. Activation of the intracellular kinase moiety of the receptor protein initiates a cascade of protein phosphorylation reactions within the cell, culminating in the functional response. Nuclear receptors are intracellular proteins, responding to mediators such as steroids and thyroid hormones that are able to enter the cell; these receptors act by controlling gene expression in the nucleus.

Drug targets are the endogenous molecules (mostly proteins) to which drug molecules bind as the first step in producing their pharmacological effects. The various type of receptors for endogenous mediators, described above, constitute one important class of drug targets, but other types of functional protein, and also DNA, are also important.

The pathologist, Paul Ehrlich (1854–1915), was impressed by the ability of chemical dyes to stain biological specimens in a very specific way, and argued that this selective binding to particular cell types might be used as a basis for finding drugs that would bind to and kill pathogenic organisms. Arsenic, in various forms, had been used as a poison and a medicine for thousands of years, so Ehrlich, working with an organic chemist, embarked on the first systematic attempt at drug discovery by chemical synthesis. They made and tested hundreds of organic arsenic compounds, based on aniline dyes (the constituents of many of the biological stains that had engaged Ehrlich's attention) as possible treatments for trypanosomiasis (sleeping sickness, a common and serious infectious tropical disease). From this came, in 1907, Compound 606, named Salvarsan, the first effective drug for this disorder, and the beginning of the era of antimicrobial chemotherapy – arguably the biggest therapeutic success story to date.

Synthetic chemistry had given rise to clinically useful drugs before this, though by serendipity rather than design. Diethyl ether was discovered in the 16th century (known then as “sweet oil of vitriol” because it was made from alcohol and sulfuric acid) and gained notoriety in the 19th century as a party drug (“ether frolics”). Nitrous oxide (laughing gas) had similar origins, and the ability of both of these agents to produce reversible insensibility led in the mid-19th century to their introduction as surgical anaesthetic agents – a vital breakthrough that allowed surgery to develop from agonising butchery to humane intervention. It was in the late 18th century that chemistry began to take over from alchemy, and the production and purification novel compounds of known structure became possible. But understanding and determination of chemical structure, and synthetic methods were still very limited, and it was not until the end of the 19th century that synthetic chemistry really took off, and some of the products were discovered to have medical uses. Among the earliest drugs that came from this were the local anaesthetic, procaine (1905), and the sedative, barbital (1907), both forerunners of important classes of clinically used drugs.

Chemistry-led drug discovery grew rapidly in the 20th century, and quickly became the leading source of new therapeutic agents, and, as a byproduct, new research tools that proved valuable in the study of physiological and pathological processes. Intervening in metabolic pathways, by synthesising “antimetabolites” – analogues of endogenous metabolites – was an approach followed for many years by the highly successful drug discovery team led by Hitchings (1905–98) and Elion (1918–99), working at Burroughs Wellcome in the USA. Earlier, Domagk (1895–1964) in Germany had developed sulfonamides, the first effective antibacterial drugs, which were later shown to work by inhibiting the synthesis of folic acid, a metabolite essential for bacterial growth. Hitchings and Elion sought other inhibitors by making and testing a range of purine and pyrimidine analogues, which acted as inhibitors of the enzyme dihydrofolate reductase. Their antimetabolite approach, begun in 1944, generated not only antibacterial drugs, but also a range of other chemotherapeutic agents, active against protozoa and human cancers. The same sulfonamide-based chemical lineage later gave rise to novel diuretics (acetazolamide, chlorothiazide), antidiabetic drugs (sulfonylureas) and antihypertensive drugs (diazoxide) – an extraordinary example of chemical inventiveness leading to important new therapeutic drug classes. Domagk was awarded the Nobel Prize in 1939, Hitchings and Elion in 1988.

Analytical chemistry later also played an important role in providing tools for identifying the signalling molecules – hormones, neurotransmitters, inflammatory mediators, etc . – that play such a major role in physiological regulation, and whose dysfunction commonly leads to disease. Chemists became very successful at inventing new drugs by synthesising analogues and derivatives of known structures. An intuitive sense – hard to pin down – possessed by successful medicinal chemists, guiding them to the kind of structures likely to yield clinically useful drugs, was an important driver of these inventions. The compounds would be handed over to biologists for testing on animals, and anything that looked interesting could be further tested and developed as a medicine. This compound-led strategy sustained a successful drug industry for many years. Nevertheless, natural products continue to be a fruitful source of new useful drugs, most notably in the discovery of penicillin, relying on the inventiveness of evolution rather than of human chemists.

From the mid-20th century “target-led” drug discovery began to rival the compound-led approach. The coming together of chemistry, physiology and pathology under the banner of pharmacology drew attention to the importance of “drug targets”, namely the endogenous molecules – in most cases proteins – to which drugs bind in order to produce their effects. Such protein targets are of many kinds, including enzymes, receptors for endogenous mediators, transporter molecules, etc . and new ones are constantly being identified. James Black (1924–2010), a British pharmacologist working in industry, was a leader in this new target-led approach. Selecting the recently identified β-adrenoceptor as a promising target for treating cardiovascular disease, he and his team developed the first β-adrenoceptor antagonist, pronethalol, to be approved for clinical use (1965). Pronethalol was quickly withdrawn owing to adverse effects, to be followed by practolol (which had even more severe toxicity), and finally by propranolol (1973), which proved to be a valuable treatment for a range of cardiovascular and other disorders, and is still widely used. Black's team went on following this approach with another major success, the first H 2 -histamine receptor antagonist, cimetidine (1975) used to treat gastric and duodenal ulcers. For this work he won the Nobel Prize in 1988. The example set by these early target-led drug discovery projects was quickly followed by pharmaceutical companies worldwide, and became the main source of new therapeutic drugs up to the late 1990s – a particularly fruitful period for drug discovery. Target-led drug discovery began with no knowledge of the molecular nature of the targets in question, the chemistry being led mainly by knowledge of the chemical nature of the relevant physiological mediators. From the 1980s, when receptors and other drug targets began to be isolated as proteins, sequenced and cloned, these new molecular approaches gave a big boost to drug discovery, both by identifying and characterising the many subtypes of receptors, transporters, enzymes and other targets, and also by providing a range of much faster and more powerful methods by which chemical leads could be screened and tested. The subdiscipline of molecular pharmacology, which emerged at this time, grew rapidly in importance, and gained a powerful boost when the human genome sequence was published in 2003. The use of genomic techniques to identify and characterise human drug targets is now a necessary part of most drug discovery projects (covered in later chapters).

As we have seen, pharmacology arose through the convergence of medicine, chemistry, pathology and physiology, its purpose being to throw light on how medicines and poisons produce their effects. Biochemistry and molecular and cell biology joined the party as these newer disciplines emerged in the 20th century. One important spin-off from molecular biology was the emergence of biopharmaceuticals in the form of protein-based therapeutic agents, such as insulin, growth hormone and a variety of monoclonal antibodies, produced by genetically engineered bacteria or eukaryotic cells as an alternative to drugs made by synthetic chemistry. Biopharmaceuticals now constitute about one-third of newly approved therapeutic agents. Since the sequencing on the human genome in 2003 genomics has had a major impact on pharmacology and drug discovery, mainly by providing abundant new information about potential new disease-relevant human drug targets, and also paving the way for “personalised” therapeutics that aims to take into account an individual's genetic make-up as a guide to maximising the efficacy and reducing drug side effects. The multidisciplinary nature of pharmacology, present throughout its history, remains its abiding characteristic, and has grown in complexity as biomedical science has progressed. Pharmacology, you could say, is sustained by hybrid vigour, rather than intellectual purity.

As well as being a key driver of drug discovery and development, pharmacology figures in many other aspects of modern life. A few examples follow:

Drugs prescribed by clinicians are often ineffective in a significant proportion of patients, and commonly cause adverse effects. 4,5   Selecting the right drug, the right dose, and where possible in the right patient, which can significantly diminish these problems, is the domain of clinical pharmacologists. The emergence of genomics-based personalised medicine is a likely to provide powerful new tools for clinical pharmacologists.

Pharmacological knowledge is essential in the design and conduct of clinical trials of new medicines, which have to be conducted according to strict protocols governing standards of ethics, experimental design and statistical analysis in order to pass scrutiny by regulatory authorities as a condition of approval of the new drug for clinical use.

Widely consumed “social” drugs, including alcohol, nicotine and caffeine have been subjected to extensive pharmacological research, the results of which provide the basis for official advice regarding their possible health risks.

Drug abuse and addiction are serious problems in many countries, and present difficult challenges for prevention, remediation, legislation and policing; understanding the pharmacological properties of abused substances, including the mechanisms by which they produce psychological reward, as well as dependence and harm, is essential in planning rational control measures. The continuing emergence of new synthetic “street drugs” is a particular problem for pharmacologists and legislators.

Drugs in sport present problems of a different kind, mainly concerned with detection, where understanding of the routes of metabolism and excretion of banned compounds, coupled with sensitive analytical methods, is the basis of most of the control measures that are used.

We do not expect to correct a fault in, say, the navigation system of an aircraft by spraying a chemical into the works, so it may seem remarkable that physiological malfunction can sometimes be put right by a circulating drug. What makes it possible is that living systems, unlike electronic ones, deploy chemical signalling to control their function, providing points of attack for chemical interventions.

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Basic Introduction to Pharmacology

The term “pharmacology” is derived from two Greek words: pharmakon , the Greek word for drugs, and logos , the Greek word for science. It is a branch of science that deals with the study of substances that interact with living systems through chemical processes, especially by binding to regulatory molecules and activating or inhibiting normal body processes. These substances may be chemicals administered to achieve a beneficial therapeutic effect on some process within the patient or for their toxic effects on regulatory processes in parasites infecting the patient.

The history of pharmacology is as old as man himself. Early man undoubtedly recognized the medicinal or toxic effects of many plant and animal materials. Belief in the curative powers of these materials rested exclusively upon traditional knowledge, that is, empirical information not subjected to critical examination. These knowledge were passed down through generations. Whatever has been used from the earliest times in the form of superstition, primitive material medica , herbal, traditional, magic and witchcraft metamorphosed now into a highly organized science in its own right called pharmacology.

• 1 Branches of pharmacology
• 2 What are drugs?
• 3.1 a. Plant Sources
• 3.2 b. Microbial sources
• 3.3 c. Animal Sources
• 3.4 d. Marine sources
• 3.5 e. Mineral sources
• 3.6 f. Semi-synthetic Sources
• 3.7 g. Synthetic sources/chemical derivatives
• 3.8 h. Biosynthetic sources (genetically engineered drugs)
• 4.1 i. Chemical name
• 4.2 ii. Generic name
• 4.3 iii. Brand name
• 5 Routes of drug administration
• 6 Effects of drugs
• 7 References

Branches of pharmacology

Pharmacology has two major branches:

• Pharmacokinetics – This describes the activities or drug’s actions as it moves through the body. These activities include absorption, distribution, metabolism, and excretion of drugs. This branch of pharmacology is also concerned with a drug’s onset of action, peak concentration level, and duration of action.
• Pharmacodynamics – Pharmacodynamics deals with the study of molecular, biochemical, and physiological effects of drugs, including drug mechanism of action. In simplest terms, it can be described as what the drug does to the body.

Others branches of pharmacology include clinical pharmacology, neuropharmacology, psychopharmacology, pharmacotherapeutics, pharmacogenetics, pharmacogenomics, toxicology, chemotherapy, posology, pharmacoeconomics, pharmacoepidemiology, molecular pharmacology, immunopharmacology, pharmacometrics etc.

Read Also: Introduction to Pharmaceutical Microbiology

What are drugs?

The word “drug” is derived from the old French word “ drogue ” which means a “dry herb”.  It is defined as any substance or product which when administered to a living organism, influences biological functions. Drugs can also be defined as any substance that is used or intended to be used to modify or explore physiological systems or pathological states for the benefit of the recipient.

The terms “drug” and “medicine” are often mistakenly used by most people (practitioners and laymen alike) without any marked distinction. However, in the strictest sense, the two have different meanings, and they can serve different purposes.

Sources of drugs

The major sources of drugs can be grouped into the following

a. Plant Sources

Many plants have been used for centuries as drugs or drug sources. These include leaves, barks, fruits, roots, stem, wood, seeds, blossoms, bulb etc. Drugs from plants may either be used without further processing (crude drugs) or with technical processing (prepared drugs).

Some pharmacologically active principles or drugs derived from plant sources include digoxin and digitoxin (from Digitalis purpurea /foxglove plant), atropine (from Atropa belladonna ), quinine (from Cinchona ), tubocurarine (from Chondrodendron tomentosum ) etc.

b. Microbial sources

Several life-saving drugs have been derived from microorganisms. Examples include penicillin produced by Penicillium chrysogenum , streptomycin from Streptomyces griseus, chloramphenicol from Streptomyces venezuelae, neomycin from Streptomyces fradiae, bacitracin from Bacillus subtilis etc.

c. Animal Sources

Many important drugs are derived from animal source. In most instances, these medicinal substances are derived from the animal’s body secretions, fluid or glands. Animal sources include cod liver oil from Gadus spp ., insulin from bovine or porcine pancreas, hirudin obtained from the European medical leech ( Hirudo medicinalis ), heparin from Mexican medical leech ( Hirudo manillensis ) etc. Like plant products, drugs from animal sources may be crude (unrefined) or refined material.

d. Marine sources

Coral, sponges, fish, and marine microorganisms produce biologically potent chemicals used in the prevention, treatment or cure of many diseases. A good example of such chemicals is Curacin A, a potent cytotoxic agent from marine cyanobacterium Lyngbya majuscule .  Other examples include eleutherobin from coral Eleutherobia sp ., discodermolide from marine sponge Discodermia dissoluta , etc.

e. Mineral sources

Chemically pure forms of both metallic and non-metallic minerals are useful pharmacotherapeutic agents. For examples, ferrous sulfate used in iron deficiency anaemia, magnesium sulphate used as purgative; magnesium trisilicate, aluminium hydroxide and sodium bicarbonate used as antacids for hyperacidity and peptic ulcer etc.

Radioactive isotopes of iodine, phosphorus, gold are increasingly becoming important in medicine both for diagnosis and treatment of diseases particularly malignant conditions.

f. Semi-synthetic Sources

Semi-synthetic drugs are generally made by chemically modifying substances that are available from natural source to improve its potency, efficacy and/or reduce side effects.  In semi-synthetic drugs, the nucleus of drug obtained from natural source is kept intact but the chemical structure is altered.

Examples of semi-synthetic medicine include heroin from morphine, bromoscopolamine from scopolamine, ampicillin from penicillin etc.

g. Synthetic sources/chemical derivatives

Synthetic drugs are manufactured in pharmaceutical or chemical laboratories using chemical synthesis, which rearranges chemical derivatives to form a new compound. They may be either organic or inorganic or a combination of both.

At present, majority of drugs used in clinical practice are prepared synthetically. One of the earliest synthetic drugs was sulphonamide, which began with the synthesis of prontosil dye. Other examples include aspirin, acetaminophen, chloroquine etc.

h. Biosynthetic sources (genetically engineered drugs)

This is relatively a new field which is being developed by mixing discoveries from molecular biology, recombinant DNA technology, DNA alteration, gene splicing, immunology, and immune pharmacology. Examples include recombinant Hepatitis B vaccine, recombinant insulin and others.

Read More: Sources of Drugs

Drug Nomenclature

Throughout the process of development, drugs may have several names assigned to them. These names are the drug’s chemical name, generic name, and brand name.

i. Chemical name

This gives the exact chemical makeup of the drug and indicates the arrangement and position of atoms or atomic groups. A chemical name looks strange to anyone who is not a chemist and is difficult for most people to pronounce e.g., 1-Cyclopropyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid Hydrochloride.

ii. Generic name

This is the name with which the drug is described in official books of reference like pharmacopoeias e.g., ciprofloxacin.

iii. Brand name

This is the name given to a drug by its manufacturer. This name is often followed by the symbol ® which indicates that the name is registered to a specific manufacturer and no one else can use that name. Examples include Ciloxan ® , Cipro ® , Neofloxin ® etc.

Read More: Drug Nomenclature: How Does A Drug Get Its Name?

Routes of drug administration

Drugs can be administered through several routes, which are sometimes referred to as transitory passages. The major routes of administration include:

• Sublingual/ Buccal route
• Rectal route
• Topical route
• Transdermal route
• Inhalational route/ pulmonary route
• Injection route e.g., subcutaneous (SC) injection, intramuscular (IM) injection, intradermal (ID) injection, intravenous (IV) injection, intra-arterial (IA) injection, intrathecal (IT) injection, intraperitoneal (IP) injection, and intravitreal injection.

Read More on Routes of Drug Administration

Effects of drugs

Drugs have multiple effects on the body. The effect produced by drugs can be recognised only as a change in a function or process that maintain the existence of the living organism since all drugs act by causing changes in some known physiological functions and processes.

Some of these effects are desirable and some are not. The therapeutic effect is the intended physiological effect or the reason the drug is being given. This can be the drug’s action against a disease such as an antibiotic destroying or slowing down the growth of bacteria. Another physiological effect can be the side effects that occur in the body such as nausea and vomiting or a skin rash.

A side effect is a physiologic effect that is not the intended action such as the drowsiness that occurs when a patient takes first-generation antihistamine. Some side effects are beneficial while others are adverse effects that can be harmful to a patient.

Read Also: Why Do the Effects of Drugs Vary Between Different People?

• Aguwa, C. and Akah, P. (2006). How Drugs Act. In C. Aguwa and J. Ogbuokiri (Eds.), A Handbook of Pharmacology for Nursing and Allied Health Professions (pp. 2-7). Nigeria: Africana First Publishers Limited.
• Alamgir, A. (2017). Therapeutic Use of Medicinal Plants and Their Extracts: Volume 1. Switzerland: Springer International Publishing AG.
• Edmunds, M. (2016). Introduction to Clinical Pharmacology (8 th ed.). USA: Mosby.
• Galbraith, A., Bullock, S., Manias, E., Hunt, B. and Richards, A. (2013). Fundamentals of Pharmacology: An Applied Approach for Nursing and Health (2 nd ed.). USA: Routledge.
• Kamienski, M. and Keogh, J. (2006). Pharmacology Demystified . New York: McGraw-Hill Companies, Inc.
• Raj, G. and Raveendran, R. (2019). Introduction to Basics of Pharmacology and Toxicology Volume 1: General and Molecular Pharmacology: Principles of Drug Action. Singapore: Springer Nature Singapore Pte Ltd.
• Visovsky, C., Zambroski, C., Hosler, S. and Workman, L. (2019). Introduction to Clinical Pharmacology (9 th ). USA: Elsevier Inc.

Related keywords: pharmacology definitions, branches of pharmacology, basic pharmacology definitions, pharmacology drugs classification, classification of drugs, pharmacology drugs pdf, introduction to pharmacology, history of pharmacology, factors influencing drug response, why do drugs not have the same effect on all patients, Why do drugs affect people differently? introduction to pharmacology and sources of drugs, plant sources of drugs, sources of drugs in pharmacognosy slideshare, factors affecting drug action slideshare, factors affecting drug action wikipedia

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The receptor concept: pharmacology's big idea

1 Emeritus Professor of Pharmacology, University College London

Chemical signalling is the main mechanism by which biological function is controlled at all levels, from the single cell to the whole organism. Chemical recognition is the function of receptors, which, in addition to recognising endogenous chemical signals, are also the target of many important experimental and therapeutic drugs. Receptors, therefore, lie at the heart of pharmacology. This article describes the way in which the receptor concept originated early in the 20th century, and evolved through a highly innovative stage of quantitative theory based on chemical kinetics, to the point where receptors were first isolated and later cloned, until we now have a virtually complete catalogue of all the receptors present in the genome. Studies on signal transduction are revealing great complexity in the events linking ligand binding to the physiological or therapeutic response. Though some simple quantitative rules of ‘receptor theory' are still useful, the current emphasis is on unravelling the pathways that link receptors to responses, and it will be some time before we know enough about them to embark on the next phase of ‘receptor theory'.

Introduction

The receptor concept is to pharmacology as homeostasis is to physiology, or metabolism to biochemistry. They provide the basic framework, and are the ‘Big Ideas' without which it is impossible to understand what the subjects are about. Try to imagine a pharmacology course that made no mention of receptors.

Pharmacology as a scientific discipline was born in the mid-19th century, amid the great biomedical resurgence of that period (see also Cuthbert, this issue). The world's first pharmacology department was set up by Buchheim in 1847, in recognition of the need to understand how therapeutic drugs and poisons produced their effects. The inadequacy (or, more precisely, ‘inverse adequacy' to use today's receptor parlance) of therapeutic drugs at the time was summed up in Oliver Wendell Holmes' comment in 1860: “… if the whole materia medica as now used could be sunk to the bottom of the sea, it would be all the better for mankind – and the worse for the fishes”. The challenge for pharmacology was clear. It had, then as now, to apply scientific principles to make medicines more effective and less dangerous.

Pharmacology took up this challenge before anything was known about chemical structure, and when ‘drugs' were all either natural products of uncertain composition or inorganic substances such as mercury or arsenic salts. It was only after Kekulé discovered the structure of the benzene ring in 1865, and the now familiar 2-dimensional representations of the structure of organic molecules began to appear – the first in 1868 – and the chemical structures of natural products began to be defined, that the idea of specific ‘lock-and-key' relationships between drugs and their receptors could emerge from the shadows. It had actually been envisaged, in a philosophical way, centuries earlier. For example, John Locke in his Essay concerning human understanding (1690) wrote:

Did we but know the mechanical affections of the particles of rhubarb, hemlock, opium and a man…we should be able to tell beforehand that rhubarb will purge, hemlock kill and opium make a man sleep…

‘Mechanical affections' are, we can now see, what pharmacology is all about, though we might prefer to call them chemical interactions.

This article describes how the receptor concept evolved to become a central theme in the thinking of pharmacologists, and assesses its present status, finishing with some speculations on where the concept may lead in the future. Space precludes more than a superficial and selective overview, and readers wishing to go deeper may wish to consult reviews by Jenkinson (1996) , Colquhoun (1998) and Kenakin (1997) .

The idea takes shape

Credit for first suggesting (in 1878) the existence of a physiological substance or substances with which pilocarpine and atropine form ‘compounds' belongs to the Cambridge physiologist, J.N. Langley, based on his experiments on salivary secretion in the dog. In 1905, Langley used the term ‘receptive substance' (as distinct from the ‘contractile substance') to explain the actions of nicotine and curare on skeletal muscle. It fell to the mathematically-minded A.V. Hill, a student working in Langley's laboratory, to express the receptor idea quantitatively in terms of a bimolecular reaction following the law of mass action. Hill's paper, published in 1909, was remarkably prescient, anticipating by many years the emergence of ‘receptor theory' and its acceptance by pharmacologists. Hill's focus was on the time-course of the contraction of the frog rectus abdominis muscle produced by nicotine, but along the way he showed that the equilibrium concentration–effect curve (in one experiment!) fitted the equation

where y is the response height, N is the nicotine concentration, M is a threshold, and k and k′ are constants. Hill noted: “This is exactly of the form required … and is very strong evidence in favour of a combination between nicotine and some constituent of the muscle”. Apart from the gratuitous M , Hill's equation is, of course, the familiar equilibrium binding equation now known as the Hill–Langmuir equation. Langmuir was an eminent physical chemist, who derived the equation in 1918 as one possible description of the adsorption of gases as monolayers on metal surfaces. It was only recently that Hill was given the credit he deserved.

Hill lost interest in this area after this early student project, but became famous later for his work on haemoglobin and skeletal muscle biophysics. In these early days, of course, neither the British Pharmacological Society nor its journal existed, and these seminal pharmacological studies were published in the Journal of Physiology. In Germany or the United States, where the emancipation of pharmacology from physiology happened much earlier than it did in Britain, things might have been different.

It is interesting that Henry Dale, whose classical studies on the adrenaline reversal phenomenon, and on the muscarinic and nicotinic actions of acetylcholine, were conceptually very similar to those of Langley, was never inclined to explain his results in terms of receptors as we do now. He was, if anything, somewhat scornful of the idea, which he viewed as speculative and a cloak for ignorance, rather than as a useful theoretical framework for understanding drug action.

Paul Ehrlich, a contemporary of Langley working in Frankfurt, came to the idea of receptors from his interest in the immunology and chemotherapy of infectious diseases. His idea was that bacterial toxins combine with nutrient-capturing structures of cells (‘sidechains'), thus starving them. The cells respond by making more of these sidechains, some of which escape into the circulation as ‘antibodies' that combine with the toxin and make it harmless. He later suggested that the sidechains of bacteria differed from those of the host, and went on to study synthetic molecules, based on aniline dyes, that might act selectively on these bacterial sidechains, an endeavour that ended triumphantly with the discovery of Salvarsan in 1909, the first effective treatment for syphilis.

After these early beginnings, nothing much happened until 1926, when A.J. Clark and J.H. Gaddum – polymaths whose interests covered anything and everything pharmacological – published almost simultaneously key papers on the on the actions of acetylcholine and atropine on the frog's isolated heart ( Clark, 1926a , 1926b ), and the actions of adrenaline and ergotamine on the rabbit uterus ( Gaddum, 1926 ). Clark and Gaddum believed in measuring things and checking whether the data fitted quantitatively with predictions derived from particular physicochemical hypotheses. They were rarely satisfied with qualitative descriptions, and were the first to introduce the log concentration–effect curve, which has become an icon of pharmacology; they would have approved warmly of the current BPS logo. In the first of these two papers ( Clark, 1926a ) Clark followed Hill (though he does not say so) in making the bold step of relating the hyperbolic shape of the dose–response curve for acetylcholine to the equilibrium binding equation. Figure 1a shows a figure from his 1933 monograph, ‘The mode of action of drugs on cells', where he concludes cautiously: “The hypothesis that the concentration-action curve of acetylcholine expresses an adsorption process of the type described by Langmuir appears to involve fewer improbable assumptions than any alternative hypothesis” – of which, it should be added, he considered many.

A.J. Clark's early contributions to the receptor concept. (a) Concentration–effect curves for acetylcholine on (A) frog heart, (B) frog rectus abdominis muscle. Continuous curves fitted to the Hill–Langmuir equation (from Clark, 1926a , 1933 ). (b) Antagonism of acetylcholine by atropine on frog heart. Ordinate: % inhibition of contraction ( y ), plotted as log10[ y /(100− y )]. Abscissa: Acetylcholine concentration (log 10 M ). Successive lines (I–VII) represent atropine concentrations from zero to 10 −3   M (from Clark, 1926b ).

In the second of these two papers, Clark (1926b) made a quantitative study of the antagonism of acetylcholine by atropine ( Figure 1b ). Both Clark and Gaddum described the now-familiar ‘parallel shift' of the log concentration–effect curve produced by a competitive antagonist. Clark's data covered an enormous 10 5 -fold concentration range, rarely attempted by present-day pharmacologists. In retrospect, it is surprising that neither Hill nor Clark pursued the idea of competitive antagonism by deriving the very simple equations for the binding of two mutually exclusive compounds at the same population of sites. This was performed for the first time by Gaddum (1937) in a short communication to the Physiological Society. Clark was actually put off the idea of competitive antagonism for quite the wrong reason. He argued that recovery from atropine ought to be accelerated in the presence of acetylcholine if the two were acting at a common site, and found that it was not. So Clark concluded: “Atropine and acetylcholine, therefore, appear to be attached to different receptors in the heart cells, and their antagonism appears to be an antagonism of effects rather than of combination”. In fact, the simple competitive model does not predict the effect that Clark failed to see.

As a measure of antagonism, Clark estimated the ratio of the concentrations of acetylcholine and atropine needed to produce a given level of response. It was an early example of the use of a null method, which has proved such a valuable principle for pharmacologists. Clark's [agonist] : [antagonist] ratio was actually a hair's breadth away from the agonist dose ratio metric, devised by Schild (see below); it was, however, a purely empirical metric, and a blind alley in relation to competitive antagonism. Clark was a very active founder member of the British Pharmacological Society. He died suddenly in 1941 at the age of 56, 5 years before the Society's journal came into being.

Quantitative pharmacologists in these early days badly wanted to understand the relationship between the amount of drug taken up by tissues and the pharmacological effect produced. The approach taken by Clark and several of his contemporaries was to estimate uptake by using a very small volume of drug solution and either applying it consecutively to several assay preparations until its effect decreased because of uptake of the drug, or by comparing the effects of the same concentration applied in a large or a very small volume. This method, the forerunner of drug binding measurements, was imprecise at best, and could not distinguish between specific and nonspecific uptake, or allow for inactivation of the drug by the tissues. Nevertheless, Clark calculated by this method that the amount of acetylcholine taken up by the frog heart in producing a 50% maximal effect was about 6 pmol/mg tissue, sufficient to cover <1% of the membrane area. He realised that this was almost certainly an overestimate of the number of receptors, and later measurements showed that it was actually about 1000 times too high.

So, though the ideas were in place by the early 1930s, it needed two more breakthroughs before the receptor concept could take hold as a major theme in pharmacology. One was the analysis of competitive antagonism, which led directly to one of the key problems with which we still struggle, namely why some drugs are agonists and others antagonists. The second breakthrough was the direct measurement of drug binding, which led on to the isolation and cloning of receptors, revealing the biochemical reality of what had hitherto been an entirely abstract concept.

The theory evolves

As we have seen, neither Hill nor Clark, having clearly established the physico-chemical basis for analysing drug–receptor interactions, took the theory one simple stage further to explain drug antagonism in terms of competition between agonist and antagonist molecules for the same receptors, though both had thought about this possibility. Gaddum (1937) derived for the first time the equation describing the binding of two drugs at the same receptor. This idea was further developed in an important paper by Schild (1947) published appropriately in a very early volume of the BJP. In this paper, Schild introduced the use of the ‘dose ratio' – the factor by which the agonist concentration must be increased in order to produce the same level of equilibrium occupancy as the concentration of antagonist is increased – a null method ostensibly very similar to the empirical [agonist] : [antagonist] ratios that Clark and others had used, but much more informative – and described the now-familiar Schild Plot of log(dose ratio –1) versus log [antagonist]. If the simple theory of competitive binding is obeyed, the dose ratio should increase linearly as a function of the antagonist concentration, and the slope of this line provided a measure, for the first time, of the affinity of a drug (the antagonist, not the agonist) for its receptors, a method that has been used countless times since. The dose ratio metric was important for two reasons. In the case of competitive antagonism, the dose ratio does not vary with the level of response at which it is measured; in other words, the log concentration–effect curve for the agonist has the same slope and maximum when the antagonist is present, merely being shifted in a parallel manner to the right along the log [agonist] axis. So the familiar ‘parallel shift' picture came to be seen as the defining feature of a competitive antagonist. Secondly, measurement of dose ratios (unlike the metric that Clark had used earlier) allows the affinity of the antagonist for the receptors to be estimated, usually expressed as an equilibrium dissociation constant, K D . The use of antagonist K D values measured in this way has played a key role in receptor classification and drug discovery.

If, as these quantitative studies clearly implied, agonists and antagonists bind to the same site, the question clearly arises: Why do agonists produce a response but antagonists do not? – a question that has exercised pharmacologists from that day to this. In the mid-1950s, the existence of partial agonists was described, both by Ariens and his colleagues in Nijmegen, and by Stephenson in Edinburgh ( Figure 2 ). Stephenson's analysis led him to the concept of efficacy , a characteristic of the drug that describes its ability to activate receptors, distinguishable from its affinity for the receptors. Critical to Stephenson's thinking was the idea that a maximal tissue response (i.e. of smooth muscle contracting in an organ bath) did not necessarily correspond to 100% receptor occupancy, but (with an agonist of high efficacy), could occur when only a small proportion of the receptors was occupied. From this evolved the concept of ‘spare receptors', and the abandonment of Clark's idea that agonist concentration–effect curves represent receptor saturation curves. Furchgott's studies with haloalkylamine antagonists, which bind irreversibly (and therefore ‘noncompetitively') to α -adrenoceptors, confirmed the existence of spare receptors by showing that progressive inactivation of the receptors caused agonist log concentration–effect curves to shift to the right before the slope or maximum was reduced. Stephenson's idea, that binding and activation are independent processes, reflecting affinity and efficacy, made an immediate impact, and it came to be accepted that, to understand structure-activity relationships of agonists, both parameters had to be measured, since a change in agonist potency could reflect a change in either or both. In fact (as Colquhoun, 1998 explains clearly) Stephenson had failed to appreciate that, for an agonist, binding – in the sense of receptor occupancy – and activation are inextricably linked, and that ‘agonist affinity' measured in the way that he proposed (or for that matter by Furchgott's method based on irreversible antagonists) depends on the characteristics of both the initial binding reaction and the resulting activation.

Concentration–effect curves for a series of alkyl trimethylammonium compounds on guinea-pig ileum (from Stephenson, 1956 ).

Though Stephenson's suggestion that affinity and efficacy are separable properties is misleading (unless, it should be pointed out, ‘affinity' is defined in relation to the initial binding reaction only. Affinity as measured by Stephenon's or Furchgott's methods, or by binding studies, does not distinguish between the initial binding step and subsequent ‘activation' steps), his recognition that response does not directly reflect occupancy, and that with agonists of high efficacy maximal tissue responses occur at low levels of occupancy, were very important. It could be said that he made partial agonists respectable.

What is efficacy?

Stephenson's definition of efficacy was strictly operational, and he avoided any mechanistic speculation. Significantly, his 1956 paper includes no hypothetical reaction scheme. In principle, there are two ways of thinking about efficacy ( Figure 3 ), namely graded activation ( Figure 3a ) and the two-state model ( Figure 3b ). Graded activation implies that agonists (A 1 , A 2 , A 3 , etc) can induce different degrees of conformational change in the receptor, and thus different levels of response. The two-state model suggests that the receptor can switch between a resting state (R) and an activated state (R * ). In the original formulation by del Castillo & Katz (1957) based on their studies of the action of acetylcholine at the motor endplate, this transition was assumed to occur only when acetylcholine was bound, with the corollary that acetylcholine was unable to dissociate from the active (R * ) conformation. Realisation that this was an arbitrary and unnecessary assumption led to the fully reversible representation of the two-state model ( Figure 3c ), which accounts neatly and plausibly for variations in efficacy between different agonists. The model suggests that, even in the absence of any ligand, there is a conformational equilibrium between R and R * . An agonist is a ligand with a preferential affinity for R * over R, which means that the ratio AR * /AR will be greater than the ratio R * /R. The greater the selectivity of the ligand for the R * conformation, the greater will be its efficacy. A ligand that binds equally well to both conformations will occupy the receptors without shifting the conformational equilibrium, and so will act as a competitive antagonist. Under conditions where the conformational equilibrium of the unliganded receptor lies strongly in favour of R (i.e. there is very little ‘constitutive activation') the model is perfectly compatible with the earlier formulations of Schild and Stephenson, and notwithstanding the many discoveries about receptor function that have emerged since, it continues to provide a very useful basis for interpreting agonist and antagonist effects. Moving on from Stephenson's ‘black-box' concept of efficacy to the idea that it simply reflects selective binding affinity for the pre-existing resting and active states was a major advance. Coming as it did, at the same time that binding studies were developed as a viable technique for studying drug-receptor interactions (see below), it seemed that it might be possible to measure directly the binding parameters that determined agonist efficacy – misguided optimism as it turned out, for reasons that are discussed below.

Hypothetical models of receptor activation by agonists (see text). (a) Graded activation model, (b) Simple 2-state model, (c) Reversible 2-state model, (d) Ternary complex model. The ternary complex model (d) includes complex formation between the receptor (R) and a G-protein (G).

The two-state model originated from observations on ligand-gated ion channels (see also Colquhoun, this issue). Early observations on the action of cholinergic agonists on the motor endplate ( Jenkinson, 1960 ) and the eel electroplax ( Changeux & Podleski, 1968 ) and of GABA on crayfish muscle ( Takeuchi & Takeuchi, 1969 ) showed the phenomenon of ‘cooperativity' (i.e. at low response levels the increase in membrane conductance varied, not linearly as predicted by the Hill–Langmuir equation, but roughly as the square of the agonist concentration). In this respect, agonist effects were similar to many enzyme–substrate interactions, and to the binding of oxygen by haemoglobin, phenomena that had been interpreted in terms of a concerted transition of the subunits of oligomeric proteins between two distinct conformational states ( Monod et al ., 1965 ). Ligand-gated ion channels seemed to behave in a very similar way, and most of the pharmacological data relating to agonist and antagonist effects could be explained on the basis of the two-state model ( Colquhoun, 1973 ).

Not surprisingly, the simple two-state model could not explain everything about receptor function, and as more phenomena and mechanisms were discovered further elaboration of the model was needed. One of these phenomena was that of the rapid receptor desensitisation commonly seen with ligand-gated ion channels, first analysed by Katz & Thesleff (1957) . It was suggested that receptor desensitisation involved at least one (and possibly more than one) ‘desensitised' state in addition to resting and activated states, an idea supported by studies with nicotinic receptor antagonists that bind selectively to receptors in this (R′) state ( Rang & Ritter, 1970 ). It is now known that several different mechanisms, operating on different time scales, contribute to desensitisation at ligand-gated ion channels and G protein-coupled receptors (GPCRs), so the ‘desensitised state' model as originally conceived is a considerable oversimplification. With GPCRs, the discovery that coupling of the activated receptor with G-protein is the first step of the signal transduction pathway (see also Milligan & Kostenis, this issue) gave rise to a further elaboration of the two-state model, known as the ‘ternary complex' model ( Figure 3d ), involving the G-protein as well as the ligand and the receptor in its resting and active states. Weiss et al . (1996 ) published a detailed analysis of the properties of this model, and De Lean et al . (1980) showed that it accounted well for the ligand binding to the β -adrenoceptor.

An important new finding, originally from a study of opioid receptor function ( Costa & Herz, 1989 ) was that receptors may be constitutively active. This property, subsequently observed for many GPCRs, is easily explained in terms of the two-state model if it is supposed that the equilibrium distribution of R and R * is not heavily biased in favour of R. It also led naturally to the concept of inverse agonism, since a ligand that binds selectively to R will reduce the population of R * , whereas a conventional agonist, favouring R * , has the opposite effect.

Getting to grips with receptors as molecules

The striking success of simple quantitative models based on the Hill–Langmuir equation in explaining the actions of agonists and competitive antagonists spurred several attempts in the 1960s to measure drug binding directly, in an effort to understand what kind of molecules these mysterious ‘receptors' really were. By analogy with enzymes, it was generally assumed that they must be proteins, or some kind of protein–lipid complex, but there was no evidence for this. Several unsuccessful attempts by biochemists to isolate acetylcholine receptors from electric tissue were reported in the late 1950s, but the first clear evidence that drug binding to receptors could be directly measured came from the beautiful autoradiographic studies of [ 14 C]-calabash curare binding to the endplate region of mouse diaphragm ( Figure 4a , Waser, 1960 ). These experiments required months of exposure of the autoradiographic film, and quantitative measurements were very uncertain, but they clearly showed the localised binding of curare to the endplate region of the diaphragm, which disappeared and became diffuse following denervation of the muscle, and was prevented by addition of curare-like drugs, but not cholinesterase inhibitors, to the bathing medium.

Early studies of receptor binding. (a) Autoradiographic image of [ 14 -C] calabash curarine to endplate regions of mouse diaphragm (from Waser, 1960 ). (b) [ 3 H]-Atropine binding to longitudinal muscle of guinea-pig ileum. Analysis of the full binding curve revealed two saturable binding sites, plus a linear component. Binding site 1 represents binding to muscarinic ACh receptors (from Paton & Rang, 1965 ).

Around this time, liquid scintillation counters became available, as well as tritium labelling of compounds by catalytic exchange methods, making it possible to carry out quantitative drug binding experiments. Possible, but not easy, since the specific activity and radiochemical purity of these tritiated compounds was low, and scintillation counters primitive and subject to many artefacts. Curve-fitting had to be performed, not at the touch of a button, but by programming a mainframe computer half a mile down the road, inputting data laboriously with punched paper tape, and waiting days in a queue for scarce computer time. Nevertheless, the first studies on atropine uptake by guinea-pig ileum smooth muscle ( Paton & Rang, 1965 ) showed clearly the existence of saturable binding with the characteristics of muscarinic receptors ( Figure 4b ), heralding the ‘grind-and-bind' era of the 1970s and 1980s. It took a full year to make the binding measurements, carry out the necessary controls and estimate the binding parameters – a task now routinely performed by a technician in less than a day. We followed-up the atropine binding experiments by preparing and labelling an irreversible atropine-like compound, benzilylcholine mustard ( Gill & Rang, 1966 ), and tried unsuccessfully to use this to purify the solubilised receptor protein, an endeavour later achieved by Birdsall and others ( Birdsall & Hulme, 1976 ). Around this time also, nicotinic acetylcholine receptors were first successfully labelled with α -bungarotoxin ( Miledi et al ., 1971 ), and β -adrenoceptors with alprenolol ( Alexander et al ., 1975 ), leading to the purification, sequencing and cloning of all these receptors and several others. Consequently, during the 1980s and 1990s, receptor cloning became a major preoccupation of molecular pharmacologists until by the end of the century the task was virtually complete and pharmacology had entered a new era.

It is often mistakenly believed that binding studies, by measuring directly the level of receptor occupancy as a function of drug concentration, provides an estimate of affinity that is independent of efficacy. However, it is easy to show, on the basis of the two-state model shown in Figure 3c that although the overall level of occupancy is hyperbolic in form as expected, the apparent K D calculated from the binding curve does not represent the drug's affinity for either R or R * , but lies somewhere in between; in other words, the calculated K D value is a function of both affinity and efficacy. Irrespective of the particular model used, it is, in principle, not possible to use equilibrium binding measurements to separate the two without methods (not yet invented) for distinguishing between molecules that are bound to the different receptor conformations.

The advent of receptor cloning had a major impact on pharmacology, and many of the articles in this volume describe advances in molecular and cellular pharmacology that have followed in its wake.

The status of ‘receptor theory'

We have moved on a long way from the early days when receptors were theoretical entities invoked to allow drug effects to be explained in simple quantitative terms by applying the principles of chemical kinetics.

The basic ideas, as formulated by Hill, Gaddum, Schild, Stephenson and elaborated by Black, Leff and Kenakin (see below) form the basis of what came to be known by pharmacologists as ‘receptor theory'. However, as detailed information is gained about the molecular events that result from the binding of a ligand to its receptor, ‘receptor theory' is becoming increasingly inadequate as an overall framework for interpreting and analysing drug effects. At one level, it is self-evident that the laws of chemical kinetics must apply at every stage of the chain of events, but this can be said of anything that happens in the physical universe. Is there anything about drug-receptor interactions that distinguishes them, as a class, from other kinds of biochemical goings-on, that might justify the use of the specific term ‘receptor theory'? Not obviously. This author, for one, would be happy to see the phrase pass into oblivion. Nevertheless, receptor theory undoubtedly provided the foundation on which the study of receptor function at the biochemical and molecular level was based, so its importance in the early stages cannot be doubted. Moreover, Schild's approach to receptor classification, based on pA 2 measurements, provided the basis for some major therapeutic discoveries, most famously Black's discovery of β -blockers and H 2 receptor antagonists (see also Parsons & Ganellin, this issue). Many other GPCR-based therapeutic drugs have subsequently been developed by following much the same approach, so the usefulness of this type of quantitative analysis in drug discovery is also beyond question.

Recognition of the complexity of the molecular and physiological events that intervene between the initial step of receptor activation and the response that is measured led Black & Leff (1983) to develop an ‘operational model' for agonist action. Following Clark and others, they assumed that receptor activation as a function of agonist concentration followed a hyperbolic saturation curve. Since, empirically, concentration–effect curves are also usually hyperbolic, it followed that all the intermediate steps could also be described by a hyperbolic saturation curve, defined by a system-specific equilibrium constant K E .

The assumptions and limitations of the operational model are clear. Being independent of the actual molecular events involved in agonist action, it throws no light on mechanism, nor does it resolve the problem, referred to earlier, that affinity and efficacy are inextricably linked. Nevertheless, it has undoubtedly proved useful as a basis for describing agonist action in quantitative terms, though to the current generation of molecular pharmacologists concerned to unravel the intricacies of signal transduction pathways, the operational model has little relevance.

So far, nearly all of the quantitative theoretical modelling of receptor function has centred on ligand-gated ion channels and GPCRs. In the case of ion channels, the use of single channel recording has been important as a method for observing the behaviour of single receptor molecules in real time at a high level of temporal resolution. As Colquhoun describes in this issue, fitting kinetic data to theoretical models can allow mechanistic conclusions to be drawn with some confidence. It gives access to the intramolecular events that cause a channel to open when an agonist binds, but of course neglects the manifold functional effects that result. With GPCRs, techniques for observing receptor function directly are less well developed, though the use of fluorescence techniques to investigate agonist-induced conformational changes may have considerable potential (see Gether & Kobilka, 1998 ; Gether, 2000 ). In most cases, researchers have to infer what they can from measurements of binding, and a variety of downstream functional changes, such as GDP/GTP exchange, alterations in enzyme activity, protein phosphorylation, levels of intracellular second messengers, membrane currents, changes in gene expression, etc, Such studies have resulted in many useful flow charts representing postulated pathways and interactions, but assigning values to the various rate and equilibrium constants to allow quantitative modelling is rarely possible. The same limitation applies, in general, to studies of nuclear receptors and receptor protein kinases.

Future prospects

In recent years, the study of receptor function has taken full advantage of the molecular biology revolution, and many discoveries are being made that challenge the simple quantitative analyses introduced by pioneers such as Hill, Stephenson, Schild and others (which, it should be emphasised, were crucial in laying the foundations of the receptor concept in pharmacology).

Some recent discoveries, particularly in the GPCR field, pose a real challenge to those seeking to construct more elaborate general theories of receptor function.

• Different agonists acting on the same GPCR activate different signal transduction pathways, a phenomenon sometimes described as ‘protean agonism' ( Kenakin, 2001 ; 2002 ), implying that different activated states are favoured by different agonists (see Perez & Karnik, 2005 ). The model begins to look more like the graded activation model ( Figure 3a ). With ligand-gated ion channels, the situation seems to be simpler, as there are few if any examples where different ligands acting on the same receptor open channels with different conductance or selectivity characteristics. Nuclear receptors are also activated differently by different ligands (see Nettles & Greene, 2005 ).
• Many GPCRs exist as dimers, sometimes forming heterodimers with other GPCRs (see Angers et al ., 2002 ). They also associate with accessory proteins, such as RAMPs which alter their pharmacological properties ( McLatchie et al ., 1998 ; see also Brain & Cox, this issue). We do not yet know whether, to what extent, or how quickly, such associations are affected by ligand binding. There are parallels with many receptor tyrosine kinases, where dimerisation occurs in response to agonist binding, and is the first step in the signal transduction pathway.
• Receptors often occur in clusters on the cell membrane (‘lipid rafts', Ostrom & Insel, 2004 ), along with other molecules involved in signal transduction, forming isolated microdomains within the cell that are only detectable by methods providing a high level of spatial resolution.
• Constitutive activity and the existence of inverse agonists calls into question the original view of receptors as ‘silent' molecules that produce effects only when activated by an agonist. Rather they may serve a controlling function, which can be turned up or down by combination with different ligands, and what we choose to call ‘up' and ‘down' is quite arbitrary. Adding to the complexity, the concept of protean agonism suggests that a given ligand could turn some functions ‘up', others ‘down' and leave others unaffected, while another ligand, acting on the same receptor, could produce a quite different profile of effects.
• There are, particularly among GPCRs and nuclear receptors, large numbers of ‘orphan receptors' whose endogenous ligands, if they exist at all, are not yet known.

In general, the reductionist focus made possible in recent years by applying the principles of molecular and cell biology to pharmacological problems is undoubtedly providing major new insights into how drug molecules interact with receptors. The Holy Grail, which may well come into view in the foreseeable future, will be reached when we can depict, at high resolution, exactly what happens when a ligand binds to its receptor, explain why this event leads on to, for example, channel opening or G-protein binding, and (most importantly) design ligands de novo which will act as agonists, antagonists or other sorts of modulator. This certainly won't be the end of pharmacology, for between the ‘molecular' response to a ligand, and its effect on the functioning of the cell, tissue, system or whole animal lie mechanisms of far greater complexity. Pharmacology, committed as it always has been to the improvement of therapeutic drugs, has to concern itself with drug effects on the functioning of sick human beings, receptor mechanisms being just the first step.

In future the receptor concept may come to be seen, not just as the Big Idea of pharmacology, but as one of the Big Ideas of biology in general. Living organisms are chemical machines, and rely on chemical signalling within and between cells, at long or short range, through the agency of ligands and receptors. Understanding the processes involved in these signalling pathways is therefore crucial to understanding biology. Pharmacologists can take pride in having started the ball rolling.

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Therapeutic Applications of Honey and its Phytochemicals pp 219–247 Cite as

Honey and Its Molecular Pharmacology: An Essay

• Summya Rashid 3 ,
• Andleeb Khan 4 ,
• Aimen Firdous 5 ,
• Yusra Al Dhaheri 6 ,
• Adil Farooq Wali 7 &
• Rehan Khan 8  
• First Online: 15 December 2020

352 Accesses

Honey is a sugary, viscous fluid being used nearly 5500 years ago, since prehistoric times. In Sumerian tablet, the first inscribed evidence of honey was found in 2100–2000 B.C. Most olden civilizations like Greeks, Chinese, Egyptians, Romans, Mayans, and Babylonians, used honey mutually aimed at nutrition as well as for medicinal purposes. It exhibits numerous health- benefits which include anti-oxidant, anti-inflammatory, anti-bacterial, anti-diabetic, and protective effects in respiration, gastrointestinal system, cardiovascular, and nervous system. Based on origin, or its way of harvest and processing, honey can be categorized as blossom honey, honeydew or forest honey, monofloral, multifloral honey, raw honey, granulated honey, strained honey, ultra-filtered honey, ultrasonicated honey, chunk honey, comb honey, dried honey, whipped or creamed honey. The methods of extraction, processing, packaging, and preservation of honey alter the physical appearance of honey. Nevertheless, some elementary properties allied with honey contribute to it, regardless of the protocols used in the formation like content of H 2 O, matter configuration, and retention of water. Other physical structures and features of honey include taste, odor, color, heat, and crystallization. Depending on honey’s source, oldness, and storage/packing conditions, liquid honey may be either clear or no color, yellow, amber to dark amber, or black in color. Honey consists of pollen grains, water, waxes, vitamins, sugars, essential minerals, amino acids, proteins, enzymes, pigments, and pollen grains, and numerous phytochemicals with other 180 types of diverse complexes. Chemically, it consists of enzymes, organic acids, and phenolic acids with gluconic acid being the most abundant organic acid. Phenolic acids include non-flavonoids and flavonoids like isoflavones, flavones, anthocyanidins, flavanones, flavonols, chalcones, and enzymes include glucose oxidase, saccharase, catalase, and diastase and others, respectively. The effect of different constituents of honey obtained have been found to inhibit inflammation, oxidative stress, proliferation, metastasis, angiogenesis, and induce apoptosis. Also, honey has been found to regulate diabetes, cardiovascular and neuropharmacological diseases. However, more mechanism- based research needs to be done to promote the consumption of this healthy food in the general population, to promote a healthy lifestyle, and to regulate normal processes of life.

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Rashid, S., Khan, A., Firdous, A., Al Dhaheri, Y., Wali, A.F., Khan, R. (2020). Honey and Its Molecular Pharmacology: An Essay. In: Rehman, M.U., Majid, S. (eds) Therapeutic Applications of Honey and its Phytochemicals . Springer, Singapore. https://doi.org/10.1007/978-981-15-7305-7_10

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How to Structure an Essay | Tips & Templates

Published on September 18, 2020 by Jack Caulfield . Revised on July 23, 2023.

The basic structure of an essay always consists of an introduction , a body , and a conclusion . But for many students, the most difficult part of structuring an essay is deciding how to organize information within the body.

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Table of contents

The basics of essay structure, chronological structure, compare-and-contrast structure, problems-methods-solutions structure, signposting to clarify your structure, other interesting articles, frequently asked questions about essay structure.

There are two main things to keep in mind when working on your essay structure: making sure to include the right information in each part, and deciding how you’ll organize the information within the body.

Parts of an essay

The three parts that make up all essays are described in the table below.

Order of information

You’ll also have to consider how to present information within the body. There are a few general principles that can guide you here.

The first is that your argument should move from the simplest claim to the most complex . The body of a good argumentative essay often begins with simple and widely accepted claims, and then moves towards more complex and contentious ones.

For example, you might begin by describing a generally accepted philosophical concept, and then apply it to a new topic. The grounding in the general concept will allow the reader to understand your unique application of it.

The second principle is that background information should appear towards the beginning of your essay . General background is presented in the introduction. If you have additional background to present, this information will usually come at the start of the body.

The third principle is that everything in your essay should be relevant to the thesis . Ask yourself whether each piece of information advances your argument or provides necessary background. And make sure that the text clearly expresses each piece of information’s relevance.

The sections below present several organizational templates for essays: the chronological approach, the compare-and-contrast approach, and the problems-methods-solutions approach.

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The chronological approach (sometimes called the cause-and-effect approach) is probably the simplest way to structure an essay. It just means discussing events in the order in which they occurred, discussing how they are related (i.e. the cause and effect involved) as you go.

A chronological approach can be useful when your essay is about a series of events. Don’t rule out other approaches, though—even when the chronological approach is the obvious one, you might be able to bring out more with a different structure.

Explore the tabs below to see a general template and a specific example outline from an essay on the invention of the printing press.

• Thesis statement
• Discussion of event/period
• Consequences
• Importance of topic
• Strong closing statement
• Claim that the printing press marks the end of the Middle Ages
• Background on the low levels of literacy before the printing press
• Thesis statement: The invention of the printing press increased circulation of information in Europe, paving the way for the Reformation
• High levels of illiteracy in medieval Europe
• Literacy and thus knowledge and education were mainly the domain of religious and political elites
• Consequence: this discouraged political and religious change
• Invention of the printing press in 1440 by Johannes Gutenberg
• Implications of the new technology for book production
• Consequence: Rapid spread of the technology and the printing of the Gutenberg Bible
• Trend for translating the Bible into vernacular languages during the years following the printing press’s invention
• Luther’s own translation of the Bible during the Reformation
• Consequence: The large-scale effects the Reformation would have on religion and politics
• Summarize the history described
• Stress the significance of the printing press to the events of this period

Essays with two or more main subjects are often structured around comparing and contrasting . For example, a literary analysis essay might compare two different texts, and an argumentative essay might compare the strengths of different arguments.

There are two main ways of structuring a compare-and-contrast essay: the alternating method, and the block method.

Alternating

In the alternating method, each paragraph compares your subjects in terms of a specific point of comparison. These points of comparison are therefore what defines each paragraph.

The tabs below show a general template for this structure, and a specific example for an essay comparing and contrasting distance learning with traditional classroom learning.

• Synthesis of arguments
• Topical relevance of distance learning in lockdown
• Increasing prevalence of distance learning over the last decade
• Thesis statement: While distance learning has certain advantages, it introduces multiple new accessibility issues that must be addressed for it to be as effective as classroom learning
• Classroom learning: Ease of identifying difficulties and privately discussing them
• Distance learning: Difficulty of noticing and unobtrusively helping
• Classroom learning: Difficulties accessing the classroom (disability, distance travelled from home)
• Distance learning: Difficulties with online work (lack of tech literacy, unreliable connection, distractions)
• Classroom learning: Tends to encourage personal engagement among students and with teacher, more relaxed social environment
• Distance learning: Greater ability to reach out to teacher privately
• Sum up, emphasize that distance learning introduces more difficulties than it solves
• Stress the importance of addressing issues with distance learning as it becomes increasingly common
• Distance learning may prove to be the future, but it still has a long way to go

In the block method, each subject is covered all in one go, potentially across multiple paragraphs. For example, you might write two paragraphs about your first subject and then two about your second subject, making comparisons back to the first.

The tabs again show a general template, followed by another essay on distance learning, this time with the body structured in blocks.

• Point 1 (compare)
• Point 2 (compare)
• Point 3 (compare)
• Point 4 (compare)
• Advantages: Flexibility, accessibility
• Disadvantages: Discomfort, challenges for those with poor internet or tech literacy
• Advantages: Potential for teacher to discuss issues with a student in a separate private call
• Disadvantages: Difficulty of identifying struggling students and aiding them unobtrusively, lack of personal interaction among students
• Advantages: More accessible to those with low tech literacy, equality of all sharing one learning environment
• Disadvantages: Students must live close enough to attend, commutes may vary, classrooms not always accessible for disabled students
• Advantages: Ease of picking up on signs a student is struggling, more personal interaction among students
• Disadvantages: May be harder for students to approach teacher privately in person to raise issues

An essay that concerns a specific problem (practical or theoretical) may be structured according to the problems-methods-solutions approach.

This is just what it sounds like: You define the problem, characterize a method or theory that may solve it, and finally analyze the problem, using this method or theory to arrive at a solution. If the problem is theoretical, the solution might be the analysis you present in the essay itself; otherwise, you might just present a proposed solution.

The tabs below show a template for this structure and an example outline for an essay about the problem of fake news.

• Introduce the problem
• Provide background
• Describe your approach to solving it
• Define the problem precisely
• Describe why it’s important
• Indicate previous approaches to the problem
• Present your new approach, and why it’s better
• Apply the new method or theory to the problem
• Indicate the solution you arrive at by doing so
• Assess (potential or actual) effectiveness of solution
• Describe the implications
• Problem: The growth of “fake news” online
• Prevalence of polarized/conspiracy-focused news sources online
• Thesis statement: Rather than attempting to stamp out online fake news through social media moderation, an effective approach to combating it must work with educational institutions to improve media literacy
• Definition: Deliberate disinformation designed to spread virally online
• Popularization of the term, growth of the phenomenon
• Previous approaches: Labeling and moderation on social media platforms
• Critique: This approach feeds conspiracies; the real solution is to improve media literacy so users can better identify fake news
• Greater emphasis should be placed on media literacy education in schools
• This allows people to assess news sources independently, rather than just being told which ones to trust
• This is a long-term solution but could be highly effective
• It would require significant organization and investment, but would equip people to judge news sources more effectively
• Rather than trying to contain the spread of fake news, we must teach the next generation not to fall for it

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Signposting means guiding the reader through your essay with language that describes or hints at the structure of what follows.  It can help you clarify your structure for yourself as well as helping your reader follow your ideas.

The essay overview

In longer essays whose body is split into multiple named sections, the introduction often ends with an overview of the rest of the essay. This gives a brief description of the main idea or argument of each section.

The overview allows the reader to immediately understand what will be covered in the essay and in what order. Though it describes what  comes later in the text, it is generally written in the present tense . The following example is from a literary analysis essay on Mary Shelley’s Frankenstein .

Transitions

Transition words and phrases are used throughout all good essays to link together different ideas. They help guide the reader through your text, and an essay that uses them effectively will be much easier to follow.

Various different relationships can be expressed by transition words, as shown in this example.

Because Hitler failed to respond to the British ultimatum, France and the UK declared war on Germany. Although it was an outcome the Allies had hoped to avoid, they were prepared to back up their ultimatum in order to combat the existential threat posed by the Third Reich.

Transition sentences may be included to transition between different paragraphs or sections of an essay. A good transition sentence moves the reader on to the next topic while indicating how it relates to the previous one.

… Distance learning, then, seems to improve accessibility in some ways while representing a step backwards in others.

However , considering the issue of personal interaction among students presents a different picture.

If you want to know more about AI tools , college essays , or fallacies make sure to check out some of our other articles with explanations and examples or go directly to our tools!

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• Post hoc fallacy
• Appeal to authority fallacy
• False cause fallacy
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The structure of an essay is divided into an introduction that presents your topic and thesis statement , a body containing your in-depth analysis and arguments, and a conclusion wrapping up your ideas.

The structure of the body is flexible, but you should always spend some time thinking about how you can organize your essay to best serve your ideas.

An essay isn’t just a loose collection of facts and ideas. Instead, it should be centered on an overarching argument (summarized in your thesis statement ) that every part of the essay relates to.

The way you structure your essay is crucial to presenting your argument coherently. A well-structured essay helps your reader follow the logic of your ideas and understand your overall point.

Comparisons in essays are generally structured in one of two ways:

• The alternating method, where you compare your subjects side by side according to one specific aspect at a time.
• The block method, where you cover each subject separately in its entirety.

It’s also possible to combine both methods, for example by writing a full paragraph on each of your topics and then a final paragraph contrasting the two according to a specific metric.

You should try to follow your outline as you write your essay . However, if your ideas change or it becomes clear that your structure could be better, it’s okay to depart from your essay outline . Just make sure you know why you’re doing so.

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Home — Essay Samples — Nursing & Health — Medical Practice & Treatment — Pharmacology

Pharmacology Essays

Essay topics.

Pharmacology is a complex and fascinating field that explores the effects of drugs on the human body. As a student of pharmacology, you will be required to write essays on a variety of topics related to drug discovery, development, and use. Choosing the right pharmacology essay topics can be challenging, but with the right guidance, you can find a topic that is both interesting and relevant to your studies.

Choosing Relevant Topics

The field of pharmacology is constantly evolving, with new drugs and treatments being developed and tested on a regular basis. As a result, it is important to choose essay topics that are current and relevant to the field. By selecting a topic that is timely and significant, you can demonstrate to your instructors that you are engaged with the latest developments in pharmacology and are capable of critically analyzing and discussing complex issues.

Furthermore, choosing a relevant topic will make it easier for you to find credible sources of information to support your arguments. When you choose a topic that is current and well-studied, you will have access to a wealth of research articles, clinical trials, and expert opinions that can help you build a strong case for your thesis. This will not only improve the quality of your essay but also demonstrate to your instructors that you have a deep understanding of the topic you are discussing.

Tips for Finding Reliable Sources

Once you have chosen a relevant topic for your pharmacology essay, the next step is to find reliable sources of information to support your arguments. This can be challenging, especially if you are new to the field of pharmacology and are not familiar with the best places to find credible research articles and scholarly publications.

One of the best ways to find reliable sources for your pharmacology essay is to use academic databases such as PubMed, Google Scholar, and ScienceDirect. These databases contain a vast collection of peer-reviewed research articles and clinical studies that are relevant to the field of pharmacology. By using these databases, you can ensure that the information you are using to support your arguments is accurate and up-to-date.

In addition to using academic databases, you can also consult textbooks, reference books, and review articles to find reliable sources of information. Textbooks are an excellent source of foundational knowledge in pharmacology and can provide you with a solid understanding of the basic principles and concepts that underpin the field. Reference books and review articles, on the other hand, can provide you with a comprehensive overview of a specific topic, making it easier for you to identify key research studies and findings.

Potential Pharmacology Essay Topics

Now that we have discussed the importance of choosing relevant topics and finding reliable sources, let's explore some potential pharmacology essay topics that you can consider for your next assignment. These topics cover a wide range of issues in pharmacology, from drug discovery and development to the impact of drug use on public health. Whether you are interested in exploring the latest advancements in pharmacology or want to delve into the ethical and social implications of drug use, there is a topic on this list for you.

• The Role of Pharmacogenomics in Personalized Medicine
• The Impact of Drug-Drug Interactions on Patient Safety
• The Ethics of Animal Testing in Drug Development
• The Rise of Antibiotic Resistance: Challenges and Solutions
• The Effect of Prescription Drug Abuse on Public Health
• The Future of Cannabis-Based Medicines
• The Role of Pharmacists in Patient Education and Adherence
• The Impact of Orphan Drugs on Rare Diseases
• The Development of Novel Drug Delivery Systems
• The Influence of Genetics on Drug Response and Adverse Reactions

These topics cover a wide range of issues in pharmacology and can serve as a starting point for your research. Whether you are interested in exploring the latest advancements in drug development or want to delve into the ethical and social implications of drug use, there is a topic on this list that will pique your interest.

Choosing the right pharmacology essay topics is essential for producing a high-quality and engaging essay. By selecting a topic that is current and relevant to the field of pharmacology, you can demonstrate to your instructors that you are engaged with the latest developments in the field. Additionally, by finding reliable sources of information to support your arguments, you can ensure that your essay is well-researched and credible. With the right topic and the right sources, you can produce a pharmacology essay that is both informative and thought-provoking.

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Pharmacology Research Paper Topics

In this page on pharmacology research paper topics , we explore the diverse and dynamic field of pharmacology and provide valuable resources for students who are tasked with writing research papers in this discipline. Pharmacology, as a branch of science, encompasses the study of how drugs interact with biological systems, aiming to understand their mechanisms of action, therapeutic uses, and potential side effects. With the growing importance of pharmacology in healthcare and drug development, it is crucial for students to delve into relevant pharmacology research paper topics that contribute to advancing knowledge and addressing current challenges in the field. Additionally, we highlight iResearchNet’s writing services, offering students the opportunity to order custom pharmacology research papers tailored to their specific needs. Our team of expert writers, equipped with in-depth knowledge of pharmacology and related fields, ensures high-quality, well-researched papers that adhere to the highest academic standards.

In the field of pharmacology, research plays a critical role in advancing our understanding of drugs, their mechanisms of action, and their impact on human health. As students of pharmacology, you may be tasked with writing research papers that explore various aspects of this dynamic discipline. To assist you in your research journey, we have curated a comprehensive list of pharmacology research paper topics that cover a wide range of subfields and emerging areas of interest. Whether you are interested in drug discovery, clinical pharmacology, pharmacogenomics, or drug safety, this list provides a wealth of ideas to inspire and guide your research endeavors.

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Drug Discovery and Development

• Role of Artificial Intelligence in Drug Discovery
• Personalized Medicine: Tailoring Drug Therapy to Individual Patients
• Drug Repurposing: Exploring New Indications for Existing Drugs
• Pharmacogenomics and Drug Response Prediction
• Nanomedicine: Applications in Drug Delivery and Targeting
• Innovative Approaches for Drug Formulation and Delivery
• Drug Combinations: Synergistic Effects and Therapeutic Opportunities
• Natural Products as Sources of Novel Therapeutic Agents
• Virtual Screening and Molecular Docking in Drug Design
• Pharmacokinetics and Pharmacodynamics of New Drug Entities

Clinical Pharmacology

• Precision Dosing: Optimizing Drug Therapy for Individual Patients
• Pharmacokinetic Variability in Special Populations (Pediatrics, Geriatrics, Pregnant Women)
• Drug-Drug Interactions: Mechanisms and Clinical Implications
• Adverse Drug Reactions: Identification, Prevention, and Management
• Pharmacovigilance and Drug Safety Monitoring
• Therapeutic Drug Monitoring: Rationale and Practical Considerations
• Clinical Trials in Pharmacology: Design, Implementation, and Analysis
• Drug Development and Regulatory Approval Processes
• Pharmacoeconomics: Evaluating the Cost-Effectiveness of Drug Therapy
• Ethical Considerations in Clinical Pharmacology Research

Neuropharmacology and Psychopharmacology

• Mechanisms of Action and Therapeutic Applications of Antidepressant Drugs
• Neurotransmitter Systems and Their Role in Mental Health Disorders
• Psychotropic Drugs and Their Impact on Cognitive Functioning
• Novel Approaches for Targeting Neurodegenerative Disorders
• Pharmacological Management of Substance Use Disorders
• Pharmacogenetics in Psychiatry: Implications for Individualized Treatment
• Role of Neuroinflammation in Neurological and Psychiatric Disorders
• Neuropharmacology of Sleep and Wakefulness
• Pharmacotherapy for Schizophrenia: Current Trends and Future Directions
• Novel Treatments for Anxiety and Mood Disorders

Pharmacokinetics and Drug Metabolism

• Drug Transporters and Their Role in Drug Disposition
• Pharmacogenetics and Personalized Drug Therapy
• Pharmacokinetic Variability and Its Impact on Drug Response
• Drug Metabolism Pathways and Enzyme Polymorphisms
• Drug-Drug Interactions: Mechanisms and Clinical Significance
• Predictive Modeling in Pharmacokinetics and Dose Optimization
• Pharmacokinetics in Special Populations: Pediatrics and Geriatrics
• Impact of Genetic Variation on Drug Clearance and Toxicity
• Role of Pharmacokinetics in Individualizing Drug Dosage
• Strategies for Improving Oral Bioavailability of Drugs

Pharmacology of Infectious Diseases

• Antimicrobial Resistance: Mechanisms, Epidemiology, and Strategies
• Development of Novel Antiviral Agents: Challenges and Opportunities
• Pharmacotherapy for Bacterial Infections: Current Approaches and Future Directions
• Antifungal Drugs: Mechanisms of Action and Resistance
• Host-Pathogen Interactions and Their Implications for Drug Development
• Pharmacokinetic Considerations in the Treatment of Viral Infections
• Targeting Virulence Factors in Bacterial Pathogens
• Drug Combination Therapy for Multidrug-Resistant Infections
• Pharmacogenomics of Antimicrobial Agents
• New Approaches for Antiparasitic Drug Development

Cardiovascular Pharmacology

• Novel Antiplatelet Agents: Mechanisms and Clinical Applications
• Antihypertensive Therapy: Current Strategies and Future Perspectives
• Pharmacotherapy for Heart Failure: Advancements and Challenges
• Role of Pharmacogenomics in Cardiovascular Drug Therapy
• Therapeutic Potential of Antiarrhythmic Agents
• Pharmacological Management of Dyslipidemia and Atherosclerosis
• Emerging Therapies for Pulmonary Hypertension
• Pharmacological Approaches to Preventing Thromboembolic Disorders
• Cardiotoxicity of Chemotherapeutic Agents: Mechanisms and Cardioprotective Strategies
• Targeting Inflammatory Pathways in Cardiovascular Disease

Pharmacology and Aging

• Geriatric Pharmacotherapy: Challenges and Approaches
• Age-Related Changes in Pharmacokinetics and Pharmacodynamics
• Polypharmacy and Its Impact on Older Adults
• Adverse Drug Reactions in the Elderly: Recognition and Prevention
• Pharmacological Management of Age-Related Neurodegenerative Disorders
• Geriatric Pharmacogenomics: Implications for Personalized Medicine
• Drug-Related Falls and Fractures in the Elderly: Prevention and Intervention
• Medication Adherence in Older Adults: Barriers and Strategies
• Geriatric Pain Management: Balancing Efficacy and Safety
• Optimizing Drug Therapy in Older Adults with Multiple Comorbidities

Pharmacology of Cancer

• Targeted Therapies for Solid Tumors: Recent Advances and Future Directions
• Immunotherapy in Cancer Treatment: Current Approaches and Challenges
• Pharmacogenomics of Chemotherapy: Implications for Personalized Treatment
• Drug Resistance in Cancer: Mechanisms and Strategies for Overcoming Resistance
• Pharmacokinetics and Pharmacodynamics of Anticancer Agents
• Combination Therapies in Oncology: Rationale and Clinical Outcomes
• Oncolytic Viruses: Exploiting Viral Infections for Cancer Treatment
• Cancer Stem Cells: Targeting Tumor Initiation and Progression
• Development of Novel Imaging Agents for Cancer Diagnosis and Monitoring
• Pharmacological Interventions for Cancer-Associated Pain Management

Pharmacology and Immunology

• Immune Checkpoint Inhibitors in Cancer Immunotherapy
• Autoimmune Diseases: Novel Pharmacological Approaches and Therapies
• Immunomodulatory Effects of Drugs: Implications for Therapeutic Interventions
• Role of Pharmacogenomics in Immunomodulatory Drug Therapy
• Immunopharmacology of Allergic Reactions: Mechanisms and Treatment Strategies
• Immunosuppressive Drugs in Transplantation: Balancing Efficacy and Safety
• Targeting Inflammatory Pathways in Autoimmune Disorders
• Immunopharmacological Interventions for Infectious Diseases
• Pharmacological Modulation of Cytokines in Inflammatory Disorders
• Vaccines: Advancements in Development and Delivery

Pharmacovigilance and Drug Safety

• Post-Marketing Surveillance: Detecting and Evaluating Adverse Drug Reactions
• Signal Detection in Pharmacovigilance: Methods and Applications
• Risk Management Strategies in Drug Development and Marketing
• Pharmacogenomic Biomarkers for Predicting Drug Safety
• Pharmacovigilance in Special Populations: Pregnant Women and Pediatrics
• Drug Safety Communication: Enhancing Patient Awareness and Education
• Role of Pharmacovigilance in Drug Regulatory Affairs
• Pharmacovigilance Data Mining: Leveraging Big Data for Drug Safety
• Pharmacovigilance Systems and Reporting Structures
• Pharmacogenetic Testing in Drug Safety Assessment

This comprehensive list of pharmacology research paper topics provides a broad range of ideas and areas to explore within the field of pharmacology. From drug discovery and development to clinical pharmacology, neuropharmacology, and pharmacokinetics, each category offers multiple topics for students to delve into and contribute to the advancement of pharmacological knowledge. Whether you are interested in the impact of pharmacogenomics on drug therapy, exploring novel treatment strategies, or investigating drug safety and pharmacovigilance, there is a wealth of research possibilities awaiting exploration. By selecting a topic of interest and following the expert advice on topic selection and research paper writing, students can embark on an enriching journey of discovery and make meaningful contributions to the field of pharmacology.

Pharmacology: Exploring the Range of Research Paper Topics

Pharmacology is a captivating and dynamic scientific discipline that focuses on the study of drugs and their effects on living organisms. It plays a crucial role in improving human health by advancing our understanding of how medications interact with biological systems. Within the field of pharmacology, there is a vast array of pharmacology research paper topics that offer students an opportunity to delve into various aspects of drug discovery, development, clinical application, and safety. In this article, we will explore the breadth and depth of pharmacology as a scientific field, highlighting the range of research paper topics it encompasses.

Drug Discovery and Development:  One exciting area of pharmacology research is drug discovery and development. This field involves the identification and development of new therapeutic agents to treat a wide range of diseases. Students interested in this area can explore topics such as the exploration of novel drug targets and therapeutic approaches, investigating natural products for drug development, advancements in targeted drug delivery systems, pharmacokinetics and pharmacodynamics of new drug entities, and understanding and overcoming drug resistance mechanisms.

Clinical Pharmacology:  Clinical pharmacology focuses on the application of pharmacological principles in the clinical setting. It plays a vital role in optimizing drug therapy and ensuring patient safety. Pharmacology research paper topics in this area may include pharmacogenomics, which explores the relationship between an individual’s genetic makeup and their response to medication. Other topics of interest include the identification, prevention, and management of adverse drug reactions, the design and ethical considerations in clinical trials, pharmacovigilance, and optimizing drug regimens for special populations such as pediatrics, geriatrics, and pregnant women.

Neuropharmacology and Psychopharmacology:  The field of neuropharmacology examines how drugs interact with the central nervous system and influence brain function. Pharmacology research paper topics in this area may involve investigating the mechanisms of action and therapeutic applications of psychotropic drugs, exploring neurotransmitter systems and their role in neurological disorders, pharmacological interventions for Alzheimer’s disease and other neurodegenerative disorders, the psychopharmacology of substance use disorders, and the pharmacological management of mental health disorders.

Pharmacokinetics and Drug Metabolism:  Pharmacokinetics and drug metabolism focus on understanding how drugs are absorbed, distributed, metabolized, and eliminated by the body. Pharmacology research paper topics in this area may include studying drug interactions, such as the mechanisms, predictions, and clinical implications of drug-drug interactions. Other topics of interest include pharmacogenetics and individual variations in drug response, the role of drug transporters in drug disposition, drug metabolism and its impact on drug-drug interactions, and the use of predictive modeling in pharmacokinetics and dosing optimization.

Pharmacology of Infectious Diseases:  The pharmacology of infectious diseases involves studying how drugs can effectively treat and prevent infections. Research topics in this area may include exploring antimicrobial resistance, including its mechanisms, epidemiology, and strategies to combat it. Additionally, students may investigate the development of new antiviral agents, the pharmacological management of bacterial infections, host-pathogen interactions, and the pharmacokinetic considerations in the treatment of infectious diseases.

Cardiovascular Pharmacology:  Cardiovascular pharmacology focuses on understanding the effects of drugs on the cardiovascular system. Research topics in this area may include exploring drug therapy for hypertension and current guidelines for treatment, novel anticoagulants in the prevention and treatment of thromboembolic disorders, pharmacological approaches to managing heart failure, drug-induced cardiotoxicity and strategies for prevention, and emerging pharmacotherapies for atherosclerosis and coronary artery disease.

Pharmacology and Aging:  Pharmacology and aging is a specialized field that investigates how drug therapy can be optimized in older adults. Research topics in this area may include exploring geriatric pharmacotherapy, age-related changes in pharmacokinetics and pharmacodynamics, the impact of polypharmacy on older adults, the recognition and prevention of adverse drug reactions, pharmacological management of age-related neurodegenerative disorders, and strategies for improving medication adherence in the elderly.

The field of pharmacology offers a wide range of exciting research paper topics that span from drug discovery and development to clinical pharmacology, neuropharmacology, pharmacokinetics, and beyond. By exploring these topics, students can contribute to the advancement of pharmacological knowledge and make meaningful contributions to the field. Remember to choose a research topic that aligns with your interests and career aspirations, and be sure to consult with your instructors or mentors for guidance throughout your research journey. With dedication, curiosity, and a passion for improving patient care, you have the opportunity to shape the future of pharmacology research.

How to Choose a Pharmacology Research Topic

Choosing the right research paper topic is crucial for a successful academic journey in pharmacology. It allows you to explore your interests, contribute to the field, and showcase your knowledge and skills. However, with the vast scope of pharmacology, selecting a research topic can be a daunting task. In this section, we will provide you with expert advice on how to choose pharmacology research paper topics that are engaging, relevant, and have the potential for significant contribution.

• Identify Your Interests : Start by identifying your areas of interest within pharmacology. Reflect on the topics that have captivated your attention during your coursework or sparked your curiosity. Consider whether you are more inclined towards drug discovery, clinical applications, pharmacokinetics, neuropharmacology, or any other subfield of pharmacology. This self-reflection will help you narrow down your options and select a topic that resonates with your passion.
• Stay Updated with Current Research : To choose a compelling research topic, it is essential to stay updated with the latest advancements and trends in pharmacology. Follow reputable scientific journals, attend conferences, and engage with the pharmacological community to gain insights into the ongoing research and emerging areas of interest. This will help you identify gaps in the current knowledge and select a topic that offers the potential for novel discoveries or addressing existing challenges.
• Consult with Faculty and Experts : Seek guidance from your faculty members, mentors, or experts in the field of pharmacology. They can provide valuable insights and suggest potential research areas based on their expertise and experience. Discuss your interests, goals, and research aspirations with them, and they can help you refine your research topic, provide relevant literature references, and offer valuable advice on the feasibility and scope of your chosen topic.
• Consider Practicality and Resources : When selecting a research topic, consider the practicality and availability of resources. Assess whether the necessary laboratory facilities, equipment, or access to clinical data are readily accessible to conduct your research. Additionally, consider the time and resources required to complete the research within the given timeframe. Choosing a topic that aligns with the available resources will enhance the feasibility and success of your research endeavor.
• Address Current Challenges or Gaps : Pharmacology is a field that constantly evolves, presenting new challenges and unanswered questions. Consider selecting a research topic that addresses current challenges or explores gaps in the existing knowledge. This could involve investigating the mechanisms of drug resistance, exploring novel drug targets, or optimizing drug regimens for specific patient populations. By tackling these challenges, you can contribute to the advancement of pharmacological science and make a meaningful impact.
• Collaborate with Peers : Consider collaborating with fellow students or researchers who share similar research interests. Collaborative research projects can provide a broader perspective, foster knowledge sharing, and enhance the overall quality of your research. Collaborating with peers also allows you to divide the workload, share resources, and receive feedback and support throughout the research process.
• Seek Ethical Considerations : When selecting a pharmacology research topic, it is essential to consider ethical considerations and adhere to the principles of research ethics. Ensure that your chosen topic respects patient confidentiality, follows the guidelines for the ethical use of animal subjects (if applicable), and aligns with the ethical principles outlined by regulatory bodies. Consulting with your institution’s ethics committee or research advisor can help ensure that your research project meets the required ethical standards.
• Evaluate Feasibility and Novelty : Evaluate the feasibility and novelty of your chosen research topic. Consider whether the research question is answerable within the available resources and time constraints. Additionally, assess whether your topic brings something new to the field, whether it fills a knowledge gap, or offers a fresh perspective on an existing topic. A balance between feasibility and novelty is essential for a successful research paper.
• Consult Literature Reviews : Conduct thorough literature reviews on your chosen topic to gain a comprehensive understanding of the existing research. Literature reviews help you identify gaps in the current knowledge and provide a foundation for your research question. They also enable you to build on previous findings, develop a robust research methodology, and position your research within the context of the broader field of pharmacology.
• Remain Flexible : Lastly, remain flexible throughout the process of choosing a research topic. As you delve deeper into the literature and research process, you may discover new avenues of interest or encounter unexpected challenges. It is essential to remain open to refining or adjusting your research topic based on new insights, emerging data, or feedback from your research advisors. Flexibility allows you to adapt and ensure that your research remains relevant and impactful.

Choosing a pharmacology research paper topic is an exciting and important step in your academic journey. By following expert advice, identifying your interests, staying updated with current research, seeking guidance, considering practicality and resources, addressing current challenges or gaps, collaborating with peers, adhering to ethical considerations, evaluating feasibility and novelty, consulting literature reviews, and remaining flexible, you can select a research topic that is engaging, relevant, and has the potential to contribute to the field of pharmacology. Remember, this is your opportunity to explore, innovate, and make a lasting impact in the dynamic field of pharmacology research.

How to Write a Pharmacology Research Paper

Writing a pharmacology research paper requires careful planning, organization, and attention to detail. It is an opportunity for you to showcase your understanding of the subject matter, critical thinking skills, and ability to communicate scientific information effectively. In this section, we will provide you with expert guidance on how to write a pharmacology research paper that is well-structured, informative, and compelling.

• Choose a Well-Defined Research Question : Start by formulating a clear and well-defined research question. Your research question should be focused, specific, and address a gap in the existing knowledge. Consider the significance of your research question in the context of pharmacology and how it contributes to the overall understanding of the field. A well-defined research question sets the foundation for your entire research paper.
• Conduct a Thorough Literature Review : Before diving into your research, conduct a thorough literature review on the chosen topic. Familiarize yourself with the existing research, theories, and findings related to your research question. This will provide you with a solid understanding of the current state of knowledge and help you identify gaps or areas for further investigation. Additionally, the literature review will inform your research methodology and discussion of results.
• Develop a Clear Structure : A well-structured research paper is essential for effectively conveying your ideas and findings. Begin with an engaging introduction that provides background information, context, and clearly states your research question. Follow with a comprehensive literature review that supports your research question and highlights the gaps in knowledge. Next, present your research methodology, including details on sample selection, data collection, and analysis methods. In the results section, present your findings in a clear and organized manner using tables, graphs, or figures as necessary. Finally, discuss your results, interpret their significance, and relate them back to your research question in the discussion section. Conclude with a concise summary of your findings and their implications.
• Use Reliable and Credible Sources : Ensure that the sources you use for your research paper are reliable, credible, and peer-reviewed. Consult reputable scientific journals, textbooks, and conference proceedings. Avoid relying solely on internet sources or non-scholarly publications. Citations are critical to acknowledge the work of other researchers and to support your claims and arguments. Use a consistent citation style, such as APA, MLA, or Chicago, and follow the guidelines carefully.
• Analyze and Interpret Your Data : If your research involves collecting and analyzing data, ensure that your data analysis is thorough and accurate. Use appropriate statistical methods to analyze your data and present the results in a clear and meaningful way. Interpret the findings in the context of your research question and discuss any limitations or potential sources of bias. Remember to relate your findings back to the existing literature and explain how they contribute to the broader understanding of pharmacology.
• Write Clearly and Concisely : Effective scientific writing is clear, concise, and free of unnecessary jargon. Use language that is precise and straightforward, avoiding ambiguous or vague statements. Clearly articulate your ideas and ensure that your arguments are logical and well-supported by evidence. Use appropriate scientific terminology, but also consider your target audience and strive to communicate your findings in a way that is accessible to readers who may not have expertise in pharmacology.
• Pay Attention to Formatting and Style : Follow the formatting and style guidelines specified by your instructor or the target journal. Pay attention to details such as font size, line spacing, margins, and headings. Use subheadings to organize your content and make it easier for readers to navigate. Adhere to the specific citation style required for your paper and ensure that your references are complete and accurate.
• Revise and Edit : Revision and editing are essential steps in the writing process. Take the time to review your research paper for clarity, coherence, and accuracy. Check for grammatical errors, spelling mistakes, and punctuation errors. Ensure that your ideas flow logically and that your paper is well-structured. Consider seeking feedback from peers, instructors, or mentors to gain different perspectives and improve the overall quality of your paper.
• Proofread : Before submitting your research paper, thoroughly proofread it to ensure that it is error-free. Check for any typos, inconsistencies, or formatting issues. Read your paper aloud to catch any awkward phrasing or unclear sentences. It can also be helpful to have someone else read your paper to identify any errors or areas that need improvement.
• Ethical Considerations : Ensure that your research paper adheres to ethical considerations. If your research involved human subjects, ensure that you have obtained the necessary approvals and informed consent. Respect patient confidentiality and anonymity when presenting your research findings. Adhere to the ethical guidelines set by your institution or the relevant regulatory bodies.

Writing a pharmacology research paper requires careful planning, thorough research, effective communication, and attention to detail. By following the expert advice provided in this section, you can develop a well-structured and informative research paper that contributes to the field of pharmacology. Remember to choose a well-defined research question, conduct a thorough literature review, use reliable sources, analyze and interpret your data, write clearly and concisely, pay attention to formatting and style, revise and edit your paper, proofread for errors, and ensure ethical considerations are met. With diligence and commitment, your pharmacology research paper has the potential to make a meaningful impact in the field of pharmacology.

iResearchNet’s Writing Services

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What is pharmacology.

Pharmacology is the study of how molecules , such as medicines , interact with the body. Scientists who study pharmacology are called pharmacologists, and they explore the chemical properties, biological effects, and therapeutic uses of medicines and other molecules. Their work can be broken down into two main areas:

• Pharmacokinetics is the study of how the body acts on a medicine, including its processes of a bsorption, d istribution, m etabolism , and e xcretion ( ADME ).
• Pharmacodynamics is the study of how a medicine acts in the body—both on its intended target and throughout all the organs and tissues in the body.

Medicine bottles have instructions based on pharmacology research. How much of it, how often and when to take it, and whether to eat or avoid certain foods while taking it are all factors that pharmacologists research to make sure you get the best results from your medicine.

Medicine instructions are based on the average bodily response to a specific medicine, but some people don’t respond in the average way. That’s where pharmacogenetics and pharmacogenomics —the study of how a gene or an entire genome , respectively, affect the body’s response to medicine—come in. Enzymes are often responsible for breaking down medicines so they can be removed from our bodies. If given a dose based on an average response, a person with a less active enzyme because of their genetics might end up with too much medicine in their body for too long of a time, which could cause negative effects. Alternatively, some medicines use enzymes to activate them before they can be effective, and genetic differences in those enzymes may result in not enough activated medicine for the desired effects. Pharmacologists work to understand how genes can change a response to a drug, which helps clinicians to choose the best medicine, dose, and treatment plan for their patients.

Being a Pharmacologist

Pharmacology is situated at the intersection of several fields, including chemistry , biology, and medicine—all of which are important to determine the interaction between molecules and the human body. And although it’s often confused with pharmacy (the clinical field that your local pharmacist practices as they prepare, dispense, and advise you about your medicine), pharmacology isn’t necessarily a clinical field with individual patients. Instead, it’s a research-based science where new findings can have significant impacts on our understanding of human health and how clinicians, like pharmacists and medical doctors, treat their patients. Pharmacologists may make these important scientific contributions by studying the properties and effects of specific medicines, working with clinicians and individual patients to optimize their medicines, or using molecules as tools to study cells, tissues, or organs in the body. 

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Pharmacology in Nursing Practice Essay

Introduction, knowledge of pharmacology, medication use, advanced practice appreciation, course knowledge and future practice.

Pharmacologic treatment and patient management are crucial among registered nurses (RNs). Therefore, the knowledge gained in this course is important for my future endeavors. During the classes, I was taught the laws and regulations of prescribing drugs, the ethical issues associated with drug administration, and the components of a correctly written prescription. Additionally, therapeutic communication helped me understand various relationships with different healthcare stakeholders. Understanding the different drugs that affect different body organs will help me avoid cases of misdiagnosis in the future. Therefore, the knowledge gained from this course will play a significant role in making me a compliant and competitive nurse.

I knew little about drugs and medication prescriptions before taking the course in pharmacology. I could only prescribe common drugs such as painkillers that do not need a professional opinion. However, the course expanded my knowledge of medical prescriptions, non-medical prescriptions, healthcare costs, insurance, and complementary alternative treatments. Prescription medication involves pharmaceutical drugs that legally require a prescription for them to be dispensed. Such drugs are prescribed because of various reasons including the potential scope of misuse and the high possibility of side effects on the patients. As an RN I have to be very cautious when prescribing and dispensing such drugs to patients.

Meanwhile, non-medical prescriptions are those drugs that do not need expert knowledge and advice before dispensing. The non-prescriptive drugs are administered to treat minor health problems such as headaches, stomachaches, and fever. Over-the-counter drugs such as acetaminophen, aspirin, and antacids are non-medical prescriptions (Greenfield, 2022). Moreover, I learned about the concepts of healthcare costs and various factors that are taken into account. Healthcare costs include the amount spent on renting hospital buildings, securing drugs, and paying practitioners, among others. Therefore, various factors are included in estimating the amount that patients pay for medical services.

The knowledge of insurance and complementary alternative treatments helped me understand how patients can relieve themselves from the burden of healthcare costs. Medical insurance policies allow employers and contracted third parties to take care of medical expenses for patients. Insurance companies require individuals to subscribe to various plans that cover different types of medical care (Greenfield, 2022). Meanwhile, organizations pay for their employees’ medical care for their business success. Patients can take complementary alternative treatments to avoid the side effects of drugs and increased healthcare costs. The alternative treatments include yoga, tai chi, massage therapy, and acupuncture. The expanded pharmacological knowledge gained will help me understand patients’ situations and appropriately manage them.

Medication use is significant in alleviating patients’ conditions and relieving their pains. However, inappropriate medication use can lead to patient complications and consequent problems such as potential lawsuits against the nurses. Accordingly, as an RN I think of medication used differently because of the potential consequences. I believe that every drug must be dispensed and taken as prescribed by a medical expert. Consequently, I am always careful when dispensing drugs to patients, and where I doubt my knowledge in prescribing a specific drug, I consult other experts in the field. Unlike nurse practitioners (NPs), RNs are not permitted to prescribe drugs, order tests, diagnose patients, or perform any duty that is normally performed by physicians. Therefore, my responsibilities of educating patients are limited when compared to an NP. As an RN I can only observe, offer minor treatments, and educate patients, under strict supervision.

Advanced nursing practice requires cutting-edge educational and clinician knowledge that proves professional competency. My knowledge of pharmacology has made me appreciate the role of advanced practice in nursing. The practice equips RNs and NPs with unconventional knowledge of helping patients and avoiding potential legal liabilities. I was encouraged to specialize in various nursing areas and take more courses on the same. However, my belief that the roles of advanced registered nurses (APRNs) and RNs are not significantly different was not changed. Although APRNs are more effective than RNs, they both perform similar functions. Therefore, advanced practice is only met to improve RNs’ effectiveness in a healthcare organization, offering more opportunities.

The knowledge gained in this course will be beneficial to my future advanced practice. I will use the knowledge of ethical medical practice in taking care of my patients within the legal requirements. Avoiding unethical medical practices such as giving wrong drug prescriptions and disrespecting patients’ privacy, will allow me to gain the trust of my patients. Moreover, having understood pharmacokinetics and dynamics, I shall assess the patients’ body biochemical reactions to drugs before dispensing them. Consequently, my patients will have minimum cases of drug-related body reactions. Furthermore, the knowledge of drug effects on different body parts encourages me to further my studies in pharmacology in the future. Therefore, this course is beneficial for my future patients and career development in advanced nursing practice.

As an RN I will interact with drugs and various medications daily. Although my role in nursing is to observe and educate patients, I can be instructed to administer drugs for minor health problems. Understanding the prescriptive and non-prescriptive medications will help me administer appropriate drugs to patients. The knowledge of medical costs and health insurance will help me in assessing a patient’s economic situation and suggesting alternative medications that are affordable and effective. Pharmacological concepts are crucial for my patients and advanced career development.

Greenfield, D. P. (2022). Psychopharmacology for Nonpsychiatrists: A Primer . Springer Nature.

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Pharmacology essays

Pharmacology pbl (problem-based) report, bipolar disorder, pharmacology, solution description, literature support, the risk of congenital autism in using paracetamol during pregnancy, parkinson disease, easy writing of a pharmacology essay with our examples.

Pharmacology plays a significant role in nursing education. It teaches nurses how medications work, how to give them, and what side effects they may cause. Nurses must know how to safely and effectively care for patients receiving medications.

Making a diagnosis and prescribing medication are the doctor’s direct responsibility. However, nurses also need knowledge of pharmacology in their practice. There are multiple reasons for this:

• To correctly calculate the medicine’s dose and its administration method.
• To evaluate the risks and possible benefits of medications for patients.
• To monitor the effectiveness and safety of medications.
• To recognize and treat side effects.

This is just one of the reasons why nurses need to study pharmacology. There are many nursing responsibilities in patient care where they apply this knowledge. That’s why you cannot overestimate the importance of pharmacology in nursing essay writing.

Features of the Essay About Pharmacology

The pharmacology in your studies can be presented with two categories – pharmacokinetics and pharmacodynamics. The first focuses on the body’s perception of the drug: absorption, metabolism, distribution & excretion. Pharmacodynamics, in turn, explores how a drug affects the body. You may need to write a paper on both of these subjects. This could be an essay, assignment, research paper, or case study. To make it simple, let’s call all papers essays.

What’s special about a pharmacology essay?

Look at examples in our sample database to define features. They have a clear structure and are very reasoned. The essay may discuss a patient’s care, the impact on nursing practice, recent findings, or an analysis of specific cases. The focus on medicinal aspects is a distinctive feature of each paper.

How to Work With Examples of Pharmacology Essay

Working with a pharmacology essay sample is easy. All of the examples are pre-sorted according to a key feature – pharmacology. Under each heading, you see a snippet of text and the topics the article also covers. Scroll to a topic related or similar to yours and view the full sample. You need to take from the example its structure, the way of presenting information, the list of literature, and design.

Our experts wrote papers for nursing course students, and now you see them as pharmacology essay samples in our database. You can’t copy them for reasons. Most importantly, uniqueness in your studies and nursing practice is crucial. Instead of risking having trouble with plagiarism, focus on adapting the selected example to your case. Use the example as a basis for your paper outline. And gradually add your unique and relevant content to the structure. Thus, with the help of a sample, you will cope with writing an essay easily on your own.

Feel Free to Ask For More Help Than Pharmacology Examples

You may not find the sample you are looking for. Our database of pharmacology examples can only cover some topics. There are two solutions. The first one is to seek in related categories. You can also try to search using associated keywords, topics, or subjects. There are over 10,000 examples, among which you may find something inspirational.

The second option is to ask our experts for help individually. They may assist you at any stage of your work, from sources search to writing from scratch. It’s a great deal. Especially if you don’t have enough time to handle this task yourself. We will write your essay at the highest level, even with the tightest deadline.

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💊 Essays on Pharmacology

Pharmacology studies how drugs interact with living organisms. It is a vital area of healthcare that helps to ensure the safe and effective use of medicines. To write a paper on pharmacology, you should have a good grasp of the subject matter. Fortunately, today, students have access to a wealth of physical and online resources.

Reading through medical articles and databases will help you produce an incredible essay on pharmacology. Another great way to learn more about the field is to read paper samples written by experts. These examples can provide valuable insights on how to structure your essay and which types of data, facts, or statistics to include. Using these resources, you can be sure that your paper on pharmacology will be impressive and well-informed.

Antimicrobial Medication and Patient Differences

The medicaments amoxicillin, ampicillin, and carbenicillin, in contrast to such typical drug groups as penicillin and mezlocillin, inhibit complete protein synthesis, which signifies the proliferation of cells. Therefore, the target groups of antimicrobial drugs are suitable for a wide range of patients. Nevertheless, the professionals, who develop hospital formularies, must...

Antimicrobial Medication and Patient Education

Though the optimal selection of the medication for hospital formulary contributes to the maximal aligning of community interests to drugs’ use, it is critical to describe cautionary characteristics of the medicaments. In fact, despite the relative optimization of amoxicillin, ampicillin, and carbenicillin use, three-drug groups have contraindications, which must be...

Hospital Formulary as a Resource to Prescribe to Patients

The main objective of using hospital formularies in clinical conditions is providing complete satisfaction with the medication needs of a certain group of patients. In this study, we provide the criteria for selecting a specific drug group, which is represented in a hospital formulary. In fact, one can state that...

The International Promotion of Drugs and Devices Regulation

According to the people in America, they are industries that the government should regulate more compared to others. These industries are the pharmaceutical and oil industries. In the United States, the representation of the people who believe pharmaceutical industries are more regulated is 51 percent. The pharmaceutical company is experiencing...

The Prescription Drugs and Its Overseas Low Price

Several prescription medications are cheaper in other countries than in the United States. The variations in costs may be considerable. Many Americans as well as citizens from some other countries like Canada question why drugs manufactured by companies in the U.S. are less expensive overseas. The reason is that some...

The Similarity of Illicit Drug Use and Prescribed Pharmaceutical Drugs

Abuse of substances has been approximated to be the actual cause of close to 120,000 deaths per year in the United States, while more 80% of them imputed to alcohol and about 20% imputed to other drug use. Alcohol and other drugs have become more likely the cause of unpremeditated...

Side Effects of Psychopharmacological Agents

Firstly, these are antianxiety agents commonly used for treating anxiety disorders and symptoms. The names of drugs belonging to this class are benzodiazepines such as alprazolam (Xanax), and other medications including buspirone (BuSpar) and paroxetine (Paxil). Antidepressant drugs are intended for treating the major depressive disorder, dysthymic disorder, and bipolar...

Upper Respiratory Infection and Antibiotics

Pharmacology is developing rapidly, and the persistent opinion that any strong antibiotic causes much harm to the body can no longer be considered consistent. Antibiotics of the new generation, among other vital advantages, show that they can work carefully about vital human systems and effectively against pathogenic bacteria. The abstract...

The Use of Metformin in the Treatment of Diabetes Mellitus

Introduction Many diseases are treated with specific medications, but the advantages and great results are not evident to some healthcare providers. This is a major shortcoming of evidence-based healthcare practice, and the information must be spread as soon as possible so that medics begin to treat their patients with useful...

The Different Processes of Pharmacokinetics and Pharmacodynamics

Substance in the organism, whereas bioavailability is a subcategory of the former concept. It is based on the portion of the drug that reaches the final circulatory system. Both of them are highly dependent on the nature of the chemical. Distribution is the process of transferring the drug through the...

Genetic Factors and Variability of Responses in Tailoring Pharmacologic Agents

Geneticists and pharmacologists understand that drug response is a process that depends on various factors, including age, co-morbidities, diet, and genetics. These attributes will have significant influences on the nature or quality of medical care available to the targeted patients. The genomics of a given person will dictate the genes...

Reproductive Toxicity of Bisphenol-A

Background information Bisphenol-A is commonly used in dentistry, fissure sea lands, hospital instruments and tools, thermal papers, containers of beverages, and cans of food. The chemical has been found to harm the reproductive system of the human body (Rochester, 2019). Ways to contact BPA include inhaling, ingestion, and skin interaction...

Responsible Prescription of Opioids in Emergency Department

Identification of the Issue and the Ethical Position The prescription of opiates by healthcare providers in the United States has recently become an issue. The painkiller abuse has led to around 500,000 emergency cases and hospital visits yearly (Bohnert et al., 2018). More than 10,000 Americans die annually due to...

Vitamin and Mineral Supplements

Vitamins are special organic substances that are not a source of energy or building material for the body. Nevertheless, they are necessary for small and often minimal quantities for its normal functioning. Vitamins are involved in metabolism, and they are biological accelerators of chemical reactions in the cell that increase...

Buprenorphine: Effectiveness Review

Introduction Buprenorphrine is replacing methadone in detoxification of opiate addiction. Buprenorphrine suppresses withdrawal symptoms in opiate addiction. This study was conducted on 200 opiate addiction patients at the Sunrise Detoxification Center. The effectiveness of buprenorphrine in reducing pulse, sweating, anxiety, tremor, and nausea among other withdrawal symptoms was evaluated. Background...

Pharmacological Management of Status Epilepticus

Abstract Status epilepticus (SE) is a serious neurological condition that requires immediate diagnosis and treatment. Among the available benzodiazepines, nurses should choose the best drug to use for SE. The purpose of this paper is to assess the pharmacological treatment of SE using benzodiazepines and determine nursing implications. Introduction Status...

Carfilzomib Drug for Multiple Myeloma

Introduction In the past decade, there have been important advances made in the treatment of various forms of cancer (Demo, Krik, & Aujay 2007). The discoveries made so far have led to increased survival rates for individuals affected with considerably risky forms of cancer. The introduction of drugs like thalidomide...

The Mechanism of Action NSAIDs as an Explanation of Their Unwanted Effects

Abstract The use of NSAIDS has been in general medical practice for many years and its therapeutic effects documented for a long time. NSAIDs have been widely known for their analgesic, antipyretic and anti-inflammatory activities. They have been used in many clinical situations with good outcomes. The local, as well...

Evolution of the Pharmacists in an Independent Prescribing Role

Abstract The thesis study aims at demonstrating that a career community pharmacist can practice as an effective clinician in a prescribing role treating patients in a primary care setting. The introduction of advanced and enhanced community pharmacy services enhances the need for pharmacists to integrate into primary care medical services....

The Human Caspases: Viral Inhibitor

Sequential Activation Apoptosis, which is the controlled death of cells in an organism, is important in order to remove damaged and aged cells from the system. A group of cysteine aspartic acid-specific proteases (also referred to as caspases) is the one that regulates this death process. Caspases are activated within...

Use of Natural Products for Osteoarthritis Treatment

Introduction Osteoarthritis is a health condition that affects the joints and muscles around the knees. It is characterized by breakdown of joint cartilage over a period of time. In normal circumstances, cartilage allows bones to slide over one another, but patients with this condition experience pain around joints because there...

Pharmaceutical industry: Generic drug

Origin and history of generic drugs Generic drugs have been around for decades. However, their regulation was necessitated by several controversial occurrences within the market. In 1937, there was an incident associated with Elixir Sulfanilamide. It caused the death of approximately one hundred and seven people and eventually prompted the...

Organizational Structure Changes in Pfizer

The rapid development of science and technology and the organizational changes are some of the factors the challenge the survival and success of the pharmaceutical industries. The dynamics of this industry have been redefined through the combined forces of social, economic, political, and technological factors. Over the past many years,...

Strategic Alliance on National Health

Abstract With an average annual growth rate of 11.1 percent from 1970 until 2006, the pharma market is one of the fastest-growing markets in the world, reaching more than US$400 billion in sales in 2003 (PhRMA, 2004). The industry is now going through a major consolidation stage where direct product...

The Issue of Polypharmacy and Ways of Its Diminishing

Introduction Polypharmacy is a major problem that can affect anybody, but it is the most common to the elderly population. The concept of polypharmacy encloses the use of five or more medications at the same time (Fick et al., 2003), prescription of more medications than required, and prescription of medications...

Psychopharmacology. Psychotropic Drug Promotion

The money spent on drug advertising is truly astounding and estimates are no longer in the billions but in the tens of billions, and increasing rapidly. According to a December 12, 2002, New York Times article, “Promotional spending in the United States by the 14 largest pharmaceutical companies increased at...

Marijuana for Medicinal Purposes in the US

Introduction First, it was medical marijuana; next, it will be alcohol and so on and so forth. The problem the country faces with medical marijuana is similar to the one it faces when the issue of legalizing abortion nationwide or physician-assisted suicide came into view. Both of these areas are...

Analysis of the Pharmaceutical Industry

Introduction The pharmaceutical industry should be discussed in the context of its global expansion. The problem is that the global business world has altered significantly in recent decades, leading to positive and negatives outcomes for globally oriented industries (Gaudillière 2015). Buyer behaviour has changed significantly, resulting in the generation of...

Use of Repeated Intravenous Ketamine Therapy in Treatment-Resistant Bipolar Depression With Suicidal Behavior

Introduction An article Use of Repeated Intravenous Ketamine Therapy in Treatment-resistant Bipolar Depression with Suicidal Behavior: a Case Report from Spain describes the efficacy of ketamine as a treatment for bipolar depression with signs of suicide (López-Díaz, et al., 2017). Main effects of ketamine The authors point out that “ketamine...

Sickle-Cell Patients and Hydroxyurea: Examining Methodology and Design

Qualitative Methodology and Design In their study, Walker, Farzan, Gaydos, DeCastro, and Jonassaint (2016) discussed the perceptions of Hydroxyurea among patients suffering from the sickle-cell disease (SCD). Since the authors of the study focused primarily on the qualitative aspects of the issue, the qualitative research method was preferred. Particularly, an...

Dose-Response Concept in Toxicology

The concept of dose-response is widely used in many biological disciplines and, in particular, in toxicology. According to Calabrese (2016), this dependency reflects the relationship between a specific dose of a particular substance and the number of those affected. In toxicology, this concept is utilized to identify the tendency to...

Psychopharmacology: Mental Health Medications

The term mental illness is used to describe a particular model or behavioral disorder characterized by unusual actions and motifs (Hart & Ksir, 2014). A patient suffering from mental disorders demonstrates a set of symptoms that deteriorate the quality of his/her life significantly. For this reason, there is a great...

Hydroxyurea Therapy for Sickle Cell Disease

HU Effects on Progression of SCD Symptoms Sickle cell disease (SCD) is associated with specific chronic and acute patient complications, including organ and tissue damage and severe episode of sickle cell crisis (SCC), which increase the risk for premature mortality. However, research evidence suggests that HU may change the prognosis...

Pharmacology of Drugs and Abuse: Alprazolam and Adderall

Alprazolam General Description Alprazolam is an anxiolytic agent, a triazolobenzodiazepine derivative that has sedative, anticonvulsant, and central muscle relaxant effect. The drug is marked by the anxiolytic activity that is expressed in the reduction of emotional stress, anxiety, and panic attacks, which is combined with a moderately pronounced hypnotic effect...

Generic Drugs vs Name Brand Drugs

Market structure According to the US government report of 2007, the market structure for both the prescription drugs (brand-name drugs) and generic drugs are changing significantly. It notes that for the last four decades there, is a small increase, in demand, for prescription drugs due to the increasing use of...

Prescription Drug Abuse as a Health Issue

Even though following the prescriptions of doctors and strict adherence to the course of treatment are mandatory conditions for the recovery process, excessive attachment to certain drugs may become a problem. In particular, prescription drug abuse is the issue that is relevant today and should be discussed at the state...

Pharmaceutical Industry in History and Future

History of the Industry The pharmaceutical industry is a relatively new industry, the origins of which can be traced to the mid-19th century. Until that time, there was no mass production of drugs; apothecaries relied mainly on natural remedies, which were ineffective in solving the most prevalent health issues of...