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Pharmacology is the body of knowledge concerned with the action of chemicals on biologic systems. Medical pharmacology is the area of pharmacology concerned with the use of chemicals in the prevention, diagnosis, and treatment of disease, especially in humans. Toxicology is the area of pharmacology concerned with the undesirable effects of chemicals on biologic systems. Pharmacokinetics describes the effects of the body on drugs, for example, absorption, metabolism, excretion, etc. Pharmacodynamics denotes the actions of the drug on the body, such as mechanism of action and therapeutic and toxic effects. The first part of this chapter reviews the basic principles of pharmacokinetics and pharmacodynamics that will be applied in subsequent chapters. The second part of the chapter reviews the discovery and development of new drugs and the regulation of drugs by government agencies.



Drugs in common use include inorganic ions, nonpeptide organic molecules, small peptides and proteins, nucleic acids, lipids, and carbohydrates. Some are found in plants or animals, and others are partially or completely synthetic. Many drugs found in nature are alkaloids, molecules that create a basic (alkaline) pH in solution, usually as a result of amine groups in their structure. Many biologically important endogenous molecules and exogenous drugs are optically active; that is, they contain one or more asymmetric centers and can exist as enantiomers. The enantiomers of optically active drugs usually differ, sometimes more than 1000-fold, in their affinity for biologic receptor sites. Furthermore, such enantiomers may be metabolized at different rates in the body, with important clinical consequences.

A. Size and Molecular Weight

Drugs vary in size from molecular weight (MW) 7 (lithium) to over MW 50,000 (thrombolytic enzymes, antibodies, other proteins). Most drugs, however, have MWs between 100 and 1000. Drugs smaller than MW 100 are rarely sufficiently selective in their actions, whereas drugs much larger than MW 1000 are often poorly absorbed and poorly distributed in the body. Most protein drugs (“biologicals”) are commercially produced in cell, bacteria, or yeast cultures using recombinant DNA technology.

B. Drug-Receptor Bonds

Drugs bind to receptors with a variety of chemical bonds. These include very strong covalent bonds (which usually result in irreversible action), somewhat weaker reversible electrostatic bonds (eg, between a cation and an anion), and much weaker interactions (eg, hydrogen, van der Waals, and hydrophobic bonds).


A. Receptors

With few exceptions, drug actions are mediated through the effects of drug ligand molecules on drug receptors in the body. Most receptors are large regulatory molecules that influence important biochemical processes (eg, enzymes involved in glucose metabolism) or physiologic processes (eg, ion channel receptors, neurotransmitter reuptake transporters, and ion transporters).

If drug-receptor binding results in activation of the receptor molecule, ...

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