New PDF release: Principles in General Pharmacology

By Ronald J. Tallarida Ph.D., Robert B. Raffa Ph.D., Paul McGonigle Ph.D. (auth.)

ISBN-10: 1461237785

ISBN-13: 9781461237785

ISBN-10: 1461283469

ISBN-13: 9781461283461

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Graph of In (plasma concentration) against time, illustrating binding to tissues [phase (1)] and elimination from plasma [phase (2)]. The quantity C; is obtained by extrapolation of phase (2) to time zero. an equation also linear in t, with slope -kl and interceptln A. It is convenient to use semilog graph paper when using this procedure. The half-life is obtained from the graph. 693/half-life. Also, the intercepts Band A are read directly from the vertical (logarithmically calibrated axis) instead of In A or InB.

Antagonists Antagonists are substances that reduce or abolish the effects of an active drug or chemical. Several examples of antagonists were given previously (p. 14). The term "pharmacologic" antagonism has been used when the agonist and antagonist act on the same drug receptor. Most pharmacologic antagonists are of the reversible (also known as competitive) type, that is, the effect of the antagonist can be overcome with sufficiently high doses of the agonist. Accordingly, the dose-response curve of the agonist is merely shifted to the right, meaning that higher doses of the agonist are needed at any level of effect.

K . D (Co - C)lh where h is the membrane thickness. 1. Flux, amount/time, through area A is proportional to the concentration gradient dc/dx. The latter is approximately (Co - CJlh. 4) The permeability constant is a characteristic of the drug and the membrane. 5) When all the drug is on the outside of the membrane, a time we call t = 0, Ci = 0, and the initial flux is proportional to the outer concentration. Experimentally, one may isolate the membrane, vary Co, and measure the initial flux. 2).

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Principles in General Pharmacology by Ronald J. Tallarida Ph.D., Robert B. Raffa Ph.D., Paul McGonigle Ph.D. (auth.)


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