The following pharmacology definition has been taken from the Pharmacology and Experimental Therapeutics Department Glossary at Boston University School of Medicine.
The period of time required for the concentration or amount of drug in the body to be reduced to exactly one-half of a given concentration or amount. The given concentration or amount need not be the maximum observed during the course of the experiment, or the concentration or amount present at the beginning of an experiment, since the half-life is completely independent of the concentration or amount chosen as the “starting point “. Half-lives can be computed and interpreted legitimately only when concentration or amount varies with time according to the law appropriate to the kinetics of a first order reaction: the common logarithm of the concentration or amount is related linearly to time, e.g.:
where C is concentration at time t, a (in logarithmic units) is the intercept of the line with the ordinate, and b (which has a negative sign) is the slope of the line. The parameters of the equation can be estimated from the plot of experimental values of log C and t. The half-life can be computed simply by dividing the slope of the curve into 0.301, the difference between the logarithm of a number (C) and the logarithm of number half as large (C/2); the symbol for half-life is t1/2.
The half-life of a drug in plasma or serum is frequently taken as indicating the persistence of the drug in its volume of distribution; this interpretation may be incorrect unless the material can move freely and rapidly from one fluid compartment of the body to another, and is not bound or stored in one or another tissue. The term “biological half-life” should not be used instead of the specific terms “plasma half-life” or “serum half-life”. The tissue for which the half-life of a drug is determined should always be specified, e.g., “serum half-life”; the half-life of a drug in muscle, kidney, etc., or in the whole organism can be determined. Drug half-lives are frequently based on the results of chemical analyses, i.e., the results of the reaction of a reagent with a specific chemical group of a drug molecule; it should be remembered that detection of the group per se does not necessarily imply its continuous existence as part of a biologically active drug molecule.
A drug molecule that leaves the plasma may have any of several fates: it can be destroyed in the blood; it can be eliminated from the body; or it can be translocated to a body fluid compartment other than the intravascular to be stored, biotransformed, or to exert its pharmacodynamic effects.
When the plot of log plasma or serum concentration (during the period of its decline) against time is composed of two straight line segments, the inference may be made that two first order processes are involved in the distribution and biotransformation and elimination of the drug. The earlier phase – represented by the line segment of greater slope – is termed the distributive phase, and corresponds to the period during which translocation of the drug to its ultimate volume of distribution occurs and is the dominant process; the later phase – represented by the line of lesser slope – is termed the eliminative phase, and corresponds to the period when biotransformation and elimination of drug are dominant processes. For two-phase systems, three phase systems, etc., half-lives of the drugs in the various phases can be determined only after more sophisticated analysis of the data than that described above.
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