ISSN:
1573-8744
Keywords:
active drug metabolites
;
methsuximide
;
glutethimide
;
procainamide
;
lidocaine
Source:
Springer Online Journal Archives 1860-2000
Topics:
Chemistry and Pharmacology
Notes:
Abstract Application of pharmacokinetic principles to patient therapy requires prior elucidation of the relationship between the plasma concentration of a drug and its pharmacological effects. This relationship is complicated by the fact that many drugs are converted to active metabolites so that observed effects represent a composite of the pharmacological activity of a drug and its metabolites. In fact, discrepancies between the observed duration of drug action and the biological half-life of a given drug should suggest that an active drug metabolite may have been formed. As is illustrated by the anticonvulsant drug methsuximide, drug metabolite levels may be so much higher than those of the parent drug that only the metabolite levels are of routine clinical significance. In other cases, levels of both the parent drug and one or more metabolites must be considered together and combined according to their relative potency to give an index of total pharmacological activity. This situation poses obvious difficulties with respect to the ease and safety of drug therapy with these agents. It generally would seem preferable to treat patients with drugs that are converted to inactive metabolites or are excreted largely unchanged.
Type of Medium:
Electronic Resource
URL:
http://dx.doi.org/10.1007/BF01066214
