Abstract
Any attempt to review the current state of knowledge in rapidly changing fields of pharmacology is faced with the common problem of all expanding areas — knowledge has advanced so fast in such a short time that good work completed as little as 10 years ago may now be rendered completely out of date. Although concepts change fairly rapidly, it is supremely technological advance that has transformed our understanding of the biotransformation and kinetics of drugs in all species. Twenty years ago the ability to detect very small quantities of drugs in biological fluids was strictly limited. The developments in gas—liquid and high pressure liquid chromatography and the application of the mass spectrometer to the identification of drug metabolites has now put certainty into many areas that were previously uncertain. With technological advance comes inevitable conceptual change. Perhaps one of the best examples of this in the context of adrenergic inhibitory drugs is the change in our appreciation of the handling of reserpine. Twenty years ago, reserpine was categorically a “hit and run” drug, that is, it could be detected, whether in humans or in animals, only for a very brief while after administration, yet its pharmacological effects clearly were prolonged. Dogma stated that the drug affected its target organ by dealing a lightning blow but the recovery from that onslaught had to continue for days or weeks after the drug had left the organism. It is clear now in retrospect that techniques for measuring both reserpine and its metabolites were simply not adequate, that reserpine enters a deep store in adrenergic vesicles and that there is no need to postulate persistence of action beyond the physical presence of the drug in the biological system.
This review covers the literature up to April/May, 1978
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Smith, A.J., Tucker, G.T. (1981). Kinetics and Biotransformation of Adrenergic Inhibitors. In: Szekeres, L. (eds) Adrenergic Activators and Inhibitors. Handbook of Experimental Pharmacology, vol 54 / 2. Springer, Berlin, Heidelberg. https://doi.org/10.1007/978-3-642-67584-3_12
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