ISSN: 2041-6792

Clinical Investigation

Drug Metabolism High Impact Factor Journals

 The metabolism or, more accurately, the biotransformation of many drugs is a major determinant of the intensity and duration of their pharmacological and toxic effects. A knowledge of routes and rates of drug metabolism, therefore, is essential to the design of better agents and to the optimal clinical use of existing ones. Much has been written about this aspect of chemical pharmacology and innumerable texts and reviews have appeared. For comprehensive overviews i recommend Gillette and Mitchell (1975), Parke and Smith (1977) and, particularly for those with a chemical bent, the book by Testa and Jenner (1976a). I shall discuss the subject briefly and with respect to some leading questions. Many drugs are denied substantial exit from the body via the kidney and gastrointestinal tract owing to the possession of lipophilic functional groups (e.g. alkyl, phenyl) that promote reabsorption. A function of drug metabolism, therefore, is to render molecules more polar so that they might be excreted efficiently. In this way metabolism ultimately protects the body against the accumulation. Protection is not guaranteed by metabolism, however, as along the way the formation of highly reactive intermediates may be responsible for serious toxicity. Similarly, metabolic products may have greater pharmacological activity than the parent drug (e.g. morphine formed from codeine) or even quite different effects (e.g. isoniazid from iproniazid). Activation of inert compounds by metabolism also occurs. For example, prontosil, one of the first synthetic drugs, is without any antibacterial effect in vitro, but in the body is converted to active sulphanilamide. and undesirable effects of drugs and of other non-nutrient chemicals (xenobiotics) presented to it from the environment.

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