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| Content Provider | World Health Organization (WHO)-Global Index Medicus |
|---|---|
| Author | Testa, Bernard |
| Description | Author Affiliation: Testa B ( Department of Pharmacy, University Hospital Centre (CHUV), Rue du Bugnon, CH-1011 Lausanne. Bernard.Testa@chuv.ch) |
| Abstract | Two related and significant issues may elicit perplexity in medicinal chemists and are discussed here. First, a broad presentation of the pharmacological and toxicological consequences of drug metabolism should justify the significance of drug metabolism and serve as an incentive to further study. When comparing the pharmacological activities of a drug and its metabolite(s), a continuum is found which ranges from soft drugs (no active metabolites) to prodrugs (inactive per se, as illustrated here with clopidogrel and prasugrel). Innumerable intermediate cases document drugs whose activity is shared by one or more metabolites, as exemplified with tamoxifen. The toxicological consequences of metabolism at the molecular, macromolecular, and macroscopic levels are manyfold. A brief overview is offered together with a summary of the reactions of toxification and detoxification of the antiepileptic valproic acid. The second issue discussed in the review is a comparison of the relative significance of cytochromes P450 and other oxidoreductases (EC 1), hydrolases (EC 3), and transferases (EC 2) in drug metabolism, based on a 'guesstimate' of the number of drug metabolites that are known to be produced by them. The conclusion is that oxidoreductases are the main enzymes responsible for the formation of toxic or active metabolites, whereas transferases play the major role in producing inactive and nontoxic metabolites. |
| File Format | HTM / HTML |
| ISSN | 16121872 |
| Issue Number | 11 |
| Volume Number | 6 |
| e-ISSN | 16121880 |
| Journal | Chemistry & Biodiversity |
| Language | English |
| Publisher | Wiley |
| Publisher Date | 2009-11-01 |
| Publisher Place | Switzerland |
| Access Restriction | One Nation One Subscription (ONOS) |
| Subject Keyword | Discipline Biochemistry Discipline Chemistry Chemistry, Pharmaceutical Pharmaceutical Preparations Metabolism Animals Biotransformation Drug-related Side Effects And Adverse Reactions Forecasting Humans Pharmacology Prodrugs Pharmacokinetics Xenobiotics Journal Article Review |
| Content Type | Text |
| Resource Type | Article |
| Subject | Chemistry Medicine Molecular Biology Biochemistry Molecular Medicine Bioengineering |
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