Medicinal Chemistry for Pharmacy Students

Author(s): Rahmat Talukder, Ashok Philip and M. O. Faruk Khan

DOI: 10.2174/9781681086873118010010

Drug Metabolism

Pp: 188-280 (93)

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Abstract

SHS investigation development is considered from the geographical and historical viewpoint. 3 stages are described. Within Stage 1 the work was carried out in the Department of the Institute of Chemical Physics in Chernogolovka where the scientific discovery had been made. At Stage 2 the interest to SHS arose in different cities and towns of the former USSR. Within Stage 3 SHS entered the international scene. Now SHS processes and products are being studied in more than 50 countries.

Abstract

This chapter is a detailed account of drug metabolism, prodrugs and related terminology that are critical knowledge base for pharmacist and pharmacy education. After study of this chapter, students will be able to: • Comprehend the fundamental concepts of drug metabolism • Describe the significance of drug metabolism • Identify key enzymes involved and the sites of drug metabolism • Explain phase I and phase II metabolic pathways, including: ♦ Phase I (Functionalization) - Oxidation of aromatic moieties, olefins, benzylic & allylic C atoms and α-C of C=O and C=N, aliphatic and alicyclic C, C-heteroatom system, C-N (N-dealkylation, Noxide formation, N-hydroxylation), C-O (O-dealkylation), C-S (S-dealkylation, Soxidation, desulfuration), alcohols and aldehydes, and miscellaneous oxidative reactions - Reduction of aldehydes and ketones, Nitro and azo compounds, and miscellaneous reductive metabolisms - Hydrolytic reactions of esters and amides, epoxides and arene oxides by epoxide hydrase ♦ Phase II (Conjugation) - Glucuronic acid conjugation, sulfate conjugation, glycine and other amino acid, glutathione or mercapturic acid, acetylation, methylation - Define and differentiate between prodrug, soft drug and antedrugs - Discuss metabolic routes of some individual drugs

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