The metabolism of benzimidazole anthelmintics

Abstract

The benzimidazole carbamates are important broad-spectrum drugs for the control of helminth parasites in mammals. David Gottschall, Vassilios Theodorides and Richard Wang explain that the metabolism of these compounds depends heavily on the substituent present on carbon-5 of the benzimidazole nucleus and involves a wide variety of reactions. Work in vitro has shown that two major enzyme systems, the cytochrome P-450 family and the microsomal flavin monooxygenases are primarily responsible for these biotransformations. The parent compound is generally short-lived and its metabolites predominate in the tissues and excreta of treated animals. The metabolic pathways can be exploited therapeutically to overcome the problems of poor water solubility and adsorbtion of benzimidazoles by the development and use of more soluble prodrugs.