The Metabolism of N-(3-Chlorobenzenesulphonyl) acetamidine in the Dog and Rat

Abstract

1. In the dog, the major metabolite of N-(3-ab-acetamidine is N-(3-chlorobenzenesulphonyl)amidinocarboxylic acid. 3-Chlorobenzenesulphonamide and an unidentified glucuronide are also formed as metabolites.

2. The drug stimulates its own metabolism in the dog, as repeated dosing causes a reduction in half-life of the drug from 35.2 to 11.7 h and an increase in the excretion of polar metabolites in the urine.

3. In the rat, N-(3-chloro-4-hydroxybenzenesulphonyl)acetamidine and its glucuronide are major metabolites. As in the case of the dog, 3-Chlorobenzenesulphonamide is also a metabolite. Repeated dosing of the drug to the rat causes an increase in the metabolism of the drug.