The absorption, metabolism and elimination of (±)-N-(2-benzoyloxyethyl)norfenfluramine (JP992) in man

Abstract

Abstract The urinary excretion of N-(2-benzoyloxyethyl)norfenfluramine (JP 992) was examined in man with normal and acidic urine after oral administration of the drug; 86–100% of the dose was excreted in 48 h as metabolites of the drug having m-trifluoromethylbenzyl and benzoyl moieties, but no unchanged drug was detected. Norfenfluramine, N-2-hydroxyethylnorfenfluramine, and a metabolite, which on treatment with zinc and hydrochloric acid gave norfenfluramine, were excreted in urine. N-2-Hydroxyethylnorfenfluramine and a second unidentified metabolite were also excreted as both sulphate and glucuronide conjugates.