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The metabolic fate of tritium labeled econazole in man

The metabolic fate of tritium labeled econazole in man

Xenobiotica 11(9): 595-608

Following single oral doses of [3H]econazole base (500 mg) to 2 human subjects, excretion of radioactivity was prolonged and incomplete after 5 days (means of 40 and 27% dose in urine and feces, respectively). Plasma concentration of unchanged econazole and total radioactivity attained peak values at about the same time for each subject (1.5-3 h) but the former declined much faster than the latter. Most of the 3H in early plasma samples was present as unchanged drug and extractable metabolites but after 24 h concentration of econazole were close to the limit of detection (0.04 .mu.g/ml) and very little plasma 3H was extractable, whereas total 3H concentrations were still measurable after 5 days (mean 1.54 .mu.g/ml). Thus, plasma contained metabolites with much longer half-lives than econazole. The main route of biotransformation of econazole in man involved multiple oxidation of the imidazole ring carbons followed by O-dealkylation and conjugation of the resulting alcohols, probably with glucuronic acid.

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