Intestinal absorption and metabolism of clioquinol in the rat.

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Abstract
Plasma concentrations of clioquinol [a drug which causes neurotoxicity] and its metabolites after single or repeated oral administration of clioquinol, absorption region of clioquinol in the gastrointestinal tract and intestinal metabolism were studied in rats. Plasma concentrations of clioquinol after oral administration of 4 different doses (20, 100, 200 and 400 mg/kg) were lower than those of the 2 metabolites, clioquinol glucuronide and sulfate. Mean maximal plasma concentration of unchanged drug was in the range of 1-8 nmol/ml. Clioquinol was absorbed poorly from the stomach and fairly from the small intestine. Bile was an important route for excretion of clioquinol in rats. The mesenteric venous plasma from the closed intestinal loops of both jejunal and ileac regions was analyzed for clioquinol and the metabolites; clioquinol glucuronide was formed predominantly in both regions. Intestinal metabolism of clioquinol is evidently a major factor in causing clioquinol intoxication.