家兎へのClioquinolの静脈内投与による中毒発現と血漿中および組織内Clioquinol濃度

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To cause clioquinol intoxication to rabbits, a fine clioquinol suspension for injection prepared with polysorbate 80 was administered intravenously and plasma concentration of clioquinol and its metabolites, clioquinol glucuronide and sulfate, and tissue concentration of clioquinol were determined. Mean plasma concentration of clioquinol 2 min after single administration of 20 mg/kg dose of clioquinol was 165 nmol/ml and only 1.4 nmol/ml 3 h later. Plasma concentrations of the two metabolites reached maximum values within 5-15 min after administration and thereafter, decreased rapidly. Clioquinol concentration was higher in the kidney and liver than those in the other tissues. In repeated administration, plasma concentrations of clioquinol and the metabolites after the initial administration were approximately similar to those in the subsequent administration. In repeated administration of 20 mg/kg/d dose of clioquinol, 2 of 10 rabbits developed ataxia on the hind legs on the 28th and 35th days, respectively, after starting administration. Pathologically, the peripheral nerves showed an overt degeneration. In the nervous system, clioquinol concentration was higher in the sciatic nerve than that in the cerebrum and spinal cord.
社団法人日本薬学会の論文
1984-04-25