Galtier P, Coche Y, Camguilhem R
J Pharm Pharmacol. 1982 May;34(5):310-3. doi: 10.1111/j.2042-7158.1982.tb04713.x.
Levamisole [phenyl-2 3H] was injected intravenously (4.7 mg kg-1) into anaesthetized controls and rats in which cirrhosis had been induced by a combination of carbon tetrachloride and phenobarbitone. The biliary excretion (6 h) of the parent drug and its metabolites formed a significant part of the administered dose. Although bile flow did not vary, biliary excretion of levamisole and metabolites were respectively increased and decreased in cirrhotic compared with control animals. These differences could be the result of cirrhosis-induced decrease in the hepatic biotransformation of levamisole and also to limited active carrier transport for the output of metabolites into bile canaliculi.
将[苯-2 3H]左旋咪唑以4.7毫克/千克的剂量静脉注射到麻醉的对照大鼠以及用四氯化碳和苯巴比妥联合诱导肝硬化的大鼠体内。母体药物及其代谢产物的胆汁排泄(6小时)占给药剂量的很大一部分。尽管胆汁流量没有变化,但与对照动物相比,肝硬化大鼠中左旋咪唑及其代谢产物的胆汁排泄分别增加和减少。这些差异可能是由于肝硬化导致左旋咪唑的肝脏生物转化减少,以及代谢产物输出到胆小管的活性载体转运受限所致。