Pentikainen P J, Neuvonen P J, Tarpila S, Syvälahti E
Br Med J. 1978 Sep 23;2(6141):861-3. doi: 10.1136/bmj.2.6141.861.
The pharmacokinetics of chlormethiazole were studied in eight patients with advanced cirrhosis of the liver and in six healthy volunteers after oral and intravenous administration of the drug. In the patients the systemic bioavailability of oral chlormethiazole was increased about tenfold, whereas its elimination was only slightly retarded. The increased bioavailability was clearly due to decreased first-pass metabolism of chlormethiazole in the cirrhotic liver. The results indicate that chlormethiazole should be used in reduced dosage when given by mouth to patients with cirrhosis of the liver.
在8例晚期肝硬化患者和6名健康志愿者口服及静脉注射氯美噻唑后,对其药代动力学进行了研究。在患者中,口服氯美噻唑的全身生物利用度提高了约10倍,而其消除仅略有延迟。生物利用度增加显然是由于肝硬化肝脏中氯美噻唑的首过代谢减少。结果表明,给肝硬化患者口服氯美噻唑时应减少剂量。