MacLeod S M, Sellers E M, Giles H G, Billings B J, Martin P R, Greenblatt D J, Marshman J A
Clin Pharmacol Ther. 1978 Nov;24(5):583-9. doi: 10.1002/cpt1978245583.
The disposition of chlordiazepoxide (50 mg, intravenously), diazepam (0.143 mg/kg, orally), and oxazepam (0.429 mg/kg, orally) were studied in normal and alcoholic men before and after chronic disulfiram administration. Decreases in the plasma clearance of chlordiazepoxide (54%, p less than 0.05), diazepam (41%, p less than 0.05), and their active N-desmethyl metabolites were observed. Oxazepam has no important active metabolites and its net disposition is minimally altered by disulfiram. Oxazepam disposition is unaffected by age and liver disease. These considerations together with that of the short half-life of oxazepam (median, 6.1 hr) suggest that oxazepam may be the drug of choice if benzodiazepine therapy is used for patients taking disulfiram.
在慢性服用双硫仑前后,对正常男性和酗酒男性研究了氯氮卓(50毫克,静脉注射)、地西泮(0.143毫克/千克,口服)和奥沙西泮(0.429毫克/千克,口服)的处置情况。观察到氯氮卓(54%,p<0.05)、地西泮(41%,p<0.05)及其活性N-去甲基代谢物的血浆清除率降低。奥沙西泮没有重要的活性代谢物,其净处置情况受双硫仑的影响最小。奥沙西泮的处置不受年龄和肝病的影响。这些因素以及奥沙西泮较短的半衰期(中位数为6.1小时)表明,如果对服用双硫仑的患者使用苯二氮䓬类药物治疗,奥沙西泮可能是首选药物。