Davi H, Guyonnet J, Sales Y, Cautreels W
Arzneimittelforschung. 1985;35(7):1061-5.
The metabolism of ethyl loflazepate (Victan), a new benzodiazepine used as an anxiolytic drug, was studied in man and several animal species. The urinary metabolites were determined and quantified following oral administration of the 14C-labeled drug. Further analysis of blood samples was carried out in order to get information on the circulating metabolites in man. Except the rat, from which only 25% of the administered dose were excreted via the kidneys, the urine appeared to be the main excretion route in man (63%) and the other animal species (80%). The major urinary metabolites were identified as being loflazepate, 3-hydroxyloflazepate, 3-hydroxydescarbethoxyloflazepate, 4'-hydroxydescarbethoxyloflazepate and 6-chloro-4-(2'-fluorophenyl)-2(1H)-quinazolinone. The observed differences on the excretion patterns between the species resulted from the presence of a large number of quantitatively minor metabolites. Analysis of human blood samples indicated that the radioactivity was almost entirely in the plasma. The main circulating metabolites were detected as descarbethoxyloflazepate, loflazepate, and 3-hydroxydescarbethoxyloflazepate.
对用作抗焦虑药物的新型苯二氮䓬类药物氯氟䓬乙酯（维克坦）在人体和几种动物物种中的代谢情况进行了研究。口服14C标记药物后，对尿液代谢物进行了测定和定量分析。为了获取人体中循环代谢物的信息，还对血样进行了进一步分析。除大鼠外，给药剂量中只有25%通过肾脏排出，尿液似乎是人体（63%）和其他动物物种（80%）的主要排泄途径。主要的尿液代谢物被鉴定为氯氟䓬乙酯、3-羟基氯氟䓬乙酯、3-羟基去甲羧基氯氟䓬乙酯、4'-羟基去甲羧基氯氟䓬乙酯和6-氯-4-(2'-氟苯基)-2(1H)-喹唑啉酮。物种间排泄模式的差异是由大量含量较少的代谢物导致的。对人体血样的分析表明，放射性几乎完全存在于血浆中。检测到的主要循环代谢物为去甲羧基氯氟䓬乙酯、氯氟䓬乙酯和3-羟基去甲羧基氯氟䓬乙酯。
