Gresser U, Kamilli I, Kronawitter U, Zöllner N
Medizinische Poliklinik, Universität München, West Germany.
Eur J Clin Pharmacol. 1990;38(5):489-91. doi: 10.1007/BF02336689.
Irtemazole 12.5 to 50 mg in 6 healthy, normouricaemic subjects caused a maximal decrease in plasma uric acid (after 8 to 12 h) of 46.5%. The uricosuric effect began during the first 60 min after drug administration and it lasted for 7 to 24 h. Renal uric acid excretion returned to its base line value after 8 to 16 h and uric acid clearance after 10.0 to 12.0 h. Doses of irtemazole between 12.5 and 37.5 mg produced a dose-related rise in the uricosuric effect. There was no essential difference between the uricosuric effect of 37.5 mg and 50 mg irtemazole. The D50 dose (that producing a half-maximal effect) was between 16.3 mg and 34.2 mg, (average 24.7 mg). The value of irtemazole in the management of hyperuricaemia and gout remains to be determined.
在6名健康、尿酸正常的受试者中,给予12.5至50毫克的伊特马唑后,血浆尿酸在8至12小时后最大降幅为46.5%。促尿酸尿作用在给药后的最初60分钟内开始,持续7至24小时。肾脏尿酸排泄在8至16小时后恢复至基线值,尿酸清除率在10.0至12.0小时后恢复。12.5至37.5毫克的伊特马唑剂量产生了与剂量相关的促尿酸尿作用增强。37.5毫克和50毫克伊特马唑的促尿酸尿作用没有本质区别。半数有效剂量(产生最大效应一半的剂量)在16.3毫克至34.2毫克之间(平均24.7毫克)。伊特马唑在高尿酸血症和痛风治疗中的价值仍有待确定。