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Irtemazole

CAS No.: 129369-64-8

Irtemazole (R 60844) is a novel uricosuric substance that is valuable in the treatment of hyperuricemia and gout.
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Description Irtemazole (R 60844) is a novel uricosuric substance that is valuable in the treatment of hyperuricemia and gout.
In vivo Irtemazole(12.5至50mg;口服;6位患者)在8至12小时后使血浆尿酸浓度最大降低46.5%。利尿酸效应在用药后首60分钟内开始,并持续7至24小时。肾脏尿酸排泄在8至16小时后回到基线值,而尿酸清除率在10.0到12.0小时后恢复。12.5至37.5mg之间的Irtemazole剂量产生了与剂量相关的利尿酸效应增加。37.5mg与50mgIrtemazole的利尿酸效应之间没有本质差异。产生半最大效应的D50剂量在16.3mg至34.2mg之间(平均24.7mg)。Irtemazole在高尿酸血症和痛风管理中的价值仍待确定。[2]
Synonyms R60844, R-60844, R 60844
molecular weight 288.35
Molecular formula C18H16N4
CAS 129369-64-8
Storage |Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Solubility DMSO: 55 mg/mL (190.74 mM)
References 1. Kamilli I, et al. Pharmacokinetics and pharmacodynamics of different doses of Irtemazole in repeated application. Z Rheumatol. 1991;50(1):23-28. 2. Gresser U, et al. Uricosuric effect of different doses of irtemazole in normouricaemic subjects. Eur J Clin Pharmacol. 1990;38(5):489-491. 3. Kamilli I, et al. Uricosuric effect of irtemazole in hyperuricemic patients without and with renal insufficiency. Z Rheumatol. 1989;48(6):307-312. 4. Gresser U, et al. Rapid onset of uricosuria after oral administration of irtemazole, an uricosuric substance. Klin Wochenschr. 1989;67(20):1058-1060. 5. Gresser U,et al. Uricosuric effect of irtemazole in healthy subjects. Klin Wochenschr. 1989;67(19):971-975.