Ebihara A, Tsuru M, Ohashi K, Fujimura A, Kondo K
Department of Clinical Pharmacology, Medical College of Oita, Japan.
Arzneimittelforschung. 1987 Dec;37(12):1388-91.
A new compound, 9-chloro-5-oxo-7-(1H-tetrazol-5-yl)-5H-[1]-benzopyrano[2,3- b]pyridine sodium salt pentahydrate (traxanox sodium, Y-12141) has been shown to exert uricosuric effect in animal experiments. This study was performed to investigate the pharmacokinetics and pharmacological effects of this compound in healthy subjects by double-blind, cross-over comparison with placebo. The urine volume and urinary electrolytes increased significantly after single oral doses of 120 and 360 mg. Urinary excretion of uric acid tended to increase and serum uric acid decreased significantly. Traxanox sodium did not induce any significant change in blood pressure and pulse rate. These results suggest that traxanox sodium is a useful diuretic agent with uricosuric effect.
一种新化合物,9-氯-5-氧代-7-(1H-四氮唑-5-基)-5H-[1]-苯并吡喃并[2,3-b]吡啶钠盐五水合物(曲克索钠,Y-12141)在动物实验中已显示出促尿酸尿作用。本研究旨在通过与安慰剂进行双盲、交叉比较,调查该化合物在健康受试者中的药代动力学和药理作用。单次口服120毫克和360毫克后,尿量和尿电解质显著增加。尿酸的尿排泄量有增加趋势,血清尿酸显著降低。曲克索钠未引起血压和脉搏率的任何显著变化。这些结果表明,曲克索钠是一种具有促尿酸尿作用的有用利尿剂。