Ticrynafen: Kinetics, protein binding, and effects on serum and urinary uric acid
Ticrynafen: Kinetics, protein binding, and effects on serum and urinary uric acid
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Ticrynafen：动力学、蛋白质结合以及对血清和尿尿酸的影响
DOI：
10.1002/cpt1978236697
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发表时间：
1978
影响因子：
6.7
通讯作者：
F. O. Simpson
中科院分区：
文献类型：
--
作者：
A. Wood;P. Bolli;H. Waal‐Manning;F. O. Simpson
本文研究了新型利尿剂替昔那芬在4例正常人体内的动力学和急性效应。在给予250毫克片剂的4名受试者中，有3名受试者在1至2小时内达到15至35微克/毫升的血浆替昔那芬浓度峰值；在第四名受试者中，在6小时时达到10µg/ml的峰值浓度。消除半衰期为2.0 ~ 3.3小时。生物利用度范围为2.5倍（61.7-154.6µg·hr·ml−1）。以2小时为间隔给予相同剂量的四分之一剂量，可使血浆替昔那芬浓度在8小时时逐渐上升至5.5至12.9µg/ml，然后以与单次剂量相似的速度下降。单剂量和分剂量治疗的降尿酸效果相似：尿酸浓度在1小时内开始下降，在7至10小时达到药物前值的53%至77%，并在24小时恢复到药物前值。两种治疗均可显著增加尿尿酸排泄达12小时。单次给药利尿作用持续4 ~ 8小时，分次给药利尿作用持续8 ~ 12小时。
The kinetics and acute effects of ticrynafen, a new diuretic and uricosuric, have been studied in 4 normal subjects. In 3 of the 4 subjects given a 250‐mg tablet, peak plasma ticrynafen concentrations of 15 to 35 µg/ml were achieved at 1 to 2 hr; in the fourth subject a peak concentration of 10 µg/ml was attained at 6 hr. Elimination half‐life was 2.0 to 3.3 hr. Bioavailability covered a 2.5‐fold range (61.7–154.6 µg · hr · ml−1). Administration of the same dose as quarter doses at 2 hr intervals produced a progressive rise in plasma ticrynafen concentration to 5.5 to 12.9 µg/ml at 8 hr and thereafter a decline at a similar rate to that seen with the single dose. The hypouricemic effect was similar for the single‐ and divided‐dose treatments: uric acid concentration began to fall within 1 hr, reached a minimum of 53% to 77% of the pre‐drug value at 7 to 10 hr, and had returned to approximately pre‐drug values at 24 hr. Urinary uric acid excretion was significantly increased for up to 12 hr with both treatments. The diuretic effect of the single dose lasted 4 to 8 hr, while that of the divided dose lasted 8 to 12 hr.