Higgens C S, Scott J T
Br J Clin Pharmacol. 1984 Sep;18(3):439-43. doi: 10.1111/j.1365-2125.1984.tb02486.x.
Azapropazone is an anti-inflammatory agent with reported uricosuric properties. The aim of the present study was to extend these observations, by examining the dose-response and to compare the uricosuric effect of azapropazone with that of probenecid. Patients were given varying doses of azapropazone from 900-2400 mg daily for 4-day periods at separated intervals. Plasma uric acid levels were measured before and at the end of each treatment period. Three other patients maintained on low purine diets were given a 4-day course of 1200 mg azapropazone daily followed at an interval by a 4-day period of probenecid 1 g daily. Plasma uric acid levels and 24 h urinary uric acid excretion were compared. The mean fall in plasma uric acid level after four days of 900 mg azapropazone daily was 31.4% (n = 9) compared with 33.9% (n = 12) on 1200 mg daily; 42.3% (n = 10) on 1800 mg daily; and 46% (n = 6) on 2400 mg daily, indicating a graded dosage response. In the three patients on low purine diets the falls in plasma uric acid levels on probenecid 1 g daily were 50.5%, 46% and 29% compared with 33.5%, 32% and 20% respectively on azapropazone 1200 mg daily. Similarly the total amount of uric acid excreted in the urine by each patient during the 4-day period on probenecid 1 g daily was 14.01; 13.03 and 8.97 mmol compared with 23.53, 10.9 and 7.69 mmol on azapropazone 1200 mg daily.(ABSTRACT TRUNCATED AT 250 WORDS)
阿扎丙宗是一种据报道具有促尿酸排泄特性的抗炎药。本研究的目的是通过研究剂量反应来扩展这些观察结果,并比较阿扎丙宗与丙磺舒的促尿酸排泄作用。患者在不同间隔期接受为期4天、每日900 - 2400毫克不等剂量的阿扎丙宗治疗。在每个治疗期开始前和结束时测量血浆尿酸水平。另外三名维持低嘌呤饮食的患者接受为期4天、每日1200毫克阿扎丙宗的疗程,之后间隔一段时间接受为期4天、每日1克丙磺舒的疗程。比较血浆尿酸水平和24小时尿尿酸排泄量。每日服用900毫克阿扎丙宗4天后,血浆尿酸水平平均下降31.4%(n = 9),而每日服用1200毫克时为33.9%(n = 12);每日服用1800毫克时为42.3%(n = 10);每日服用2400毫克时为46%(n = 6),表明存在剂量反应梯度。在三名低嘌呤饮食患者中,每日服用1克丙磺舒时血浆尿酸水平下降分别为50.5%、46%和29%,而每日服用1200毫克阿扎丙宗时分别为33.5%、32%和20%。同样,在每日服用1克丙磺舒的4天期间,每位患者尿中排泄的尿酸总量分别为14.01、13.03和8.97毫摩尔,而每日服用1200毫克阿扎丙宗时分别为23.53、10.9和7.69毫摩尔。(摘要截断于250字)