Wortmann R L, Ridolfo A S, Lightfoot R W, Fox I H
J Rheumatol. 1985 Jun;12(3):540-3.
The antihyperuricemic properties of amflutizole were investigated in studies designed to determine its efficacy and mechanisms of action in individuals with gout and hyperuricemia. In a randomized double blind, multiple dose, crossover study of 29 patients, amflutizole caused a significant dose dependent reduction in serum urate concentrations. Mean serum urate concentrations decreased significantly from 9.6 +/- 1.5 mg/dl to 7.2 +/- 1.3 mg/dl with the 500 mg dosage (p less than 0.01). Detailed studies in 5 patients demonstrated evidence for modest xanthine oxidase inhibition. However, the majority of the antihyperuricemic effect was derived from an enhanced renal clearance of uric acid. Although the drug has significant antihyperuricemic properties, these were inadequate to achieve adequate control of the serum urate concentration in hyperuricemia and gout at the doses utilized.
在旨在确定安氟噻唑对痛风和高尿酸血症患者的疗效及作用机制的研究中,对其抗高尿酸血症特性进行了调查。在一项针对29名患者的随机双盲、多剂量、交叉研究中,安氟噻唑使血清尿酸盐浓度出现显著的剂量依赖性降低。500毫克剂量组的平均血清尿酸盐浓度从9.6±1.5毫克/分升降至7.2±1.3毫克/分升,差异有统计学意义(p<0.01)。对5名患者的详细研究显示有适度抑制黄嘌呤氧化酶的证据。然而,抗高尿酸血症作用的大部分源自尿酸肾清除率的提高。尽管该药物具有显著的抗高尿酸血症特性,但在所使用的剂量下,这些特性不足以充分控制高尿酸血症和痛风患者的血清尿酸盐浓度。