Ilson B E, Martin D E, Boike S C, Jorkasky D K
SmithKline Beecham Clinical Pharmacology Unit, Presbyterian Medical Center of Philadelphia, University of Pennsylvania Health System 19104, USA.
J Clin Pharmacol. 1998 May;38(5):437-41. doi: 10.1002/j.1552-4604.1998.tb04450.x.
The effects of antihypertensive agents, including angiotensin II receptor antagonists, on urine uric acid excretion may have important clinical consequences. Therefore, the effects of single and repeated doses of eprosartan on uric acid excretion were evaluated in 57 male patients with mild-to-moderate essential hypertension in a double-blind, randomized, placebo-controlled, repeated dose, dose-rising, two-period, period-balanced, crossover study conducted in two parts. In part 1 (n = 33), the effects of eprosartan dose regimens of 50 mg, 100 mg, and 350 mg once daily and 150 mg every 12 hours on uric acid excretion were assessed. In part 2 (n = 24), the effects of eprosartan dose regimens of 600 mg, 800 mg, and 1,200 mg once daily on uric acid excretion were assessed. Eprosartan was well tolerated. There were no appreciable changes from predose values in fractional excretion of uric acid (FEua), urine uric acid excretion, urine uric acid to creatinine (Uua/Ucr) ratios, or serum uric acid concentrations after single or repeated doses of eprosartan. Mean Uua/Ucr ratios for eprosartan doses of 50 mg, 100 mg, or 350 mg daily or 150 mg every 12 hours were comparable to those for placebo. Mean FEua values and Uua/Ucr ratios for eprosartan doses of 600 mg, 800 mg, or 1,200 mg daily also were comparable to those for placebo. Single and repeated oral doses of eprosartan ranging from 50 mg to 1,200 mg daily had no effect on serum uric acid concentrations or urine uric acid excretion in patients with mild-to-moderate essential hypertension.
包括血管紧张素II受体拮抗剂在内的抗高血压药物对尿尿酸排泄的影响可能具有重要的临床意义。因此,在一项双盲、随机、安慰剂对照、重复给药、剂量递增、两阶段、阶段平衡的交叉研究中,对57例轻度至中度原发性高血压男性患者评估了单剂量和重复剂量依普罗沙坦对尿酸排泄的影响。该研究分为两个部分。在第1部分(n = 33)中,评估了每日一次50 mg、100 mg和350 mg以及每12小时150 mg的依普罗沙坦给药方案对尿酸排泄的影响。在第2部分(n = 24)中,评估了每日一次600 mg、800 mg和1200 mg的依普罗沙坦给药方案对尿酸排泄的影响。依普罗沙坦耐受性良好。单剂量或重复剂量依普罗沙坦给药后,尿酸排泄分数(FEua)、尿尿酸排泄、尿尿酸与肌酐比值(Uua/Ucr)或血清尿酸浓度与给药前值相比无明显变化。每日50 mg、100 mg或350 mg或每12小时150 mg依普罗沙坦剂量的平均Uua/Ucr比值与安慰剂相当。每日600 mg、800 mg或1200 mg依普罗沙坦剂量的平均FEua值和Uua/Ucr比值也与安慰剂相当。每日50 mg至1200 mg的单剂量和重复口服依普罗沙坦对轻度至中度原发性高血压患者的血清尿酸浓度或尿尿酸排泄无影响。