Stokes G S, Mennie B A, Marwood J F
Clin Pharmacol Ther. 1986 Jul;40(1):56-63. doi: 10.1038/clpt.1986.139.
A randomized crossover trial was conducted in 15 patients with essential hypertension to compare the actions of prazosin, a specific alpha 1-adrenoceptor blocker, and ketanserin, an antagonist at alpha 1-adrenergic and serotonin receptors. After placebo dosing for 2 weeks, active drug was given double-blind in two 4-week phases. Satisfactory control of supine blood pressure was obtained in nine of the 12 subjects who completed the prazosin phase and 11 of the 15 subjects who completed the ketanserin phase. Whether comparison was based on supine, erect, postexercise, or ambulatory values, the blood pressure responses to prazosin (2 or 4 mg/day) and ketanserin (40 or 80 mg/day) were closely similar. Neither of the drugs significantly altered supine or erect pulse rates, body weight, serum triglyceride concentrations, plasma renin activity, or urinary aldosterone excretion, and their side effect profiles were similar. The serum cholesterol concentration was lowered by prazosin but was not affected by ketanserin. However, no other features were observed that distinguished the clinical effects of ketanserin from those of prazosin.
对15例原发性高血压患者进行了一项随机交叉试验，以比较特异性α1肾上腺素能受体阻滞剂哌唑嗪和α1肾上腺素能及5-羟色胺受体拮抗剂酮色林的作用。在服用2周安慰剂后，在两个4周阶段双盲给予活性药物。在完成哌唑嗪阶段的12名受试者中有9名以及完成酮色林阶段的15名受试者中有11名仰卧血压得到了满意控制。无论比较是基于仰卧、直立、运动后还是动态血压值，哌唑嗪（2或4毫克/天）和酮色林（40或80毫克/天）的血压反应都非常相似。两种药物均未显著改变仰卧或直立脉搏率、体重、血清甘油三酯浓度、血浆肾素活性或尿醛固酮排泄，且它们的副作用情况相似。哌唑嗪可降低血清胆固醇浓度，但酮色林对其无影响。然而，未观察到其他能区分酮色林和哌唑嗪临床效果的特征。
