Andrén L, Svensson A, Dahlöf B, Eggertsen R, Hansson L
Acta Med Scand. 1983;214(2):125-30.
Ketanserin, a new 5-hydroxy-tryptamine antagonist, was given at three different dosage levels (double-blind, randomized) in a dose finding study for 2 months to 31 patients with mild to moderately severe essential hypertension. Treatment with ketanserin was then continued until 9 months had been completed. A significant antihypertensive effect was demonstrated at daily dosages of 20 mg t.i.d. or 40 mg t.i.d. The antihypertensive effect was similar to that of previous multiple drug treatment with conventional drugs. However, 60 mg t.i.d. was not acceptable, at least not as initial dosage. At this dose level, 8 out of 10 patients had to be withdrawn from the study during the initial phase due to unwanted effects. It is conceivable that alpha 1-adrenoceptor blockade may have played a role at this dose level, since postural reactions were observed which was otherwise not the case during this study. Ketanserin is a new and interesting alternative in the treatment of hypertension. At the same time it offers a tool by which the role of 5-hydroxy-tryptamine in the regulation of arterial pressure can be investigated.
酮色林是一种新型5-羟色胺拮抗剂，在一项剂量探索研究中，以三种不同剂量水平（双盲、随机）对31例轻度至中度重度原发性高血压患者进行了为期2个月的治疗。随后继续使用酮色林治疗，直至满9个月。每日剂量20毫克，每日三次或40毫克，每日三次时显示出显著的降压效果。其降压效果与先前使用传统药物进行的多种药物治疗相似。然而，每日三次60毫克是不可接受的，至少不能作为初始剂量。在此剂量水平下，10名患者中有8名在初始阶段因不良反应而不得不退出研究。可以想象，α1-肾上腺素能受体阻滞可能在这个剂量水平上起了作用，因为观察到了体位反应，而在本研究中其他情况下并未出现这种情况。酮色林是治疗高血压的一种新型且有趣的替代药物。同时，它提供了一种工具，通过它可以研究5-羟色胺在动脉血压调节中的作用。
