Pettersson A, Persson B, Berglund G, Hedner T
Clin Pharmacol Ther. 1985 Aug;38(2):188-94. doi: 10.1038/clpt.1985.157.
We evaluated the long-term antihypertensive effects of ketanserin, a selective serotonin2-receptor blocker with weak adrenergic receptor blocker properties. Ketanserin was given alone, 40 mg o.d. or b.i.d., for 2 years to 12 patients with essential hypertension. Systolic and diastolic blood pressures (BPs) were significantly reduced 14 days after the start of therapy and remained lowered during the 2-year follow-up period. In a larger group of patients who received ketanserin monotherapy for 2 to 3 months, the response to therapy varied considerably between subjects, with an overall response rate (BP less than 165/95 mm Hg) of 60% to 75%. During steady-state conditions, the maximum and minimum ketanserin plasma concentrations varied from threefold to fourfold between subjects and did not correlate with individual reductions in BP, but for each individual there was a positive correlation between BP reduction and ketanserin plasma concentration throughout a study day. In combination with beta-blockers, ketanserin effectively reduced BP in the supine and standing positions. The plasma concentration profile was not altered as much during combination therapy as when ketanserin was given alone. Side effects were few and tolerable. Ketanserin effectively reduces BP both alone and in combination with beta-blockers and may be still another drug useful in the treatment of essential hypertension.
我们评估了酮色林（一种具有弱肾上腺素能受体阻断特性的选择性5-羟色胺2受体阻滞剂）的长期降压效果。12例原发性高血压患者单独服用酮色林，每日40毫克，一日一次或一日两次，持续2年。治疗开始14天后，收缩压和舒张压均显著降低，并在2年随访期内持续保持较低水平。在一大组接受酮色林单药治疗2至3个月的患者中，个体对治疗的反应差异很大，总体有效率（血压低于165/95毫米汞柱）为60%至75%。在稳态条件下，个体间酮色林的最大和最小血浆浓度相差3至4倍，且与个体血压降低情况无关，但在整个研究日中，每个个体的血压降低与酮色林血浆浓度之间呈正相关。与β受体阻滞剂联合使用时，酮色林能有效降低仰卧位和站立位的血压。联合治疗期间，血浆浓度曲线的变化幅度不如单独使用酮色林时大。副作用很少且可耐受。酮色林单独使用或与β受体阻滞剂联合使用时均能有效降低血压，可能是另一种治疗原发性高血压的有效药物。
