McCormack P M, Cox J P, Marron J, Mee F, Atkins N, O'Brien E, O'Malley K
Blood Pressure Unit, Beaumont Hospital, Dublin, Ireland.
J Hum Hypertens. 1990 Oct;4(5):565-70.
To assess the role of the serotonin antagonist ketanserin in the management of hypertension in the elderly, 12 patients with a mean age of 68 years (range 60-79 years) were treated with ketanserin in a randomised double-blind placebo-controlled cross-over trial. Clinic BP, ambulatory BP, renal function, and pharmacokinetics were assessed. The doses of ketanserin used were 40 mg (ten patients) and 20 mg (two patients) twice daily for 8 weeks. Mean clinic sitting BP was reduced from 169 +/- 5/98 +/- 2 on placebo to 155 +/- 5/88 +/- 3 mmHg (NS/P less than 0.05/P less than 0.05) and standing pressure from 168 +/- 6/100 +/- 3 to 157 +/- 5/91 +/- 3 mmHg (NS/P less than 0.01). Mean ambulatory systolic BP was unaffected by active treatment (167 +/- 7 vs 164 +/- 5) while diastolic pressure was lowered from 99 +/- 2 to 94 +/- 2 mmHg (P less than 0.05). This effect appeared to be mainly confined to the first two hours after drug administration. Renal blood flow was unaltered by treatment. The mean plasma half-life of ketanserin was 20.9 +/- 5.5 hours. Side effects were minimal. In conclusion, while ketanserin may be effective as assessed in the clinic, its efficacy on ambulatory monitoring is substantially less impressive.
为评估5-羟色胺拮抗剂酮色林在老年高血压治疗中的作用,在一项随机双盲安慰剂对照交叉试验中,对12例平均年龄68岁(范围60 - 79岁)的患者使用酮色林进行治疗。评估了临床血压、动态血压、肾功能和药代动力学。所用酮色林的剂量为每日两次,40 mg(10例患者)和20 mg(2例患者),共8周。平均临床坐位血压从安慰剂组的169±5/98±2降至155±5/88±3 mmHg(无显著性差异/ P < 0.05 / P < 0.05),站立位血压从168±6/100±3降至157±5/91±3 mmHg(无显著性差异/ P < 0.01)。主动治疗对平均动态收缩压无影响(167±7对164±5),而舒张压从99±2降至94±2 mmHg(P < 0.05)。这种效应似乎主要局限于给药后的前两小时。治疗未改变肾血流量。酮色林的平均血浆半衰期为20.9±5.5小时。副作用极小。总之,虽然酮色林在临床评估中可能有效,但其对动态血压监测的疗效远不如预期。