Leonetti G, Sala C, Bianchini C, Terzoli L, Zanchetti A
Eur J Clin Pharmacol. 1980 Nov;18(5):375-82. doi: 10.1007/BF00636788.
In 12 in-patients with moderate uncomplicated hypertension, maintained on constant sodium intake for 15 days, single-blind oral administration of verapamil 80-160 mg t.i.d. for 10 days had a significant antihypertensive effect: in the supine position systolic blood pressure decreased from 177 +/- 5 to 150 +/- 3 mmHg, and diastolic pressure from 111 +/- 3 to 96 +/- 2 mmHg; standing values were similarly lowered from 171 +/- 7 to 143 +/- 4 mmHg, systolic, and from 118 +/- 4 to 97 +/- 2 mmHg, diastolic. The heart rate did not show any significant change (from 79 +/- 3 to 77 +/- 2 beats/min, supine, and from 92 +/- 3 to 87 +/- 3 beats/min, upright). The antihypertensive effect was uniform throughout the day, being similar 2, 3, 6 and 8 h after administration of a dose. Dynamic exercise (75-100 watts on a cycle-ergometer) caused identical increases in arterial pressure and heart rate on the last day of placebo and again on the last day with verapamil, but the peak levels of systolic pressure reached during exercise were lower after verapamil than with placebo, because of the lower blood pressure before exercise. Reduction of arterial pressure by verapamil was not accompanied by increased plasma renin activity, or by renal retention of sodium and water: there was a small increase in sodium excretion, at least during the first days of verapamil administration (from 107 +/- 15 to 113 +/- 15 mEq Na+/day), and a slight significant reduction in body weight (from 74.2 +/- 3.7 to 73.5 +/- 3.7 kg). It is concluded that oral administration of verapamil significantly lowers blood pressure without simultaneously inducing cardiac stimulation, renin secretion or salt and water retention.
12例中度单纯性高血压住院患者,维持恒定钠摄入量15天,单盲口服维拉帕米80 - 160mg,每日3次,共10天,有显著降压效果:仰卧位收缩压从177±5降至150±3mmHg,舒张压从111±3降至96±2mmHg;站立位收缩压从171±7降至143±4mmHg,舒张压从118±4降至97±2mmHg。心率无显著变化(仰卧位从79±3降至77±2次/分钟,站立位从92±3降至87±3次/分钟)。全天降压效果均一,给药后2、3、6和8小时相似。动态运动(在自行车测力计上75 - 100瓦)在安慰剂最后一天和维拉帕米最后一天引起的动脉压和心率升高相同,但由于运动前血压较低,维拉帕米治疗后运动期间收缩压峰值低于安慰剂。维拉帕米降低动脉压未伴有血浆肾素活性增加,也未伴有钠和水的肾潴留:至少在维拉帕米给药的最初几天,钠排泄略有增加(从107±15增至113±15mEq Na⁺/天),体重略有显著下降(从74.2±3.7降至73.5±3.7kg)。结论是口服维拉帕米可显著降低血压,同时不会引起心脏刺激、肾素分泌或盐和水潴留。