Zachariah P K, Sheps S G, Schriger A
J Clin Hypertens. 1986 Sep;2(3 Suppl):133S-142S.
The potential antihypertensive effect of sustained-release (SR) verapamil was compared to immediate-release (IR) verapamil in a group of patients with essential hypertension. All patients were withdrawn from their previous antihypertensive medication(s) and were entered into an open-label IR verapamil study (dose varying from 80 to 120 mg TID). Patients were subsequently randomized in a double-blind fashion to continue the same dose of IR verapamil or an equivalent dose of SR verapamil. Automatic ambulatory blood pressure recordings were carried out with a Del Mar Avionics PIII Unit in eight patients who were randomized into the SR group. An initial 24-hour recording was performed on the IR verapamil group during the open-label phase and repeated following treatment with SR verapamil. Mean 24-hour systolic blood pressure (SPB) and diastolic blood pressure (DBP) were 143 +/- 18 mmHg and 89 +/- 6 mmHg, respectively, on IR verapamil and 142 +/- 22 and 90 +/- 6 mmHg, respectively, on SR verapamil. There were no statistically significant differences noted between the two groups. Mean SBP and DBP varied similarly during waking and sleeping periods with IR and SR verapamil: With IR verapamil, SBP was 139 +/- 18 and 124 +/- 20 mmHg and DBP was 92 +/- 11 and 84 +/- 13 mmHg during waking and sleeping hours, respectively; with SR verapamil, SBP was 138 +/- 21 and 122 +/- 22 mmHg and DBP 92 +/- 10 and 80 +/- 10 mmHg during waking and sleeping hours, respectively. DBP was less than or equal to 90 mmHg in approximately 70% and 60% of patients in the IR verapamil and SR verapamil groups, respectively. Trough plasma levels of 92 +/- 44 and 67 +/- 32 ng/ml were measured by HPLC, 2 and 4 weeks, respectively, after treatment with IR verapamil. During a similar time interval, SR verapamil revealed plasma levels of 64 +/- 59 and 92 +/- 57 ng/ml, respectively. No correlation between change in DBP and plasma level of verapamil was demonstrated. No significant change in heart rate was observed during the 4-week period. In summary, verapamil is an effective antihypertensive medication and can be administered once a day as a slow-releasing preparation; it is most useful in patients in whom adrenergic blocking drugs are indicated.
在一组原发性高血压患者中，比较了缓释维拉帕米与速释维拉帕米的潜在降压效果。所有患者均停用先前的抗高血压药物，进入一项开放标签的速释维拉帕米研究（剂量为每日三次，每次80至120毫克）。随后，患者以双盲方式随机分组，继续服用相同剂量的速释维拉帕米或等效剂量的缓释维拉帕米。对随机分配到缓释组的8名患者，使用德尔玛航空电子PIII装置进行自动动态血压记录。在开放标签阶段，对速释维拉帕米组进行了首次24小时记录，并在接受缓释维拉帕米治疗后重复记录。服用速释维拉帕米时，平均24小时收缩压（SPB）和舒张压（DBP）分别为143±18 mmHg和89±6 mmHg；服用缓释维拉帕米时，分别为142±22 mmHg和90±6 mmHg。两组之间未发现统计学上的显著差异。服用速释和缓释维拉帕米时，平均收缩压和舒张压在清醒和睡眠期间的变化相似：服用速释维拉帕米时，清醒和睡眠时的收缩压分别为139±18 mmHg和124±20 mmHg，舒张压分别为92±11 mmHg和84±13 mmHg；服用缓释维拉帕米时，清醒和睡眠时的收缩压分别为138±21 mmHg和122±22 mmHg，舒张压分别为92±10 mmHg和80±10 mmHg。速释维拉帕米组和缓释维拉帕米组分别约70%和60%的患者舒张压≤90 mmHg。服用速释维拉帕米治疗2周和4周后，通过高效液相色谱法测得的谷浓度血浆水平分别为92±44 ng/ml和67±32 ng/ml。在相似的时间间隔内，缓释维拉帕米的血浆水平分别为64±59 ng/ml和92±57 ng/ml。未证明舒张压变化与维拉帕米血浆水平之间存在相关性。在4周期间未观察到心率有显著变化。总之，维拉帕米是一种有效的抗高血压药物，可作为缓释制剂每日给药一次；对需要使用肾上腺素能阻断药物的患者最为有用。
