维拉帕米也是一种非选择性受体阻滞剂吗?

M D Drici, Y Jacomet, P Iacono, P Lapalus
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引用次数: 0

摘要

维拉帕米是一种钙通道阻滞剂,广泛用作降压药,其药理作用可能部分归因于某种程度的β阻断。为了评估β -2肾上腺素能受体密度的变化,在一项双盲随机研究中,40名轻中度高血压患者在安慰剂适应期后,在30天内接受维拉帕米240 mg(每天一次)或卡托普利20 mg(每天两次)治疗。在给药前和治疗15 d后测定淋巴细胞膜β -2肾上腺素能受体密度(Bmax)。治疗一个月后,大多数患者的舒张压明显降低:维拉帕米组从98.2 +/- 3.2 mmHg降至81.2 +/- 4.0 mmHg (p < 0.05),卡托普利组从95.0 +/- 6.0 mmHg降至82.5 +/- 4.8 mmHg (p < 0.05)。治疗15 d后,维拉帕米诱导β -2肾上腺素受体从39.5 +/- 8.3 fmol/mg蛋白上调至58.5 +/- 12.0 fmol/mg蛋白(p < 0.05),而卡托普利组Bmax无显著变化。两个解离常数没有明显变化。这种在β -2阻滞剂中常见的上调现象,支持了维拉帕米的β阻断效力的假设。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Is verapamil also a non-selective beta blocker?

Verapamil is a calcium channel blocker widely used as an antihypertensive agent, and its pharmacological effects may partly be due to some degree of beta blockade. In order to evaluate the changes occurring in beta-2 adrenoceptor density, 40 patients with mild to moderate hypertension received verapamil 240 mg (once a day) or captopril 20 mg (twice a day) during 30 days, in a double-blind randomized study, after a placebo run-in period. The lymphocytic membrane beta-2 adrenoceptor density (Bmax) was determined before the administration of active drugs and after a 15-day treatment. After a month of treatment, most patients showed a marked reduction of their diastolic blood pressure: from 98.2 +/- 3.2 mmHg to 81.2 +/- 4.0 mmHg (p < 0.05), in the verapamil group, and from 95.0 +/- 6.0 mmHg to 82.5 +/- 4.8 mmHg (p < 0.05) in the captopril group. After 15 days of treatment, verapamil induced an up-regulation of beta-2 adrenoceptors from 39.5 +/- 8.3 fmol/mg protein to 58.5 +/- 12.0 fmol/mg protein (p < 0.05), whereas the Bmax in the captopril group did not significantly change. No significant change occurred in the two dissociation constants. This up-regulation phenomenon, common among beta-2 blockers, supports the hypothesis of verapamil's beta blockade potency.

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