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维拉帕米也是一种非选择性β受体阻滞剂吗?

Is verapamil also a non-selective beta blocker?

作者信息

Drici M D, Jacomet Y, Iacono P, Lapalus P

机构信息

Department of Experimental and Clinical Pharmacology, Faculty of Medicine, Nice, France.

出版信息

Int J Clin Pharmacol Ther Toxicol. 1993 Jan;31(1):27-30.

PMID:8095251
Abstract

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.

摘要

维拉帕米是一种广泛用作抗高血压药物的钙通道阻滞剂,其药理作用可能部分归因于一定程度的β受体阻滞作用。为了评估β₂肾上腺素能受体密度的变化,在一项双盲随机研究中,40例轻至中度高血压患者在经过安慰剂导入期后,接受30天的维拉帕米240毫克(每日一次)或卡托普利20毫克(每日两次)治疗。在给予活性药物前及治疗15天后测定淋巴细胞膜β₂肾上腺素能受体密度(Bmax)。治疗一个月后,大多数患者舒张压显著降低:维拉帕米组从98.2±3.2毫米汞柱降至81.2±4.0毫米汞柱(p<0.05),卡托普利组从95.0±6.0毫米汞柱降至82.5±4.8毫米汞柱(p<0.05)。治疗15天后,维拉帕米使β₂肾上腺素能受体上调,从39.5±8.3飞摩尔/毫克蛋白升至58.5±12.0飞摩尔/毫克蛋白(p<0.05),而卡托普利组的Bmax无显著变化。两个解离常数无显著改变。这种上调现象在β₂受体阻滞剂中很常见,支持了维拉帕米具有β受体阻滞效力的假说。

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