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硝苯地平与缓释阿替洛尔固定复方制剂(尼夫坦)治疗动脉高血压和心绞痛的药理作用及临床应用

[Pharmacology and clinical use of a fixed combination of nifedipine and slow release atenolol (Niften) in the treatment of arterial hypertension and angina pectoris].

作者信息

Verdecchia P

机构信息

Unità Organica di Medicina, Ospedale Generale Regionale R. Silvestrini, Perugia.

出版信息

Minerva Cardioangiol. 1993 Sep;41(9):349-63.

PMID:7903118
Abstract

Nifedipine and atenolol are first choice drugs in the treatment of arterial hypertension and angina pectoris. In both these pathologies the administration of nifedipine and atenolol in free or fixed combinations has proved extremely efficacious in patients who were not adequately controlled by either drug in monotherapy. A fixed combination of intestinal slow-release nifedipine and atenolol (Niften) was recently developed and has already undergone several comparative and double-blind clinical trials for the treatment of arterial hypertension and angina pectoris. The pharmacokinetic and pharmacodynamic characteristics of atenolol and nifedipine are not altered when these drugs are administered in fixed or free combination. It has been shown that the nifedipine-atenolol combination causes anti-hypertensive and anti-anginous effects at doses which are lower, for either of its two components, in comparison to the doses required to achieve the same effects using monotherapy. In arterial hypertension a clinically striking anti-hypertensive effect on systolic and diastolic levels is maintained for 24 hours after a single administration of slow-release nifedipine 20 mg+atenolol 50 mg. In angina pectoris, this dose must be administered every 12 hours to ensure a constant and prolonged effect of the calcium antagonist component. The association of nifedipine and atenolol does not induce notable depressive effects on myocardial contractility, except in patients with severely compromised basal resting contractile function.

摘要

硝苯地平和阿替洛尔是治疗动脉高血压和心绞痛的首选药物。在这两种病症中,对于单药治疗未能充分控制病情的患者,使用游离或固定组合形式的硝苯地平和阿替洛尔已证明极为有效。最近研发出了肠道缓释硝苯地平和阿替洛尔的固定组合制剂(硝苯洛尔),并且已经针对动脉高血压和心绞痛的治疗进行了多项比较性和双盲临床试验。当阿替洛尔和硝苯地平以固定或游离组合形式给药时,它们的药代动力学和药效学特性不会改变。研究表明,与单药治疗达到相同效果所需的剂量相比,硝苯地平 - 阿替洛尔组合以较低剂量就能产生抗高血压和抗心绞痛作用,其中两种成分中的任何一种都是如此。在动脉高血压患者中,单次服用20毫克缓释硝苯地平 + 50毫克阿替洛尔后,对收缩压和舒张压水平的显著抗高血压作用可维持24小时。在心绞痛患者中,必须每12小时服用此剂量,以确保钙拮抗剂成分产生持续且延长的作用。硝苯地平和阿替洛尔的组合除了对基础静息收缩功能严重受损的患者外,不会对心肌收缩力产生明显的抑制作用。

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