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马尼地平:用于高血压管理的综述

Manidipine: a review of its use in the management of hypertension.

作者信息

McKeage Kate, Scott Lesley J

机构信息

Adis International Limited, Auckland, New Zealand.

出版信息

Drugs. 2004;64(17):1923-40. doi: 10.2165/00003495-200464170-00011.

DOI:10.2165/00003495-200464170-00011
PMID:15329044
Abstract

Manidipine is a lipophilic, third-generation dihydropyridine calcium channel antagonist with a high degree of selectivity for the vasculature, thereby inducing marked peripheral vasodilation with negligible cardiodepression. In addition, manidipine does not significantly affect norepinephrine levels, suggesting a lack of sympathetic activation. It has a gradual onset of action and a long duration of action enabling once daily administration. Furthermore, manidipine dilates both the efferent and the afferent renal arterioles and appears to have beneficial renal effects unrelated to its antihypertensive effect. Once-daily oral manidipine is an effective and generally well tolerated antihypertensive agent for younger and elderly adult patients with mild-to-moderate hypertension. In particular, in a large double-blind trial, the incidence of ankle oedema was significantly lower in manidipine than in amlodipine recipients. Manidipine is also effective in hypertensive patients with comorbidities, such as type 2 diabetes mellitus and/or renal impairment, and appears to improve insulin sensitivity without affecting metabolic function. Thus, manidipine represents a first-line treatment option for patients with essential mild-to-moderate hypertension.

摘要

马尼地平是一种亲脂性的第三代二氢吡啶类钙通道拮抗剂,对血管系统具有高度选择性,从而可引起显著的外周血管舒张,而心脏抑制作用可忽略不计。此外,马尼地平对去甲肾上腺素水平无显著影响,提示不存在交感神经激活。其起效缓慢,作用持续时间长,可每日给药一次。此外,马尼地平可扩张肾出球小动脉和入球小动脉,且似乎具有与其降压作用无关的有益肾脏效应。每日一次口服马尼地平对轻至中度高血压的年轻和老年成年患者是一种有效且耐受性普遍良好的抗高血压药物。特别是,在一项大型双盲试验中,马尼地平治疗患者的踝部水肿发生率显著低于氨氯地平治疗患者。马尼地平对合并2型糖尿病和/或肾功能损害等合并症的高血压患者也有效,且似乎可改善胰岛素敏感性而不影响代谢功能。因此,马尼地平是原发性轻至中度高血压患者的一线治疗选择。

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Effects of efonidipine, an L- and T-Type dual calcium channel blocker, on heart rate and blood pressure in patients with mild to severe hypertension: an uncontrolled, open-label pilot study.L型和T型双钙通道阻滞剂依福地平对轻至重度高血压患者心率和血压的影响:一项非对照、开放标签的试点研究。
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