Clavijo G A, de Clavijo I V, Weart C W
Broward Family Health Center, Ft. Lauderdale, FL.
Am J Hosp Pharm. 1994 Jan 1;51(1):59-68.
The chemistry, pharmacology, pharmacokinetics, efficacy, and adverse effects of amlodipine are reviewed. Amlodipine belongs to the dihydropyridine subclass of calcium antagonists. Amlodipine is a potent peripheral and coronary vasodilator with high selectivity for vascular smooth muscle and minimal effect on myocardial contractility or cardiac conduction. Absorption after oral administration is slow, and the duration of action is long, with a half-life of 36-45 hours. Amlodipine has FDA-approved labeling for use in the treatment of hypertension, chronic stable angina, and vasospastic angina. The agent is also indicated for use in hypertensive or anginal patients who also have congestive heart failure due to systolic dysfunction (New York Heart Association classes II and III). Clinical trials suggest that effective 24-hour control of hypertension and angina is provided by once-daily administration of amlodipine 5-10 mg alone or in combination with other drugs. No clinically important drug interactions have been observed to date. Amlodipine has not shown any unfavorable effects on serum glucose or lipid levels. The most common adverse effect is peripheral edema. Amlodipine is effective and well tolerated when given alone or in combination with other drugs for the treatment of hypertension and angina. Amlodipine may offer advantages over verapamil, diltiazem, and nifedipine in patients with hypertension or angina with associated congestive heart failure due to systolic dysfunction.
本文综述了氨氯地平的化学性质、药理学、药代动力学、疗效及不良反应。氨氯地平属于钙拮抗剂的二氢吡啶类。氨氯地平是一种强效的外周和冠状动脉血管扩张剂，对血管平滑肌具有高度选择性，对心肌收缩力或心脏传导影响极小。口服后吸收缓慢，作用持续时间长，半衰期为36 - 45小时。氨氯地平已获得美国食品药品监督管理局（FDA）批准用于治疗高血压、慢性稳定型心绞痛和血管痉挛性心绞痛。该药物也适用于因收缩功能障碍而患有充血性心力衰竭的高血压或心绞痛患者（纽约心脏协会II级和III级）。临床试验表明，每日一次单独服用5 - 10毫克氨氯地平或与其他药物联合使用，可有效控制高血压和心绞痛达24小时。迄今为止，尚未观察到任何具有临床意义的药物相互作用。氨氯地平对血清葡萄糖或脂质水平未显示出任何不良影响。最常见的不良反应是外周水肿。氨氯地平单独使用或与其他药物联合使用治疗高血压和心绞痛时，疗效显著且耐受性良好。在因收缩功能障碍而患有充血性心力衰竭的高血压或心绞痛患者中，氨氯地平可能比维拉帕米、地尔硫䓬和硝苯地平更具优势。
