Lee C R, Bryson H M
Adis International Limited, Auckland, New Zealand.
Drugs. 1994 Aug;48(2):274-96. doi: 10.2165/00003495-199448020-00010.
Lacidipine is an orally administered calcium channel blocker of the dihydropyridine class, which shows selectivity for vascular smooth muscle over cardiac tissue and has a long duration of action. In studies using ambulatory blood pressure monitoring, lacidipine 2 to 8mg administered once daily in the morning reduced blood pressure over 24 hours, with the reductions being greater during the day than at night in some studies. 77 to 87% of patients with mild to moderate hypertension had their blood pressure controlled by treatment with lacidipine 2 to 8 mg/day for 1 to 4 months in dose-finding studies. When administered once daily, lacidipine 4 to 6 mg was equivalent in antihypertensive efficacy to hydrochlorothiazide 25 to 50 mg/day, atenolol 50 to 100 mg/day, and the prototype calcium channel blocker nifedipine 20 to 40 mg twice daily (sustained-release formulation). The adverse effects of lacidipine are those common to other dihydropyridine calcium channel blockers, and include headache, flushing, ankle oedema, dizziness and palpitations. The long term effects of lacidipine on cardiovascular morbidity and mortality, and possible additional clinical benefits in terms of its antiatherosclerotic effects, are under investigation; the outcome of these studies will be important in defining the future role of this agent in the treatment of hypertension. Thus, available evidence suggests lacidipine provides a further alternative to the dihydropyridine calcium channel blockers currently available for the treatment of essential hypertension.
拉西地平是一种口服的二氢吡啶类钙通道阻滞剂,对血管平滑肌的选择性高于心脏组织,且作用持续时间长。在使用动态血压监测的研究中,每日早晨一次服用2至8毫克拉西地平可使血压在24小时内降低,在一些研究中,白天的降幅大于夜间。在剂量探索研究中,77%至87%的轻度至中度高血压患者通过每日服用2至8毫克拉西地平治疗1至4个月,血压得到控制。每日一次服用时,4至6毫克拉西地平的降压疗效与每日25至50毫克氢氯噻嗪、每日50至100毫克阿替洛尔以及原型钙通道阻滞剂硝苯地平每日两次(缓释制剂)20至40毫克相当。拉西地平的不良反应是其他二氢吡啶类钙通道阻滞剂常见的不良反应,包括头痛、面部潮红、脚踝水肿、头晕和心悸。拉西地平对心血管发病率和死亡率的长期影响以及其抗动脉粥样硬化作用可能带来的额外临床益处正在研究中;这些研究的结果对于确定该药物在高血压治疗中的未来作用至关重要。因此,现有证据表明拉西地平为目前可用于治疗原发性高血压的二氢吡啶类钙通道阻滞剂提供了又一种选择。