McCormack Paul L, Wagstaff Antona J
Adis International Limited, Auckland, New Zealand.
Drugs. 2003;63(21):2327-56. doi: 10.2165/00003495-200363210-00008.
Lacidipine (Caldine, Lacimen, Lacipil, Midotens, Motens) is a once-daily, orally-administered, lipophilic dihydropyridine calcium antagonist with an intrinsically slow onset of activity, resulting in a lack of reflex tachycardia. It has a long duration of action and a high degree of vascular selectivity. In addition to calcium channel-modulated vasodilation, lacidipine displays antioxidant activity greater than that of other dihydropyridine calcium antagonists. In randomised, well-controlled trials, lacidipine 2-6 mg orally once daily had antihypertensive efficacy similar to that of other long-acting dihydropyridine calcium antagonists, thiazide diuretics, atenolol (a beta-blocker) and enalapril (an ACE inhibitor). Lacidipine was effective in elderly patients (including those with isolated systolic hypertension), African Nigerian patients and patients with concurrent type 2 diabetes mellitus. During long-term treatment for 4 or 5 years in patients with isolated systolic hypertension or essential hypertension, the incidence of cardiovascular events and mortality with lacidipine was similar to that with chlorthalidone or atenolol. The European Lacidipine Study on Atherosclerosis (ELSA), in which 2334 patients with hypertension were randomised to 4 years of therapy with lacidipine 4-6 mg/day or the beta-blocker atenolol 50-100 mg/day, demonstrated significantly lower atherosclerotic progression and plaque formation with lacidipine compared with atenolol in patients completing the full 4 years of the study. Between-group differences in favour of lacidipine for the primary efficacy variable (mean change in carotid artery intima-media thickness) did not reach statistical significance in the intent-to-treat population. The tolerability profile of lacidipine (headache, flushing, pedal oedema, dizziness and palpitations) is similar to that of other dihydropyridine calcium antagonists, but with a lower incidence of peripheral oedema. Data from the ELSA study suggest that the incidence of serious adverse events during long-term lacidipine therapy is similar to that with atenolol.
Lacidipine is an effective, well tolerated, once-daily, oral antihypertensive agent that can be used in a wide variety of patients. As with other members of its class, lacidipine has shown potentially beneficial antiatherosclerotic effects, although definitive data with respect to possible superiority over other drug classes are still required. Therefore, lacidipine is an attractive therapy for the long-term management of essential hypertension.
拉西地平(卡尔地平、乐息平、司乐平、米多坦、莫坦)是一种每日服用一次的口服亲脂性二氢吡啶类钙拮抗剂,起效内在缓慢,不会引起反射性心动过速。它作用持续时间长,具有高度的血管选择性。除了钙通道调节的血管舒张作用外,拉西地平还表现出比其他二氢吡啶类钙拮抗剂更强的抗氧化活性。在随机、严格对照试验中,每日口服一次2 - 6毫克拉西地平的降压疗效与其他长效二氢吡啶类钙拮抗剂、噻嗪类利尿剂、阿替洛尔(一种β受体阻滞剂)和依那普利(一种ACE抑制剂)相似。拉西地平对老年患者(包括单纯收缩期高血压患者)、非洲尼日利亚患者以及合并2型糖尿病的患者均有效。在单纯收缩期高血压或原发性高血压患者中进行4或5年的长期治疗期间,拉西地平治疗的心血管事件发生率和死亡率与氯噻酮或阿替洛尔相似。欧洲拉西地平动脉粥样硬化研究(ELSA)将2334例高血压患者随机分为两组,分别接受4年的4 - 6毫克/天拉西地平治疗或50 - 100毫克/天β受体阻滞剂阿替洛尔治疗,结果显示,在完成整个4年研究的患者中,与阿替洛尔相比,拉西地平组的动脉粥样硬化进展和斑块形成明显更低。在意向性治疗人群中,拉西地平在主要疗效变量(颈动脉内膜中层厚度的平均变化)方面优于阿替洛尔的组间差异未达到统计学意义。拉西地平的耐受性特征(头痛、面部潮红、足部水肿、头晕和心悸)与其他二氢吡啶类钙拮抗剂相似,但外周水肿的发生率较低。ELSA研究的数据表明,长期使用拉西地平治疗期间严重不良事件的发生率与阿替洛尔相似。
拉西地平是一种有效、耐受性良好的每日一次口服降压药,可用于各类患者。与其同类其他药物一样,拉西地平已显示出潜在有益的抗动脉粥样硬化作用,尽管仍需要关于其相对于其他药物类别可能具有优越性的确切数据。因此,拉西地平是原发性高血压长期管理的一种有吸引力的治疗药物。