乐卡地平：其在高血压管理中的功效综述。,Drugs

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乐卡地平：其在高血压管理中的功效综述。
Drugs ( IF 13.0 ) Pub Date : 2003-11-12 , DOI: 10.2165/00003495-200363220-00013
Lynne M Bang ₁ , Therese M Chapman , Karen L Goa

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UNLABELLED乐卡地平（Zanidip）是一种血管选择性二氢吡啶钙通道拮抗剂，可通过阻止钙离子通过细胞膜中的L型钙通道流入而引起全身性血管舒张。它是一种高度亲脂性药物，与其他钙通道拮抗剂相比，起效较慢，作用时间更长。此外，乐卡地平可能具有与其降压作用无关的抗动脉粥样硬化活性。在两项涉及约16000例轻至中度高血压患者的大型，无盲，非对照研究中，使用10-20 mg乐卡地平治疗12周后，收缩压（BP）[SBP]和舒张压（DBP）显着降低/天。此外，在最大的研究中，有64％的患者为缓解者（DBP < 治疗12周后，血压恢复至90 mm Hg（90 mm Hg），另有32％的血压恢复正常（BP <140/90 mm Hg）。在比较试验中，乐卡地平10-20 mg /天与硝苯地平20-40 mg每天两次，氨氯地平10 mg /天，非洛地平10-20 mg /天，硝苯地平胃肠治疗系统（GITS）30一样有效在2-16周的治疗后，轻度至中度高血压的患者每天-60 mg或维拉帕米SR 240 mg /天，可降低SBP和DBP。此外，乐卡地平治疗4周（10毫克/天）与卡托普利25毫克/天，阿替洛尔50毫克/天或氢氯噻嗪12.5毫克/天一样有效。乐卡地平5-30 mg /天与轻度至中度高血压或单纯收缩期高血压的老年患者（> 60岁）有效降低BP，其程度与氨氯地平5-10 mg /天相同，治疗24-26周后，硝苯地平GITS 30-60 mg /天或拉西地平2-4 mg /天。此外，有限的研究表明，lercanidipine在重度或耐药性高血压患者，2型糖尿病高血压患者和绝经后轻度至中度原发性高血压患者中可能具有降压功效。乐卡地平具有良好的耐受性，大多数与血管舒张有关的紧急治疗事件。常见的不良事件包括头痛，潮红和周围水肿。重要的是，接受乐卡地平的患者血管舒张性水肿的发生率明显低于接受其他钙通道拮抗剂的患者。结论每天一次乐卡地平是轻度至中度高血压患者的一种有效且耐受性良好的降压药。

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Lercanidipine : a review of its efficacy in the management of hypertension.

UNLABELLED Lercanidipine (Zanidip) is a vasoselective dihydropyridine calcium channel antagonist that causes systemic vasodilation by blocking the influx of calcium ions through L-type calcium channels in cell membranes. It is a highly lipophilic drug that exhibits a slower onset and longer duration of action than other calcium channel antagonists. Furthermore, lercanidipine may have antiatherogenic activity unrelated to its antihypertensive effect. In two large, nonblind, noncomparative studies involving approximately 16 000 patients with mild-to-moderate hypertension, systolic blood pressure (BP) [SBP] and diastolic BP (DBP) were significantly reduced after 12 weeks' treatment with lercanidipine 10-20 mg/day. Furthermore, in the largest study, 64% of patients were responders (DBP <90 mm Hg) after 12 weeks of treatment and an additional 32% had their BP normalised (BP <140/90 mm Hg). In comparative trials, lercanidipine 10-20 mg/day was as effective as nifedipine slow release (SR) 20-40 mg twice daily, amlodipine 10 mg/day, felodipine 10-20 mg/day, nifedipine gastrointestinal therapeutic system (GITS) 30-60 mg once daily or verapamil SR 240 mg/day at reducing SBP and DBP in patients with mild-to-moderate hypertension after 2-16 weeks of therapy. In addition, 4 weeks of lercanidipine therapy (10 mg/day) was as effective as captopril 25mg twice daily, atenolol 50 mg/day or hydrochlorothiazide 12.5 mg/day. Lercanidipine 5-30 mg/day effectively decreased BP in elderly patients (aged >60 years) with mild-to-moderate hypertension or isolated systolic hypertension to the same extent as amlodipine 5-10 mg/day, nifedipine GITS 30-60 mg/day or lacidipine 2-4 mg/day after 24-26 weeks of therapy. In addition, a limited number of studies suggest that lercanidipine may have antihypertensive efficacy in patients with severe or resistant hypertension, in hypertensive patients with type 2 diabetes mellitus and in postmenopausal women with mild-to-moderate essential hypertension. Lercanidipine is well tolerated, with most treatment-emergent events related to vasodilation. Common adverse events included headache, flushing and peripheral oedema. Importantly, the incidence of vasodilatory oedema was significantly lower in patients receiving lercanidipine than in those receiving some other calcium channel antagonists. CONCLUSION Once-daily lercanidipine is an effective and well tolerated antihypertensive agent in patients with mild-to-moderate hypertension.

更新日期：2019-11-01

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