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拉西地平。对其药效学、药代动力学特性及治疗高血压的潜力的综述。

Lacidipine. A review of its pharmacodynamic and pharmacokinetic properties and therapeutic potential in the treatment of hypertension.

作者信息

Lee C R, Bryson H M

机构信息

Adis International Limited, Auckland, New Zealand.

出版信息

Drugs. 1994 Aug;48(2):274-96. doi: 10.2165/00003495-199448020-00010.

DOI:10.2165/00003495-199448020-00010
PMID:7527328
Abstract

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.

摘要

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。

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2
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本文引用的文献

1
Radioligand and functional estimates of the interaction of the 1,4-dihydropyridines, isradipine and lacidipine, with calcium channels in smooth muscle.1,4 - 二氢吡啶类药物伊拉地平与拉西地平与平滑肌钙通道相互作用的放射性配体及功能评估
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Effects of lacidipine on experimental models of atherosclerosis.
从 FDA 批准药物库中筛选和鉴定拉沙病毒进入抑制剂。
J Virol. 2018 Jul 31;92(16). doi: 10.1128/JVI.00954-18. Print 2018 Aug 15.
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Effect assessment of "film coating and packaging" on the photo-stability of highly photo-labile antihypertensive products.“薄膜包衣与包装”对光敏感性高的抗高血压产品光稳定性的影响评估
Int J Pharm Investig. 2013 Apr;3(2):77-87. doi: 10.4103/2230-973X.114903.
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[Headache and hypertension. Myth and evidence].[头痛与高血压。误区与证据]
Nervenarzt. 2010 Aug;81(8):963-72. doi: 10.1007/s00115-010-2996-6.
6
Lacidipine: a review of its use in the management of hypertension.拉西地平:用于高血压管理的综述
Drugs. 2003;63(21):2327-56. doi: 10.2165/00003495-200363210-00008.
7
Dose linearity of lacidipine pharmacokinetics after single and repeated oral doses in healthy volunteers.健康志愿者单次及多次口服拉西地平后药代动力学的剂量线性关系。
Clin Pharmacokinet. 2003;42(1):99-106. doi: 10.2165/00003088-200342010-00004.
拉西地平对动脉粥样硬化实验模型的影响。
J Hypertens Suppl. 1993 Mar;11(1):S61-6. doi: 10.1097/00004872-199303001-00011.
4
Effects of calcium antagonists on left ventricular structure and function.钙拮抗剂对左心室结构和功能的影响。
J Hypertens Suppl. 1993 Mar;11(1):S33-7. doi: 10.1097/00004872-199303001-00006.
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Differences between calcium antagonists: duration of action and trough to peak ratio.钙拮抗剂之间的差异:作用持续时间和谷峰比。
J Hypertens Suppl. 1993 Mar;11(1):S21-6. doi: 10.1097/00004872-199303001-00004.
6
Calcium channel blockers protect transplant patients from cyclosporine-induced daily renal hypoperfusion.钙通道阻滞剂可保护移植患者免受环孢素诱导的每日肾脏低灌注影响。
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Heart Vessels. 1993;8(1):16-22.
8
Metabolic effects of lacidipine: a placebo-controlled study using the euglycaemic hyperinsulinaemic clamp.拉西地平的代谢效应:一项采用正常血糖高胰岛素钳夹技术的安慰剂对照研究。
Br J Clin Pharmacol. 1993 Jan;35(1):40-5.
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Ca2+ channel blocking activity of lacidipine and amlodipine in A7r5 vascular smooth muscle cells.拉西地平与氨氯地平对A7r5血管平滑肌细胞的钙离子通道阻滞活性
Eur J Pharmacol. 1993 Jan 15;244(2):139-44. doi: 10.1016/0922-4106(93)90019-6.
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In vitro effects of the new calcium antagonist lacidipine.新型钙拮抗剂拉西地平的体外效应
Jpn J Pharmacol. 1993 Jul;62(3):289-96. doi: 10.1254/jjp.62.289.