Nilvadipine:概要文件的一个新钙拮抗剂。概述。

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罗森塔尔J

Nilvadipine:概要文件的一个新钙拮抗剂。概述。

J Cardiovasc杂志。1994;24增刊2:s92 - 107。

PubMed ID

7898101 (在PubMed

]

文摘

Nilvadipine是一种新型的钙拮抗剂dihydropyridine组。由于其高受体亲和力,nilvadipine块l型钙通道在血管肌肉细胞。这导致长期血管放松和降低血压。与硝苯地平相比,dihydropyridines的原型,nilvadipine拥有特殊的药动学和药效学性质。行动的持续时间较长,常影响5-16倍。与硝苯地平相比,cardiodepressive行动和肾上腺素能counterregulation nilvadipine没那么强烈。Nilvadipine高等vasoselectivity表示251年血管/心脏功效系数,是硝苯地平的9倍。在治疗剂量nilvadipine没有负性肌力,变时性的,或者变导作用。在各种体外和动物实验,nilvadipine antiatherogenic行动。Nilvadipine迅速而完全被吸收。 Owing to a marked first-pass effect, the absolute bioavailability is 14-19%. The final elimination half-life is between 15 and 20 h, probably due to slow redistribution from the tissue. Nilvadipine is mainly excreted via the kidneys in the form of inactive metabolites. The pharmaceutical preparation as a depot form prevents an over-increase of the plasma level, and therefore reduces the typical side effects of dihydropyridine calcium antagonists. The pharmacokinetics of nilvadipine are not affected by reduced renal function. The bioavailability is increased in liver cirrhosis, but with repeated administration no cumulative effect takes place. Because of nilvadipine's long half-life, a once-daily administration is adequate to reduce blood pressure over 24 h in the treatment of arterial hypertension. At a daily dosage of 8-16 mg, the responder rate (RRdiast < 90 mm Hg) is 60-70% in single-drug therapy and up to 80% in combination therapy. Nilvadipine can be used to treat hypertensive patients who are also suffering from diabetes mellitus, lipometabolic disturbances, chronic obstructive respiratory tract disease, or cerebral circulatory disturbances. Owing to its high vascular selectivity, antiatherogenic properties, 24-h action, and good tolerance, nilvadipine fulfills the requirements for a modern antihypertensive agent.

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药物靶点

药物	目标	类	生物	药理作用	行动
Nilvadipine	压敏电阻器l型钙通道亚基alpha-1C	蛋白质	人类	是的	抑制剂	细节
Nilvadipine	压敏电阻器l型钙通道亚基beta 2	蛋白质	人类	是的	抑制剂	细节