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钙拮抗剂之间的差异:作用持续时间和谷峰比。

Differences between calcium antagonists: duration of action and trough to peak ratio.

作者信息

Meredith P A, Reid J L

机构信息

Department of Medicine and Therapeutics, Gardiner Institute, Western Infirmary, Glasgow, UK.

出版信息

J Hypertens Suppl. 1993 Mar;11(1):S21-6. doi: 10.1097/00004872-199303001-00004.

Abstract

UNLABELLED

Comparison of first- and second-generation calcium antagonists: Despite their diversity of structure, the first-generation calcium antagonists nifedipine, verapamil and diltiazem all have a short elimination half-life and a relatively short duration of action. In contrast, there appears to be wide diversity in these properties among the newer calcium antagonists, which are mostly dihydropyridines. The longer half-life and physicochemical properties of some of the newer agents allow full 24-h blood pressure control. Duration of action of lacidipine: Taken only once a day, lacidipine has proved as potent an antihypertensive agent as slow-release nifedipine administered twice a day. Lacidipine produces a satisfactory fall in blood pressure not only during waking hours but also during sleep at night, as shown by 24-h ambulatory monitoring. Moreover, this blood pressure fall is obtained without any reflex tachycardia or associated side effects. Compared with patients treated with placebo, systolic and mean arterial blood pressure variability (standard deviation) is reduced by lacidipine treatment.

CONCLUSIONS

Control of blood pressure using lacidipine once a day meets the criteria proposed by the United States Food and Drugs Administration for antihypertensive drug efficacy and duration of action.

摘要

未标注

第一代与第二代钙拮抗剂的比较:尽管第一代钙拮抗剂硝苯地平、维拉帕米和地尔硫䓬结构各异,但它们的消除半衰期均较短,作用持续时间也相对较短。相比之下,较新的钙拮抗剂(大多为二氢吡啶类)在这些特性上似乎存在很大差异。一些较新药物较长的半衰期和理化性质使得能够实现全天24小时的血压控制。拉西地平的作用持续时间:每天仅服用一次,拉西地平已被证明是一种与每天服用两次的缓释硝苯地平效力相当的抗高血压药物。24小时动态监测显示,拉西地平不仅在清醒时间,而且在夜间睡眠期间都能使血压令人满意地下降。此外,这种血压下降是在没有任何反射性心动过速或相关副作用的情况下实现的。与接受安慰剂治疗的患者相比,拉西地平治疗可降低收缩压和平均动脉血压变异性(标准差)。

结论

每天使用一次拉西地平控制血压符合美国食品药品监督管理局提出的抗高血压药物疗效和作用持续时间的标准。

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