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三种不同剂量伊拉地平单次给药对高血压患者心血管和肾脏的影响。不同效应的剂量反应曲线。

Cardiovascular and renal effects of single administration of three different doses of isradipine in hypertensive patients. Dose-response curves of the different effects.

作者信息

Rupoli L, Fruscio M, Gradnik R, Chianca R, Leonetti G, Zanchetti A

机构信息

Istituto di Clinica Medica Generale e Terapia Medica, Università di Milano, Italy.

出版信息

Am J Med. 1989 Apr 17;86(4A):65-6. doi: 10.1016/0002-9343(89)90193-9.

Abstract

The antihypertensive, humoral, and renal effects of acute single oral administration of placebo and isradipine, a new dihydropyridine calcium antagonist, at doses of 2.5 mg, 5.0 mg, and 7.5 mg once daily were investigated in 11 patients with mild-to-moderate uncomplicated essential hypertension. The patients maintained a constant daily intake of 100 mmol of sodium and 40 mmol of potassium. Placebo and isradipine were randomly administered to each patient, according to a Latin-square design, at intervals of at least 48 hours. The antihypertensive effect was dose-dependent and peaked at two hours after oral administration; changes at the lowest dose were already statistically significant (p less than 0.01). Increases in heart rate were mild and similar with all isradipine doses. Glomerular filtration rate and renal plasma flow showed a trend towards a dose-dependent rise; plasma renin activity was statistically increased (p less than 0.05) following the highest isradipine dose, whereas plasma aldosterone was unmodified. Isradipine resulted in a statistically significant rise (p less than 0.05) in sodium excretion and urine volume, which was similar with all active doses. In conclusion, the antihypertensive efficacy of isradipine is dose-dependent, whereas the natriuretic and diuretic effects are already at maximum following 2.5 mg per day, the lowest dose in this study.

摘要

对11例轻度至中度无并发症的原发性高血压患者,研究了每日一次口服安慰剂以及2.5毫克、5.0毫克和7.5毫克剂量的新型二氢吡啶类钙拮抗剂伊拉地平的急性单剂量给药后的降压、体液和肾脏效应。患者维持每日100毫摩尔钠和40毫摩尔钾的恒定摄入量。根据拉丁方设计,在至少48小时间隔下,将安慰剂和伊拉地平随机给予每位患者。降压作用呈剂量依赖性,口服后两小时达到峰值;最低剂量时的变化已具有统计学意义(p小于0.01)。所有伊拉地平剂量下心率的增加均较轻微且相似。肾小球滤过率和肾血浆流量呈剂量依赖性升高趋势;最高伊拉地平剂量后血浆肾素活性有统计学意义的增加(p小于0.05),而血浆醛固酮未改变。伊拉地平使钠排泄和尿量有统计学意义的增加(p小于0.05),所有有效剂量下均相似。总之,伊拉地平的降压疗效呈剂量依赖性,而利钠和利尿作用在本研究的最低剂量每日2.5毫克时已达最大。

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