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拉贝洛尔的R,R-异构体二利洛尔对轻至中度原发性高血压患者血压及肾功能的影响。

Effects of dilevalol, an R, R-isomer of labetalol, on blood pressure and renal function in patients with mild-to-moderate essential hypertension.

作者信息

Baba T, Murabayashi S, Aoyagi K, Ishizaki T

机构信息

Third Department of Internal Medicine, Hirosaki University School of Medicine, Tokyo, Japan.

出版信息

Eur J Clin Pharmacol. 1988;35(1):9-15. doi: 10.1007/BF00555500.

Abstract

The effects of oral dilevalol (an R, R-isomer of labetalol), a new beta-adrenoceptor blocker with beta 2-receptor stimulating and alpha-recepter blocking properties on blood pressure, renal function, plasma renin activity (PRA) and plasma aldosterone have been studied in 15 patients with mild-to-moderate essential hypertension treated with it for 6 weeks. Two patients with apparent treatment failure and one patient who developed muscle pain and cramps, and had an elevated creatine phosphokinase level, were excluded from the study. Dilevalol monotherapy 100 mg once daily for 6 weeks significantly lowered both the systolic and diastolic blood pressure compared to placebo. Total renal vascular resistance was significantly reduced, and RBF and GFR remained unchanged. Dilevalol significantly decreased PRA. The results suggest that prolonged daily treatment with dilevalol preserves renal function and produces a concomitant hypotensive action in patients with mild-to-moderate essential hypertension. The ancillary pharmacological properties of dilevalol rather than PRA suppression may be relevant to its renal effects.

摘要

已对15例轻度至中度原发性高血压患者进行了为期6周的研究,观察新型β肾上腺素能受体阻滞剂口服双醋洛尔(拉贝洛尔的R,R-异构体),该药物具有刺激β2受体和阻断α受体的特性,对血压、肾功能、血浆肾素活性(PRA)和血浆醛固酮的影响。两名明显治疗失败的患者以及一名出现肌肉疼痛和痉挛且肌酸磷酸激酶水平升高的患者被排除在研究之外。与安慰剂相比,每日一次100 mg双醋洛尔单药治疗6周可显著降低收缩压和舒张压。总肾血管阻力显著降低,肾血流量(RBF)和肾小球滤过率(GFR)保持不变。双醋洛尔显著降低PRA。结果表明,对于轻度至中度原发性高血压患者,长期每日使用双醋洛尔可保护肾功能并产生相应的降压作用。双醋洛尔的辅助药理特性而非PRA抑制作用可能与其肾脏效应有关。

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