布那唑嗪治疗轻至中度动脉高血压的剂量反应研究

[Dose-response study of bunazosin in the treatment of light-to-moderate arterial hypertension].

作者信息

Marchegiano R, Lamenza F, Sarno D, Tozzi N, Fontana D, De Luca N

机构信息

II Facoltà di Medicina e Chirurgia, I Clinica Medica, Napoli.

出版信息

Minerva Cardioangiol. 1993 Oct;41(10):451-6.

PMID:7905614

Abstract

INTRODUCTION

The antagonists of alpha-adrenergic receptors were introduced in the therapy of arterial hypertension in 1950, but have had limited use due to the poor efficacy and safety of some drugs belonging to this pharmacological class. A recent molecule from this class, bunazosin, is a highly selective alpha 1-antagonist, whose long half-life allows a single daily administration. The aim of this study was to identify the minimum effective dose of bunazosin in the treatment of mild-moderate arterial hypertension.

MATERIALS AND METHODS

Patients of both sexes, aged over eighteen years, suffering from mild/moderate essential arterial hypertension were admitted to the study. The experimental design was controlled between patients; and the study was carried out in accordance with the principles of Helsinki anf Tokyo. Dosage was of 3 and 6 mg/day per os; after 2 weeks' treatment, if DBP in clinostatism > or = 95 mmHg, the dose was doubled. Treatment lasted four weeks.

RESULTS

At the end of treatment, in the group of patients initially treated with 3 mg/day, SBP, in clinostatism fell by 10.0% and DBP by 8.4% (p < 0.01 between times); in the group of patients initially treated with 6 mg/day, the reductions were of 9.2% and 6.5% respectively (p < 0.01 between times). Heart rate, electrocardiograph traces and laboratory parameters showed no clinically significant modifications. The safety profile of the treatment was excellent in 80% of the patients treated overall.

DISCUSSION

This study allowed the minimum effective dose of bunazosin, equal to 3-6 mg/day, to be identified, as well as confirming the antihypertensive efficacy of the drug and its ample safety margin. In fact, this range of daily dosage led to a fall in pressure values, without causing clinically significant alterations of heart rate, electrocardiograph traces and laboratory parameters.

CONCLUSIONS

In conclusions, in mild/moderate arterial hypertension, bunazosin in monotherapy at the dosage of 3-6 mg/day, is an effective and safe treatment.

摘要

引言

α-肾上腺素能受体拮抗剂于1950年被引入动脉高血压的治疗，但由于该类药物中某些药物疗效不佳且安全性差，其应用受到限制。该类药物中的一种新药布那唑嗪是一种高度选择性的α1-拮抗剂，其半衰期长，允许每日单次给药。本研究的目的是确定布那唑嗪治疗轻中度动脉高血压的最小有效剂量。

材料与方法

纳入年龄超过18岁、患有轻/中度原发性动脉高血压的男女患者进行研究。实验设计为患者间对照；研究按照赫尔辛基和东京宣言的原则进行。口服剂量为每日3毫克和6毫克；治疗2周后，如果卧立位舒张压≥95毫米汞柱，则剂量加倍。治疗持续四周。

结果

治疗结束时，初始治疗剂量为每日3毫克的患者组，卧立位收缩压下降10.0%，舒张压下降8.4%（不同时间点间p<0.01）；初始治疗剂量为每日6毫克的患者组，收缩压和舒张压分别下降9.2%和6.5%（不同时间点间p<0.01）。心率、心电图和实验室参数无临床显著改变。总体治疗的患者中80%安全性良好。