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日本地拉普利的临床评估。日本地拉普利研究组报告。

Clinical evaluation of delapril in Japan. Report from the Japan Study Group on Delapril.

作者信息

Ogihara T, Kaneko Y, Ikeda M, Yamada K, Omae T, Arakawa K, Ishii M, Yoshinaga K, Kumahara Y, Kokubu T

机构信息

Osaka University, Japan.

出版信息

Am J Hypertens. 1991 Jan;4(1 Pt 2):42S-45S. doi: 10.1093/ajh/4.1.42s.

Abstract

Delapril, a new angiotensin converting enzyme (ACE) inhibitor discovered in the laboratory of Takeda Chemical Industries, Ltd., is the result of drug design based on the structure-activity relationships of ACE inhibitors. Delapril is an antihypertensive agent with a relatively long duration of action and no SH moiety in its structure. Following administration, it is converted into two active metabolites. Delapril effectively lowered blood pressure in 73% of 1,008 patients with hypertension during clinical trials in Japan. Efficacy rates were 73% for essential hypertension, 85% for renal hypertension, and 80% for renovascular hypertension. Excellent hypotensive response was observed in all age groups, from young to elderly patients. Side effects during administration of delapril, based on subjective evidence, were reported in 80 out of the 1,008 cases (7.9%). The main symptoms included orthostatic dizziness (1.7%), dizziness (1.3%), and nausea (1.1%). Dry cough, which has attracted attention in recent years as a side effect of ACE inhibitors, was reported at a low incidence of 1.1%. In a double-blind, controlled study in patients with mild to moderate essential hypertension in which captopril served as a positive control, delapril showed superior hypotensive effect and greater safety. Data derived from the Japan Study Group on Delapril indicate that this ACE inhibitor has excellent hypotensive effects and a high level of safety. It is suitable as a first-line drug in both monotherapy and combined therapy.

摘要

地拉普利是在武田化学工业株式会社实验室发现的一种新型血管紧张素转换酶(ACE)抑制剂,它是基于ACE抑制剂的构效关系进行药物设计的成果。地拉普利是一种作用持续时间相对较长且结构中无SH基团的抗高血压药物。给药后,它会转化为两种活性代谢产物。在日本的临床试验中,地拉普利使1008例高血压患者中的73%有效降低了血压。原发性高血压的有效率为73%,肾性高血压为85%,肾血管性高血压为80%。在所有年龄组,从年轻患者到老年患者,均观察到了良好的降压反应。根据主观证据,1008例病例中有80例(7.9%)报告了地拉普利给药期间的副作用。主要症状包括体位性头晕(1.7%)、头晕(1.3%)和恶心(1.1%)。近年来作为ACE抑制剂副作用而受到关注的干咳,报告发生率较低,为1.1%。在一项以卡托普利作为阳性对照的轻至中度原发性高血压患者双盲对照研究中,地拉普利显示出更好的降压效果和更高的安全性。来自日本地拉普利研究组的数据表明,这种ACE抑制剂具有出色的降压效果和高度的安全性。它适用于单药治疗和联合治疗中的一线药物。

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