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β-肾上腺素能阻滞剂中β1选择性和内在拟交感活性的临床意义。

Clinical significance of beta 1-selectivity and intrinsic sympathomimetic activity in a beta-adrenergic blocking drug.

作者信息

Frishman W H

出版信息

Am J Cardiol. 1987 May 15;59(13):33F-37F. doi: 10.1016/0002-9149(87)90039-7.

DOI:10.1016/0002-9149(87)90039-7
PMID:2883876
Abstract

Almost all beta-adrenergic blockers, regardless of their pharmacologic characteristics, appear to have blood pressure-lowering activity in hypertensive patients. Comparisons between nonselective beta-blocking agents, such as propranolol and nadolol, with beta 1-selective drugs, such as metoprolol, atenolol and acebutolol, have demonstrated close similarities in their antihypertensive effects in patients. Similarly, beta blockers with and without intrinsic sympathomimetic activity (ISA) have comparable antihypertensive effects. However, beta-selective agents may offer some advantages over conventional beta blockers in hypertensive patients with concurrent conditions such as chronic obstructive airways disease, peripheral vascular disease, diabetes and hyperlipidemia. Beta 1-selective drugs are also preferred in diabetic patients receiving hypoglycemic agents because they do not interfere with glycogenolysis. Agents lacking ISA, such as propranolol, acutely increase peripheral resistance. beta blockers with ISA usually lower resistance. ISA may also minimize the bradycardia frequently found in elderly patients. Agents with ISA may protect against the decrease in high density lipoprotein cholesterol and the modest increase in triglycerides noted with some beta blockers that do not have ISA. Thus, in a large number of clinical situations in which hypertension is found, the properties of beta 1 selectivity and ISA allow beta blockers to be used with greater safety. Therefore, agents possessing both of these properties may be particularly valuable.

摘要

几乎所有的β-肾上腺素能阻滞剂,无论其药理特性如何,在高血压患者中似乎都具有降压活性。非选择性β-阻滞剂(如普萘洛尔和纳多洛尔)与β1选择性药物(如美托洛尔、阿替洛尔和醋丁洛尔)之间的比较表明,它们在患者的降压效果上非常相似。同样,具有和不具有内在拟交感神经活性(ISA)的β-阻滞剂具有相当的降压效果。然而,在患有慢性阻塞性气道疾病、外周血管疾病、糖尿病和高脂血症等并发疾病的高血压患者中,β-选择性药物可能比传统的β-阻滞剂具有一些优势。在接受降糖药物治疗的糖尿病患者中,β1选择性药物也更受青睐,因为它们不会干扰糖原分解。缺乏ISA的药物,如普萘洛尔,会急性增加外周阻力。具有ISA的β-阻滞剂通常会降低外周阻力。ISA还可能使老年患者中常见的心动过缓降至最低。具有ISA的药物可能有助于防止一些不具有ISA的β-阻滞剂所导致的高密度脂蛋白胆固醇降低和甘油三酯适度升高。因此,在发现高血压的大量临床情况下,β1选择性和ISA的特性使β-阻滞剂使用起来更安全。因此,同时具备这两种特性的药物可能特别有价值。

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Clinical significance of beta 1-selectivity and intrinsic sympathomimetic activity in a beta-adrenergic blocking drug.β-肾上腺素能阻滞剂中β1选择性和内在拟交感活性的临床意义。
Am J Cardiol. 1987 May 15;59(13):33F-37F. doi: 10.1016/0002-9149(87)90039-7.
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