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阿替洛尔:对其药理特性以及在心绞痛和高血压治疗中的疗效的综述。

Atenolol: a review of its pharmacological properties and therapeutic efficacy in angina pectoris and hypertension.

作者信息

Heel R C, Brogden R N, Speight T M, Avery G S

出版信息

Drugs. 1979 Jun;17(6):425-60. doi: 10.2165/00003495-197917060-00001.

Abstract

Atenolol is a beta-selective (cardioselective) adrenoceptor blocking drug without partial agonist or membrane stabilising activity. Its profile of action most closely resembles that of metoprolol which differs only in that it has some membrane stabilising activity. Atenolol has been well studied and is effective in the treatment of hypertension and in the prophylactic management of angina. Its narrow dose response range obviates the need for highly individualised dose titration. In patients with angina its long duration of beta-blocking activity allows once daily dosage, whereas other beta-blockers, unless in sustained release dosage forms, need to be given in divided doses. Other beta-blockers can be given once daily in hypertension, but at presnt the evidence for effective control with a once daily regimen is more convincing with atenolol. Further studies are need to clarify any important differences in blood pressure control between the various beta-blocking drugs, both in conventional or sustained release dosage forms. As with metoprolol, atenolol is preferable to non-selective beta-blockers in patients with asthma or diabetes mellitus. Atenolol has been well tolerated in most patients, its profile of adverse reactions generally resembling that of other beta-blocking drugs, although its low lipid solubility and limited penetration into the brain results in a lower incidence of central nervous system effects than seen with propranolol. Atenolol is eliminated virtually entirely as unchanged drug in the urine and dosage needs to be reduced in patients with moderate to severely impaired renal function (glomerular filtration rate less than 30 ml/min). There is no need for modification of dosage of atenolol in liver disease.

摘要

阿替洛尔是一种β选择性(心脏选择性)肾上腺素能受体阻断药物,无部分激动剂或膜稳定活性。其作用特点与美托洛尔最为相似,区别仅在于美托洛尔有一定的膜稳定活性。阿替洛尔已得到充分研究,对治疗高血压和心绞痛的预防性管理有效。其狭窄的剂量反应范围无需高度个体化的剂量滴定。对于心绞痛患者,其较长的β受体阻断活性持续时间允许每日给药一次,而其他β受体阻滞剂,除非是缓释剂型,则需要分次给药。其他β受体阻滞剂在治疗高血压时也可每日给药一次,但目前,每日一次给药方案有效控制血压的证据在阿替洛尔方面更具说服力。需要进一步研究以阐明各种β受体阻断药物(无论是传统剂型还是缓释剂型)在血压控制方面的任何重要差异。与美托洛尔一样,对于哮喘或糖尿病患者,阿替洛尔比非选择性β受体阻滞剂更可取。大多数患者对阿替洛尔耐受性良好,其不良反应特征通常与其他β受体阻断药物相似,尽管其低脂溶性和有限的脑内渗透导致中枢神经系统效应的发生率低于普萘洛尔。阿替洛尔几乎完全以原形药物经尿液排泄,肾功能中度至重度受损(肾小球滤过率低于30 ml/分钟)的患者需要减少剂量。肝病患者无需调整阿替洛尔的剂量。

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