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理想的β-肾上腺素能受体拮抗剂的特性以及现有药物与新型心脏选择性亲水性血管舒张性β-肾上腺素能受体拮抗剂塞利洛尔的比较

Qualities of an ideal beta-adrenoceptor antagonist and comparison of existing agents with a new cardioselective hydrophilic vasodilator beta-adrenoceptor antagonist, celiprolol.

作者信息

Opie L H

机构信息

Department of Medicine, University of Cape Town, Observatory, South Africa.

出版信息

Am J Cardiol. 1988 Feb 10;61(5):8C-13C. doi: 10.1016/0002-9149(88)90478-x.

Abstract

Beta-adrenoceptor blockade is established therapy for cardiovascular conditions including hypertension and angina pectoris. The important qualities of a beta-adrenoceptor antagonist relate to cardioselectivity, hydrophilicity, peripheral vasodilation, ideal pharmacokinetics and maintenance of the quality of life. Celiprolol, with its known cardioselectivity, hydrophilicity and peripheral vasodilator capacity, measures well by several of these criteria; more data on pharmacokinetics are required. Further testing is indicated, particularly in relation to effects on epinephrine-induced hypokalemia, blood lipid profiles, clinical vasodilatory properties and effects on the quality of life, especially in geriatric patients.

摘要

β-肾上腺素能受体阻滞剂是治疗包括高血压和心绞痛在内的心血管疾病的既定疗法。β-肾上腺素能受体拮抗剂的重要特性与心脏选择性、亲水性、外周血管舒张、理想的药代动力学以及生活质量的维持有关。塞利洛尔具有已知的心脏选择性、亲水性和外周血管舒张能力,根据其中几项标准表现良好;还需要更多关于药代动力学的数据。需要进一步测试,特别是关于对肾上腺素诱导的低钾血症、血脂谱、临床血管舒张特性以及对生活质量的影响,尤其是在老年患者中。

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