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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.

DOI:10.1016/0002-9149(88)90478-x
PMID:2893535
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。

相似文献

1
Qualities of an ideal beta-adrenoceptor antagonist and comparison of existing agents with a new cardioselective hydrophilic vasodilator beta-adrenoceptor antagonist, celiprolol.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
Am J Cardiol. 1988 Feb 10;61(5):8C-13C. doi: 10.1016/0002-9149(88)90478-x.
2
Celiprolol: a new beta adrenoceptor antagonist with novel ancillary properties.塞利洛尔:一种具有新型辅助特性的新型β肾上腺素能受体拮抗剂。
J Cardiovasc Pharmacol. 1986;8 Suppl 4:S29-32.
3
Antihypertensive therapy with celiprolol: a new cardioselective beta blocker.塞利洛尔的抗高血压治疗:一种新型心脏选择性β受体阻滞剂。
Am J Cardiol. 1988 Feb 10;61(5):14C-22C. doi: 10.1016/0002-9149(88)90479-1.
4
Celiprolol. A preliminary review of its pharmacodynamic and pharmacokinetic properties and its therapeutic use in hypertension and angina pectoris.塞利洛尔。对其药效学、药代动力学特性及其在高血压和心绞痛治疗中的应用的初步综述。
Drugs. 1987 Oct;34(4):438-58. doi: 10.2165/00003495-198734040-00002.
5
Preclinical pharmacology of celiprolol: a cardioselective beta-adrenergic antagonist and mild vasodilator.塞利洛尔的临床前药理学:一种心脏选择性β-肾上腺素能拮抗剂和轻度血管扩张剂。
Am Heart J. 1991 Feb;121(2 Pt 2):677-83. doi: 10.1016/0002-8703(91)90445-n.
6
Celiprolol. An updated review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy in cardiovascular disease.塞利洛尔:对其药效学、药代动力学特性及在心血管疾病中治疗效果的最新综述。
Drugs. 1991 Jun;41(6):941-69. doi: 10.2165/00003495-199141060-00009.
7
Celiprolol. An evaluation of its pharmacological properties and clinical efficacy in the management of hypertension and angina pectoris.塞利洛尔:对其治疗高血压和心绞痛的药理特性及临床疗效的评估
Drugs Aging. 1995 Nov;7(5):394-411. doi: 10.2165/00002512-199507050-00006.
8
Celiprolol and the heart.塞利洛尔与心脏
Am J Cardiol. 1988 Feb 10;61(5):34C-40C. doi: 10.1016/0002-9149(88)90482-1.
9
Clinical pharmacology of vasodilatory beta-blocking drugs.
Am Heart J. 1991 Mar;121(3 Pt 2):1006-11. doi: 10.1016/0002-8703(91)90612-l.
10
No evidence for a direct vasodilatory effect of celiprolol on human vasculature in vivo or in vitro.在体内或体外均无证据表明塞利洛尔对人体血管有直接舒张作用。
J Cardiovasc Pharmacol. 1987 Nov;10(5):589-92. doi: 10.1097/00005344-198711000-00015.

引用本文的文献

1
Celiprolol. An evaluation of its pharmacological properties and clinical efficacy in the management of hypertension and angina pectoris.塞利洛尔:对其治疗高血压和心绞痛的药理特性及临床疗效的评估
Drugs Aging. 1995 Nov;7(5):394-411. doi: 10.2165/00002512-199507050-00006.
2
Effect of beta-blockade on exercise capacity in hypertensive subjects: a one-year double-blind study of celiprolol and metoprolol.β受体阻滞剂对高血压患者运动能力的影响:塞利洛尔与美托洛尔的一年双盲研究
Cardiovasc Drugs Ther. 1995 Feb;9(1):133-9. doi: 10.1007/BF00877753.
3
Association between serum lipids, glucose tolerance, and insulin sensitivity during 12 months of celiprolol treatment.
塞利洛尔治疗12个月期间血清脂质、糖耐量和胰岛素敏感性之间的关联。
Cardiovasc Drugs Ther. 1995 Apr;9(2):295-304. doi: 10.1007/BF00878674.
4
The applied pharmacology of beta-adrenoceptor antagonists (beta blockers) in relation to clinical outcomes.β-肾上腺素能受体拮抗剂(β受体阻滞剂)的应用药理学与临床结局的关系。
Cardiovasc Drugs Ther. 1991 Jun;5(3):561-76. doi: 10.1007/BF03029726.
5
Pharmacology of celiprolol.塞利洛尔的药理学
Cardiovasc Drugs Ther. 1991 Jan;4 Suppl 6:1281-5. doi: 10.1007/BF00114234.
6
Effects of celiprolol on cardiovascular responses to smoking in normotensive smokers.塞利洛尔对血压正常吸烟者吸烟时心血管反应的影响。
Cardiovasc Drugs Ther. 1992 Oct;6(5):543-4. doi: 10.1007/BF00055615.