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β肾上腺素能阻滞剂的内在拟交感活性

Intrinsic sympathomimetic activity of beta-adrenoceptor blocking agents.

作者信息

Cocco G, Burkart F, Chu D, Follath F

出版信息

Eur J Clin Pharmacol. 1978 Mar 17;13(1):1-4. doi: 10.1007/BF00606672.

DOI:10.1007/BF00606672
PMID:25186
Abstract

The pharmacological methods used to assess the intrinsic sympathomimetic activity (ISA) of beta-blockers are discussed. The clinical relevance of ISA to respiratory function, peripheral resistance and cardiac function is reviewed. It appears doubtful whether ISA is always of predominant clinical significance and an alternative explanation is offered for many clinical effects observed with certain beta-blockers, e.g. pindolol, oxprenolol, tolamolol, metoprolol, etc. Some effects of these beta-blockers resemble those of labetalol, a new drug with both alpha and beta-blocking activity. Some clinical effects of certain beta-blockers are more likely to be due to alpha-blocking activity than to their ISA.

摘要

讨论了用于评估β受体阻滞剂内在拟交感活性(ISA)的药理学方法。综述了ISA与呼吸功能、外周阻力和心脏功能的临床相关性。ISA是否始终具有主要临床意义似乎值得怀疑,并且针对某些β受体阻滞剂(如吲哚洛尔、氧烯洛尔、甲磺胺心定、美托洛尔等)所观察到的许多临床效应提供了另一种解释。这些β受体阻滞剂的一些效应类似于拉贝洛尔(一种具有α和β受体阻滞活性的新药)的效应。某些β受体阻滞剂的一些临床效应更可能是由于α受体阻滞活性而非其ISA。

相似文献

1
Intrinsic sympathomimetic activity of beta-adrenoceptor blocking agents.β肾上腺素能阻滞剂的内在拟交感活性
Eur J Clin Pharmacol. 1978 Mar 17;13(1):1-4. doi: 10.1007/BF00606672.
2
Cardiac effects of beta-adrenoceptor blockade with intrinsic sympathomimetic activity during submaximal exercise.次极量运动期间具有内在拟交感活性的β-肾上腺素能受体阻滞剂的心脏效应
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Central hemodynamics of beta-adrenoceptor blocking drugs: beta 1 selectivity versus intrinsic sympathomimetic activity.β-肾上腺素能受体阻断药的中心血流动力学:β1选择性与内在拟交感活性
J Cardiovasc Pharmacol. 1983;5 Suppl 1:S21-5.
4
A study of the relationship between cardiac beta-adrenoceptor blockade and intrinsic sympathomimetic activity in rats depleted of catecholamines.一项关于去甲肾上腺素耗竭大鼠心脏β-肾上腺素能受体阻断与内在拟交感活性之间关系的研究。
Clin Exp Pharmacol Physiol. 1979 Jan-Feb;6(1):1-9. doi: 10.1111/j.1440-1681.1979.tb00001.x.
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Differential changes in lymphocyte beta 2-adrenoceptor density by beta-blocker administration: role of intrinsic sympathomimetic activity.β受体阻滞剂给药后淋巴细胞β2-肾上腺素能受体密度的差异变化:内在拟交感活性的作用
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Potential benefit of combination therapy with diuretics and beta blockers having intrinsic sympathomimetic activity.利尿剂与具有内在拟交感活性的β受体阻滞剂联合治疗的潜在益处。
Eur Heart J. 1990 Jun;11(6):560-5. doi: 10.1093/oxfordjournals.eurheartj.a059750.
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Br J Clin Pharmacol. 1982;13(Suppl 2):167S-174S. doi: 10.1111/j.1365-2125.1982.tb01906.x.
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The additional properties of beta adrenoceptor blocking drugs.β肾上腺素能受体阻断药的其他特性。
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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。
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Influence of intrinsic sympathomimetic activity and cardioselectivity on beta adrenoceptor blockade.内在拟交感活性和心脏选择性对β肾上腺素能受体阻滞的影响。
Clin Pharmacol Ther. 1977 May;21(5):556-66. doi: 10.1002/cpt1977215556.

引用本文的文献

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How Carvedilol activates β-adrenoceptors.卡维地洛如何激活β-肾上腺素能受体。
Nat Commun. 2022 Nov 19;13(1):7109. doi: 10.1038/s41467-022-34765-w.
2
Influence of propranolol and pindolol on the haemodynamic effects of papaverine, isoprenaline and noradrenaline in hypertensive patients.普萘洛尔和吲哚洛尔对高血压患者罂粟碱、异丙肾上腺素及去甲肾上腺素血流动力学效应的影响
Eur J Clin Pharmacol. 1980 Aug;18(2):141-6. doi: 10.1007/BF00561581.
3
Clinical use of beta-adrenoceptor blockade in systemic hypertension.β-肾上腺素能受体阻滞剂在系统性高血压中的临床应用。

本文引用的文献

1
Pharmacology of a new adrenergic beta-receptor-blocking compound (Nethalide).一种新型肾上腺素能β受体阻滞剂化合物(奈他洛尔)的药理学
Lancet. 1962 Aug 18;2(7251):311-4. doi: 10.1016/s0140-6736(62)90103-4.
2
Pharmacological properties of H 56-28--a beta-adrenergic receptor antagonist.H 56-28的药理学特性——一种β-肾上腺素能受体拮抗剂。
Acta Pharmacol Toxicol (Copenh). 1967;25:9-40.
3
[Comparative studies with beta-receptor blocking agents and quinidine].[β受体阻滞剂与奎尼丁的比较研究]
Drugs. 1990 Jun;39(6):862-76. doi: 10.2165/00003495-199039060-00005.
Helv Physiol Pharmacol Acta. 1967;25(4):CR432+.
4
Beta-adrenergic receptor blocking drugs. Mechanisms of action and clinical applications.β-肾上腺素能受体阻断药物。作用机制与临床应用。
N Engl J Med. 1966 Nov 24;275(21):1175-83 concl. doi: 10.1056/NEJM196611242752108.
5
Comparative chronotropic activity of beta-adrenoceptive antagonists.β-肾上腺素能拮抗剂的比较变时活性
Br J Pharmacol. 1970 Nov;40(3):373-81. doi: 10.1111/j.1476-5381.1970.tb10619.x.
6
Clinical pharmacology of beta-reccer-atefoygolocarahp lnilcc clinical pharmacology of beta-receptor-blocking drugs.β受体阻滞剂的临床药理学 (原文中“beta-reccer-atefoygolocarahp lnilcc”可能有误,推测正确表述应为“beta-receptor-blocking”)
Clin Pharmacol Ther. 1969 Nov-Dec;10(6):765-99.
7
Evidence favouring the existence of a single adrenergic receptor.支持单一肾上腺素能受体存在的证据。
Nature. 1968 Mar 16;217(5133):1077-8. doi: 10.1038/2171077a0.
8
Myocardial alpha and beta adrenergic receptors as demonstrated by atrial functional refractory-period changes.通过心房功能不应期变化所证实的心肌α和β肾上腺素能受体
J Pharmacol Exp Ther. 1966 Nov;154(2):255-63.
9
An analysis of the alpha- and beta-effects of isoprenaline on the isolated nictitating membraen.异丙肾上腺素对离体瞬膜的α-效应和β-效应分析。
Naunyn Schmiedebergs Arch Pharmacol. 1974;285(4):375-93. doi: 10.1007/BF00501466.
10
The beta-blocking potency and cardioselectivity of tolamolol and its isomers in rodents.托拉洛尔及其异构体在啮齿动物中的β受体阻滞效能和心脏选择性
Eur J Pharmacol. 1974 Feb;25(2):170-5. doi: 10.1016/0014-2999(74)90046-6.