Clinical Relevance of Intrinsic Sympathomimetic Activity of Beta Blockers Used in Angina

Kostis, John B.; DeFelice, Eugene A.; Frishman, William H.; Hosler, Maryhelen; Krieger, Susan; Aglitz, N; Kuo, Peter T.

doi:10.1177/000331978103201106

Cited by 6 publications

(2 citation statements)

References 6 publications

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“…Other comparative studies by Frishmann (78) and Thadani (79) showed no difference between propranolol and pindolol. Dwyer et al (80) compared 15 and 30 mg pindolol daily with placebo in 12 anginal subjects and concluded that whilst it reduced trinitrin consumption and the number of anginal episodes, it did not increase exercise tolerance.…”

Section: Efficacymentioning

confidence: 84%

The Possible Role of the Ancillary Properties of Beta Adrenoceptor Antagonists in the Management of Angina Pectoris

Jd¹

1985

Journal of Internal Medicine

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ABSTRACT. Beta adrenoceptor antagonists are effective in the symptomatic management of angina pectoris. This paper examines critically the possible influence of the ancillary properties of β1 selectivity, partial agonism and membrane‐stabilizing action on the response in anginal patients. The response is categorized according to experimental, pharmacological and clinical end‐points, placing emphasis on the possible errors which may arise from extrapolation from the former to the latter. It is concluded: That selective beta adrenoceptor antagonism confers limited, but tangible advantages over non‐selective antagonists in regard to patients with reversible airways obstruction, and also in the metabolic and haemodynamic response to acute hypoglycaemia. Cardioselectivity does not influence the central haemodynamic response to exercise, but lessens adrenaline‐mediated hypertensive responses to smoking and hypoglycaemia. Non‐selective partial agonists cause less reduction in resting ventricular function, but their effects on cardiac output during exercise are indistinguishable from full antagonists. Membrane stabilizing properties have a marked influence on the tolerability of these agents in terms of unwanted, nonspecific central nervous system symptoms. Unresolved questions relate to the influence of partial agonism on fatigue, metabolic responses, especially blood lipids and glucose, and the possibility of lesser efficacy in angina compared to full antagonists.

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Section: Efficacymentioning

confidence: 84%

The Possible Role of the Ancillary Properties of Beta Adrenoceptor Antagonists in the Management of Angina Pectoris

Jd¹

1985

Journal of Internal Medicine

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“…A primary therapeutic indication of celiprolol will be in the treatment of angina pectoris in patients with coronary heart disease. The efficacy of P-adrenoceptor antagonists in angina has been well established (25,43,46,52) and probably is based on @,-antagonism only (61). As a cardioselective @-antagonist, celiprolol should be especially effective for this indication.…”

Section: Antianginal Effectsmentioning

confidence: 99%

Celiprolol

Smith¹,

Wolf²

1984

Cardiovascular Drug Reviews

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Celiprolol is a new cardioselective beta-receptor antagonist discovered by Chemie Linz AG, Linz (Austria), now being developed worldwide in collaboration with Revlon Health Care Group, Tuckahoe,. This chapter summarizes the published preclinical and clinical experience with celiprolol. These data characterize celiprolol as a potent and specific cardioselective P-adrenoceptor antagonist with mild intrinsic sympathomimetic activity (ISA), little or no membrane stabilizing effects, and with other interesting and unexpected cardiovascular and bronchiolar effects. In early clinical trials, celiprolol is well tolerated and effective in the treatment of hypertension, angina, and hyperkinetic heart syndrome. CHEMISTRY Celiprolol hydrochloride' (ST-1396; REV 5320A) is 3-[3-acetyl-4-[3-(tert-b~tylamino)-2-hydroxypropoxy]phenyl]-1,1 -diethylurea hydrochloride (Fig. 1). It was synthesized and patented by Zoelss and co-workers at Chemie Linz (64,65). Several synthetic pathways for celiprolol have been developed (64). Physically, celiprolol is a crystalline material with a molecular weight of 416 and a melting point of 198 to 200°C; it is soluble in water (17.6 g/lOO ml). Colorimetric and high performance liquid chromatography techniques have been developed to assay celiprolol in biological fluids (15,56,57). PRECLINICAL PHARMACOLOGY P-Adrenoceptor BlockadeThe P-adrenoceptor blocking actions of celiprolol in vitro were determined in a number of isolated tissue preparations using isoproterenol (ISO) as the beta-agonist (35). The relative magnitude of the blockade in each tissue was expressed as a PA, value2 (47). Celiprolol was shown to be a potent inhibitor of IS0 in spontaneously 'The hydrochloride salt of celiprolol was utilized in all studies, unless otherwise indicated, and 2pA, values are the negative logs of the antagonist concentrations that require twice as much agonist hereafter is referred to as celiprolol.(ISO) to be added to elicit the same response achieved without the antagonist.

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Drug treatment of angina pectoris

Johnston¹

1985

Drugs in the Management of Heart Disease

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Clinical Relevance of Intrinsic Sympathomimetic Activity of Beta Blockers Used in Angina

Cited by 6 publications

References 6 publications

The Possible Role of the Ancillary Properties of Beta Adrenoceptor Antagonists in the Management of Angina Pectoris

The Possible Role of the Ancillary Properties of Beta Adrenoceptor Antagonists in the Management of Angina Pectoris

Celiprolol

Drug treatment of angina pectoris

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