A Risk-Benefit Assessment of Celiprolol in the Treatment of Cardiovascular Disease

Kendall, M. J.; Rajman, Iris

doi:10.2165/00002018-199410030-00004

Cited by 5 publications

(1 citation statement)

References 88 publications

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“…Celiprolol also significantly delays the onset of angina during exercise testing (reviewed by Milne & Buckley[l] and Kendall & Rajman [91]). Celiprolol also significantly delays the onset of angina during exercise testing (reviewed by Milne & Buckley[l] and Kendall & Rajman [91]).…”

Section: Use Of Celiprolol In Angina Pectorismentioning

confidence: 99%

Celiprolol

Dunn¹,

Spencer²

1995

Drugs & Aging

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Celiprolol is a beta 1-selective adrenoceptor antagonist (beta-blocker) which acts as a weak agonist at beta 2-adrenoceptors. The drug demonstrates vasodilator properties and does not depress heart rate to the same extent as propranolol, atenolol or metoprolol. Celiprolol has shown equivalent antihypertensive efficacy to other beta-blockers, notably propranolol, atenolol, metoprolol and pindolol, in patients aged 18 to 75 years with mild to moderate essential hypertension. The drug has also shown similar antihypertensive efficacy to the angiotensin converting enzyme inhibitor enalapril and to combination diuretic therapy with hydrochlorothiazide and amiloride. Celiprolol was equally effective in adult patients of all ages, although no data are available for patients aged over 75 years. Data from a small number of clinical trials indicate celiprolol to be as effective as both propranolol and atenolol in improving work capacity and reducing the frequency of anginal attacks in patients with stable effort angina. However, the drug has not yet been evaluated in postmyocardial infarction patients. Celiprolol offers advantages over other beta-blockers, including reduction of peripheral vascular resistance and maintenance of resting heart rate, cardiac output and renal perfusion. The drug is also associated with improvements in plasma lipid profiles and does not appear to adversely affect carbohydrate metabolism or lung function, although its use in patients with reversible obstructive pulmonary disease is not recommended. Celiprolol is therefore a highly cardioselective beta-blocker with ancillary characteristics which are potentially useful in patients with hypertension and angina complicated by other conditions commonly associated with advanced age. These include impaired glucose tolerance or diabetes mellitus, peripheral vascular disease and hyperlipidaemia. The drug may also be preferred to other beta-blockers in patients in whom a reduction in heart rate would be particularly undesirable. Further long term (> 12 months) clinical trials and pharmacoeconomic data are now required to confirm the clinical relevance of the pharmacodynamic advantages of celiprolol therapy.

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Section: Use Of Celiprolol In Angina Pectorismentioning

confidence: 99%

Celiprolol

Dunn¹,

Spencer²

1995

Drugs & Aging

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Molecular Organization of the β-Adrenergic System

Rohrer¹

1998

From Hypertension to Heart Failure

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Physiological consequences of β-adrenergic receptor disruption

Rohrer

1998

Journal of Molecular Medicine

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Activation of beta-adrenergic receptors (beta-ARs) in vivo is an important means by which animals regulate cardiac performance, vascular tone, lipid and carbohydrate metabolism, and behavior. The advent of targeted gene disruption in mice has led to significant advances in our understanding of the role that beta-AR subtypes play in these processes, and this technique has become an important tool for the study of G protein coupled receptors in general. To date, targeted disruption of both beta1- and beta3-ARs in mice has been reported. Mice lacking beta1-ARs are unresponsive to cardiac beta-AR stimulation, suggesting that neither beta2- nor beta3-ARs couple to inotropic or chronotropic responses in the mouse. Conversely, mice lacking beta3-ARs retain at least some adipose beta-AR responsiveness through remaining beta1- and beta2-ARs, suggesting that all three beta-AR subtypes mediate similar functions in this tissue. While these knockout models have been extremely valuable tools for revealing the roles that individual beta-ARs play in whole animal physiology, it is also useful to integrate the results of experiments derived from either transgenic overexpression of beta-ARs or purely pharmacological approaches to the study of beta-AR function in order to create a comprehensive model of beta-AR function in vivo.

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A Risk-Benefit Assessment of Celiprolol in the Treatment of Cardiovascular Disease

Cited by 5 publications

References 88 publications

Celiprolol

Celiprolol

Molecular Organization of the β-Adrenergic System

Physiological consequences of β-adrenergic receptor disruption

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