Importance of ancillary properties of beta blockers in angina: a study of celiprolol and atenolol.

McLenachan, James M.; Wilson, John T.; Dargie, Henry J.

doi:10.1136/hrt.59.6.685

Cited by 13 publications

(5 citation statements)

References 7 publications

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“…duction Impaired baroreceptor and cardiopulmonary reflexes; syncope of unknown cause Decreased liver blood flow May need decreased dose of beta blockers, especially in smokers, not relevant to beta blockers primarily excreted by kidneys (applies to propranolol and metoprolol, not to atenolol, nadolol, and celiprolol). When glomerular filtration rate falls substantially (e.g., [25][26][27][28][29][30][31][32][33][34][35] ml/min), dose of water-soluble beta-blocker needs reduction (atenolol, nadolol, and celiprolol). Regarded by some as rationale for nombeta-blocker therapy in the elderly.…”

Section: Change Commentmentioning

confidence: 99%

“…These data suggest that celiprolol increases cardiac function with little or no change in heart rate and that it has an indirect positive inotropic effect. In patients with stable angina pectoris [31], celiprolol had an equal antianginal effect, as did atenolol (as judged by exercise stress testing), yet heart rate and cardiac output were higher.…”

Section: Hemodgnamic Changes With Agementioning

confidence: 99%

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Required beta blocker profile in the elderly

Opie

1991

Cardiovasc Drug Ther

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In the truly elderly, a complex balance between compensatory processes and impaired organ function allows reasonably normal physical function. It is argued that beta blockade should have certain desirable qualities to minimize any impairment of organ function, thereby upsetting the quality of life. Thus a simple pharmacokinetic pattern without hepatic metabolism is less likely to cause unexpected variation in blood levels of the beta blocking agents and to have fewer risks of interactions with other drugs including nicotine. Renal-excreted beta blockers--such as atenolol, nadolol, and celiprolol--do, however, need downward dose adjustment when the glomerular filtration rates fall. The elderly are frequently categorized as having a low renin profile, which in the view of some workers may make a vasodilatory beta blocker more desirable. Hemodynamic advantages of such agents include the prime site of attack in hypertension on the increased peripheral vascular resistance, increasingly fundamental with a prolonged duration of hypertension and therefore with the aging process. Furthermore, a normal heart rate with a sustained cardiac output may avoid symptomatic bradycardia. In the elderly, respiratory function may be impaired so that loss of elastic recoil causes elderly emphysema. A highly cardioselective beta blocker should be an advantage. Finally, minimal interference with glucose and lipid metabolism should also be desirable goals.

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Section: Change Commentmentioning

confidence: 99%

Section: Hemodgnamic Changes With Agementioning

confidence: 99%

Required beta blocker profile in the elderly

Opie

1991

Cardiovasc Drug Ther

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“…Fig. This was possibly related to ~2agonism and/or direct vasodilator activity [62]. Effect of celiprolol on myocardial oxygen demand and heart rate in patients with stable angina pectoris.…”

mentioning

confidence: 95%

“…This suggests an adverse effect on myocardial oxygen consumption for cardiac work at a given pressure [62]. 2.…”

mentioning

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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“…In both in-vitro and in-vivo studies, celiprolol was shown to possess partial agonist activity (PAA), a property that attenuates the depression of myocardial chronotropy and inotropy associated with beta blockers that lack this property [14][15][16]. Thus, compared with beta blockers that do not possess PAA, celiprolol is less likely to produce sinus bradycardia or myocardial depression.…”

mentioning

confidence: 99%

Evaluation of celiprolol, a new cardioselective beta1-adrenergic blocker with vasodilating properties, in the treatment of mild to moderate hypertension in the elderly

Kd¹

1991

Cardiovasc Drug Ther

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Celiprolol hydrochloride is a cardioselective beta 1-adrenergic antagonist with partial agonist activity. The studies discussed were designed to assess celiprolol's pharmacokinetic disposition, its efficacy versus placebo and other beta blockers, its relative safety profile, and its therapeutic ratio in the elderly population. The results of a postmarketing surveillance study are also presented. Pharmacokinetic results indicate good dose-related bioavailability in the elderly, no accumulation on multiple dosing, and pharmacokinetics equivalent to those in a younger age group. Celiprolol effectively lowers blood pressure in elderly patients with mild to moderate hypertension, resulting in reductions of 12-15 mmHg and 8-11 mmHg in systolic and diastolic blood pressures, respectively. A clinically insignificant reduction in resting pulse rate is observed with celiprolol treatment. Its adverse experience profile is equivalent to that of placebo, and the incidence of beta-blocker-associated side effects is lower compared with that of atenolol and propranolol. Celiprolol also effectively controlled hypertension in the elderly in the postmarking surveillance study. Collectively, the results of these studies demonstrate that the pharmacokinetics and efficacy of celiprolol in the treatment of mild to moderate hypertension are equivalent in younger and older populations, and that the therapeutic ratio (i.e., efficacy/safety) of celiprolol is superior to that of atenolol and propranolol in the elderly.

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Importance of ancillary properties of beta blockers in angina: a study of celiprolol and atenolol.

Cited by 13 publications

References 7 publications

Required beta blocker profile in the elderly

Required beta blocker profile in the elderly

Celiprolol

Evaluation of celiprolol, a new cardioselective beta1-adrenergic blocker with vasodilating properties, in the treatment of mild to moderate hypertension in the elderly

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