Cardioselectivity and Partial Agonist Activity in the Antianginal Efficacy of the β-Adrenoceptor Antagonists A Clinical Comparison Between Atenolol and Pindolol

Magnani, B; Mantovani, Beatrice; Brancaleoni, M.; Gubelli, S.; Амбросиони, Е.

doi:10.2165/00003495-198300252-00050

Cited by 12 publications

(5 citation statements)

References 13 publications

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“…tp < 0-001, difference between atenolol and celiprolol. 3 (2)t *p < 0-02, tp < 0 005, $p < 0 001, difference between placebo and drug. EF, ejection fraction.…”

Section: Effects On Heart Rate and Blood Pressurementioning

confidence: 96%

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

McLenachan

Wilson²,

Dargie³

1988

Heart

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SUMMARY Celiprolol (400 mg) and atenolol (100 mg) were given once a day to 16 patients with stable angina pectoris in a double blind placebo controlled crossover study. Celiprolol produced less suppression of heart rate both at rest and during exercise than atenolol. Both drugs were equally effective in reducing the frequency of angina and in delaying the onset of ischaemia during exercise. Radionuclide ventriculography showed that atenolol but not celiprolol lowered cardiac output at rest and during exercise.Thus the ancillary properties of celiprolol, including partial 1)2 agonist activity and direct vasodilating activity, have detectable effects on cardiac function that may be beneficial in patients with angina.The notable success of ,B adrenoceptor antagonists in the treatment of myocardial ischaemia in patients with coronary heart disease reflects the fact that effort is the main stimulus to the development of such ischaemia. There are some disadvantages associated with the principal therapeutic action of ,B blockade, which is suppression of the increase in heart rate and contractility that normally accompanies exercise.'These include an increase in left ventricular volume, which is energy wasting, and a reduction in cardiac output during exercise. Thus the interest in ,B blockers with ancillary properties that confer a more favourable haemodynamic profile while retaining the beneficial effect on myocardial ischaemia.Celiprolol is a new 1, selective adrenoceptor antagonist with partial agonist effects at the 1)2 receptor and direct vasodilating activity. It is orally active, undergoes minimal hepatic metabolism, and is active for at least 24 hours when given in a dose of 400 mg.'We compared the effects of a daily dose of celiprolol (400 mg) with that of atenolol (100 mg) on angina frequency, effort capacity, and indices of myocardial ischaemia and function at rest and during dynamic exercise in a double blind randomised crossover study of 16

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“…tp < 0-001, difference between atenolol and celiprolol. 3 (2)t *p < 0-02, tp < 0 005, $p < 0 001, difference between placebo and drug. EF, ejection fraction.…”

Section: Effects On Heart Rate and Blood Pressurementioning

confidence: 96%

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

McLenachan

Wilson²,

Dargie³

1988

Heart

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show abstract

“…Despite a high level of PAA both pindolol (Dwyer et al, 1982;Golightly, 1982) and xamoterol (Barrios et al, 1986;Detry et al, 1984) have anti-ischaemic actions. Comparative data with pure j-adrenoceptor blockers are not available for xamoterol, but pindolol is reported to be less effective in angina than atenolol (Magnani et al, 1983;Quyyumi et al, 1984). In particular nocturnal ischaemia with pindolol is more prolonged, possibly associated with the higher resting heart rate.…”

Section: Anginamentioning

confidence: 99%

Beta‐adrenoceptor partial agonists: a renaissance in cardiovascular therapy?

Waller

1990

Brit J Clinical Pharma

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“…Despite a high level of PAA both pindolol (Dwyer et al, 1982;Golightly, 1982) andxamoterol (Barrios et al, 1986;Detry et al, 1984) have anti-ischaemic actions. Comparative data with pure j-adrenoceptor blockers are not available for xamoterol, but pindolol is reported to be less effective in angina than atenolol (Magnani et al, 1983;Quyyumi et al, 1984). In particular nocturnal ischaemia with pindolol is more prolonged, possibly associated with the higher resting heart rate.…”

Section: Anginamentioning

confidence: 99%

Untitled

1990

Brit J Clinical Pharma

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Cardioselectivity and Partial Agonist Activity in the Antianginal Efficacy of the β-Adrenoceptor Antagonists A Clinical Comparison Between Atenolol and Pindolol

Cited by 12 publications

References 13 publications

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

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

Beta‐adrenoceptor partial agonists: a renaissance in cardiovascular therapy?

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