Reduction of exercise tachycardia in man after propranolol, atenolol and bisoprolol in comparison to beta-adrenoceptor occupancy

Wellstein, Anton; Palm, D.; Belz, G. G.; Butzer, R.; Polsak, R.; Pett, B.

doi:10.1093/eurheartj/8.suppl_m.3

Cited by 53 publications

(38 citation statements)

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“…In the present study, using bisoprolol, the most selective β 1 -blocker, 9) the antiarrhythmic effects in patients with confirmed diurnal episodes of P-AF were investigated, taking into consideration the involvement of sympathetic activities and the concomitant use of class I antiarrhythmic drugs. In addition, in the patients in whom bisoprolol proved effective in a short-term evaluation, the longterm suppressive effects by continuous administration were evaluated.…”

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Antiarrhythmic Effect of Bisoprolol, a Highly Selective .BETA.1-Blocker, in Patients With Paroxysmal Atrial Fibrillation

et al. 2008

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SUMMARYIn the treatment of arrhythmia, β-blockers are mainly used to regulate the heart rate. However, β-blockers are also known as drugs with an antiarrhythmic effect due to the suppression of sympathetic activity. We evaluated the antiarrhythmic effects of a highly selective β 1 -blocker, bisoprolol, in patients with diurnal paroxysmal atrial fibrillation (P-AF).A total of 136 patients with symptomatic diurnal P-AF were enrolled. Patients were divided into a diurnal-specific P-AF group and a diurnal & nocturnal P-AF group, as well as into a bisoprolol single use group and a combined use group with an antiarrhythmic drug. The effects of bisoprolol were evaluated in 3 categories: subjective symptom improvement, quality of life (QOL) improvement, and elimination of P-AF episode in Holter electrocardiograms (ECGs). For patients with effective treatment, a long-term effect up to 24 months was evaluated.Five patients (3.7%) discontinued bisoprolol due to side effects. Following administration of bisoprolol, 109 patients (80%) experienced subjective symptom improvement, 103 patients (76%) experienced QOL improvement, and elimination of P-AF episodes in ECGs was observed in 84 patients (62%). The elimination rate of P-AF episodes in ECGs was higher in the diurnal P-AF group than in the diurnal & nocturnal P-AF group (P = 0.042). There was no significant difference between the bisoprolol single use group and the combined use group. A long-term suppressive effect by bisoprolol was observed in 70 of 83 patients (84%).The results demonstrate that bisoprolol has an antiarrhythmic effect against sympathetic diurnal P-AF, improving subjective symptoms and QOL and eliminating P-AF episodes in ECGs. (Int Heart J 2008; 49: 281-293)

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confidence: 99%

Antiarrhythmic Effect of Bisoprolol, a Highly Selective .BETA.1-Blocker, in Patients With Paroxysmal Atrial Fibrillation

et al. 2008

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“…of the antagonist activity of atenolol, metoprolol and propranolol in the CNS by determining the extent to which the drugs occupy animal 1l-and ,82-receptors (Wellstein et al, 1987) in lumbar CSF and plasma following oral drug administration. The extent of receptor occupancy of the agents in CSF was compared with the literature concerning their effects on the CNS.…”

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confidence: 99%

Receptor occupancy in lumbar CSF as a measure of the antagonist activity of atenolol, metoprolol and propranolol in the CNS.

Kaila

Marttila

1993

Brit J Clinical Pharma

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1 The antagonist activity of atenolol, metoprolol and propranolol in the CNS was estimated by determining the extent to which the drugs occupy animal r3l-and f32-receptors in CSF ex vivo at the time of lumbar puncture. 2 Five CSF and plasma samples were obtained 4 h after drug intake from subjects treated for hypertension with atenolol, 100 mg once daily and five from subjects treated with metoprolol, 50 mg three times daily. Twenty-four samples were obtained 1, 2, 4 or 12 h after drug intake from subjects receiving a single 40 mg dose of propranolol.3 The receptor occupancy in the samples was determined by adding ,3l-receptors of rabbit lung and P2-receptors of rat reticulocytes into the samples and labeling the receptors with a nonselective ,3-adrenoceptor antagonist, (-)-[3H]-CGP-12177. 4 Atenolol and metoprolol occupied, as expected, larger fractions of ,l-than ,82-receptors in CSF and plasma samples. The receptor fraction occupied by atenolol in CSF was significantly (P < 0.05) lower than that occupied by metoprolol. The differences in occupancy between the drugs in plasma, however, were not statistically significant.5 Propranolol occupied larger fractions of 132-than ,3l-receptors in the samples.Although propranolol concentrations in CSF were only 1/20-1/40 of those in plasma, the receptor occupancy of propranolol in CSF was similar to that in plasma. The differences in the extent of receptor occupancy at the various time points were not statistically significant (ANOVA for the differences, P > 0.05), because of the high variation in the occupancy at 1 and 12 h following the dose. 6 The 40 mg dose of propranolol occupied the largest, metoprolol therapy the intermediate and atenolol therapy the least fraction of P2-receptors in CSF at 4 h after drug intake.The order for receptor occupancy was thus identical to the reported order for the incidence of CNS side effects.7 Thus, we can quantitate accurately the 13l-and ,82-antagonist activity of atenolol, metoprolol and propranolol in CSF. The data on how these drugs occupy animal ,8-receptors in CSF ex vivo may be of value in analyzing their CNS-related effects.

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“…First, bisoprolol is the most β1-selective agent among the oral beta-blockers 17,18) , which allows it to be administered to patients with respiratory diseases. Bisoprolol also has only a mild negative effects on glucose metabolism.…”

Section: Discussionmentioning

confidence: 99%

Clinical Impact of Bisoprolol Versus Carvedilol in Patients Undergoing Femoropopliteal Stenting

Soga

Iida

Suzuki

et al. 2014

JAT

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Reduction of exercise tachycardia in man after propranolol, atenolol and bisoprolol in comparison to beta-adrenoceptor occupancy

Cited by 53 publications

References 0 publications

Antiarrhythmic Effect of Bisoprolol, a Highly Selective .BETA.1-Blocker, in Patients With Paroxysmal Atrial Fibrillation

Antiarrhythmic Effect of Bisoprolol, a Highly Selective .BETA.1-Blocker, in Patients With Paroxysmal Atrial Fibrillation

Receptor occupancy in lumbar CSF as a measure of the antagonist activity of atenolol, metoprolol and propranolol in the CNS.

Clinical Impact of Bisoprolol Versus Carvedilol in Patients Undergoing Femoropopliteal Stenting

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