ISSN:
1432-1041
Keywords:
Celiprolol
;
Bisoprolol
;
β-Adrenoceptor blockade
;
radioreceptor assay
;
RRA-kinetics
;
impedance cardiography
;
ergometry
Source:
Springer Online Journal Archives 1860-2000
Topics:
Chemistry and Pharmacology
,
Medicine
Notes:
Summary The cardiovascular effects at rest and during exercise and β1- and β2-adrenoceptor occupancy following a single dose of 1200 mg celiprolol p. o. were investigated in 8 healthy subjects with or without pretreatment with a single dose of 20 mg bisoprolol p. o., using a place-bo-controlled, 2-way cross-over design. The ergometric responses of heart rate (HR) and systolic blood pressure (SBP) after celiprolol were reduced to a similar extent as after bisoprolol, but the cardiovascular function at rest was affected in a different way: there was a rise in HR, clear enhancement of cardiac systolic performance, and a considerable drop in the estimated total peripheral vascular resistance, associated with median β1-RRA and β2-RRA occupancies of 88 and 34%, respectively. The cardiovascular effects of celiprolol were not affected by pretreatment with bisoprolol. Celiprolol thus binds extensively to β1-adrenoceptors, moderately to β2-adrenoceptors, acts as β1-adrenergic antagonist (exemplified by the ergometric effects) but has vasodilator, positive chronotropic and cardiac systolic performance enhancing properties, which do not involve either direct or indirect β1-adrenergic agonism, but which might reflect β2-adrenergic agonism.
Type of Medium:
Electronic Resource
URL:
http://dx.doi.org/10.1007/BF00316470
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