Titre du document / Document title

Different effects of exercise on plasma concentrations of nebivolol, bisoprolol and carvedilol

Auteur(s) / Author(s)

STOSCHITZKY Kurt ⁽¹⁾ ; STOSCHITZKY Gergana ⁽¹⁾ ; KLEIN Werner ⁽¹⁾ ; MÜLLER Frank ⁽²⁾ ; BÜHRING Karl ⁽³⁾ ; LAMPRECHT Günther ⁽⁴⁾ ; LINDNER Wolfgang ⁽⁴⁾ ;

Affiliation(s) du ou des auteurs / Author(s) Affiliation(s)

⁽¹⁾ Department of Medicine/Division of Cardiology, Karl Franzens University, Graz, AUTRICHE
⁽²⁾ Berlin-Chemie, Berlin, ALLEMAGNE
⁽³⁾ Merck, Grafing, ALLEMAGNE
⁽⁴⁾ Department of Analytical Chemistry, University of Vienna, AUTRICHE

Résumé / Abstract

Background: In-vitro studies have shown that beta-blockers are taken up into and released from adrenergic cells together with epinephrine and norepinephrine. Consequently, studies in humans revealed an increase in plasma concentrations of propranolol and atenolol, whereas those of carvedilol were not affected by physical exercise. However, nebivolol and bisoprolol never were investigated on this issue. Methods: Ten healthy males received oral doses of 5 mg nebivolol, 5 mg bisoprolol, and 50 mg carvedilol daily for one week in a cross-over fashion. Exercise was performed at 3 hours following oral intake of the respective last drugs on the eighth day. Blood samples were taken at rest, during the last minute of exercise, and after 15 min of recovery. Results: At rest and during exercise, heart rates were as follows: Nebivolol, 57 ± 7 and 137 ± 11 beats/min; bisoprolol, 55 ± 5 and 139 ± 14 beats/min; carvedilol, 56 ± 5 and 135 ± 13 beats/min, with no significant differences between the drugs. Plasma concentrations were as follows: Nebivolol-rest 0.273 ± 0.029 ng/ml, exercise 0.274 ± 0.035 ng/ml, recovery 0.272 ± 0.035 ng/ml (n.s.). Bisoprolol-rest 4.99 ± 2.73 ng/ml, exercise 6.49 ± 5.58 ng/ml, recovery 4.90 ± 3.06 ng/ml (p < 0.01). Carvedilol-rest 10.3 ± 9.3 ng/ml, exercise 9.7 ± 8.2 ng/ml, recovery 6.5 ± 5.6 ng/ml (p < 0.05). Discussion: Plasma concentrations of bisoprolol increased during exercise and returned to baseline during recovery, a behaviour which would have been predicted according to present knowledge. However, exercise had no effect on plasma concentrations of nebivolol and carvedilol, a finding that is in contrast to previous results with other beta-blockers such as propranolol and atenolol. We conclude that both nebivolol and carvedilol are not taken up into and released from adrenergic nerves during exercise, a feature that clearly distinguishes these drugs from other beta-blockers so far investigated.

Revue / Journal Title

Cardiovascular drugs and therapy   ISSN 0920-3206   CODEN CDTHET 

Source / Source

2004, vol. 18, n^o2, pp. 135-138 [4 page(s) (article)] (16 ref.)

Langue / Language

Anglais

Editeur / Publisher

Springer, Dordrecht, PAYS-BAS  (1987) (Revue)

Mots-clés anglais / English Keywords

β2-Adrenergic receptor ; α1-Adrenergic receptor ; Alpha blocking agent ; β1-Adrenergic receptor ; Beta blocking agent ; Antagonist ; Vasodilator agent ; Antihypertensive agent ; Pharmacokinetics ; Carvedilol ; Nebivolol ; Concentration ; Blood plasma ; Biological fluid ; Exercise tolerance test ; Physical exercise ; Bisoprolol ;

Mots-clés français / French Keywords

Récepteur β2-adrénergique ; Récepteur α1-adrénergique ; Bloquant α-adrénergique ; Récepteur β1-adrénergique ; Bloquant β-adrénergique ; Antagoniste ; Vasodilatateur ; Antihypertenseur ; Pharmacocinétique ; Carvédilol ; Nébivolol ; Concentration ; Plasma sanguin ; Liquide biologique ; Epreuve effort ; Exercice physique ; Bisoprolol ;

Mots-clés espagnols / Spanish Keywords

Receptor β2-adrenérgico ; Receptor α1-adrenérgico ; Bloqueador α-adrenérgico ; Receptor β1-adrenérgico ; Bloqueador β-adrenérgico ; Antagonista ; Vasodilatador ; Antihipertensivo ; Farmacocinética ; Carvedilol ; Nebivolol ; Concentración ; Plasma sanguíneo ; Líquido biológico ; Prueba esfuerzo ; Ejercicio físico ; Bisoprolol ;

Mots-clés d'auteur / Author Keywords

nebivolol ; carvedilol ; bisoprolol ; pharmacokinetics ; exercise ;

Localisation / Location

INIST-CNRS, Cote INIST : 21146, 35400011212637.0080