Oral pharmacokinetics of bisoprolol in resting and exercising healthy volunteers.
The effects of exercise on bisoprolol oral pharmacokinetics were studied in eight healthy male volunteers in an open, randomized, three-period, crossover trial. Oral bisoprolol (20 mg) was given either at rest during 24 h or with iterative stress tests before and 2.5, 5, 10, and 24 h after dosing. Exercise tests were repeated on a third placebo period. Bisoprolol was assayed in plasma and urines, and plasma catecholamines were measured before and after stress tests, Cmax, Tmax, elimination t1/2, and renal clearance of bisoprolol were not significantly modified by exercise. AUC0-infinity significantly decreased by 7.5% (p less than 0.05) with stress test resulting in an increase in apparent oral clearance. The beta-blocking effect peaked at 2.5 h, lasted greater than 24 h, and was related to plasma levels. The exercise-induced increase in plasma norepinephrine levels was significantly augmented with bisoprolol. These results suggest that repeated exercise tests exerted only limited effects on the oral pharmacokinetics of bisoprolol.
Le Coz
F
F
Clinical Pharmacology Unit, St. Antoine University Hospital, Paris, France.
Sauleman
P
P
Poirier
J M
JM
Cuche
J L
JL
Midavaine
M
M
Rames
A
A
Lecocq
B
B
Jaillon
P
P
D000319:Adrenergic beta-Antagonists / Q000493:pharmacokinetics* / Q000494:pharmacology; D000328:Adult; D017298:Bisoprolol; D001794:Blood Pressure / Q000187:drug effects; D002395:Catecholamines / Q000097:blood; D015444:Exercise; D005080:Exercise Test; D006207:Half-Life; D006339:Heart Rate / Q000187:drug effects; D006801:Humans; D008297:Male; D009638:Norepinephrine / Q000097:blood; D011412:Propanolamines / Q000493:pharmacokinetics* / Q000494:pharmacology
D000319:Adrenergic beta-Antagonists; D002395:Catecholamines; D011412:Propanolamines; D009638:Norepinephrine; D017298:Bisoprolol