Effect of oxidative polymorphism (debrisoquine/sparteine type) on hepatic first-pass metabolism of bufuralol.
Bufuralol is a beta-adrenoceptor blocking drug whose oxidative metabolism is under the same genetic control as debrisoquine and sparteine. The pharmacokinetics of bufuralol were studied in 10 healthy subjects (7 extensive and 3 poor metabolizers of debrisoquine) after oral and intravenous administration. In extensive metabolizers the systemic availability of bufuralol was 43%. Poor metabolizers were characterized by a considerable increase in systemic availability due to a corresponding decrease in hepatic first-pass metabolism. After oral administration of bufuralol non-linear kinetics may occur.
Dayer
P
P
Balant
L
L
Kupfer
A
A
Striberni
R
R
Leemann
T
T
D000319:Adrenergic beta-Antagonists / Q000378:metabolism*; D000328:Adult; D003647:Debrisoquin / Q000378:metabolism; D004983:Ethanolamines / Q000378:metabolism*; D006801:Humans; D007700:Kinetics; D008099:Liver / Q000378:metabolism*; D010084:Oxidation-Reduction; D011110:Polymorphism, Genetic; D013034:Sparteine / Q000378:metabolism
D000319:Adrenergic beta-Antagonists; D004983:Ethanolamines; D013034:Sparteine; C010831:bufuralol; D003647:Debrisoquin