[Pharmacokinetics of two beta blocking drugs: detection of a pharmacogenetic abnormality].
10 healthy male volunteers received orally either 100 mg tolamolol or 20 mg bufuralol. These experiments were repeated by intravenous administration of 10 and 5 mg respectively of these two drugs. Plasma levels of the parent drugs and their main metabolite were measured. In one subject, the apparent half-life of elimination was increased from 2.5 h (normal subjects) to 5 h for both drugs. This prolongation of the half-life is associated with low plasma levels of the metabolites, a peculiarity which can be explanined by a decreased rate of metabolism for these two drugs. This anomaly may explain the marked orthostatic hypotension observed only in this subject. The likelihood of a pharmacogenetic defect is discussed.
D000284:Administration, Oral; D000319:Adrenergic beta-Antagonists / Q000008:administration & dosage / Q000378:metabolism / Q000494:pharmacology*; D000328:Adult; D001572:Benzofurans / Q000494:pharmacology; D004983:Ethanolamines / Q000494:pharmacology*; D006207:Half-Life; D006801:Humans; D007024:Hypotension, Orthostatic / Q000139:chemically induced; D007275:Injections, Intravenous; D008297:Male; D010597:Pharmacogenetics; D011412:Propanolamines / Q000494:pharmacology*
D000319:Adrenergic beta-Antagonists; D001572:Benzofurans; D004983:Ethanolamines; D011412:Propanolamines
Pharmacocinétique de deux médicaments bêta-bloquants: détection d'une anomalie pharmacogénétique