RESUMO
Nifedipine, being a nitro aromatic compound, is capable of undergoing reduction via hydroxyl-amino intermediate to an amine. Such an intermediate is a mutagenic culprit. The urinary metabolites of nifedipine were investigated in order to allay the fear of the existence of this metabolic route in humans. Nifedipine (20 mg) was administered twice daily for 2 weeks. No nitro-reduction product was detected over a 1-month period. Nifedipine lacks mutagenicity in the absence or presence of drug metabolizing microsomes in Salmonella typhimurium TA 98 and Salmonella typhimurium TA 100.
Assuntos
Mutagênicos , Nifedipino/farmacocinética , Biotransformação , Humanos , Masculino , Testes de Mutagenicidade , Nifedipino/urinaRESUMO
The anticoagulant activities of 6-, 7-, 8-, 4'-hydroxy, 6-chloro- and 6-bromowarfarin were determined in rabbits after intraperitoneal administration of 16.2 mumol kg-1 over 96 h. Substitution on the 4-hydroxycoumarin moiety resulted in reduction of the anticoagulant activity. 6-Chlorowarfarin was more potent than 6-bromowarfarin suggesting that the molecular size of 4-hydroxycoumarin moiety may be crucial for biological activity.
