EFFECT OF MICROSOMAL ENZYME INDUCERS ON THE BILIARY EXCRETION OF CARDIAC GLYCOSIDES

摘要: Digitoxin (2.5 mg/kg), digoxin (7 mg/kg) or ouabain (5 was given i.v. to rats pretreated for 4 days with phenobarbital (PB, 50 pregnenolone-16α-carbonitrile (PCN, 75 spironolactone (S, 3-methylcholanthrene (3-MC, 20 mg/kg). Plasma disappearance and biliary excretion of the cardiac glycosides were measured 2 hours. PCN S increased rate radioactivity associated digitoxin by 1000 400% respectively. PB-treatment only 25% 3-MC decreased it. Similarly 3 H-digoxin, tritium 400 150%, respectively, whereas PB it The as polar metabolites in H-digoxin not has been reported digitoxin. due a more lipid-soluble metabolite, digoxin-bisdigitoxoside, parent compound. PCN, ouabain, glcoside that is biotransformed before its excretion, 150, 80%, These studies demonstrate there marked difference ability microsomal enzyme inducers enhance mechanism solely dependent on biotransformation glycoside metabolites.