[Dose-dependent serum concentration of ISDN and its metabolites following administration of ISDN-retard. Studies under steady-state conditions].
In a randomized cross-over trial of four groups of patients (total 49 patients) the serum concentrations of isosorbide dinitrate (ISDN), isosorbide-2-mononitrate (IS-2-MN) and isosorbide-5-mononitrate (IS-5-MN) were measured under steady-state conditions after administration of 20, 40, 60 and 80 mg, respectively, of two ISDN preparations, the two being bioequivalent. At the studied dosage there was a linear relationship between dose and serum concentration of ISDN and its two metabolites in the proportion of 1:6:70. Because the serum concentration of IS-5-MN is so high under steady-state conditions, there is the potential problem of tolerance developing. The drug should therefore be administered at a lower dose twice daily.
D000368:Aged; D002986:Clinical Trials as Topic; D003327:Coronary Disease / Q000097:blood / Q000188:drug therapy*; D003692:Delayed-Action Preparations / Q000008:administration & dosage; D004305:Dose-Response Relationship, Drug; D005260:Female; D006801:Humans; D007548:Isosorbide Dinitrate / Q000008:administration & dosage* / Q000031:analogs & derivatives / Q000097:blood; D008297:Male; D011897:Random Allocation
D003692:Delayed-Action Preparations; C030398:isosorbide-2-mononitrate; D007548:Isosorbide Dinitrate; C030397:isosorbide-5-mononitrate
Dosisabhängige Serumkonzentration von ISDN und seinen Metaboliten nach ISDN-retard. Untersuchungen unter Steady-state-Bedingungen.