Concentrations of the vasodilator isosorbide dinitrate and its metabolites in the blood of human subjects.
An oral dose of 5 mg of 14C-isosorbide dinitrate was rapidly absorbed, biotransformed and excreted by human subjects. Peak whole blood concentrations of radioactivity were reached after 1.5 to 2 hours and declined relatively slowly. The radioactivity in whole blood mainly represented metabolites, isosorbide mononitrates. The peak concentrations found were 4.5, 11.7 and 34.3 ng/ml of isosorbide dinitrate, isosorbide 2-mononitrate and isosorbide 5-mononitrate, respectively, in the blood of one subject and 5.9, 15 and 61.3 ng/ml, respectively, in the blood of another subject. However, concentrations of the metabolites declined relatively slowly during 6 h after the oral urine of the first day (ca. 78%). The results showed that isosorbide mononitrates were available to contribute to the pharmacological action.
D001711:Biotransformation; D002250:Carbon Radioisotopes; D006801:Humans; D007548:Isosorbide Dinitrate / Q000097:blood*; D007700:Kinetics; D008297:Male; D008875:Middle Aged; D009566:Nitrates / Q000097:blood
D002250:Carbon Radioisotopes; D009566:Nitrates; D007548:Isosorbide Dinitrate