Concentrations of the vasodilator isosorbide dinitrate and its metabolites in the blood of human subjects |
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Authors: | L. F. Chasseaud W. H. Down R. K. Grundy |
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Affiliation: | (1) Department of Metabolism and Pharmacokinetics, Huntingdon Research Centre, Huntingdon, England |
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Abstract: | Summary An oral dose of 5 mg of14C-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 dose. Up to 99% of an oral dose of isosorbide dinitrate was excreted during 5 days, mainly in the urine of the first day (ca. 78%). The results showed that isosorbide mononitrates were available to contribute to the pharmacological action. |
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Keywords: | Isosorbide dinitrate pharmacokinetics metabolism pharmacological action nitrates |
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