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  • Title: Biotransformation of the stable prostacyclin analogue, iloprost, in the rat.
    Author: Krause W, Hümpel M, Hoyer GA.
    Journal: Drug Metab Dispos; 1984; 12(5):645-51. PubMed ID: 6209077.
    Abstract:
    The metabolic pathway of the stable prostacyclin analogue, iloprost (ZK 36 374), was studied in the rat, both in vivo and in vitro by a rat liver perfusion model. Metabolites were isolated from both experiments by preparative high performance liquid chromatography and identified by GC/MS and NMR analysis. In vitro, iloprost was metabolized by consecutive beta-oxidation of the upper side chain. Both dinor- and tetranoriloprost could be isolated from the perfusion medium. The metabolic pattern in bile was similar to that in the perfusion medium. In vivo, iloprost was totally metabolized by beta-oxidation of the upper side chain and by subsequent hydroxylation and conjugation. The compounds identified in rat urine were tetranoriloprost which represented about 3/4 of all metabolites, hydroxylated tetranoriloprost with the additional hydroxyl group presumably at position 17 and a conjugate of tetranoriloprost. Dinoriloprost and unchanged drug were not observed. beta-Oxidation of the upper side chain was stereoselective to give a 6 alpha-H/6 beta-H ratio of 86:14.
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