The disposition of suramin in the isolated perfused rat liver

Biochemical Pharmacology
M D Coleman, K K Adjepon-Yamoah

Abstract

We have investigated the disposition of suramin in the isolated perfused rat liver preparation (IPRL) after the administration of suramin (18 mg, 8 muCi). At 30 min post drug administration, almost 100% of the [14C]radioactivity and unchanged suramin were located in the perfusate plasma. During the course of the study, the elimination of suramin from the IPRL was barely perceptible. The AUC0-5 hr of suramin (730.6 +/- 86.2 micrograms hr/ml) corresponded to that of [14C] radioactivity (815.1 +/- 105.5 micrograms ml/hr) at 5 hr, indicating a lack of perfusate suramin metabolites. At 5 hr only a small proportion of [14C] radioactivity was recovered from the livers (2.5 +/- 1.1%). Subsequent HPLC analysis of the liver tissue indicated this to be unchanged suramin. Sub-cellular fractionation of the homogenised livers revealed suramin to be distributed in the liposomal rich tissue fractions (10,000 g pellet, 1.6 +/- 0.8%; 105,000 g supernatant, 1.1 +/- 0.35%). Biliary excretion of [14C] radioactivity was low (2.1 +/- 0.7%), however, none could be accounted for as unchanged suramin. Previously undetected metabolites of suramin may have accounted for the unidentified biliary radioactivity.

References

Nov 1, 1982·Hepatology : Official Journal of the American Association for the Study of Liver Diseases·G W MihalyF J Vajda
May 1, 1984·Hepatology : Official Journal of the American Association for the Study of Liver Diseases·D B JonesN P Madsen

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Citations

Jan 1, 1986·Advances in Enzyme Regulation·D Häussinger
Feb 9, 2000·Pharmacology & Therapeutics·J A RingD J Morgan
Nov 15, 1996·Journal of Chromatography. B, Biomedical Applications·M Kassack, P Nickel
May 22, 1998·Journal of Pharmacological and Toxicological Methods·S Sahin, M Rowland
Dec 9, 1998·Journal of Pharmacological and Toxicological Methods·B AlexanderI S Benjamin

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