Effect of cyclosporine on colchicine partitioning in the rat liver

Kermit V. Speeg, Alma L. Maldonado

Research output: Contribution to journalArticlepeer-review

11 Scopus citations

Abstract

Colchicine is secreted into bile as a major pathway of elimination. Cyclosporine (CsA) inhibits colchicine biliary secretion. In the present study, the effects of cyclosporine and its vehicle (cremophor) on the partitioning of colchicine across the liver were studied. CsA decreased the colchicine bile/plasma ratio from 484±39 to 53±3 (P<0.001). This effect was due to both a decrease in bile/liver partitioning (control, 35.1±1.2, vs CsA treatment, 9.2±0.5;p<0.001) as well as a decrease in liver/plasma partitioning (conrol, 13.7±0.8, vs CsA treatment, 5.7±0.4;P<0.001). Cremophor also decreased the colchicine bile/plasma ratio (317±19, P<0.02 vs control), but this effect was due to a decrease in the liver/plasma ratio (9.99±0.7, P<0.02 vs control) rather than the bile/liver ratio (31.9±2.1, P>0.2 vs control). Inhibition at the canalicular membrane is consistent with the location of gp-170, the presumed transporter of colchicine.

Original languageEnglish (US)
Pages (from-to)434-436
Number of pages3
JournalCancer Chemotherapy and Pharmacology
Volume32
Issue number6
DOIs
StatePublished - Nov 1 1993

ASJC Scopus subject areas

  • Oncology
  • Toxicology
  • Pharmacology
  • Cancer Research
  • Pharmacology (medical)

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