A single dose of ursodiol does not affect cyclosporine absorption in liver transplant patients.
OBJECTIVE
To study the possible influence of ursodiol (ursodeoxycholic acid), a hydrophilic bile acid, on cyclosporine (CsA) bioavailability.


METHODS
Seven adult liver transplant recipients participated in a randomised cross-over pharmacokinetic study comparing ursodiol (600 mg) with placebo in single doses. Blood concentrations of CsA were measured by HPLC.


RESULTS
There was no significant effect of ursodiol on CsA absorption: AUC was 5011 vs 5486 ng.h.ml-1, Cmax was 832 vs 871 ng.ml-1 and tmax was 2 vs 2 h, after ursodiol and placebo, respectively.


CONCLUSIONS
Although a significant period effect was observed, we conclude that a single dose of ursodiol has little effect on CsA absorption in liver transplant patients and that an interaction in the intestinal lumen between these two drugs is unlikely.
Maboundou
C W
CW
Department of Clinical Pharmacology, Besançon University Hospital, F-25030 Besançon, France.
Paintaud
G
G
Vanlemmens
C
C
Magnette
J
J
Bresson-Hadni
S
S
Mantion
G
G
Miguet
J P
JP
Bechtel
P R
PR
D000284:Administration, Oral; D000328:Adult; D000368:Aged; D001682:Biological Availability; D002756:Cholagogues and Choleretics / Q000008:administration & dosage / Q000494:pharmacology*; D018592:Cross-Over Studies; D016572:Cyclosporine / Q000097:blood / Q000493:pharmacokinetics*; D004359:Drug Therapy, Combination; D006801:Humans; D007166:Immunosuppressive Agents / Q000097:blood / Q000493:pharmacokinetics*; D007408:Intestinal Absorption / Q000187:drug effects* / Q000502:physiology; D016031:Liver Transplantation / Q000502:physiology*; D008297:Male; D008875:Middle Aged; D014580:Ursodeoxycholic Acid / Q000008:administration & dosage / Q000494:pharmacology*
D002756:Cholagogues and Choleretics; D007166:Immunosuppressive Agents; D014580:Ursodeoxycholic Acid; D016572:Cyclosporine