Pharmacokinetics of cyclosporine G in patients with renal failure

M. Wenk*, M. Bindschedler, E. Costa, M. Zuber, S. Vozeh, G. Thiel, E. Abisch, H. P. Keller, T. Beveridge, F. Follato

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

12 Citations (Scopus)

Abstract

The pharmacokinetics of the cyclosporine A (CsA, Sandimmune) analogue Nva2-cyclosporine, or cyclosporine G (CsG) was investigated in 6 patients with terminal renal failure after a 4-hr intravenous infusion (3.5 mg/kg) and after oral administration (600 mg) of the drug. Blood samples were collected up to 38 hr and CsG concentrations were measured by radioimmunoassay and high-performance liquid chromatography. The resulting pharmacokinetic parameters of CsG were similar to those described for CsA in the same patient population. Based on HPLC determinations, a mean terminal elimination half-life of 18.9 hr was calculated. The total body clearance was 0.55 L/hr/kg, the volume of the central compartment was 0.32 L/kg, and the steady-state volume of distribution was 5.97 L/kg. After oral administration maximum CsG concentrations in blood were reached between 2.5 and 3 hr, and the bioavailability was in the range of 24–55% (mean 36%). The ratios between the polivalent RIA and HPLC determinations were considerably larger after oral dosing than after i.v. infusion. The blood-to-plasma ratio was 1.23, which is smaller than that observed for CsA. These results suggest that in patients undergoing renal transplantation the same dosing strategies can be applied for CsG as have been established for CsA.

Original languageEnglish
Pages (from-to)558-561
Number of pages4
JournalTransplantation
Volume45
Issue number3
DOIs
Publication statusPublished - Mar 1988
Externally publishedYes

Fingerprint

Dive into the research topics of 'Pharmacokinetics of cyclosporine G in patients with renal failure'. Together they form a unique fingerprint.

Cite this