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Trimethoprim–sulphamethoxazole does not affect the pharmacokinetics of sirolimus in renal transplant recipients
Author(s) -
Böttiger Ylva,
Brattström Christina,
Bäckman Lars,
Claesson Kerstin,
Burke James T.
Publication year - 2005
Publication title -
british journal of clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.216
H-Index - 146
eISSN - 1365-2125
pISSN - 0306-5251
DOI - 10.1111/j.1365-2125.2005.02475.x
Subject(s) - sirolimus , pharmacokinetics , trimethoprim , medicine , prednisolone , transplantation , kidney transplantation , urology , pharmacology , azathioprine , antibacterial agent , antibiotics , chemistry , biochemistry , disease
Aims The influence of the trimethoprim–sulphamethoxazole combination on the steady‐state pharmacokinetics of sirolimus, a potent macrocyclic immunosuppressant, was studied in renal transplant recipients. Methods Fifteen kidney transplant recipients were treated with sirolimus 8–23 mg m −2 in combination with azathioprine and prednisolone from the day of transplantation. Whole blood sirolimus AUC and C max were determined on days 6 and 7 after transplantation. On day 7, sirolimus was coadministered with the first dose of trimethoprim (80 mg) and sulphamethoxazole (400 mg). Results On day 6, the mean (95% confidence interval) whole blood sirolimus AUC (0−24 h) was 1040 (846, 1234) ng ml −1 and mean C max was 109 (88, 129) ng ml −1 . Corresponding values on day 7 were AUC (0−24 h) 1060 (826, 1293) ng ml −1 and C max mean 107 (87, 127) ng ml −1 . The mean difference in the dose‐corrected AUC (0−24 h) was 0.40% (−9.4, +10). Conclusions A single dose of trimethoprim–sulphamethoxazole does not affect the pharmacokinetics of sirolimus in renal transplant patients.