Immunosuppression With Sirolimus After Solid Organ Transplantation in Children

Marcia L. Buck, Pharm.D., FCCP

Pediatr Pharm. 2006;12(2) 

In This Article

Drug Interactions

Administration of sirolimus with CYP3A4 inhibitors will result in a decrease in metabolism and an increase in sirolimus concentrations.

Drugs known to inhibit CYP3A4 include:

bromocriptine ketoconazole
cimetidine metoclopramide
cisapride nicardipine
clarithromycin telithromycin
clotrimazole telithromycin
danazole troleandomycin
erythromycin verapamil
fluconazole voriconazole
itraconazole all protease inhibitors

Grapefruit juice also reduces CYP3A4 activity and should not be administered with sirolimus. In contrast, concomitant use with CYP3A4 inducers, such as carbamazepine, phenobarbital, phenytoin, rifabutin, rifampin, rifapentine, or St. John's wort, may increase the rate of CYP3A4 activity and reduce sirolimus concentrations.[2,3]

Sirolimus concentrations may also be increased with concomitant administration of cyclosporine or diltiazem. It is recommended that sirolimus be administered 4 hours after cyclosporine to minimize variations in trough sirolimus concentrations.[2,3]

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