Cyclosporine pharmacokinetic drug interactions.
Cyclosporine (CyA) is commonly prescribed as an immunosuppressive to prevent rejection of organ transplants. Numerous pharmacokinetic drug interactions of potential clinical significance exist because other drugs may induce or inhibit the metabolism of CyA. Case reports and studies demonstrate that rifampin, phenytoin, phenobarbital, and carbamazepine may induce the hepatic metabolism of CyA, causing decreased CyA concentrations. Graft rejection through inadequate immunosuppression may be associated with subtherapeutic or decreased CyA levels. Erythromycin, ketoconazole, calcium channel blockers, and sex hormones appear to inhibit CyA metabolism, causing increased CyA concentrations. Signs and symptoms of renal, hepatic, or neurotoxicity may be evident with increased or toxic CyA levels. Mutual inhibition of metabolism occurs between CyA and corticosteroids. Intravenous sulphadimidine and trimethoprim may cause decreased CyA concentrations by an unknown mechanism.
Baciewicz
A M
AM
Department of Pharmacy Services, University Hospitals of Cleveland, Ohio 44106.
Baciewicz
F A
FA
D000305:Adrenal Cortex Hormones / Q000494:pharmacology; D000927:Anticonvulsants / Q000494:pharmacology; D002121:Calcium Channel Blockers / Q000494:pharmacology; D003524:Cyclosporins / Q000493:pharmacokinetics*; D004917:Erythromycin / Q000494:pharmacology; D006801:Humans; D007654:Ketoconazole / Q000494:pharmacology; D012293:Rifampin / Q000494:pharmacology; D013449:Sulfonamides / Q000494:pharmacology
D000305:Adrenal Cortex Hormones; D000927:Anticonvulsants; D002121:Calcium Channel Blockers; D003524:Cyclosporins; D013449:Sulfonamides; D004917:Erythromycin; D007654:Ketoconazole; D012293:Rifampin