Clinical relevance of sirolimus drug interactions in transplant patients.

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Sadaba B, Campanero MA, Quetglas EG, Azanza JR

Clinical relevance of sirolimus drug interactions in transplant patients.

Transplant Proc. 2004 Dec;36(10):3226-8. doi: 10.1016/j.transproceed.2004.10.056.

PubMed ID

15686733 [ View in PubMed

]

Abstract

Sirolimus, a new immunosuppressant drug; is metabolized by cytochrome P450 3A4 (CYP3A4) and is a substrate of the P-glycoprotein drug efflux pump. The CYP3A4/P-glycoprotein system is mainly localized in the liver and intestine. It is responsible for the severe first pass metabolism of sirolimus with a low bioavailability. Drugs like voriconazole, itraconazole, fluconazole, and erytrhomycin may decrease the metabolic activity of this enzymatic system. This report documents in five patients that coadministration of these antimicrobials with sirolimus increases the blood concentrations of the immunosuppressant. The dose-normalized trough blood concentration showed a mean increase of sevenfold with the coadministration of these drugs. It is essential to monitor the blood sirolimus concentrations and to adjust the sirolimus doses before and after coadministration of these drugs.

DrugBank Data that Cites this Article

Drug Enzymes

Drug	Enzyme	Kind	Organism	Pharmacological Action	Actions
Sirolimus	Cytochrome P450 3A4	Protein	Humans	No	Substrate	Details

Drug Interactions

• Approved
• Vet approved
• Nutraceutical
• Illicit
• Withdrawn
• Investigational
• Experimental
• All Drugs

Drugs	Interaction
Integrate drug-drug interactions in your software
Sirolimus Ketoconazole	The serum concentration of the active metabolites of Sirolimus can be increased when Sirolimus is used in combination with Ketoconazole.
Sirolimus Itraconazole	The serum concentration of the active metabolites of Sirolimus can be increased when Sirolimus is used in combination with Itraconazole.
Sirolimus Voriconazole	The serum concentration of Sirolimus can be increased when it is combined with Voriconazole.
Temsirolimus Ketoconazole	The serum concentration of the active metabolites of Temsirolimus can be increased when Temsirolimus is used in combination with Ketoconazole.
Temsirolimus Itraconazole	The serum concentration of the active metabolites of Temsirolimus can be increased when Temsirolimus is used in combination with Itraconazole.