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A macrolide compound obtained from Streptomyces hygroscopicus that acts by selectively blocking the transcriptional activation of cytokines thereby inhibiting cytokine production. It is bioactive only when bound to immunophilins. Sirolimus is a potent immunosuppressant and possesses both antifungal and antineoplastic properties.


Prophylaxis of Organ Rejection in Renal Transplantation.


Oral: Adjust dose to obtain whole blood trough 4-12ng/mL.



Special Precautions

Hepatic or renal impairment. Avoid sunlight exposure. Not recommended in lung or liver transplant. Paediatric: Safety below 13 years not established. Pregnancy: Category C; Use if risk to fetus outweighs benefits. Lactation: Secreted in milk. Elderly: Use with caution.

Side Effects

Increased suspectibility to infection, Lymphoma and malignancy, Excess mortality, graft loss, and hepatic artery thrombosis in liver transplant patients, Bronchial anastomotic dehiscence in lung transplant patients, hypersensitivity reactions, Exfoliative dermatitis, angioedema, fluid accumulation and wound healing, hypertriglyceridemia, hypercholesterolemia, decline in renal function in long-term combination of cyclosprine with Rapamune, Proteinuria, interstitial lung disease, Increased risk of

Drug Interactions

Inhibitors of CYP3A4 such as ketoconazole and protease inhibitors may increase the plasma concentrations of sirolimus. Do not take with ciclosporin, at least 4 hr apart. May cause angioneurotic oedema-type reactions when used with ACE inhibitor. May decrease response to vaccines.

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