(should not be prescribed as rapamycin)
As an adjunct to or substitute to a calcineurin phosphatase inhibitor for immunosuppression in patients in whom ciclosporin/tacrolimus have been implicated in allograft pathology.
- Hypersensitivity to sirolimus and its derivatives.
- Pregnancy and breast feeding
- Presentation – 1mg and 2mg tablet
Dosage and Administration
Sirolimus is not used de-novo and is generally switched for tacrolimus. The following doses can be started and tacrolimus continued at half the current dose until sirolimus levels are therapeutic.
- Doses should be given on an empty stomach.
- Day 1 – 6mg daily
- Day 2 onwards – 2mg daily adjusted according to levels
- Check sirolimus level at 1 week
Target range 5-15ng/ml depending on whether it is an adjunct to or substitute for a CNI.
Note that target in SYMPHONY study when used in place of a CNI was 4/8 ng/ml and many dropped out due to adverse events despite this lower goal level.
Raised triglycerides and cholesterol
|Delayed wound healing||Lymphocele||Rash|
Compounds which modulate CYP3A4 activity may affect Sirolimus levels.
Drugs which may increase sirolimus levels:
|Azole antifungals||Cimetidine||Protease inhibitors|
|Macrolide antibiotics||Danazol||Grapefruit juice|
Drugs which may decrease sirolimus levels: Rifampicin, anticonvulsants