Drug Index


Mechanism :

Sirolimus inhibits T lymphocyte activation and proliferation that occurs in response to antigenic and cytokine (Interleukin IL-2, IL-4, and IL-15) stimulation by a mechanism that is distinct from that of other immunosuppressants. Sirolimus also inhibits antibody production. In cells, sirolimus binds to the immunophilin, FK Binding Protein-12 (FKBP-12), to generate an immunosuppressive complex. The sirolimus:FKBP-12 complex has no effect on calcineurin activity. This complex binds to and inhibits the activation of the mammalian Target of Rapamycin (mTOR), a key regulatory kinase. This inhibition suppresses cytokine-driven T-cell proliferation, inhibiting the progression from the G1 to the S phase of the cell cycle.

Indication :

  • Kidney transplant rejection prophylaxis

Contraindications :

Hypersensitivity to drug/class/component, Lung transplant use, Liver transplant use.

Caution if hepatic impairment, renal impairment, concurrent nephrotoxic agent use, delayed graft function, BMI >30 kg/m², hyperlipidemia.

Dosing :

>13 years, <40 kg:
Start with 3 mg/m² PO after kidney transplant and then maintenance dose of 1 mg/m² PO once daily. Max: 40 mg/day.
>13 years, >40 kg:
Start: 6 mg PO after transplant and then a maintenance dose of 2 mg PO once daily. Max: 40 mg/day.
Adjust dose based on trough levels. Adjust maintenance dose no more frequently than every 7-14 days.

Adverse Effect :

Serious Reactions: Immunosuppression, malignancy, lymphoma, infection, PML, BK virus-associated nephropathy, nephrotic syndrome, hemolytic uremic syndrome, TTP, thrombotic microangiopathy, venous thromboembolism, myelosuppression, hypersensitivity reaction, anaphylaxis/anaphylactoid reaction, angioedema, exfoliative dermatitis, impaired wound healing, lymphocele, ascites, pericardial effusion, pleural effusion, interstitial lung disease, hepatotoxicity, hypokalemia, osteonecrosis.

Common Reactions: Peripheral edema, hyperlipidemia, hypertension, constipation, diarrhea, headache, fever, anemia, nausea, arthralgia, thrombocytopenia, acne, rash, proteinuria, tachycardia, stomatitis, leukopenia, abnormal healing, hypokalemia, epistaxis, pyelonephritis, ovarian cysts, menstrual disorder.

Interaction :

Adenovirus vaccine, live; BCG live intravesical; Cidofovir; Influenza nasal vaccine, live; Ketoconazole; Measles/mumps/rubella vaccine, live; Mifepristone; Posaconazole; Rotavirus vaccine, live; Smallpox vaccine (live vaccinia virus); Streptozocin; Typhoid vaccine, live; Varicella vaccine, live; Voriconazole; Yellow fever vaccine, live; Zoster vaccine, live.

Renal Dose :

Dose in Renal Impairment GFR (mL/min)
20-50Dose as in normal renal function
10-20Dose as in normal renal function
<10Dose as in normal renal function

Dose in Patients undergoing Renal Replacement Therapies
CAPDUnlikely to be dialysed. Dose as in normal renal function
HDNot dialysed. Dose as in normal renal function
HDF/High fluxUnknown dialysability. Dose as in normal renal function
CAV/VVHDUnlikely to be dialysed. Dose as in normal renal function

Hepatic Dose :

There is no change of dose in loading dose.
Mild to moderate hepatic impairment: The maintenance dose should be reduced by one-third.
Severe hepatic impairment: The maintenance dose should be reduced by 50%.
12/20/2023 06:37:11 Sirolimus
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