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Sirolimus

Immunosuppressant · Organ Transplant Rejection Prophylaxis

ImmunosuppressantOrgan Transplant Rejection Prophylaxis
CDSCO approvedSchedule H
EXCRETION
not curated
INTERACTIONS
12 major
incl. contraindicated
PREGNANCY
not curated
Top interactionssee all 12
  • PosaconazoleContraindicatedDatabaseKimi deep-research + Cla
  • AzolesSevereTextbookHarrison 22e · p1742
  • CiprofloxacinSevereTextbookKDT 7e · p882
  • LopinavirSevereTextbookKDT 7e · p882

Mechanism

Sirolimus functions as a non-calcineurin inhibiting immunosuppressant. It is used to suppress rejection in organ transplant recipients by modulating the immune response.

Indications

Prophylaxis of organ rejection in kidney allograft recipientsPrevention of transplant rejectionprophylaxis of organ transplant rejectionincorporated into stents to inhibit occlusionanticancer effects

Dosing

Adult
Initially 6 mg for 1 dose, to be given after surgery once wound has healed, then 2 mg once daily. To be given in combination with ciclosporin and corticosteroid for 2–3 months (sirolimus doses should be given 4 hours after ciclosporin), ciclosporin should then be withdrawn over 4–8 weeks (if not possible, sirolimus should be discontinued and an alternate immunosuppressive regimen used).…

Pharmacokinetics

Bioavailability
∼15%
Protein binding
40%
Metabolism
CYP3A
Excretion

Side effects

Common
Abdominal painAnaemiaArthralgiaAscitesConstipationDiabetes mellitusDiarrhoeaDyslipidaemiaElectrolyte imbalanceEmbolism and thrombosisFeverHaemolytic uraemic syndromeHaemorrhageHeadacheHealing impairedHyperglycaemiaHypertensionIncreased risk of infection (especially urinary-tract infection)LeucopeniaLymphatic vessel disorderhyperlipidemiaanemialeukopeniathrombocytopeniagi effectsmouth ulcershyperkalemia
Serious
  • Increased susceptibility to lymphoma and other malignancies (particularly of the skin)
  • Embolism and thrombosis
  • Haemolytic uraemic syndrome

Drug interactions

Posaconazole
Contraindicated
Database

Markedly increased sirolimus levels

Contraindicated per label

Source: Kimi deep-research + Cla

Azoles
Severe
Textbook

Increased plasma levels of sirolimus.

Source: Harrison 22e · p1742

Ciprofloxacin
Severe
Textbook

Significantly altered (increased) sirolimus blood levels, requiring monitoring.

Blood level monitoring is required.

Source: KDT 7e · p882

Lopinavir
Severe
Textbook

Significantly altered (increased) sirolimus blood levels, requiring monitoring.

Blood level monitoring is required.

Source: KDT 7e · p882

Rifampin
Severe
Textbook

Significantly altered (decreased) sirolimus blood levels, requiring monitoring.

Blood level monitoring is required.

Source: KDT 7e · p882

Acyclovir
Severe
Database

Drug interaction classified as: synergy.

Source: DDInter

Adalimumab
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Amikacin
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Amphotericin B
Severe
Database

Drug interaction classified as: synergy.

Source: DDInter

Amprenavir
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Apalutamide
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Atazanavir
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Related guidelines

Other Immunosuppressant drugs

Ask House about Sirolimus

Continue into a citation-backed clinical answer with the drug context already attached.

Sources: KD Tripathi 7e, Goodman & Gilman 14e, Katzung, BNF·Verified: 2026-05-13 · House clinical team