Sirolimus

Sirolimus Uses, Dosage, Side Effects, Food Interaction and all others data.

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.

Sirolimus, a macrocyclic lactone produced by Streptomyces hygroscopicus, is an immunosuppressive agent indicated for the prophylaxis of organ rejection in patients receiving renal transplants. It is recommended that sirolimus be used in a regimen with cyclosporine and corticosteroids.

Sirolimus
Uses
Dosage
Side Effect
Precautions
Interactions
Uses during Pregnancy
Uses during Breastfeeding
Accute Overdose
Food Interaction
Half Life
Volume of Distribution
Clearance
Interaction With other Medicine
Contradiction
Storage

Trade Name	Sirolimus
Availability	Prescription only
Generic	Sirolimus
Sirolimus Other Names	Rapamycin, Sirolimús, Sirolimus, Sirolimusum
Related Drugs	Sabril, Rapamune, tacrolimus, azathioprine, cyclosporine, mycophenolate mofetil, CellCept, Imuran
Weight	1mg/ml, 0.5mg, 1mg, 2mg
Type	Oral solution, oral tablet
Formula	C₅₁H₇₉NO₁₃
Weight	Average: 914.187 Monoisotopic: 913.555141608
Protein binding	92%
Groups	Approved, Investigational
Therapeutic Class
Manufacturer
Available Country	United States
Last Updated:	September 19, 2023 at 7:00 am

Uses

Sirolimus is an immunosuppressant used to prevent organ transplant rejections and to treat lymphangioleiomyomatosis.

For the prophylaxis of organ rejection in patients receiving renal transplants.

Sirolimus is also used to associated treatment for these conditions: Chordomas, Graft Versus Host Disease (GVHD), Heart Transplant Rejection, Liver Transplant Rejection, Lung Transplant Rejection, Lymphangioleiomyomatosis, Renal Angiomyolipomas, Moderate renal transplant rejection

How Sirolimus works

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.

Food Interaction

Avoid grapefruit products. Grapefruit inhibits the CYP3A4 metabolism of sirolimus and increases its serum concentration.
Exercise caution with St. John's Wort. This herb induces CYP3A4 and P-gp; thus it may reduce sirolimus serum concentrations.
Take with or without food. Take consistently with regard to food.

[Moderate] ADJUST DOSING INTERVAL: Consumption of food can decrease the rate and extent of gastrointestinal absorption of sirolimus.

Also, the consumption of grapefruit juice may result in increased sirolimus trough concentrations.

MANAGEMENT: Experts recommend that this drug be taken either at least one hour prior to eating or consistently with or without food to avoid variations in sirolimus blood levels.

The manufacturer recommends against using grapefruit juice for dilution of sirolimus doses.

Patients should be monitored for clinical and laboratory evidence of altered immunosuppressant effects.