Sirolimusum

Sirolimusum 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. Sirolimusum is a potent immunosuppressant and possesses both antifungal and antineoplastic properties.

Sirolimusum, 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.

Trade Name Sirolimusum
Availability Prescription only
Generic Sirolimus
Sirolimus Other Names Rapamycin, Sirolimús, Sirolimus, Sirolimusum
Related Drugs Sabril, Rapamune, tacrolimus, azathioprine, cyclosporine, mycophenolate mofetil, CellCept, Imuran
Type
Formula C51H79NO13
Weight Average: 914.187
Monoisotopic: 913.555141608
Protein binding

92%

Groups Approved, Investigational
Therapeutic Class
Manufacturer
Available Country
Last Updated: September 19, 2023 at 7:00 am
Sirolimusum
Sirolimusum

Uses

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

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

Sirolimusum 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 Sirolimusum works

Sirolimusum 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. Sirolimusum 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.

Sirolimusum Cholesterol interaction

[Moderate] The use of sirolimus may increase serum cholesterol and triglycerides.

Care should be taken when prescribing this agent to hyperlipidemic patients.

It is recommended to assess the risk

It is recommended to monitor patients regularly for elevated lipids.

Half Life

57-63 hours

Innovators Monograph

You find simplified version here Sirolimusum

*** Taking medicines without doctor's advice can cause long-term problems.
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