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Home / Drugs / Starting with S / Sirolimus
 
Sirolimus
 

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. [PubChem]
BrandsRapamune
CategoriesAnti-Bacterial Agents
Antifungals
Immunosuppressive Agents
Antifungal Agents
Antibiotics, Antineoplastic
Macrolides
ManufacturersWyeth pharmaceuticals inc
PackagersCardinal Health
Hangzhou Zhongmei Huadong Pharmaceutical Co. Ltd.
Lake Erie Medical and Surgical Supply
Patheon Inc.
Poli Industria Chimica SPA
Wyeth Pharmaceuticals
Synonyms(-)-Rapamycin
Rapamycin

indication

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

pharmacology

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.

mechanism of action

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.

half life

57-63 hours

drug interactions

Atazanavir: Increases the effect and toxicity of immunosuppressant

Clarithromycin: The macrolide, clarithromycin, may increase the serum concentration of sirolimus.

Cyclosporine: Increases the effect and toxicity of sirolimus

Diltiazem: Increases the effect and toxicity of sirolimus

Erythromycin: The macrolide, erythromycin, may increase the serum concentration of sirolimus.

Fosphenytoin: The hydantoin decreases sirolimus levels

Itraconazole: Itraconazole may increase the effect and toxicity of sirolimus.

Ketoconazole: Ketoconazole may increase the effect and toxicity of sirolimus.

Phenytoin: The hydantoin decreases sirolimus levels

Rifabutin: The rifamycin decreases the effect of sirolimus

Rifampin: The rifamycin decreases the effect of sirolimus

Tacrolimus: Sirolimus may decrease the blood concentration of Tacrolimus. Monitor for changes in the therapeutic/toxic effects of Tacrolimus if Sirolimus therapy is initiated, discontinued or altered.

Telithromycin: Telithromycin may reduce clearance of Sirolimus. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Sirolimus if Telithromycin is initiated, discontinued or dose changed.

Tipranavir: Tipranavir may affect the efficacy/toxicity of Sirolimus.

Trandolapril: Increased risk of angioedema. Monitor for signs and symptoms of facial and systemic edema and/or erythema.

Trastuzumab: Trastuzumab may increase the risk of neutropenia and anemia. Monitor closely for signs and symptoms of adverse events.

Voriconazole: Voriconazole may increase the serum concentration of sirolimus likely by inhibition of CYP3A4-mediated metabolism or p-glyprotein transport of sirolimus. Consider alternate therapy or reduce the dose of sirolimus and monitor serum levels during concomitant therapy.