RAPAMUNE (Sirolimus)

RAPAMUNE (Sirolimus)

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What is this medication?

Sirolimus, Rapamune
Immunosuppressant Agent
mTOR Kinase Inhibitor

Sirolimus is indicated for treatment of lymphangioleiomyomatosis, renal transplantation (rejection prophylaxis).      

“ALERT: US Boxed Warning

Increased susceptibility to infection and the possible development of lymphoma and other malignancies may result from immunosuppression.

Experienced physician:
Only physicians experienced in immunosuppressive therapy and management of renal transplant patients should use sirolimus for prophylaxis of organ rejection in patients receiving renal transplants. Patients receiving sirolimus should be managed in facilities equipped and staffed with adequate laboratory and supportive medical resources. The physician responsible for maintenance therapy should have complete information requisite for the follow-up of the patient.

Liver transplantation:
The use of sirolimus in combination with tacrolimus was associated with excess mortality and graft loss in a study in de novo liver transplant patients. Many of these patients had evidence of infection at or near the time of death. In this and another study in de novo liver transplant patients, the use of sirolimus in combination with cyclosporine or tacrolimus was associated with an increase in hepatic artery thrombosis; most cases of hepatic artery thrombosis occurred within 30 days posttransplantation, and most led to graft loss or death. The safety and efficacy of sirolimus as immunosuppressive therapy have not been established in liver transplant patients; therefore, such use is not recommended.

Lung transplantation:
Cases of bronchial anastomotic dehiscence, most fatal, have been reported in de novo lung transplant patients when sirolimus has been used as part of an immunosuppressive regimen. The safety and efficacy of sirolimus as immunosuppressive therapy have not been established in lung transplant patients; therefore, such use is not recommended.”

How does this medication work? 

Sirolimus, Rapamune has a mechanism that differs from other immunosuppressive agents.  It inhibits T-lymphocyte activation and proliferation in response to antigenic and cytokine stimulation and inhibits antibody production. It does this via binding FKBP-12, an intracellular protein, to form an immunosuppressive complex which inhibits the regulatory kinase, mTOR (mechanistic target of rapamycin). This inhibition suppresses cytokine mediated T-cell proliferation.  It prolongs graft survival and inhibits acute rejection of allografts.  In lymphangioleiomyomatosis, the mTOR signaling pathway is activated through loss of the tuberous sclerosis complex gene function.  By inhibiting the mTOR pathway, sirolimus prevents the proliferation of lymphangioleiomyomatosis cells.

How should I take this medication? 

Dosing is complex and must be tailored to the patient based on various factors and requires a physician experienced with immunosuppressive therapies.

How to Take: Administer at the same times per day and consistently either with food or without food.  Do not crush, split, or chew tablets.

You Need to Avoid: Do not consume grapefruit juice as it may decrease clearance of sirolimus. Ingestion with high-fat meals effects the absorption of the medication and so take consistently (either with or without food) to minimize variability.

What should I watch for while using this medication?

Before starting Sirolimus, Rapamune make sure your physician is aware of any allergies or medications you currently take, if you have hepatic impairment, are pregnant, or breastfeeding. Sirolimus, Rapamune use has been associated with adverse events such as anaphylaxis/hypersensitivity reactions, angioedema, infections, interstitial lung disease, hyperlipidemia, lymphocele/fluid accumulation, malignancy, proteinuria, renal effects, and wound dehiscence.

What if I miss a dose?

If you miss a dose of medication, try to take it as soon as possible. However, if it is almost time for your next dose, take only that scheduled dose. Do not take double or extra doses.

How should I store this medication?

Keep out of the reach of children at all times. Store at room temperature, 59 to 86° F (15 to 30° C). Protect from light. Keep the container tightly closed.  Properly dispose of any unused medication after the expiration date.

What are the possible side effects of using this medication? 

Peripheral edema, hypertension, edema, deep vein thrombosis, pulmonary embolism, tachycardia, headache, pain, dizziness, acne vulgaris, skin rash, hypertriglyceridemia, hypercholesterolemia, amenorrhea, diabetes mellitus, hypermenorrhea, hypervolemia, hypokalemia, increased lactate dehydrogenase, menstrual disease, ovarian cyst, constipation, abdominal pain, diarrhea, nausea, stomatitis, urinary tract infection, anemia, thrombocytopenia, lymphoproliferative disorder, skin carcinoma, hemolytic-uremic syndrome, leukopenia, lymphocele, thrombotic thrombocytopenic purpura, herpes simplex infection, herpes zoster, sepsis, arthralgia, myalgia, osteonecrosis, increased serum creatinine, pyelonephritis, nasopharyngitis, epistaxis, pneumonia, upper respiratory tract infection, wound healing impairment.