Sirolimus

Graft vs Host Disease, NA

Drug Status

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Government Approvals

US(FDA), UK(BNF)

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WHO Essential Medicine

NO

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Known Teratogen

NO

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Pharmaceutical Class

Kinase Inhibitor and MTOR Inhibitor Immunosuppressant

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Controlled Drug Substance

NO

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Drug Ingredient

Sirolimus

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Summary

  • Sirolimus is typically used to prevent organ rejection in kidney transplant patients. It is also effective in treating lymphangioleiomyomatosis (LAM), a rare lung disease.

  • Sirolimus works by suppressing the immune system. It inhibits the activation and proliferation of T-cells, which are crucial for immune response. This prevents the immune system from attacking the transplanted organ.

  • The usual starting dose of Sirolimus for adults is a 6 mg loading dose, followed by 2 mg once daily. For children aged 13 years and older, the dosing is similar to adults. Always follow your doctor's instructions.

  • Common side effects include fatigue, weakness, headaches, abdominal pain, diarrhea, nausea, and weight changes. Serious adverse effects include increased risk of infections, lymphoma and skin cancer. Always report any severe or persistent symptoms to your healthcare provider.

  • Sirolimus can harm an unborn baby and should not be used during pregnancy unless absolutely necessary. It can also pass into breast milk and is not recommended for breastfeeding mothers. It increases the risk of infections and certain cancers. It should not be used in liver or lung transplant patients due to serious complications. Regular monitoring of blood levels and kidney function is essential.

Indications and Purpose

How does one know if Sirolimus is working?

The benefit of Sirolimus is evaluated through regular monitoring of blood levels to ensure they are within the target range. Doctors also assess the patient's response to treatment by checking for signs of organ rejection, side effects, and overall health status. Regular follow-up appointments are crucial for effective management.

How does Sirolimus work?

Sirolimus works by inhibiting the activation and proliferation of T-lymphocytes, which are essential for the immune response. It binds to a protein called FKBP-12, forming a complex that inhibits the mammalian target of rapamycin (mTOR), a key regulatory kinase. This action suppresses the immune system, preventing organ rejection.

Is Sirolimus effective?

Sirolimus is proven effective in preventing organ rejection in kidney transplant patients. Clinical trials have shown that it significantly reduces the incidence of acute rejection episodes when used in combination with other immunosuppressants like cyclosporine and corticosteroids. It is also effective in treating lymphangioleiomyomatosis (LAM), a rare lung disease.

What is Sirolimus?

Sirolimus is an immunosuppressant used to prevent organ rejection in kidney transplant patients and to treat lymphangioleiomyomatosis (LAM). It works by suppressing the immune system, preventing it from attacking the transplanted organ. Sirolimus inhibits T-cell activation and proliferation, which are crucial for immune response.

What is Sirolimus used for?

Sirolimus is indicated for preventing organ rejection in kidney transplant patients and treating lymphangioleiomyomatosis (LAM), a rare lung disease. It is used in combination with other immunosuppressants to enhance its effectiveness in preventing the immune system from attacking the transplanted organ.

Directions for Use

For how long do I take Sirolimus?

Sirolimus is typically used long-term to prevent organ rejection in kidney transplant patients. The duration of use depends on the individual's medical condition and response to treatment. Always follow your doctor's guidance regarding the length of treatment.

How do I take Sirolimus?

Sirolimus should be taken once daily, consistently with or without food, to maintain stable blood levels. Avoid grapefruit juice, as it can interfere with the medication's effectiveness. Follow your doctor's instructions on dosing and any additional dietary restrictions.

How long does it take for Sirolimus to start working?

Sirolimus begins to work within a few days, but it may take several weeks to achieve its full effect in preventing organ rejection. Regular monitoring of blood levels helps ensure the medication is working effectively. Always follow your doctor's guidance on treatment duration and monitoring.

How should I store Sirolimus?

Store Sirolimus tablets at room temperature, between 20°C to 25°C (68°F to 77°F), away from light, excess heat, and moisture. Keep the liquid form in the refrigerator and dispose of any unused medication one month after opening. Do not freeze. Keep all forms of Sirolimus out of reach of children.

What is the usual dose of Sirolimus?

For adults, the usual starting dose of Sirolimus is a 6 mg loading dose followed by 2 mg once daily. For children aged 13 years and older, the dosing is similar to adults. The dose may be adjusted based on blood levels and individual response. Always follow your doctor's instructions.

Warnings and Precautions

Can I take Sirolimus with other prescription drugs?

Sirolimus interacts with drugs that affect CYP3A4 and P-glycoprotein, such as ketoconazole, rifampin, and cyclosporine. These interactions can alter Sirolimus levels in the blood, affecting its effectiveness and safety. Patients should inform their doctor of all medications they are taking to avoid potential interactions.

Can Sirolimus be taken safely while breastfeeding?

It is not known whether Sirolimus passes into breast milk, but due to the potential for serious adverse effects in breastfed infants, breastfeeding is not recommended during treatment with Sirolimus. Mothers should discuss feeding options with their doctor to ensure the safety of their child.

Can Sirolimus be taken safely while pregnant?

Sirolimus can harm an unborn baby and should not be used during pregnancy unless absolutely necessary. Women of childbearing potential should use effective contraception during treatment and for 12 weeks after stopping Sirolimus. There is limited data on its use in pregnant women, so consult your doctor for personalized advice.

Is Sirolimus safe for the elderly?

Clinical studies did not include enough elderly patients to determine if they respond differently from younger patients. However, dose selection for elderly patients should be cautious, usually starting at the low end of the dosing range, due to the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy.

Who should avoid taking Sirolimus?

Sirolimus increases the risk of infections and certain cancers, such as lymphoma and skin cancer. It should not be used in liver or lung transplant patients due to serious complications. Patients should avoid grapefruit juice and certain medications that interact with Sirolimus. Regular monitoring of blood levels and kidney function is essential.