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Overview: Sirolimus is used to prevent kidney transplant rejection and to treat lymphangioleiomyomatosis (LAM), a rare lung disease. It prevents organ rejection by suppressing the immune system and helps manage LAM by slowing overactive cell growth. Examples of common side effects include fluid retention, high cholesterol, nausea, diarrhea, and mouth sores. Serious side effects may include severe allergic reactions, lung inflammation, and an increased risk of infections or certain cancers. Sirolimus is available as a tablet or liquid that you take by mouth.

Uses

What is sirolimus used for?

Sirolimus is commonly used to prevent organ rejection after a kidney transplant. Organ rejection can happen if your immune system sees the new organ as something that does not belong in your body and attacks it.

Sirolimus is also commonly used to treat LAM lung disease, a rare condition where you have trouble breathing due to cysts in your lungs.

Sirolimus may also be used for other conditions as determined by your health care provider.

How does sirolimus work (mechanism of action)?

After a kidney transplant, sirolimus prevents organ rejection by suppressing the immune system. Sirolimus is an mTOR inhibitor. mTOR is a protein that controls the growth and activity of certain cells in the immune system. Sirolimus blocks mTOR, which prevents these cells from attacking the transplanted kidney. 

In LAM lung disease, mTOR is overly active, causing abnormal cell growth in the lungs. By blocking mTOR, sirolimus slows the growth of these cells. This can help reduce lung damage and improve breathing in people with LAM.

How is sirolimus supplied (dosage forms)?

Brands and other names

  • Rapamune

Dosage forms and strengths

  • 1 mg/mL oral solution
  • 0.5 mg, 1 mg, 2 mg oral tablets

Sirolimus is also available in a topical form that is applied to the skin. See Hyftor for more information.

How should I store sirolimus?

Oral Liquid. Sirolimus oral liquid should be stored in the refrigerator, between 36 F and 46 F (2 C and 8 C). If needed, it can be kept at room temperature, between 68 F and 77 F (20 C and 25 C), for up to 15 days. Protect from light. Once opened, the bottle should be used within one month. If the liquid looks cloudy after being refrigerated, let the bottle sit at room temperature and gently shake it until it clears. Use a new oral syringe for each dose. Sirolimus oral liquid may be kept in an oral syringe for up to 24 hours at room temperature or refrigerated.

Oral Tablet. Sirolimus oral tablets should be stored at room temperature, between 68 F and 77 F (20 C and 25 C). It can be exposed to temperatures between 59 F and 86 F (15 C and 30 C) for shorter periods of time, such as when transporting it. Store in a cool, dry place that is protected from light.

Side Effects

What are the most common side effects of sirolimus?

The most common side effects of sirolimus are listed below. These side effects may vary depending on the condition that is being treated. Tell your health care provider if you have any of these side effects that bother you.

There may be other side effects of sirolimus that are not listed here. Contact your health care provider if you think you are having a side effect of a medicine. In the U.S., you can report side effects to the FDA at www.fda.gov/medwatch or by calling 800-FDA-1088 (800-332-1088). In Canada, you can report side effects to Health Canada at www.health.gc.ca/medeffect or by calling 866-234-2345.

What are the serious side effects of sirolimus?

While less common, the most serious side effects of sirolimus are described below, along with what to do if they happen.

Severe Allergic Reactions. Sirolimus may cause allergic reactions, which can be serious. Stop taking sirolimus and get help right away if you have any of the following symptoms of a serious allergic reaction.

  • Breathing problems or wheezing
  • Racing heart
  • Fever or general ill feeling
  • Swollen lymph nodes
  • Swelling of the face, lips, mouth, tongue, or throat
  • Trouble swallowing or throat tightness
  • Itching, skin rash, or pale red bumps on the skin called hives
  • Skin peeling or flaking
  • Nausea or vomiting
  • Dizziness, feeling lightheaded, or fainting
  • Stomach cramps
  • Joint pain

Angioedema. Sirolimus may cause a rare reaction called angioedema. The usual symptoms of this reaction include swelling of the lips, face, tongue, or throat. The risk of angioedema may be higher if you are taking certain other medicines. Stop taking this medicine and contact your health care provider if you have this type of swelling. If you are having trouble breathing, get medical attention right away.

Infections. Sirolimus can weaken your immune system and increase your risk of infections, including serious infections that can lead to death. It may also increase the risk of a rare but serious brain infection called progressive multifocal leukoencephalopathy (PML) or an infection called BK viral nephritis. Call your health care provider right away if you have an infection or any of the following symptoms.

  • Fever, sweats, chills, or muscle aches
  • Sore throat or feeling more tired than usual
  • Cough or coughing up blood
  • Burning or stinging when you pee or blood in your pee
  • Shortness of breath
  • Diarrhea or stomach pain
  • Weight loss
  • Clumsiness or loss of coordination
  • Trouble walking, speaking, or thinking clearly
  • Facial drooping or vision problems
  • Weakness on one side of your body that gets worse
  • Seizures

Cancer. Sirolimus can cause a new cancer to develop, including blood or skin cancer, or cause a previously treated cancer to come back. If you need to be in sunlight, wear sunscreen, a hat, and clothing that covers your skin. Tell your health care provider about any new symptoms or skin changes.

Fluid Retention (Edema). Sirolimus can cause fluid retention, also called edema. Fluid may build up around your heart or lungs, or cause swelling in areas you can see, such as your feet. Call your health care provider right away if you have any of the following symptoms of fluid retention.

  • Chest pain
  • Irregular heartbeat
  • Shortness of breath or trouble breathing
  • Stretched or shiny skin
  • Swelling in your legs, ankles, feet, belly, or other body parts

High Cholesterol Levels (Hyperlipidemia). Sirolimus can increase the levels of fats in your blood, which may cause high cholesterol and triglycerides. This does not usually cause symptoms, but it can lead to serious health problems if left untreated. Keep all appointments to have your blood checked while taking sirolimus. Follow any advice given by your health care provider about exercise, dietary changes, or medicine that may be needed to lower the levels of fats in your blood. 

Kidney Damage. Kidney damage can happen when taking sirolimus. Your risk may be higher if you take sirolimus for a long time with certain medicines. Sirolimus may also increase the risk of protein in the urine (pee), also known as proteinuria. Keep all appointments to have your kidneys checked, which may include blood and urine tests. Call your health care provider right away if you have any of the following symptoms.

  • Peeing less or more than usual
  • Foamy or bubbly pee
  • Swelling in your feet, ankles, or legs
  • Weakness or unusual tiredness
  • Trouble catching your breath or chest pain/pressure
  • Confusion
  • Nausea or loss of appetite

Lung Inflammation. Sirolimus can cause inflammation in your lungs, also called interstitial lung disease or pneumonitis. This can be serious or even life-threatening. Get emergency help if you have trouble breathing. You may also have a cough, fever, or chest pain. 

Warnings & Precautions

Who should not take sirolimus?

Allergies to Ingredients. People who are allergic to any of the following should not take sirolimus.

  • Rapamune
  • Sirolimus
  • Any of the ingredients in the specific product dispensed

Your pharmacist can tell you all of the ingredients in the specific sirolimus products they stock.

What should I know about sirolimus before taking it?

Do not take sirolimus unless it has been prescribed to you by a health care provider. Take it as prescribed. 

Do not share sirolimus with other people, even if they have the same condition as you. It may harm them.

Keep sirolimus out of the reach of children. Since sirolimus liquid may be kept in a refrigerator, take special precautions to keep it away from children who also use the refrigerator. 

Do not chew, cut, or crush sirolimus tablets. They should be swallowed whole.

If you are taking sirolimus liquid, read and follow the instructions that come with the medicine. It explains the steps for how to properly measure, mix, and take the liquid by mouth. Use the oral syringe that comes with your product to measure your dose. A household spoon is not an accurate measuring device and may cause you to take the wrong dose. Ask your pharmacist what measuring device to use if you are not sure.

Sirolimus may cause fertility problems. Tell your health care provider if you have questions or concerns about this.

It is important to keep all appointments with your health care provider, including for blood work, before starting and while taking sirolimus.

Taking sirolimus with certain other medicines to prevent organ rejection may increase your risk of a blood clotting problem. Tell your health care provider if you have any unusual bleeding or bruising.

What should I tell my health care provider before taking sirolimus?

Tell your health care provider about all of your health conditions and any prescription or over-the-counter (OTC) medicines, vitamins/minerals, herbal products, and other supplements you are using. This will help them determine if sirolimus is right for you.

In particular, make sure that you discuss any of the following.

Wound Healing Issues. Sirolimus can make it hard for your body to heal from wounds. Tell your health care provider if your surgical wound is painful, swollen, bleeding, or leaking fluid. Let your health care provider know if you have any planned surgeries or if you have any injuries that occur while taking sirolimus.

Vaccines. Talk with your health care provider about any vaccines that you may need. You should not receive certain vaccines right before or while taking sirolimus. Tell your health care provider about any vaccines you have recently received or have scheduled.

Other Medicines and Supplements. Sirolimus may interact with other medicines and supplements. Before taking sirolimus, tell your health care provider about any prescription or over-the-counter (OTC) medicines, vitamins/minerals, herbal products, and other supplements you are using. See the Interactions section for more details.

Current and Past Health Conditions. Tell your health care provider if you have or have had any of the following.

  • Liver problems
  • High levels of fats in your blood (high cholesterol or triglycerides)
  • Infections
  • Cancer, including skin cancer or if someone in your family has had skin cancer

Lung or Liver Transplant. Sirolimus is commonly used after a kidney transplant. It may raise the risk of serious problems in some people taking it to prevent organ rejection after a lung or liver transplant. Tell your health care provider about any other organ transplants you have had or plan to have.

Pregnancy. Sirolimus may cause harm to an unborn baby. If you are able to get pregnant, you should use effective birth control while taking sirolimus and for 12 weeks after your last dose. Talk with your health care provider about birth control options. Tell your health care provider if you are pregnant or plan to become pregnant. If you become pregnant or think you might be pregnant, contact your health care provider right away.

Breastfeeding. It is not known if sirolimus passes into breast milk. Tell your health care provider if you are breastfeeding or plan to breastfeed. Your health care provider will let you know if you should take sirolimus while breastfeeding.

Interactions

Does sirolimus interact with foods or drinks?

Food may affect how well your body absorbs sirolimus. Take sirolimus the same way each time, either with food or without food. This helps keep a steady level of the medicine in your blood, which helps sirolimus work the way it should.

Grapefruit interacts with sirolimus. Do not take sirolimus with grapefruit or grapefruit juice. Grapefruit may raise the blood levels of sirolimus, which can increase your risk of side effects.

It is unknown if drinking alcohol will affect sirolimus. 

Does sirolimus interact with other medicines (drug interactions)?

Always tell your health care provider about any prescription or over-the-counter (OTC) medicines, vitamins/minerals, herbal products, and other supplements you are using. 

In particular, make sure to discuss if you are using any of the following before taking sirolimus.

  • Cannabidiol (Epidiolex), which is a medicine used for seizures, or a supplement that contains cannabidiol (CBD)
  • Cimetidine (Tagamet HB), which is a medicine used for heartburn
  • Cyclosporine (Gengraf, Neoral, Sandimmune, and others), which is a medicine that suppresses your immune system
  • Metoclopramide (Reglan and others), which is a medicine for certain stomach problems
  • Rifampin (Rifadin) or rifapentine (Priftin), which is a medicine commonly used to treat an infection called tuberculosis
  • Any other medicine that suppresses your immune system, such as tacrolimus (Prograf, Envarsus XR, and others) or a corticosteroid
  • An antibiotic, such as clarithromycin or erythromycin (Ery-Tab and others), which is a medicine used for bacterial infections
  • An antifungal medicine, such as clotrimazole, fluconazole (Diflucan), itraconazole (Sporanox, Tolsura), ketoconazole, posaconazole (Noxafil), or voriconazole (Vfend), which is a medicine used for fungal infections
  • An angiotensin-converting enzyme (ACE) inhibitor, such as enalapril or lisinopril, which is a medicine for high blood pressure, heart failure, and certain kidney problems
  • A medicine for high blood pressure or heart problems, including diltiazem or verapamil
  • A medicine for HIV, AIDS, or hepatitis C
  • A medicine for seizures, such as carbamazepine, phenytoin, or phenobarbital
  • A medicine for lowering the levels of fats in your blood (cholesterol or triglycerides)
  • St. John’s wort, which is a supplement that may be used for depression

Many other medicines may alter the blood levels of sirolimus. Tell your health care provider about all medicines that you take or have recently taken.

This is not a complete list of medicines that can interact with sirolimus. Always check with your health care provider.

Does interact with other drugs you are taking?

Enter your medication into the WebMD interaction checker

Overdose/Missed Dose

What should I do if I accidentally use too much sirolimus?

If you or someone else has taken too much sirolimus, get medical help right away, call 911, or contact a Poison Control center at 800-222-1222.

What should I do if I miss a dose of sirolimus?

Missing doses of sirolimus can cause it to not work as well. So it is important not to miss or skip doses. If you miss a dose, take it as soon as you remember. If it is almost time for your next dose, skip the missed dose and only take the next dose. Do not take double or extra doses.