Rapamune (Sirolimus) is an immunosuppressant agent. It is normally used along with corticosteroid medications and Cyclosporine to prevent the rejection of kidney organ transplants. Together, these medications suppress (decrease) the body's natural defense, the immune system.

Rapamune (Sirolimus) works by preventing the formation of cells (white blood cells) that would normally attack the transplanted organ.

Your doctor may have suggested Rapamune (Sirolimus) for conditions other than those listed in these drug information articles. If you have not discussed this with your doctor or are not sure why you are taking Rapamune (Sirolimus), speak to your doctor. Do not stop taking Rapamune (Sirolimus) without consulting your doctor.

Do not give Rapamune (Sirolimus) to anyone else, even if they have the same symptoms as you do. It can be harmful for people to take Rapamune (Sirolimus) if their doctor has not prescribed it.

Rapamune (Sirolimus) is normally started as soon as possible after transplant. The dose prescribed will depend on your situation. The recommended first dose of Rapamune (Sirolimus) for new transplant recipients is 6 mg followed by a regular dose of 2 mg daily. For people who have previously had a transplant rejection or are at high risk of rejecting the transplant, the first dose is often 15 mg with a regular dose of 5 mg per day.

Many things can affect the dose of medication that a person needs, such as body weight, other medical conditions, and other medications. If your doctor has recommended a dose different from the ones listed here, do not change the way that you are using the medication without consulting your doctor.

Do not stop taking Rapamune (Sirolimus) without talking with your doctor.

Rapamune (Sirolimus) is normally given along with cyclosporine and corticosteroids. Rapamune (Sirolimus) should be taken approximately 4 hours after the cyclosporine.

Rapamune (Sirolimus) should be taken at the same time each day, and taken the same way, either with or without food. It should not be taken with grapefruit juice.

Rapamune (Sirolimus) is available as an oral (by mouth) solution and in tablet form. If you are taking the tablets, do not crush, chew, or split them.

The oral solution bottles have oral dose syringes which should be used to withdraw the prescribed amount of Rapamune (Sirolimus) from the bottle. Empty the correct amount of Rapamune (Sirolimus) from the syringes into a glass or plastic container holding at least 2 ounces (60 mL) of water or orange juice. No other liquids should be used for dilution. Stir vigorously and drink at once. Rinse the container with an additional volume (minimum of 4 ounces or 120 mL) of water or orange juice, stir vigorously, and drink at once. This ensures that all the medication is rinsed from the container and that the entire dose is taken.

The preparation should be used immediately after dilution and the syringe discarded after one use.

Rapamune (Sirolimus) solutions provided in bottles may develop a slight haze when refrigerated. If this occurs, allow the bottle to stand at room temperature and shake gently until the haze disappears. The presence of this haze does not affect the quality of the product.

Do not allow water or juice to contaminate the medication in the bottle. If the mouth of the bottle needs to be cleaned, wipe the bottle with a dry cloth.

The tablets should only be taken with water or orange juice.

It is extremely important to take Rapamune (Sirolimus) exactly as prescribed, since missing even a few doses of Rapamune (Sirolimus) may cause your body to reject the organ. Check with your doctor or pharmacist for the proper way to take Rapamune (Sirolimus).

If you miss a dose, take the missed dose as soon as you remember, but not within 4 hours of your cyclosporine dose. If it is less than four hours until your next scheduled dose of Rapamune (Sirolimus), skip the missed dose and continue with your regular dosing schedule. Do not take a double dose to make up for a missed one. If you are not sure what to do after missing a dose, contact your doctor or pharmacist for advice.

Store Rapamune (Sirolimus) solution in the refrigerator, protect it from light, and keep it out of the reach of children. Once the bottle is opened, it should be kept in a refrigerator and the contents used within one month. If left at room temperature, the opened bottle must be used within 5 days. If the amber syringe is pre-filled, it may be kept at room temperature or in the refrigerator for a maximum of 24 hours.

Store Rapamune (Sirolimus) tablets at room temperature (15°C to 30°C), protect them from light and moisture, and keep out of the reach of children.

Do not dispose of medications in wastewater (e.g. down the sink or in the toilet) or in household garbage. Ask your pharmacist how to dispose of medications that are no longer needed or have expired.

Many medications can cause side effects. A side effect is an unwanted response to a medication when it is taken in normal doses. Side effects can be mild or severe, temporary or permanent.

The side effects listed below are not experienced by everyone who takes Rapamune (Sirolimus). If you are concerned about side effects, discuss the risks and benefits of Rapamune (Sirolimus) with your doctor.

The following side effects have been reported by at least 1% of people taking Rapamune (Sirolimus). Many of these side effects can be managed, and some may go away on their own over time.

Contact your doctor if you experience these side effects and they are severe or bothersome. Your pharmacist may be able to advise you on managing side effects.

• Acne
• Constipation
• Diarrhea
• headache
• heartburn
• increased growth of body hair
• mouth ulcers or Cold Sores
• nausea
• sleeping problems (Insomnia)
• trembling
• weakness
• weight gain

Although most of the side effects listed below don't happen very often, they could lead to serious problems if you do not seek medical attention.

Check with your doctor as soon as possible if any of the following side effects occur:

• anxiousness
• bone pain
• change in menstrual periods
• dizziness
• high blood pressure
• increased occurrence of infections
• irregular or rapid heartbeat
• joint pain
• lower back or side pain
• muscle pain or cramps
• rash
• sexual problems
• slowed healing
• signs of Anemia (low red blood cells; e.g., pale skin, unusual tiredness, or weakness)
• signs of bleeding (e.g., bloody nose, blood in urine, coughing blood, bleeding gums, cuts that don't stop bleeding)
• signs of fluid build-up (e.g., breathing problems; swelling of hands, ankles, feet, or lower legs; swollen abdomen)
• signs of liver problems (e.g., nausea, vomiting, diarrhea, loss of appetite, weight loss, yellowing of the skin or whites of the eyes, dark urine, pale stools)
• signs of a urinary tract infection such as difficult or painful urination, blood in the urine or cloudy urine
• symptoms of high blood sugar (e.g., frequent urination, increased thirst, excessive eating, unexplained weight loss, poor wound healing, infections, fruity breath odour)
• swollen glands
• vision changes
• vomiting
• weakness or heaviness of legs

Stop taking the medication and seek immediate medical attention if any of the following occur:

• flu-like symptoms (sudden lack of energy, Fever, cough, sore throat)
• signs of a serious allergic reaction (e.g., abdominal cramps, difficulty breathing, nausea and vomiting, or swelling of the face and throat)
• signs of a severe skin reaction such as blistering, peeling, a rash covering a large area of the body, a rash that spreads quickly, or a rash combined with fever or discomfort
• signs of bleeding in the stomach (e.g., bloody, black, or tarry stools, spitting up of blood, vomiting blood or material that looks like coffee grounds)
• signs of heart problems (e.g., fast, irregular heartbeat or pulse, chest pain, difficulty breathing)
• signs of infection (symptoms may include fever or chills, severe diarrhea, shortness of breath, prolonged dizziness, headache, stiff neck, swollen glands, weight loss, or listlessness)
• signs of pancreatitis (e.g., abdominal pain on the upper left side, back pain, nausea, fever, chills, rapid heartbeat, swollen abdomen)

Some people may experience side effects other than those listed. Check with your doctor if you notice any symptom that worries you while you are taking Rapamune (Sirolimus).

Tablets

1 mg
Each white, triangular-shaped tablet, marked "RAPAMUNE 1 mg" on one side, contains 1 mg of Rapamune (Sirolimus). Nonmedicinal ingredients: calcium sulfate anhydrous NF, carnauba wax NF, glyceryl monooleate, ink, lactose monohydrate NF, magnesium stearate NF, microcrystalline cellulose NF, pharmaceutical glaze NF, polaxamer 188, polyethylene glycol 8000 powdered NF, polyethylene glycol type 20 000, povidone USP, sucrose NF, talc USP, titanium dioxide USP, and vitamin E (dl-alpha tocopherol).

2 mg
Each yellow-to-beige triangular-shaped tablet, marked "RAPAMUNE 2 mg" on one side, contains 2 mg of Rapamune (Sirolimus). Nonmedicinal ingredients: calcium sulfate anhydrous NF, carnauba wax NF, glyceryl monooleate, ink, lactose monohydrate NF, magnesium stearate NF, microcrystalline cellulose NF, pharmaceutical glaze NF, polaxamer 188, polyethylene glycol 8000 powdered NF, polyethylene glycol type 20 000, povidone USP, sucrose NF, talc USP, titanium dioxide USP, vitamin E (dl-alpha tocopherol), Brown #70 Iron Oxide NF and Yellow #10 Iron Oxide NF.

5 mg
Each tan, triangular-shaped tablet, marked "RAPAMUNE 5 mg" on one side, contains 5 mg of Rapamune (Sirolimus). Nonmedicinal ingredients: calcium sulfate anhydrous NF, carnauba wax NF, glyceryl monooleate, ink, lactose monohydrate NF, magnesium stearate NF, microcrystalline cellulose NF, pharmaceutical glaze NF, polaxamer 188, polyethylene glycol 8000 powdered NF, polyethylene glycol type 20 000, povidone USP, sucrose NF, talc USP, titanium dioxide USP, vitamin E (dl-alpha tocopherol), Brown #75 Iron Oxide NF and Yellow #10 Iron Oxide NF.

Oral solution

Each mL of oral solution contains 1 mg of Rapamune (Sirolimus). The solution is supplied in amber glass 60 mL bottles with oral syringes for measuring the dose. Nonmedicinal ingredients: Phosal 50 PG® (phosphatidylcholine, propylene glycol, sunflower mono- and diglycerides, ascorbyl palmitate, ethanol, and soybean oil fatty acids) and polysorbate 80.

Do not use Rapamune (Sirolimus) if you are allergic to Rapamune (Sirolimus) or any ingredients of the medication.

There may be an interaction between Rapamune (Sirolimus) and any of the following:

• acitretin
• Amiodarone
• angiotensin-converting enzyme inhibitors (ACEIs; e.g., Captopril, Enalapril, Ramipril)
• Aprepitant
• Atorvastatin
• "azole" antifungals (e.g., ketoconazole, posaconazole, Voriconazole)
• BCG
• Bicalutamide
• Bosentan
• calcium channel blockers (e.g., Amlodipine, Diltiazem, Nifedipine, Verapamil)
• Carbamazepine
• Carvedilol
• Clozapine
• Cobicistat
• conivaptan
• cyclosporine
• Dabrafenib
• Deferasirox
• Denosumab
• Dexamethasone
• diabetes medications (e.g., chlorpropamide, glipizide, Glyburide, insulin, Metformin,  Rosiglitazone)
• dipyrone
• Dronedarone
• echinacea
• Enzalutamide
• Fingolimod
• grapefruit juice
• Haloperidol
• Hepatitis C antivirals  (e.g., ombitasvir,  paritaprevir,  ritonavir, dasabuvir, simeprevir)
• HIV non-nucleoside reverse transcriptase inhibitors (NNRTIs; e.g., delavirdine, efavirenz, etravirine, nevirapine)
• HIV protease inhibitors (e.g., darunavir, indinavir, lopinavir, saquinavir, tipranavir)
• Ivacaftor
• Leflunomide
• Lomitapide
• macrolide antibiotics (e.g., clarithromycin, erythromycin, telithromycin)
• Mefloquine
• Metoclopramide
• mifepristone
• Mitotane
• Modafinil
• Natalizumab
• nefazodone
• Nivolumab
• Norfloxacin
• Phenobarbital
• Phenytoin
• Pimecrolimus
• Pimozide
• primidone
• rifabutin
• rifampin
• Roflumilast
• St. John's wort
• Stiripentol
• Tacrolimus
• Tocilizumab
• tyrosine kinase inhibitors (e.g., Crizotinib, Dasatinib, imatinib, Nilotinib)
• vaccines
• Venetoclax

If you are taking any of these medications, speak with your doctor or pharmacist. Depending on your specific circumstances, your doctor may want you to:

• stop taking one of the medications,
• change one of the medications to another,
• change how you are taking one or both of the medications, or
• leave everything as is.

An interaction between two medications does not always mean that you must stop taking one of them. Speak to your doctor about how any drug interactions are being managed or should be managed.

Medications other than those listed above may interact with Rapamune (Sirolimus). Tell your doctor or prescriber about all prescription, over-the-counter (non-prescription), and herbal medications that you are taking. Also tell them about any supplements you take. Since caffeine, alcohol, the Nicotine from cigarettes, or street drugs can affect the action of many medications, you should let your prescriber know if you use them.