Generic Name: sirolimus (sih RO lim us)Brand Names: Rapamune
Sirolimus lowers your body's immune system. The immune system helps your body fight infections. The immune system can also fight or "reject" a transplanted organ such as a liver or kidney. This is because the immune system treats the new organ as an invader.
Sirolimus is used to prevent your body from rejecting a transplanted kidney. Sirolimus is sometimes used in a combination treatment with cyclosporine (Neoral, Sandimmune) and a steroid medicine such as prednisone.
Sirolimus may also be used for other purposes not listed in this medication guide.
The oral liquid form of sirolimus must be mixed with water or orange juice only. Do not use any other liquids to mix this medicine.
Do not mix this medicine with grapefruit juice or potentially dangerous effects may result. Avoid eating grapefruit or drinking grapefruit juice while you are taking sirolimus.
If you also take cyclosporine, take the sirolimus at least 4 hours after taking cyclosporine.
You may take sirolimus with or without food, but take it the same way every time.
Sirolimus can lower the blood cells that help your body fight infections. Avoid contact with people who have colds, the flu, or other contagious illnesses. Do not receive any vaccines without your doctor's advice. Contact your doctor immediately if you develop signs of infection.Avoid getting this medication on your skin, or around your nose and mouth. If it does get onto any of these areas, wash with soap and water. If this medicine gets into your eyes, rinse them with plain water.
Sirolimus may increase your risk of developing lymphoma or other forms of cancer. Talk with your doctor about your specific cancer risk.Avoid exposure to sunlight or artificial UV rays (sunlamps or tanning beds). Sirolimus may increase your risk of skin cancer. Use a sunscreen (minimum SPF 15) and wear protective clothing if you must be out in the sun.
Sirolimus may increase your risk of developing lymphoma or other forms of cancer. Talk with your doctor about your specific cancer risk.You should not use this medication if you are allergic to sirolimus.
If you have certain conditions, you may need a dose adjustment or special tests to safely use this medication. Before you take sirolimus, tell your doctor if you are allergic to any drugs, or if you have:
high cholesterol or triglycerides;
liver disease; or
Take this medication exactly as it was prescribed for you. Do not take the medication in larger amounts, or take it for longer than recommended by your doctor. Your doctor may occasionally change your dose to make sure you get the best results from this medication. Follow your doctor's dosing instructions carefully.Take the sirolimus tablet with a full glass of water. Do not crush, chew, or break a sirolimus tablet. Tell your doctor if you have trouble swallowing the tablet whole.
You may take sirolimus with or without food, but take it the same way every time.
The oral liquid (solution) comes with patient instructions for safe and effective use. Follow these directions carefully. Ask your doctor or pharmacist if you have any questions.
The oral liquid must be mixed with at least 2 ounces (1/4 cup) of water or orange juice. Do not use any other liquids to mix this medicine.
Stir the mixture and drink all of it right away. Then add at least 4 ounces (1/2 cup) more water or orange juice to the same glass, stir again and drink right away.
Sirolimus is usually taken once a day. If you also take cyclosporine, wait at least 4 hours after your cyclosporine dose before you take sirolimus.
Sirolimus can lower the blood cells that help your body fight infections. This can make it easier for you to bleed from an injury or get sick from being around others who are ill. To be sure your blood cells do not get too low, your blood will need to be tested on a regular basis. Your kidney function may also need to be tested. Do not miss any scheduled visits to your doctor.Avoid getting sirolimus liquid on your skin or around your nose. If it does get onto any of these areas, wash with soap and water. If this medicine gets into your eyes, rinse them with plain water. Store sirolimus tablets at room temperature, away from heat, moisture, and light. Store sirolimus oral liquid in the refrigerator. Do not freeze. You may notice a slight haze to the liquid after it has been refrigerated. This haze will not affect the medication, and should disappear when the medicine reaches room temperature.
If you are taking Rapamune oral liquid with a disposable syringe, you may store a loaded syringe in the carrying case provided. Keep the case at room temperature and use the medicine within 24 hours. Use a disposable syringe only once and then throw it away.
See also: Sirolimus dosage in more detail
Take the missed dose as soon as you remember. If it is almost time for your next dose, skip the missed dose and take the medicine at the next regularly scheduled time. Do not take extra medicine to make up the missed dose.
Grapefruit and grapefruit juice may interact with sirolimus and could lead to potentially dangerous effects. Do not mix this medicine with grapefruit juice. Avoid eating grapefruit or drinking grapefruit juice while you are taking sirolimus.
Avoid contact with people who have colds, the flu, or other contagious illnesses. Contact your doctor immediately if you develop signs of infection.Do not receive a vaccine while you are being treated with sirolimus. The vaccine may not work as well during this time, and may not fully protect you from disease. Avoid exposure to sunlight or artificial UV rays (sunlamps or tanning beds). Sirolimus may increase your risk of skin cancer. Use a sunscreen (minimum SPF 15) and wear protective clothing if you must be out in the sun.
fast heart rate;
pain when you breathe, feeling short of breath;
chest pain, feeling weak or tired;
coughing up blood or mucus;
feeling like you might pass out;
pale skin, easy bruising or bleeding, weakness;
fever, chills, body aches, flu symptoms;
night sweats, weight loss;
swelling in your face, stomach, hands or feet;
rapid weight gain;
pain or burning when you urinate; or
slow healing of a wound.
Less serious side effects may include:
nausea, vomiting, diarrhea, constipation, stomach pain;
acne or skin rash.
This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.
Usual Adult Dose for Organ Transplant -- Rejection Prophylaxis:
For the prophylaxis of organ rejection in patients receiving renal transplants:For patients at low to moderate immunologic risk:Dosing by body weight:Less than 40 kg:Loading dose: 3 mg/m2 on day 1Maintenance: 1 mg/m2 once dailyGreater than or equal to 40 kg:Loading dose: 6 mg orally on day 1Maintenance: 2 mg orally once daily It is recommended that sirolimus be used in a regimen with cyclosporine and corticosteroids.In patients at high immunologic risk (defined as Black transplant recipients and/or repeat renal transplant recipients who lost a previous allograft for immunologic reason and/or patients with high-panel reactive antibodies [PRA; peak PRA level greater than 80%]):For patients receiving sirolimus with cyclosporine:Loading Dose: up to 15 mg on day one post-transplantation.Maintenance Dose: Beginning on day 2, an initial maintenance dose of 5 mg/day should be given. A trough level should be obtained between days 5 and 7, and the daily dose of sirolimus should be adjusted thereafter.Antibody induction therapy may be used.Intestinal transplant:Initial loading dose: 2 to 3 orally mg/m2Maintenance dose: 1 mg/m2 orally once daily to achieve blood levels of 8 to 10 ng/mLMaintenance therapy after withdrawal of cyclosporine:Cyclosporine withdrawal is not recommended in high-immunological risk patients. Following two to four months of combined therapy, withdrawal of cyclosporine may be considered in low-to-moderate risk patients. Cyclosporine should be discontinued over four to eight weeks, and a necessary increase in the dosage of sirolimus (up to fourfold) should be anticipated due to removal of metabolic inhibition by cyclosporine and to maintain adequate immunosuppressive effects. Dose-adjusted trough target concentrations are typically 16 to 24 ng/mL for the first year post-transplant and 12 to 20 ng/mL thereafter (measured by chromatographic methodology).
Usual Pediatric Dose for Organ Transplant -- Rejection Prophylaxis:
Greater than or equal to 13 years who weigh less than 40 kg:Loading dose: 3 mg/m2Initial maintenance dose: 1 mg/m2/day divided every 12 hours or once daily; adjust dose to achieve target sirolimus trough blood concentration
Tell your doctor if you are using any of the following drugs:
amphotericin B (Fungizone, AmBisome, Amphotec, Abelcet);
metoclopramide (Reglan );
rifampin (Rifater, Rifadin, Rimactane), rifabutin (Mycobutin), rifapentine (Priftin);
St. John's wort;
an ACE inhibitor such as benazepril (Lotensin), captopril (Capoten), fosinopril (Monopril), enalapril (Vasotec), lisinopril (Prinivil, Zestril), moexipril (Univasc), perindopril (Aceon), quinapril (Accupril), ramipril (Altace), or trandolapril (Mavik);
an antibiotic such clarithromycin (Biaxin), erythromycin (E-Mycin, Ery-Tab, Erythrocin, E.E.S), telithromycin (Ketek), capreomycin (Capastat), or troleandomycin (Tao);
an antifungal medication such as clotrimazole (Mycelex Troche), fluconazole (Diflucan), itraconazole (Sporanox), ketoconazole (Nizoral), or voriconazole (Vfend);
a calcium channel blocker such as diltiazem (Tiazac, Cardizem), nicardipine (Cardene), or verapamil (Calan, Covera, Verelan);
HIV medicines such as indinavir (Crixivan) or ritonavir (Norvir); or
seizure medicine such as carbamazepine (Tegretol), phenytoin (Dilantin), phenobarbital (Luminal).
This list is not complete and there may be other drugs that can interact with sirolimus. Tell your doctor about all the prescription and over-the-counter medications you use. This includes vitamins, minerals, herbal products, and drugs prescribed by other doctors. Do not start using a new medication without telling your doctor.