Rapamune

DRUG DESCRIPTION

Rapamune (sirolimus) is an immunosuppressive agent. Sirolimus is a macrocyclic lactone produced by Streptomyces hygroscopicus. The chemical name of sirolimus (also known as rapamycin) is (3S,6R,7E,9R,10R,12R,14S,15E,17E,19E,21S,23S,26R,27R,34aS)9,10,12,13,14,21,22,23,24,25,26,27,32,33,34, 34a-hexadecahydro-9,27-dihydroxy-3-[(1R)-2[(1S,3R,4R)-4-hydroxy-3-methoxycyclohexyl]-1-methylethyl]-10,21-dimethoxy6,8,12,14,20,26-hexamethyl-23,27-epoxy-3H-pyrido[2,1-c][1,4] oxaazacyclohentriacontine1,5,11,28,29 (4H,6H,31H)-pentone. Its molecular formula is C51H79NO13 and its molecular weight is 914.2. The structural formula of sirolimus is illustrated as follows.

RAPAMUNE (sirolimus) Structural Formula Illustration

Sirolimus is a white to off-white powder and is insoluble in water, but freely soluble in benzyl alcohol, chloroform, acetone, and acetonitrile.

Rapamune (sirolimus) is available for administration as an oral solution containing 1 mg/mL sirolimus. Rapamune (sirolimus) is also available as a tan, triangular-shaped tablet containing 0.5 mg sirolimus, as a white, triangular-shaped tablet containing 1 mg sirolimus, and as a yellow-to-beige triangular-shaped tablet containing 2 mg sirolimus.

The inactive ingredients in Rapamune (sirolimus) Oral Solution are Phosal 50 PG® (phosphatidylcholine, propylene glycol, mono- and di-glycerides, ethanol, soy fatty acids, and ascorbyl palmitate) and polysorbate 80. Rapamune (sirolimus) Oral Solution contains 1.5% - 2.5% ethanol.

The inactive ingredients in Rapamune (sirolimus) Tablets include sucrose, lactose, polyethylene glycol 8000, calcium sulfate, microcrystalline cellulose, pharmaceutical glaze, talc, titanium dioxide, magnesium stearate, povidone, poloxamer 188, polyethylene glycol 20,000, glyceryl monooleate, carnauba wax, dl-alpha tocopherol, and other ingredients. The 0.5 mg and 2 mg dosage strengths also contain yellow iron (ferric) oxide and brown iron (ferric) oxide.

What are the possible side effects of sirolimus (Rapamune)?

Get emergency medical help if you have any of these signs of an allergic reaction: hives; difficulty breathing; swelling of your face, lips, tongue, or throat.

Call your doctor at once if you have any of these serious side effects:

  • 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...

Read All Potential Side Effects and See Pictures of Rapamune »

What are the precautions when taking sirolimus (Rapamune)?

Before taking sirolimus, tell your doctor or pharmacist if you are allergic to it; or to other macrolide medications (e.g., tacrolimus, erythromycin); or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.

Before using this medication, tell your doctor or pharmacist your medical history, especially of: liver disease, kidney disease, high cholesterol/triglyceride levels, any recent/current infections, cancer.

This medication may increase your risk of developing skin cancer. Avoid prolonged sun exposure, tanning booths, and sunlamps. Use a sunscreen with a high protection factor and wear protective clothing when outdoors.

Do not have...

Read All Potential Precautions of Rapamune »


Rapamune Consumer (continued)

SIDE EFFECTS: See also Warning section.

Diarrhea, joint pain, shaking, acne, or trouble sleeping may occur. If any of these effects persist or worsen, notify your doctor promptly.

Remember that your doctor has prescribed this medication because he or she has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.

Tell your doctor immediately if any of these unlikely but serious side effects occur: muscle pain/cramps, bone pain, increased thirst/hunger, frequent urination, vision changes, hearing problems (e.g., hearing loss, ringing in the ears), unusual tiredness/weakness, fast/slow/irregular heartbeat, easy bruising/bleeding, mental/mood changes, swelling ankles/feet, severe headache, dizziness, stomach/abdominal pain.

This drug increases the risk of a possibly fatal brain infection (PML - progressive multifocal leukoencephalopathy). Tell your doctor right away if you have any of these symptoms: clumsiness, sudden change in your thinking (such as confusion, difficulty concentrating), difficulty moving muscles, seizure, difficulty speaking.

Tell your doctor immediately if any of these rare but very serious side effects occur: change in the amount of urine, frothy urine, chest pain, shortness of breath, pain/redness/swelling of arms or legs, swelling abdomen, dark urine, yellowing eyes/skin, persistent nausea/vomiting.

Sirolimus may slow wound healing after surgery. Tell your doctor immediately if you have signs that your surgery wound is not healing well (e.g., redness, swelling, pain). The risk of poor wound healing is higher if you are obese.

Sirolimus may cause your cholesterol/triglycerides to increase. You may be required to have your cholesterol/triglycerides checked periodically and/or take another medication to control your cholesterol/triglycerides.

A very serious allergic reaction to this drug is rare. However, seek immediate medical attention if you notice any of the following symptoms of a serious allergic reaction: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.

Sirolimus can commonly cause a mild rash that is usually not serious. However, you may not be able to tell it apart from a rare rash that could be a sign of a severe allergic reaction. Therefore, seek immediate medical attention if you develop any rash.

This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.

In the US -

Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.

PRECAUTIONS: Before taking sirolimus, tell your doctor or pharmacist if you are allergic to it; or to other macrolide medications (e.g., tacrolimus, erythromycin); or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.

Before using this medication, tell your doctor or pharmacist your medical history, especially of: liver disease, kidney disease, high cholesterol/triglyceride levels, any recent/current infections, cancer.

This medication may increase your risk of developing skin cancer. Avoid prolonged sun exposure, tanning booths, and sunlamps. Use a sunscreen with a high protection factor and wear protective clothing when outdoors.

Do not have immunizations/vaccinations without the consent of your doctor, and avoid contact with people who have recently received oral polio vaccine or flu vaccine inhaled through the nose.

Since this medication can increase your risk of developing serious infections, wash your hands well to prevent the spread of infections. Avoid contact with people who have illnesses that may spread to others (e.g., flu, chickenpox).

This medication is not recommended for use during pregnancy. Consult your doctor for more details and to discuss reliable forms of birth control. It is recommended that men and women using this medication use two effective forms of birth control (e.g., condoms and birth control pills) before starting this medication, while taking this medication, and for 12 weeks after stopping this medication. Consult your doctor.

This drug may pass into breast milk and could have undesirable effects on a nursing infant. Therefore, breast-feeding is not recommended while using this drug. Consult your doctor before breast-feeding.


Rapamune Patient Information Including Side Effects

Brand Names: Rapamune

Generic Name: sirolimus (Pronunciation: sih RO lim us)

  • What is sirolimus (Rapamune)?
  • What are the possible side effects of sirolimus (Rapamune)?
  • What is the most important information I should know about sirolimus (Rapamune)?
  • What should I discuss with my doctor before taking sirolimus (Rapamune)?
  • How should I take sirolimus (Rapamune)?
  • What happens if I miss a dose (Rapamune)?
  • What happens if I overdose (Rapamune)?
  • What should I avoid while taking sirolimus (Rapamune)?
  • What other drugs will affect sirolimus (Rapamune)?
  • Where can I get more information?

What is sirolimus (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.

What are the possible side effects of sirolimus (Rapamune)?

Get emergency medical help if you have any of these signs of an allergic reaction: hives; difficulty breathing; swelling of your face, lips, tongue, or throat.

Call your doctor at once if you have any of these serious side effects:

  • 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:

  • joint pain;
  • nausea, vomiting, diarrhea, constipation, stomach pain;
  • headache; or
  • 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.

What is the most important information I should know about sirolimus (Rapamune)?

This medication may be harmful to an unborn baby. Tell your doctor if you are pregnant or plan to become pregnant. Use an effective form of birth control while you are using this medication and for at least 12 weeks after your treatment ends.

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.

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