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Rapamune

Generic name: sirolimus [sih-RO-lim-us]
Drug classes: MTOR inhibitors, selective immunosuppressants

What is Rapamune?

Rapamune helps to weaken your immune system so that it doesn't "reject" a transplanted kidney. When the immune system attacks the new organ, it is called "organ rejection".Rapamune is a prescription medication used to prevent rejection in patients 13 years of age and older after a renal transplant. Rejection occurs when the immune system attacks the new organ. Rapamune can be used in conjunction with cyclosporine (Gengraf Neoral Sandimmune) and corticosteroids.Rapamune may also be used alone to treat lymphangioleiomyomatosis (LAM). LAM is a condition that primarily affects women who are pregnant or have children. LAM is a disorder that affects mostly women. It causes lung tumors, which are not cancerous. However, they can cause breathing problems.

Side effects of Rapamune 

Rapamune can cause a serious infection of the brain that may lead to death or disability. If you notice any changes in your mental health—reduced vision, weakness of one side, or difficulties with walking or speaking—call your doctor immediately. These symptoms can start slowly and then get worse very quickly.If you experience any of the following symptoms of an allergic reaction: hives or rash; difficulty breathing; chest pain, tightness, or discomfort; feeling as if you may pass out; swelling on your face, lips, or tongue; or a feeling of being about to faint, seek emergency medical attention.

If you experience:

  • Redness, oozing, or slow healing in a skin injury;
  • A new lesion or mole that has changed size or color
  • Unusual bleeding or bruises
  • Coughing, chest discomfort or pain, and feeling short of breath are all symptoms that may accompany sudden chest pain.
  • Tenderness around the transplanted renal
  • Signs and symptoms of infection: fever, chills; painful skin lesions; sores on the lips, mouth, or throat; flu or cold symptoms; burning or pain when you urinate.
  • Anemia (low red blood cells): pale skin and unusual fatigue; light-headedness or feeling short-of-breath; cold hands, feet, and legs

Side effects of Rapamune include:

  • Fever, sore neck, stuffy nose,
  • Mouth sores;
  • Diarrhea and stomach pain.
  • Muscle pains;
  • Chest pain;
  • Dizziness;
  • Acne.

There may be other side effects.For medical advice regarding side effects, call your physician. For FDA reporting purposes, dial 1-800-FDA-1088.

Warnings

Rapamune should not be used if you've ever had a lung transplant.Rapamune can cause an overproduction of white blood cells. This can cause cancer, brain infections that are severe enough to be fatal or severely disabled, or viral infections that result in kidney transplant failure.If you experience any of the following symptoms, call your doctor immediately: a fever, flu-like symptoms, burning in your urination, changes in your mental condition, decreased vision, weakness to one side, difficulty speaking or walking, or pain near your transplant.

Before you take this drug

Rapamune should not be used if sirolimus makes you allergic or if a liver or lung transplant has been performed in the past.Discuss with your doctor the risks and benefits associated with using this medication. Rapamune may affect your immune system and cause an overproduction of white blood cells. It can cause cancer, a severe brain infection that causes disability or death, or a viral infection that results in kidney transplant failure.

Tell your doctor about any of the following to ensure that Rapamune will be safe for you:

  • High cholesterol (or triglycerides);
  • Cytomegalovirus (CMV);
  • Liver disease
  • A family history of skin (melanoma) cancer

Rapamune should not be used if you're pregnant. You should use effective birth control during the time you take this medication and for 12 weeks following your last dose.Breastfeeding mothers should avoid taking this medicine.Rapamune is not recommended for children younger than 13 years of age.

Similar/related drugs

Azathioprine, Cyclosporine, Mycophenolate Mofetil, CellCept, Imuran, and Sirolimus

How to take Rapamune?

Follow the instructions on your prescription label and read all medication guides or instruction sheets. Read all the instructions and directions that come with your medication. Sometimes your doctor will change the dose.Rapamune can be taken only once per day. Take cyclosporine for at least four hours before taking this medication.Rapamune can be taken with or without food. However, it must always be taken the same way.Rapamune tablets should not be crushed, chewed, or broken. If you are having trouble swallowing the whole tablet, tell your doctor.Please read and follow all instructions for use that come with your medication. If you don't understand the instructions, ask your doctor or pharmacist.Rapamune oral fluid must only be mixed with orange juice or water. No other liquids or juices are allowed. Measuring the liquid is important. Use the provided dosing device or a dose-measuring tool (not a spoon).

Sirolimus alters the immune system's function, which can increase your infection risk. You will be required to undergo frequent medical testing. The results of the tests may affect your dosing schedule.Rapamune should only be stopped with your doctor's approval. Your condition could worsen if you stop suddenly.Keep the tablet out of direct sunlight, moisture, heat, or other forms of environmental harm.Keep the liquid in a refrigerator. Don't freeze. The liquid may appear slightly hazy. The haze will disappear once the liquid reaches room temperature.You can store the syringe that you use to administer Rapamune orally in the case provided. Use the medicine within 24 hours, and keep the case at room temperature. Dispose of the disposable syringe after use.

Details on dosage

Adult Rapamune Dose: Rejection Prevention:

PERSONNELS AT LOW OR MODERATE RISK IMMUNOLOGICAL:
Dosing based on body weight
Less than 40 kg
Loading dose: 3 mg/m2 on day 1
Maintenance: 1 mg/m2 once daily.
greater or equal to 40 kg
Dosage for loading: 6 mg taken orally every day.
Maintenance: 2 mg once daily orally
Patients at high immunological risk (defined as black kidney transplant recipients, repeat recipients of renal transplants who have lost a previous transplant due to an immune-related reason, and/or patients whose panel reactive antibodies are higher than 80%):
For patients receiving sirolimus and cyclosporine
Loading dose: up to 15 mg the first day after transplantation
Maintenance Dose: Starting on the second day, a maintenance dose of five milligrams per day should be administered. Between days 5 and 7, a trough should be measured, and then the daily dose should be adjusted.
Antibody induction therapy can be used.
Comments:
It is recommended to use this sirolimus in conjunction with cyclosporine, corticosteroids, and other medications.
Sirolimus may be taken with or without food.
After the maintenance dose of sirolimus is adjusted, the patient should continue to take the new dose for 7–14 days before adjusting the dosage with concentration monitoring.
MAINTENANCE THERAPY AFTER CYCLOSPORINE WITHDRAWAL
Patients with high immunological risk should not be advised to withdraw from cyclosporine. After 2 to 4 months of combined therapy, low- to moderate-risk patients may consider cyclosporine withdrawal. After discontinuing cyclosporine over a period of 4–8 weeks, a dosage increase of up to fourfold is required to maintain the immunosuppressive effect. The dose-adjusted target concentrations for the first year after transplantation are 16–24 ng/mL and 12–20 ng/mL afterwards (measured using chromatographic methods).

Usual Adult Dose of Rapamune for Pulmonary Lymphangioleiomyomatosis:

Initial dose: 2 mg/day
The concentration of sirolimus in the whole blood should be measured after 10–20 days. Adjust the dosage to maintain a concentration between 5 and 15 ng/mL.
Comment:
This drug can be taken with or without food.

The Usual Pediatric Rapamune Dose for Organ Transplantation—Rejection Prevention:

FOR PATIENTS WITH LOW OR MODERATE IMMUNOLOGIC RISE:
Aged 13 or older:
Dosing based on body weight
Less than 40 kg
Loading dose: 3 mg/m2 on day 1
Maintenance: 1 mg/m2 once daily.
greater or equal to 40 kg
Dosage for loading: 6 mg taken orally every day.
Maintenance: 2 mg once daily orally

What happens if I miss the dose?

If you are almost due for your next dose, skip the missed one. Never take two doses of the same medicine at once.

What happens if I overdose?

Reach out for help immediately if you suspect a poison exposure by calling 1-800-222-1222 or seeking medical attention immediately.

What should be avoided?

Avoid tanning beds or exposure to the sun. Rapamune can increase your skin cancer risk. When you're outdoors, wear protective clothing and apply sunscreen (SPF 30 or higher).Avoid being around people who are sick. If you suspect an infection, inform your physician immediately.Rapamune liquid should not be applied to the skin. If this happens, wash the affected skin with soap and warm water. If you get the medicine in your eyes, wash them with water.Sirolimus may cause unwanted side effects if grapefruit is consumed. Rapamune can cause side effects if you consume grapefruit or grapefruit juice.Rapamune should not be used in conjunction with a live vaccine. The vaccine might not work well and protect you as much during this period. Live vaccines are available for measles (MMR), rubella, mumps (MMR), yellow fever, typhoid (chickenpox), varicella, and zoster (shingles).

Interaction with other drug

Inform your physician of any medications you are currently taking.Rapamune can be affected by many drugs, including:

  • Bromocriptine (Cycloset, Parlodel);
  • Cyclosporine;
  • Danazol;
  • St. John's Wort;
  • Tacrolimus;
  • Cholesterol-lowering medication;
  • Antifungal or antibacterial medicine
  • Antiviral medicines to treat HIV and hepatitis C
  • Heart or blood pressure medications;
  • Medicine to treat ulcers or reduce stomach acid;
  • Seizure medicine.

The list of drugs that may interact with sirolimus is not exhaustive. These include prescription and over-the-counter medicines, vitamins, and herbal products. This list does not include all drug interactions.