1 What is Rapamune?

Brand: Rapamune

Generic: Sirolimus

Rapamune is an immunosuppressive agent that is used to suppress the immune system of a patient who has received a kidney from a donor.

Using Rapamune weakens your immune system thus making you more susceptible to infections. Assess risks and benefits of the use of taking Rapamune. You can get this medicine only after your doctor prescribes it for you.

Rapamune is also used to treat lymphangioleiomyomatosis, a rare lung disease commonly affecting women in their childbearing years. It is available as:

  • Tablet
  • Solution

2 What to Know Before Using

Before using Rapamune, you must know all about the risks and complications associated with it. Together with your doctor, you can decide whether the medication will provide you more goods than the harms.

Here are some factors to be considered before deciding to use this medicine:

Allergies: Inform your doctor about the allergies you have, such as to this medication, other medications, or to foods, dyes, or preservatives.

Pediatric: It’s not clear if sirolimus is safe or effective in children below 13 years.

Geriatric: It may be used cautiously in elderly after adjusting the dose.

Pregnancy: It falls under category C for all trimesters, meaning that due to lack of sufficient studies, it’s not clear if this medication is safe for use in pregnancy.

Breastfeeding: It may be used cautiously in a nursing mother after assessing both risks and benefits of the use.

Drug Interactions: Taking two medicines together can be harmful due to possible interactions. In other cases, even if there is a possible interaction between two medicines your doctor may advise you to take them together after adjusting the dose or issuing precautions.

Here is a list of the medicines which in general are not recommended to be used with this medicine.

Inform your doctor if you are using any of these medicines:

  • Clarithromycin
  • Erythromycin
  • Itraconazole
  • Rifampin
  • Telithromycin
  • Voriconazole

Though usually not recommended, your doctor may decide, after adjusting dose or frequency of one or both medicines, to use sirolimus with any of the following medicines:

  • Adalimumab
  • Live Adenovirus Vaccine Type 4
  • Live Adenovirus Vaccine Type 7
  • Amiodarone
  • Live BCG Vaccine
  • Boceprevir
  • Captopril
  • Clarithromycin
  • Cobicistat
  • Crizotinib
  • Fluconazole
  • Infliximab
  • Live Influenza Virus Vaccine
  • Ketoconazole
  • Live Measles Virus Vaccine
  • Live Moexipril Mumps Virus Vaccine
  • Phenobarbital
  • Live Poliovirus Vaccine
  • Rifampin
  • Live Rotavirus Vaccine
  • Live Rubella Virus Vaccine
  • Smallpox Vaccine
  • St John's Wort
  • Tacrolimus
  • Typhoid Vaccine
  • Varicella Virus Vaccine
  • Yellow Fever Vaccine

Rarely and only when absolutely needed, this medicine may be used with the following medicines even if using them together may put you at risk of certain side effects.

In such cases, you may have to take the adjusted dose or change the frequency of intake.

  • Amprenavir
  • Aprepitant
  • Cyclosporine
  • Diltiazem
  • Erythromycin
  • Fosphenytoin
  • Micafungin
  • Nevirapine
  • Phenytoin
  • Rifabutin
  • Verapamil

Other Interactions: Talk to your doctor to know if using this medicine with food, alcohol, or tobacco is safe. Do not take grapefruit or grapefruit juice while taking sirolimus.

Inform your doctor if you have any of the following conditions:

  • Ascites (fluid accumulation in stomach)
  • Blood clotting disorders such as thrombotic thrombocytopenic purpura
  • Heart disease
  • Hyperlipidemia (high blood cholesterol and fat levels)
  • Infection
  • Lung diseases
  • Lymphoma (cancer of the lymph glands)
  • Peripheral edema (swelling of the limbs)
  • Proteinuria (protein in the urine)
  • History of skin cancer: Use cautiously.
  • Liver disease: Use cautiously.
  • Liver or Lung transplantation: Do not use sirolimus.

3 Proper Usage

To use Rapamune properly, you must follow all instructions given by your doctor. Here are some points to watch for:

Follow your doctor’s instructions about the use of any medicine. Read the Medication Guide carefully and follow accordingly. Talk to your doctor if you have any query.

You may need this medicine for your whole life. For proper use of sirolimus when prescribed along with a corticosteroid and cyclosporine, discuss with your doctor.

Swallow an entire tablet instead of breaking or chewing it. If you cannot take the tablets, you may opt for an oral liquid. Here is “how to use” the oral liquid:

  • Use the amber syringe supplied with the medication to pump out the recommended dose.
  • Drop content of the syringe into a glass or plastic cup containing at least 2 ounces (60 milliliters) of water or orange juice, and stir.
  • Consume it immediately.
  • Pour at least 4 ounces (120 milliliters) of extra water or orange juice into the cup, stir vigorously and consume immediately.
  • Do not use the same syringe again.
  • If you are carrying the dose in a syringe, remember that it should be used within 24 hours.
  • Wash your skin with soap and water if this medicine falls on your skin. If your eyes come into contact with the medicine, immediately rinse with water.
  • Do not take grapefruit or grapefruit juice while taking sirolimus.

Dosing: For best results, follow your doctor to know what amount of medicine you should take in a single dose.

The doses of a medicine can differ according to the conditions for which it is being prescribed. If not stated otherwise, the doses here refer to an average dose. Remember your doses can differ.

The doses of oral solution or tablets are:

For preventing rejection of transplanted kidney: 

  • Adults and children 13 and 13+ years, weight ≥ 40 kilograms (kg): After a single dose of 6 mg, take 2 milligrams (mg) per day. You may need a larger dose but do not take more than 40 mg per day.
  • Children 13 years and 13+ years, weight < 40 kg: After a single dose of 3 mg per square meter of body surface area (BSA), take 1 mg per square meter of BSA.
  • Children younger than 13 years: Use and dose must be determined by your doctor.

For treating lymphangioleiomyomatosis:

  • Adults: Start with 2 mg per day, then after the dose may be adjusted.
  • Children: Your doctor will decide the use and dose.

Storage: Store in a closed container at room temperature.

  • Keep your medicines protected from heat, moisture, and direct light.
  • Do not freeze.
  • Keep away from children.
  • Discard any unused or expired medicines.
  • Store the oral liquid under refrigeration.
  • Do not store the oral liquid at room temperature for more than 15 days.

4 Precautions to Take

In using Rapamune, you must be careful and take some precautions as advised by your doctor. Your progress should be regularly monitored to determine if you are responding to the treatment.

Your doctor may order blood and urine tests to look for undesirable effects. Remember:

Do not get pregnant while using this medicine and at least 12 weeks after discontinuing it. If you suspect of pregnancy, inform your doctor immediately.

During the treatment, do not take clarithromycin, erythromycin, itraconazole, ketoconazole, rifabutin, rifampin, telithromycin, or voriconazole. Using them together may put you at a risk of skin cancer or cancer of the lymph system (lymphoma).

You may also become more prone to infections. Therefore, to reduce your risk:

  • Stay away from ill people or those who have received vaccines against measles, influenza, rubella, mumps, and other live vaccines.
  • Maintain proper hygiene.
  • Inform your doctor about any illness you had before starting sirolimus or any other chronic illness.
  • Consult your doctor before getting vaccinated during the treatment.

Sirolimus may cause life-threatening allergic conditions like anaphylaxis. Seek immediate help if you experience following symptoms after getting tacrolimus injections:

  • Itching, welts
  • Hoarseness
  • Breathing or swallowing problems
  • Swollen hands, face, or mouth.

You may also develop bleeding disorders or have delayed wound healing. Therefore:

  • Avoid the situations that may hurt you such as involving in sports.
  • Take care while brushing and flossing your teeth.
  • Take care while using sharp objects such as razors.
  • Inform your doctor immediately if you experience abnormal bleeding or bruising, black, tarry stools, bloody urine or stools, or red spots on your skin.

Sirolimus can also make you more susceptible to a rare and serious viral infection caused by BK virus which can lead to failure of the transplanted kidney.

Consult your doctor immediately if you develop two or more these symptoms:

  • bloody urine decreased the frequency or urine volume
  • increased thirst
  • loss of appetite
  • lower back or side pain
  • nausea
  • swollen face, fingers or lower legs
  • breathing difficulties
  • excessive tiredness or weakness

If you develop two or more of the following symptoms, see your doctor immediately as they might indicate progressive multifocal leukoencephalopathy (PML), a serious and rare brain infection.

  • Vision problems
  • Coordination, memory or speech problems
  • Confusion
  • Leg weakness

Protect your skin from UV rays by applying a sun block and avoiding sunlamps and tanning beds. Inform your doctor about the appearance of a new mole, changes in existing mole, if any.

Maintain proper oral health and schedule regular dental appointments. Avoid raw oysters or other shellfish while you are taking sirolimus.

Consult your doctor before using any prescription or nonprescription medicines and herbal or vitamin supplements.

5 Potential Side Effects

As with many medications, there are several potential side effects associated with Rapamune.

Consult your doctor immediately if you experience any of the following side effects:

More common:

  • Abdominal cramps
  • Black, tarry stools
  • Unusual bleeding from gums or nose
  • Vision problems
  • Itching, welts
  • Hoarseness
  • Breathing or swallowing problems
  • Swollen hands, face, or mouth.
  • Coordination, memory or speech problems
  • Confusion
  • Leg weakness
  • Loss of consciousness
  • Swelling in lymph glands of the neck, armpit, or groin
  • Yellowish skin and eyes

Less common:

  • Changes in mole
  • Hoarseness
  • Discharge from mole
  • Appearance of new mole
  • Abdominal pain radiating to the back
  • Skin ulcer or sores

Mild and non-serious side effects usually go away on their own without requiring medical intervention. You may also ask your doctor to learn more about how you may prevent or reduce the side effects.

Talk to your doctor if the side effects persist or worry you, including:

More common:

  • Breathing difficulties
  • Vision problems
  • Itchy, red and irritated skin
  • Excessive stomach acid
  • Numbness and abnormal sensations like a pinprick
  • Hearing abnormal sounds
  • Decreased frequency of urination
  • Depersonalization
  • Rapid heartbeats
  • Impotence
  • Dysphoria
  • Paranoia
  • Impaired concentration

The side effects of the medicine are not limited to the ones listed above. Call your doctor immediately if you experience any side effects that are uncommon or worry you. To report side effects to the FDA, contact at 1-800-FDA-1088.

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