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Drugs reference index «Rapamune»

Rapamune
Rapamune


Rapamune

Generic Name: sirolimus (Oral route)

sir-OH-li-mus

Oral routeTabletSolution
  • Immunosuppression, use is not recommended in liver or lung transplant patients
    • Increased susceptibility to infection and the possible development of lymphoma and other malignancies may result from immunosuppression
      • Increased susceptibility to infection and the possible development of lymphoma may result from immunosuppression. Only physicians experienced in immunosuppressive therapy and management of renal transplant patients should use sirolimus. Patients receiving the drug should be managed in facilities equipped and staffed with adequate laboratory and supportive medical resources. The physician responsible for maintenance therapy should have complete information requisite for the follow-up of the patient.
    • The safety and efficacy of sirolimus as immunosuppressive therapy have not been established in liver or lung transplant patients, and therefore, such use is not recommended.
      • Liver Transplantation – Excess Mortality, Graft Loss, and Hepatic Artery Thrombosis (HAT)
      • The use of sirolimus in combination with tacrolimus was associated with excess mortality and graft loss in a study in de novo liver transplant patients. Many of these patients had evidence of infection at or near the time of death.
      • In this and another study in de novo liver transplant patients, the use of sirolimus in combination with cyclosporine or tacrolimus was associated with an increase in HAT; most cases of HAT occurred within 30 days post-transplantation and most led to graft loss or death.
      • Lung Transplantation – Bronchial Anastomotic Dehiscence
      • Cases of bronchial anastomotic dehiscence, most fatal, have been reported in de novo lung transplant patients when sirolimus has been used as part of an immunosuppressive regimen.

Increased susceptibility to infection and the possible development of lymphoma and other malignancies may result from immunosuppression. Only physicians experienced in immunosuppressive therapy and management of renal transplant patients should prescribe sirolimus and they should have complete information requisite for the follow-up of the patient. The use of sirolimus in combination with cyclosporine or tacrolimus was associated with excess mortality, graft loss, and hepatic artery thrombosis in studies in de novo liver transplant patients. Cases of bronchial anastomotic dehiscence, most fatal, have been reported in de novo lung transplant patients when sirolimus has been used as part of an immunosuppressive regimen. The safety and efficacy of sirolimus as immunosuppressive therapy have not been established in liver or lung transplant patients, and therefore, such use is not recommended .

Commonly used brand name(s):

In the U.S.

  • Rapamune

Available Dosage Forms:

  • Tablet
  • Solution

Therapeutic Class: Immune Suppressant

Uses For Rapamune

Sirolimus belongs to a group of medicines known as immunosuppressive agents. It is used to lower the body's natural immunity in patients who receive kidney transplants.

When a patient receives an organ transplant, the body's white blood cells will try to get rid of (reject) the transplanted organ. Sirolimus works by preventing the white blood cells from getting rid of the transplanted organ.

Sirolimus is a very strong medicine. It can cause side effects that can be very serious, such as kidney problems. It may also reduce the body's ability to fight infections. You and your doctor should talk about the good this medicine will do as well as the risks of using it.

Sirolimus is available only with your doctor's prescription.

Before Using Rapamune

In deciding to use a medicine, the risks of taking the medicine must be weighed against the good it will do. This is a decision you and your doctor will make. For this medicine, the following should be considered:

Allergies

Tell your doctor if you have ever had any unusual or allergic reaction to this medicine or any other medicines. Also tell your health care professional if you have any other types of allergies, such as to foods, dyes, preservatives, or animals. For non-prescription products, read the label or package ingredients carefully.

Pediatric

Appropriate studies have not been performed on the relationship of age to the effects of sirolimus in children below 13 years of age or in children considered to be at high immunologic risk. Safety and efficacy have not been established .

Geriatric

Appropriate studies performed to date have not demonstrated geriatrics-specific problems that would limit the usefulness of sirolimus in the elderly. However, elderly patients are more likely to have liver and heart problems which may require caution in patients receiving sirolimus .

Pregnancy

Pregnancy CategoryExplanation
All TrimestersCAnimal studies have shown an adverse effect and there are no adequate studies in pregnant women OR no animal studies have been conducted and there are no adequate studies in pregnant women.

Breast Feeding

There are no adequate studies in women for determining infant risk when using this medication during breastfeeding. Weigh the potential benefits against the potential risks before taking this medication while breastfeeding.

Interactions with Medicines

Using this medicine with any of the following medicines is not recommended. Your doctor may decide not to treat you with this medication or change some of the other medicines you take.

  • Posaconazole
  • Voriconazole

Using this medicine with any of the following medicines is usually not recommended, but may be required in some cases. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.

  • Amiodarone
  • Bacillus of Calmette and Guerin Vaccine, Live
  • Carbamazepine
  • Clarithromycin
  • Efavirenz
  • Etravirine
  • Fluconazole
  • Itraconazole
  • Ketoconazole
  • Measles Virus Vaccine, Live
  • Mumps Virus Vaccine, Live
  • Pazopanib
  • Phenobarbital
  • Poliovirus Vaccine, Live
  • Rotavirus Vaccine, Live
  • Rubella Virus Vaccine, Live
  • Smallpox Vaccine
  • St John's Wort
  • Tacrolimus
  • Typhoid Vaccine
  • Varicella Virus Vaccine
  • Yellow Fever Vaccine

Using this medicine with any of the following medicines may cause an increased risk of certain side effects, but using both drugs may be the best treatment for you. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.

  • Amprenavir
  • Cyclosporine
  • Diltiazem
  • Erythromycin
  • Micafungin
  • Nevirapine
  • Phenytoin
  • Rifabutin
  • Rifampin
  • Saquinavir
  • Telithromycin
  • Verapamil

Interactions with Food/Tobacco/Alcohol

Certain medicines should not be used at or around the time of eating food or eating certain types of food since interactions may occur. Using alcohol or tobacco with certain medicines may also cause interactions to occur. Discuss with your healthcare professional the use of your medicine with food, alcohol, or tobacco.

Using this medicine with any of the following may cause an increased risk of certain side effects but may be unavoidable in some cases. If used together, your doctor may change the dose or how often you use this medicine, or give you special instructions about the use of food, alcohol, or tobacco.

  • Grapefruit Juice

Other Medical Problems

The presence of other medical problems may affect the use of this medicine. Make sure you tell your doctor if you have any other medical problems, especially:

  • Cancer or
  • Hyperlipidemia (high amount of cholesterol and fats in the blood) or
  • Lung disease (e.g., pneumonitis or pulmonary fibrosis)—Sirolimus can make these conditions worse.
  • Chickenpox (including recent exposure) or
  • Herpes zoster (shingles)—Risk of severe disease affecting other parts of the body.
  • Infection—Sirolimus decreases the body's ability to fight infection.
  • Liver transplantation—or
  • Lung transplantation—Sirolimus is not recommended in liver or lung transplant patients.

Proper Use of Rapamune

This medicine usually comes with patient information or directions. Read them carefully and make sure you understand them before taking this medicine. If you have any questions, ask your doctor .

Take this medicine only as directed by your doctor. Do not use more or less of it, and do not use it more often than your doctor ordered. The exact amount of medicine you need has been carefully worked out. Using too much will increase the risk of side effects, while using too little may lead to rejection of your transplanted kidney.

To help you remember to take your medicine, try to get into the habit of taking it at the same time each day. This will help sirolimus work better by keeping a constant amount in the blood.

Absorption of this medicine may be changed if you change your diet. This medicine should be taken consistently with respect to meals. You should not change the type or amount of food you eat unless you discuss it with your doctor .

Grapefruits and grapefruit juice may increase the effects of sirolimus by increasing the amount of this medicine in your body. You should not eat grapefruit or drink grapefruit juice while you are taking this medicine.

Do not stop taking this medicine without first checking with your doctor. You may have to take this medicine for the rest of your life to prevent your body from rejecting the transplant.

Sirolimus usually is used along with a corticosteroid (cortisone-like medicine) and cyclosporine (another immunosuppressive agent). Sirolimus should be taken 4 hours after cyclosporine modified oral solution (Neoral®) or cyclosporine modified capsules (Neoral®). If you have any questions about this, ask your doctor .

If you have been taking sirolimus together with cyclosporine for 2 to 4 months after your transplant, your doctor may want you to stop using cyclosporine and increase the dose of sirolimus. However, some patients (e.g., black patients or those with transplant rejection in the past) may need to continue using cyclosporine for up to one year after the transplant. Your doctor will tell you if you need to keep taking cyclosporine .

Sirolimus tablets should not be crushed, chewed, or split. If you are unable to take the tablet form, your doctor will give you an oral solution of sirolimus and be given instructions on how to take it .

Mix sirolimus oral solution with at least 2 ounces (¼ cup, 60 milliliters [mL]) of water or orange juice in a glass or plastic container. Stir the mixture well and drink it immediately. Then, rinse the container with at least 4 ounces (½ cup, 120 mL) of additional water or orange juice, stir it well, and drink it to make sure that all of the medicine is taken.

Dosing

The dose of this medicine will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of this medicine. If your dose is different, do not change it unless your doctor tells you to do so.

The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.

  • For oral dosage form (oral solution or tablets):
    • To prevent kidney transplant rejection:
      • Adults and children 13 years of age and older weighing 88 pounds (40 kilograms) or more—The usual dose is 2 milligrams (mg) a day after an initial one-time dose of 6 mg. Some patients may require a dose of up to 5 mg a day after an initial one-time dose of 15 mg.
      • For children 13 years of age and older who weigh less than 88 pounds (40 kilograms)—The dose is based on body size. It is usually 1 mg per square meter of body surface area once a day after an initial one-time dose of 3 mg per square meter of body surface area.
      • For children up to 13 years of age—Use and dose must be determined by your doctor .

Storage

Keep out of the reach of children.

Do not keep outdated medicine or medicine no longer needed.

Ask your healthcare professional how you should dispose of any medicine you do not use.

Store tablets at room temperature. Store the oral liquid form in the refrigerator.

Precautions While Using Rapamune

It is very important that your doctor check your progress at regular visits to make sure that this medicine is working properly and to check for unwanted effects.

While you are taking sirolimus, it is important to maintain good dental hygiene and see a dentist regularly for teeth cleaning.

Raw oysters or other shellfish may contain bacteria that can cause serious illness and possibly death. This is more likely to be a problem if these foods are eaten by patients with certain medical conditions. Even eating oysters from “clean” water or good restaurants does not guarantee that the oysters do not contain the bacteria. Eating raw shellfish is not a problem for most healthy people; however, patients with the following conditions may be at greater risk: cancer, immune disorders, organ transplantation, long-term corticosteroid use (as for asthma, arthritis, or organ transplantation), liver disease (including viral hepatitis), excess alcohol intake (2 to 3 drinks or more per day), diabetes, stomach problems (including stomach surgery and low stomach acid), and hemochromatosis (an iron disorder). Do not eat raw oysters or other shellfish while you are taking sirolimus. Be sure oysters and shellfish are fully cooked.

While you are being treated with sirolimus, and after you stop treatment with it, it is important to see your doctor about the immunizations (vaccinations) you should receive. Do not get any immunizations without your doctor's approval. Sirolimus may lower your body's resistance and there is a chance you might get the infection the immunization is meant to prevent. In addition, other persons living in your household should not take oral polio vaccine since there is a chance they could pass the polio virus on to you. Also, avoid other persons who have taken the oral polio vaccine. Do not get close to them, and do not stay in the same room with them for very long. If you cannot take these precautions, you should consider wearing a protective face mask that covers the nose and mouth.

Treatment with sirolimus may increase the chance of getting other infections. If you can, avoid people with colds or other infections. If you think you are getting a cold or other infection, check with your doctor .

This medicine may also increase your risk of bleeding. Check with your doctor immediately if you notice any unusual bleeding or bruising; black, tarry stools; blood in urine or stools; or pinpoint red spots on your skin .

Sirolimus may cause serious types of allergic reactions, especially when used with certain medicines. Tell your doctor right away if you have a rash; itching; large, hive-like swelling on the face, eyelids, lips, tongue, throat, hands, legs, feet, or sex organs; trouble with breathing; or chest tightness while you are using this medicine .

Sirolimus may cause you to have a greater risk for getting cancer, especially skin cancer. When you begin taking this medicine:

  • Stay out of direct sunlight, especially between the hours of 10:00 a.m. and 3:00 p.m., if possible.
  • Wear protective clothing, including a hat. Also, wear sunglasses.
  • Apply a sun block product that has a skin protection factor (SPF) of at least 15. Some patients may require a product with a higher SPF number, especially if they have a fair complexion. If you have any questions about this, check with your doctor.
  • Apply a sun block lipstick that has an SPF of at least 15 to protect your lips.
  • Do not use a sunlamp or tanning bed or booth .

Check with your doctor right away if you notice a new mole; a change in size, shape or color of an existing mole; or a mole that leaks fluid or bleeds.

Rapamune Side Effects

Along with its needed effects, a medicine may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.

Check with your doctor immediately if any of the following side effects occur:

More common
  • Abdominal cramps or pain
  • accumulation of pus
  • anxiousness, unexplained
  • backache
  • black or red, tarry stools
  • bleeding from gums or nose
  • blindness
  • bloody or cloudy urine
  • blue lips and fingernails
  • blurred vision
  • body aches or pain
  • bone pain
  • bruising
  • burning or stinging of skin
  • burning while urinating
  • burning, dry, or itching eyes
  • burning, tingling, numbness, or pain in the hands, arms, feet, or legs
  • change in mental status
  • changes in skin color
  • chest pain
  • chills
  • cold hands and feet
  • cold sweats
  • confusion
  • convulsions (seizures)
  • cough; cough producing mucus; cough that sometimes produces a pink frothy sputum
  • coughing up blood
  • dark or bloody urine
  • deafness
  • decreased urge to urinate
  • decreased urine output
  • decreased vision
  • difficult, fast, noisy breathing sometimes with wheezing
  • difficulty in breathing or swallowing
  • difficulty speaking
  • dilated neck veins
  • discharge from eye
  • dizziness
  • drowsiness
  • dry mouth
  • ear congestion
  • earache
  • excessive tearing
  • extreme fatigue
  • eye pain
  • facial hair growth in females
  • fainting
  • faintness or lightheadedness when getting up from lying or sitting position
  • fast, slow, or irregular heartbeat
  • fatigue
  • feeling faint
  • feeling of warmth or heat
  • fever
  • flushed, dry skin
  • flushing or redness of skin, especially on face and neck
  • fractures
  • frequent urge to urinate
  • fruit-like breath odor
  • full or round face, neck, or trunk
  • general feeling of discomfort or illness
  • increased hunger
  • increased menstrual flow or vaginal bleeding
  • increased sweating
  • increased thirst
  • increased urination
  • irregular breathing
  • irritability
  • itching, pain, redness, swelling, tenderness, or warmth on skin
  • lab results that show problems with liver
  • lack or loss of appetite
  • large, flat, blue or purplish patches in the skin
  • lightheadedness
  • loss of consciousness
  • loss of sexual ability, desire, drive, or performance
  • loss of voice
  • lower back or side pain
  • lump in abdomen
  • menstrual irregularities
  • mood changes
  • muscle cramps in hands, arms, feet, legs, or face
  • muscle pain
  • muscle wasting
  • nasal congestion
  • nausea or vomiting
  • noisy breathing
  • numbness or tingling around lips, hands, or feet
  • pain in chest, groin, or legs, especially the calves
  • pain, tenderness, swelling of foot or leg
  • painful blisters on trunk of body
  • painful cold sores or blisters on lips, nose, eyes, or genitals
  • painful or difficult urination
  • pale skin
  • paralysis
  • pinpoint red spots on skin
  • pounding or racing heartbeat or pulse
  • prolonged bleeding from cuts
  • pus in urine
  • rapid heartbeat
  • rapid, shallow breathing
  • rash
  • red or dark brown urine
  • redness or swelling in ear
  • redness, pain, swelling of eye, eyelid, or inner lining of eyelid
  • ringing in the ears
  • runny nose
  • sensation of pins and needles
  • severe constipation
  • severe vomiting
  • severe, sudden headache
  • shortness of breath
  • slurred speech
  • sneezing
  • sore mouth or tongue
  • sore throat
  • sores or white spots on lips or in mouth
  • stabbing pain
  • stomach pain or upset
  • stomachache
  • sudden decrease in amount of urine
  • sudden loss of coordination
  • sudden, severe weakness or numbness in arm or leg
  • sudden, unexplained shortness of breath
  • sweating
  • swelling of face, fingers, hands, ankles, feet, or lower legs
  • swollen glands
  • swollen, painful or tender lymph glands in neck, armpit, or groin
  • swollen, red, tender area of infection
  • tenderness, pain, swelling, warmth, skin discoloration, and prominent superficial veins over affected area
  • tightness in chest
  • tiredness
  • tremor
  • trouble breathing
  • ulcers on lips or in mouth
  • unusual bleeding or bruising
  • unusual tiredness or weakness
  • vision changes
  • weakness or heaviness of legs
  • weight gain, unusual
  • weight loss, unusual
  • wheezing
  • white patches in mouth and/or on tongue
  • yellow skin and eyes
Less common
  • Bloating
  • change is size, shape, or color of existing mole
  • darkened urine
  • hoarseness
  • mole that leaks fluid or bleeds
  • new mole
  • pains in stomach, side or abdomen, possibly radiating to the back
  • skin ulcer or sores
Incidence not known
  • Abnormal wound healing
  • hives
  • itching
  • large, hive-like swelling on face, eyelids, lips, tongue, throat, hands, legs, feet, or sex organs
  • nails loose or detached
  • puffiness or swelling of the eyelids or around the eyes, face, lips, or tongue
  • swelling of arms or legs
  • yellow nails lacking a cuticle

Some side effects may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects. Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:

More common
  • Abdomen enlarged
  • abnormal vision
  • acne
  • belching
  • blistering, crusting, irritation, itching, or reddening of skin
  • burning feeling in chest or stomach
  • burning, crawling, itching, numbness, prickling, "pins and needles", or tingling feeling
  • constipation
  • continuing ringing or buzzing or other unexplained noise in ears
  • cracked, dry, or scaly skin
  • crying
  • decrease in frequency of urination
  • decrease in height
  • decreased interest in sexual intercourse
  • degenerative disease of the joint
  • depersonalization
  • diarrhea
  • difficulty in moving
  • difficulty in passing urine (dribbling)
  • discouragement
  • dysphoria
  • ear pain
  • euphoria
  • excess air or gas in stomach or intestines
  • excessive muscle tone, muscle tension or tightness
  • fear
  • feeling sad or empty
  • headache
  • hearing loss
  • heartburn
  • inability to have or keep an erection
  • increase in heart rate
  • increased hair growth, especially on the face
  • increased urge to urinate during the night
  • indigestion
  • irritation in mouth
  • itching skin
  • joint pain or swelling
  • kidney pain
  • leg cramps
  • loss of bladder control
  • loss of energy or weakness
  • loss of interest or pleasure
  • loss of strength
  • lower abdominal pain
  • mental depression
  • muscle aches, pain, stiffness, or weakness
  • nervousness
  • pain
  • pain in back, ribs, arms, or legs
  • pain or burning in throat
  • pain or tenderness around eyes and cheekbones
  • paranoia
  • passing gas
  • pelvic pain
  • quick to react or overreact emotionally
  • rapid breathing
  • rapidly changing moods
  • inflammation, redness, or swelling of gums or mouth
  • shaking or trembling
  • shivering
  • sleepiness
  • sunken eyes
  • swelling
  • swelling of the scrotum
  • tender or enlarged gums
  • tenderness in stomach area
  • thickening of the skin
  • trouble concentrating
  • trouble in sleeping
  • waking to urinate at night
  • wrinkled skin

Other side effects not listed may also occur in some patients. If you notice any other effects, check with your healthcare professional.

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

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  • Rapamune Prescribing Information (FDA)
  • Rapamune Concise Consumer Information (Cerner Multum)
  • Rapamune MedFacts Consumer Leaflet (Wolters Kluwer)
  • Sirolimus Professional Patient Advice (Wolters Kluwer)