Description and Brand Names

Drug information provided by: Micromedex

US Brand Name

  1. Rapamune

Descriptions


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 benefits of this medicine as well as the risks.

This medicine is available only with your doctor's prescription.

This product is available in the following dosage forms:

  • Tablet
  • Solution

Before Using

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 younger than 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 geriatric-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

Information about this sirolimus-oral-route
Pregnancy Category Explanation
All Trimesters C Animal 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.

Breastfeeding

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.

Drug Interactions

Although certain medicines should not be used together at all, in other cases two different medicines may be used together even if an interaction might occur. In these cases, your doctor may want to change the dose, or other precautions may be necessary. When you are taking this medicine, it is especially important that your healthcare professional know if you are taking any of the medicines listed below. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.

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.

  • Amifampridine
  • Mifepristone
  • 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.

  • Adalimumab
  • Adenovirus Vaccine Type 4, Live
  • Adenovirus Vaccine Type 7, Live
  • Alefacept
  • Amiodarone
  • Bacillus of Calmette and Guerin Vaccine, Live
  • Boceprevir
  • Carbamazepine
  • Ceritinib
  • Clarithromycin
  • Cobicistat
  • Crizotinib
  • Dabrafenib
  • Dronedarone
  • Efavirenz
  • Enzalutamide
  • Eslicarbazepine Acetate
  • Etravirine
  • Fluconazole
  • Idelalisib
  • Infliximab
  • Influenza Virus Vaccine, Live
  • Itraconazole
  • Ketoconazole
  • Lomitapide
  • Measles Virus Vaccine, Live
  • Mitotane
  • Mumps Virus Vaccine, Live
  • Nilotinib
  • Pazopanib
  • Phenobarbital
  • Piperaquine
  • Poliovirus Vaccine, Live
  • Primidone
  • Rifampin
  • Rotavirus Vaccine, Live
  • Rubella Virus Vaccine, Live
  • Saquinavir
  • Siltuximab
  • Simeprevir
  • Smallpox Vaccine
  • St John's Wort
  • Tacrolimus
  • Telaprevir
  • Telithromycin
  • Tocophersolan
  • Typhoid Vaccine
  • Ulipristal
  • 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
  • Aprepitant
  • Cyclosporine
  • Diltiazem
  • Erythromycin
  • Fosphenytoin
  • Micafungin
  • Nevirapine
  • Phenytoin
  • Rifabutin
  • Verapamil

Other Interactions

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. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.

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:

  • Ascites (fluid in the abdomen or stomach) or
  • Cancer or
  • Heart disease (e.g., pericardial effusion) or
  • Hyperlipidemia (high amount of cholesterol and fats in the blood) or
  • Lung disease (e.g., bronchitis obliterans organizing pneumonia [BOOP], pleural effusion, pneumonitis, or pulmonary fibrosis) or
  • Peripheral edema (swelling of the hands, ankles, or feet)—Use with caution. May make these conditions worse.
  • Infection (including cytomegalovirus infection)—May decrease body's ability to fight infection.
  • Liver disease—You may require a smaller dose.
  • Liver transplantation or
  • Lung transplantation—Use is not recommended for these conditions.

Proper Use

Take this medicine only as directed by your doctor. Do not take more of it, do not take it more often, and do not take it for a longer time 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.

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.

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.

You may take this medicine with or without food. However, you should take it the same way (with or without food) each time.

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 checking first 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 is usually used along with a corticosteroid (cortisone-like medicine) and cyclosporine (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 liquid and be given instructions on how to take it.

To use the oral liquid:

  • Open the solution bottle and insert the adapter tightly into the bottle.
  • Insert the amber syringe (plastic needle) that comes with the bottle to draw the right amount of medicine out of the bottle.
  • Empty the medicine from the syringe into a glass or plastic cup.
  • Mix the medicine with at least 2 ounces (¼ cup or 60 milliliters [mL]) of water or orange juice. Stir the mixture well and drink it immediately.
  • Add at least 4 ounces (½ cup or 120 mL) of additional water or orange juice, stir it well, and drink it to make sure that all of the medicine is taken.
  • If you have been instructed by your doctor to carry your medicine, you may keep your daily dose of sirolimus in a tightly-capped syringe for a maximum of 24 hours at room temperature or in the refrigerator. Throw away the used syringe after each use.

If this medicine gets into your skin, wash it with soap and water right away. If it gets in your eyes, rinse them with water.

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 forms (oral solution or tablets):
    • To prevent kidney transplant rejection:
      • Adults and teenagers 13 years of age and older weighing 88 pounds (40 kilograms) or more—2 milligrams (mg) per day after an initial one-time dose of 6 mg. Some patients may require a dose of up to 5 mg per day after an initial one-time dose of 15 mg. However, the dose is usually not more than 40 mg per day.
      • Teenagers 13 years of age and older weighing less than 88 pounds (40 kilograms)—Dose is based on body size as determined by your doctor. The dose is 1 milligram (mg) per square meter [m(2)] of body surface area once a day after an initial one-time dose of 3 mg per square meter [m(2)] of body surface area.
      • 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 the oral tablets at room temperature in a closed container, away from heat, moisture, and direct light.

Store the oral liquid in the refrigerator. Protect it from direct light and moisture. Do not freeze. You may store the oral liquid at room temperature for a short period of time (not more than 15 days). If you see a slight haze or cloudiness in the bottle, leave it out at room temperature and shake it until the haze disappears. Throw away any unused medicine after 30 days.

Precautions

It is very important that your doctor check the progress of you or your child at regular visits to make sure that this medicine is working properly. Blood and urine tests may be needed to check for unwanted effects.

Using this medicine while you are pregnant can harm your unborn baby. Use an effective form of birth control to keep from getting pregnant, and keep using it for at least 12 weeks after you stop taking sirolimus. If you think you have become pregnant while using the medicine, tell your doctor right away.

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 or your child are getting a cold or other infection, check with your doctor.

This medicine may also increase your risk of bleeding and cause delay in wound healing. Stay away from rough sports or other situations where you could be bruised, cut, or injured. Brush and floss your teeth gently. Be careful when using sharp objects, including razors and fingernail clippers. Check with your doctor immediately if you or your child notice any unusual bleeding or bruising; black, tarry stools; blood in the 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 or your child have a rash; itching; large, hive-like swelling on the face, eyelids, lips, tongue, throat, hands, legs, feet, or sex organs; red, swollen skin; 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 or cancer of the lymph glands (lymphoma). When you or your child 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 sunblock 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.

This medicine may increase your cholesterol and fats in the blood. If this condition occurs, your doctor may give you or your child some medicines that can lower the amount of cholesterol and fats in the blood.

This medicine may increase your risk of developing a rare and serious virus infection called BK virus-associated nephropathy (BKVAN). The BK virus may affect how your kidneys work and cause a transplanted kidney to fail. Check with your doctor right away if you or your child are having more than one of these symptoms: bloody urine; a decreased frequency or amount of urine; increased thirst; loss of appetite; lower back or side pain; nausea; swelling of the face, fingers, or lower legs; trouble with breathing; unusual tiredness or weakness; vomiting; or weight gain.

This medicine may increase your risk of developing a serious and rare brain infection called progressive multifocal leukoencephalopathy (PML). Check with your doctor right away if you or your child are having more than one of these symptoms: vision changes, loss of coordination, clumsiness, confusion, memory loss, difficulty speaking or understanding what others say, and weakness in the legs.

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.

Do not take other medicines unless they have been discussed with your doctor. This includes prescription or nonprescription (over-the-counter [OTC]) medicines and herbal or vitamin supplements.

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

  1. Abdominal or stomach cramps or pain
  2. accumulation of pus
  3. anxiousness, unexplained
  4. backache
  5. black or red, tarry stools
  6. bleeding from the gums or nose
  7. blurred vision
  8. body aches or pain
  9. bone pain
  10. bruising
  11. burning or stinging of the skin
  12. burning while urinating
  13. burning, dry, or itching eyes
  14. burning, tingling, numbness, or pain in the hands, arms, feet, or legs
  15. change in mental status
  16. changes in skin color
  17. chest pain
  18. chills
  19. confusion
  20. convulsions (seizures)
  21. cough
  22. dark or bloody urine
  23. deafness
  24. decreased urine output
  25. decreased vision
  26. difficulty with breathing or swallowing
  27. dilated neck veins
  28. discharge from the eyes
  29. dizziness
  30. drowsiness
  31. dry mouth
  32. earache
  33. excessive tearing
  34. extreme fatigue
  35. eye pain
  36. facial hair growth in females
  37. faintness or lightheadedness when getting up from lying or sitting position
  38. fast, slow, or irregular heartbeat
  39. fever
  40. flushing or redness of the skin, especially on the face and neck
  41. general feeling of discomfort or illness
  42. increased hunger
  43. increased menstrual flow or vaginal bleeding
  44. itching, pain, redness, swelling, tenderness, or warmth on the skin
  45. lack or loss of appetite
  46. large, flat, blue, or purplish patches in the skin
  47. loss of sexual ability, desire, drive, or performance
  48. loss of voice
  49. mood changes
  50. muscle pain
  51. nasal congestion
  52. nausea or vomiting
  53. numbness or tingling around the lips, hands, or feet
  54. pain in the chest, groin, or legs, especially the calves
  55. painful cold sores or blisters on the lips, nose, eyes, or genitals
  56. pale skin
  57. prolonged bleeding from cuts
  58. rapid heartbeat
  59. rash
  60. red or dark brown urine
  61. redness or swelling in the ear
  62. redness, pain, or swelling of the eye, eyelid, or inner lining of the eyelid
  63. ringing in the ears
  64. runny nose
  65. sensation of pins and needles
  66. severe constipation
  67. severe vomiting
  68. severe, sudden headache
  69. shortness of breath
  70. slurred speech
  71. sore throat
  72. sores or white spots on the lips or in the mouth
  73. stomach pain or upset
  74. sudden decrease in the amount of urine
  75. sudden loss of coordination
  76. sudden, severe weakness or numbness in the arm or leg
  77. sudden, unexplained shortness of breath
  78. sweating
  79. swollen, painful, or tender lymph glands in the neck, armpit, or groin
  80. tenderness, pain, swelling, warmth, skin discoloration, and prominent superficial veins over affected area
  81. tremor
  82. trouble breathing
  83. ulcers on the lips or in the mouth
  84. unusual tiredness or weakness
  85. vision changes
  86. weakness or heaviness of the legs
  87. white patches in the mouth or on the tongue
  88. yellow skin and eyes

Less common

  1. Bloating
  2. change is size, shape, or color of existing mole
  3. darkened urine
  4. hoarseness
  5. mole that leaks fluid or bleeds
  6. new mole
  7. pains in the stomach, side or abdomen, possibly radiating to the back
  8. skin ulcer or sores

Incidence not known

  1. Abnormal wound healing
  2. headache
  3. hives
  4. itching
  5. large, hive-like swelling on the face, eyelids, lips, tongue, throat, hands, legs, feet, or sex organs
  6. nails loose or detached
  7. puffiness or swelling of the eyelids or around the eyes, face, lips, or tongue
  8. swelling of the arms or legs
  9. 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

  1. Abnormal vision
  2. acne
  3. belching
  4. blistering, crusting, irritation, itching, or reddening of the skin
  5. burning feeling in the chest or stomach
  6. burning, crawling, itching, numbness, prickling, "pins and needles", or tingling feeling
  7. constipation
  8. continuing ringing or buzzing or other unexplained noise in the ears
  9. cracked, dry, or scaly skin
  10. crying
  11. decrease in frequency of urination
  12. degenerative disease of the joint
  13. depersonalization
  14. diarrhea
  15. difficulty in passing urine (dribbling)
  16. difficulty with moving
  17. dysphoria
  18. ear pain
  19. enlarged abdomen or stomach
  20. euphoria
  21. excess air or gas in the stomach or intestines
  22. excessive muscle tone, muscle tension or tightness
  23. fear
  24. feeling sad or empty
  25. hearing loss
  26. heartburn
  27. inability to have or keep an erection
  28. increase in heart rate
  29. increased hair growth, especially on the face
  30. increased urge to urinate during the night
  31. indigestion
  32. irritation in the mouth
  33. itching skin
  34. joint pain or swelling
  35. kidney pain
  36. leg cramps
  37. loss of bladder control
  38. loss of energy or weakness
  39. loss of interest or pleasure
  40. loss of strength
  41. lower abdominal or stomach pain
  42. mental depression
  43. muscle aches, pain, stiffness, or weakness
  44. nervousness
  45. pain in the back, ribs, arms, or legs
  46. pain or burning in the throat
  47. pain or tenderness around the eyes and cheekbones
  48. paranoia
  49. pelvic pain
  50. quick to react or overreact emotionally
  51. rapid breathing
  52. rapidly changing moods
  53. inflammation, redness, or swelling of the gums or mouth
  54. shaking or trembling
  55. shivering
  56. sleepiness
  57. sunken eyes
  58. swelling
  59. swelling of the scrotum
  60. tender or enlarged gums
  61. tenderness in the stomach area
  62. thickening of the skin
  63. trouble concentrating
  64. trouble with sleeping
  65. waking to urinate at night

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.