sirolimus
Sirolimus (Rapamune) lowers the activity of your immune system to prevent rejection after a kidney transplant. It can also help with a condition that affects your lymphatic system, which is related to your immune system. Your provider will check the levels of sirolimus (Rapamune) in your blood, and this will help guide the dosing. Sirolimus (Rapamune) is available as tablets and as an oral solution, and it's usually only taken once a day. Common side effects include changes in your lab values (e.g., more cholesterol and fat in the blood, change in kidney labs), which is another reason to get your blood checked regularly while taking this medication.
What is Sirolimus (Rapamune)?
What is Sirolimus (Rapamune) used for?
- Prevention of kidney transplant rejection
- Treatment of lymphangioleiomyomatosis (LAM)
How Sirolimus (Rapamune) works
Sirolimus (Rapamune) is an immunosuppressant that lowers the activity of your immune system. You need a suppressed (lowered) immune system after receiving a transplant so your body doesn't reject the new kidney.
Drug facts
Side effects of Sirolimus (Rapamune)
The following side effects may get better over time as your body gets used to the medication. Let your healthcare provider know immediately if you continue to experience these symptoms or if they worsen over time.
Common Side Effects
- Swelling in arms and legs (up to 58%)
- More cholesterol and fat in the blood (up to 57%)
- High blood pressure (up to 49%)
- Change in kidney labs (up to 40%)
- Constipation (up to 36%)
- Headache (up to 34%)
- Pain (up to 33%)
- Stomach pain (up to 29%)
- Urinary tract infection (up to 26%)
Less Common Side Effects
- Fever
- Acne
- Diarrhea
- Muscle pain
- Nausea
Sirolimus (Rapamune) serious side effects
Contact your healthcare provider immediately if you experience any of the following.
- Infection: fever, chills, fatigue, muscle aches
- Serious lung problems (interstitial lung disease): breathing problems, chest pain, cough, tiredness
- Serious allergic reaction: trouble breathing, swelling of the face, tightening of the throat, rash, hives, welts, peeling or blistering skin
More on Sirolimus (Rapamune) side effects
The following Sirolimus (Rapamune) side effects have also been reported
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 or stomach cramps or pain
accumulation of pus
anxiousness, unexplained
backache
black or red, tarry stools
bleeding from the gums or nose
blurred vision
body aches or pain
bone pain
bruising
burning or stinging of the 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
chills
confusion
convulsions (seizures)
dark or bloody urine
deafness
decreased urine output
decreased vision
difficulty with breathing or swallowing
dilated neck veins
discharge from the eyes
dizziness
drowsiness
excessive tearing
extreme fatigue
facial hair growth in females
faintness or lightheadedness when getting up from lying or sitting position
fast, slow, or irregular heartbeat
flushing or redness of the skin, especially on the face and neck
general feeling of discomfort or illness
increased hunger
increased menstrual flow or vaginal bleeding
itching, pain, redness, swelling, tenderness, or warmth on the skin
lack or loss of appetite
large, flat, blue, or purplish patches in the skin
loss of sexual ability, desire, drive, or performance
loss of voice
nausea or vomiting
numbness or tingling around the lips, hands, or feet
pain in the chest, groin, or legs, especially the calves
painful cold sores or blisters on the lips, nose, eyes, or genitals
pale skin
prolonged bleeding from cuts
rapid heartbeat
rash
red or dark brown urine
redness or swelling in the ear
redness, pain, or swelling of the eye, eyelid, or inner lining of the eyelid
ringing in the ears
sensation of pins and needles
severe constipation
severe vomiting
severe, sudden headache
slurred speech
sores or white spots on the lips or in the mouth
stomach pain or upset
sudden decrease in the amount of urine
sudden loss of coordination
sudden, severe weakness or numbness in the arm or leg
sudden, unexplained shortness of breath
sweating
swollen, painful, or tender lymph glands in the neck, armpit, or groin
tenderness, pain, swelling, warmth, skin discoloration, and prominent superficial veins over affected area
ulcers on the lips or in the mouth
unusual tiredness or weakness
vision changes
weakness or heaviness of the legs
white patches in the mouth or on the tongue
yellow skin and eyes
Less common
change in size, shape, or color of existing mole
hoarseness
mole that leaks fluid or bleeds
new mole
pains in the stomach, side or abdomen, possibly radiating to the back
skin ulcer or sores
Incidence not known
Abnormal wound healing
headache
large, hive-like swelling on the 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 the 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
Abnormal vision
belching
blistering, crusting, irritation, itching, or reddening of the skin
burning feeling in the chest or stomach
burning, crawling, itching, numbness, prickling, "pins and needles", or tingling feeling
continuing ringing or buzzing or other unexplained noise in the ears
cracked, dry, or scaly skin
crying
decrease in frequency of urination
degenerative disease of the joint
depersonalization
difficulty with moving
difficulty with passing urine (dribbling)
dysphoria
ear pain
enlarged abdomen or stomach
euphoria
excess air or gas in the stomach or intestines
excessive muscle tone, muscle tension or tightness
fear
feeling sad or empty
hearing loss
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 the mouth
joint pain or swelling
leg cramps
loss of bladder control
loss of energy or weakness
loss of interest or pleasure
loss of strength
lower abdominal or stomach pain
muscle aches, pain, stiffness, or weakness
nervousness
pain in the back, ribs, arms, or legs
pain or burning in the throat
pain or tenderness around the eyes and cheekbones
paranoia
pelvic pain
quick to react or overreact emotionally
rapid breathing
rapidly changing moods
inflammation, redness, or swelling of the gums or mouth
shaking or trembling
shivering
sleepiness
sunken eyes
swelling
swelling of the scrotum
tender or enlarged gums
tenderness in the stomach area
thickening of the skin
trouble concentrating
trouble sleeping
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.
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Pros and cons of Sirolimus (Rapamune)
Pros
- Taken once a day
- Can be taken with or without food
- Comes as an oral solution for people who have a hard time swallowing pills
- Available as a generic medication, which can be less expensive
Cons
- Not meant for children age 12 and younger
- Not a good option during pregnancy
- Can cause fertility problems
- Must be used with other immunosuppressants
Pharmacist tips for Sirolimus (Rapamune)
- Take sirolimus (Rapamune) at the same time every day. If you're taking it with cyclosporine (Neoral), be sure to take sirolimus (Rapamune) 4 hours after cyclosporine (Neoral).
- Swallow the tablets whole. Don’t crush, chew, or split them. If you have a hard time swallowing the tablets, ask your provider about the oral solution.
- Talk to your transplant team about family planning. Sirolimus (Rapamune) can affect fertility and harm an unborn baby. Women who can become pregnant should use reliable birth control while they're taking sirolimus (Rapamune) and for 12 weeks after the medication is stopped. Talk to your provider about your options for birth control or if you wish to become pregnant; there are anti-rejection medications that might be safer in pregnancy.
- Many medications can change the amount of sirolimus (Rapamune) in your body. Talk to your transplant provider before starting any medication or supplement.
- Avoid grapefruit, pomelo, pomegranate, and Seville oranges while on sirolimus (Rapamune). These citrus fruits and their juices can interact with sirolimus (Rapamune) and cause the levels to get too high in your body, which can be very dangerous.
More tips for sirolimus (Rapamune) oral solution:
- Store sirolimus (Rapamune) oral solution in the fridge. If you don't have a fridge, you can store the solution at room temperature for up to 15 days. Any medication leftover after 15 days at room temperature should be thrown away. Bottles of sirolimus (Rapamune) in the fridge are good for 30 days after they're opened.
- Sometimes the sirolimus (Rapamune) solution turns hazy in the fridge. This doesn't mean the medication has gone bad. If you see a slight haze in the bottle, let it sit at room temperature and then gently shake the bottle until the haze goes away.
- If needed, sirolimus (Rapamune) oral solution can be mixed with 2 ounces of water or orange juice, but no other liquids. Once added to water or orange juice, stir the mixture well and then drink it right away.
Common questions about Sirolimus (Rapamune)
Sirolimus (Rapamune) stays in your body longer than its newer counterpart, everolimus (Zortress). This means that sirolimus (Rapamune) can be taken once a day, whereas everolimus (Zortress) is taken twice a day. Even though it lasts longer, you still need to take sirolimus (Rapamune) every day as directed in order to maintain a "target" level in your blood. Missing doses can lead to rejection or worsening of your condition if you're taking it for LMA.
Sirolimus (Rapamune) and tacrolimus (Prograf) are both immunosuppressants that prevent organ rejection, but they work differently to do so. Tacrolimus (Prograf) is a calcineurin inhibitor that blocks your immune cells (T cells) from activating, growing, and attacking your new organ. Sirolimus (Rapamune), on the other hand, stops a protein called mTOR, which your immune system needs in order to make fighter cells and antibodies. Tacrolimus (Prograf) can be used to prevent heart, liver, and kidney transplant rejection, whereas sirolimus (Rapamune) is only approved to prevent kidney transplant rejection. Both immunosuppressants are adjusted based on blood levels. If you've had a kidney transplant, talk to your transplant provider about which would be best for you.
Yes, sirolimus (Rapamune) and rapamycin are different names for the same medication. Scientists originally discovered the medication from a soil sample in Easter Island and named it rapamycin. The U.S. pharmaceutical world named the generic medication, sirolimus.
Blood draws are important because your provider determine your dose of sirolimus (Rapamune) based on its level in your blood. If your sirolimus (Rapamune) level is too low, you're at higher risk for transplant rejection. If it's high, it can lead to side effects. If you've had a kidney transplant, your transplant team will provide you with a schedule that will tell you which days to go for blood draws.
Sirolimus (Rapamune) can be taken with or without food, but it's important to be consistent (either always take it with food or always take it without food). Food in your stomach can change how much of the medication is absorbed, which means your levels might be too high or too low if you switch between taking the medication with food or on an empty stomach. If you usually get an upset stomach with medications, taking sirolimus (Rapamune) with food might be a good choice for you.
When a new organ is placed into your body, your immune system sees it as a foreign object and will want to get rid of it. The immune system's response can lead to a lot of inflammation, which will damage the new organ. Sirolimus (Rapamune) stops a protein called mTOR, which your immune system needs in order to make fighter cells and antibodies. This results in a lower immune system that isn't able to reject your new organ.
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Risks and warnings for Sirolimus (Rapamune)
Sirolimus (Rapamune) can cause some serious health issues. This risk may be even higher for certain groups. If this worries you, talk to your doctor or pharmacist about other options.
Risk for cancer
- Risk factors: Long-term use
Though not common, long-term use of sirolimus (Rapamune) can cause skin cancer, as well as lymphoma (a cancer of the immune system). Limit your exposure to sunlight and ultraviolet light, wear protective clothing, and use sunblock. Also, make sure to keep up your blood work appointments so your provider can make sure this medication remains safe for you.
Serious infections
- Risk factors: Taking other immunosuppressants
Sirolimus (Rapamune) can raise your risk of serious or life-threatening bacterial, fungal, and viral infections. Be sure to stay away from people who are sick. Wash your hands often. In some cases, infections can happen when an inactive virus in your body, like tuberculosis (TB) or hepatitis B virus (HBV), reactivates (makes you sick again). If you develop symptoms of fever, chills, muscle aches, change in appetite or weight loss, vomiting, or skin rash, tell your transplant provider right away.
Not recommended for liver and lung transplants
Sirolimus (Rapamune) isn't recommended for the prevention of rejection after liver and lung transplants. During clinical trials for liver transplants, people using sirolimus (Rapamune) had a higher risk of serious problems including death. There have also been reports of deadly breathing complications when used for lung transplants.
Slower wound healing
- Risk factors: BMI greater than 30 | Higher levels of sirolimus (Rapamune)
Sirolimus (Rapamune) can make it harder for your body to heal itself. This can be a problem when your body is recovering from surgery and is more likely to happen in people who are obese and those on higher doses of sirolimus (Rapamune). Your transplant team will monitor your healing process closely.
High lipids (cholesterol and triglycerides)
Sirolimus (Rapamune) can raise your cholesterol and triglyceride levels and put you at risk for heart problems. Your provider will monitor your labs and might recommend exercise and dietary changes that can help lower your levels. If the levels remain high, your provider can prescribe a cholesterol-lowering medication like a "statin."
Serious medication interactions
Sirolimus (Rapamune) can interact with many medications. Certain interactions, such as with erythromycin and rifampin (Rifadin), can be more dangerous because they lower the levels of sirolimus (Rapamune) in your body. When this happens, there's a higher chance that your body will reject the new transplant. Other medications might raise the level of sirolimus (Rapamune) in your body and make it more likely for you to experience side effects. Let your provider know what other medications you're currently taking so they can help check for interactions.
Kidney damage
- Risk factors: Taking other medications that can damage kidneys | Long-term use of sirolimus (Rapamune)
Your kidney health will be closely monitored after your kidney transplant. Some of your anti-rejection medications, like sirolimus (Rapamune), can slow down your kidney function and lead to protein in your urine. It's more likely to happen the longer you take sirolimus (Rapamune) and if you take other medications that can damage your kidney. If your provider suspects kidney damage, they can lower your dose or switch you to another medication to see if that helps.
Harm to unborn babies and lower sperm count
Sirolimus (Rapamune) can harm unborn babies and shouldn't be used during pregnancy. Females who want to become pregnant should continue to avoid pregnancy for 3 months after stopping the medication. Males taking sirolimus (Rapamune) can experience lower sperm counts. Family planning is an important conversation to have with your transplant provider to discuss your anti-rejection options.
Vaccines
Transplant medications like sirolimus (Rapamune) can change the way your immune system responds to vaccines. Avoid live vaccines while taking this medication because they can make you sick. Also be sure to stay away from people who recently got a live vaccine, because they could make you sick. Always tell your provider or pharmacist that you're taking an immunosuppressant like sirolimus (Rapamune) before getting vaccinated and they can let you know if it's a live vaccine or not.
Sirolimus (Rapamune) dosage
Tablet| Dosage | Quantity | Price as low as | Price per unit |
|---|---|---|---|
| 0.5mg | 90 tablets | $91.84 | $1.02 |
| 1mg | 90 tablets | $76.65 | $0.85 |
| 2mg | 30 tablets | $61.43 | $2.05 |
Typical dosage for Sirolimus (Rapamune)
Prevention of kidney transplant rejection
- If you have a lower risk of rejection: The typical starting dose is 6 mg by mouth on the day after your transplant, followed by 2 mg by mouth every day.
- If you have a higher risk of rejection: The typical starting dose is 15 mg by mouth on the day after your transplant, followed by 5 mg by mouth every day.
Your provider will adjust your dose based on the level of medication in your blood.
Lymphangioleiomyomatosis
- The typical starting dose is 2 mg by mouth every day. Your provider will likely measure the level of medication in your blood after a few weeks and will adjust your dose accordingly.
Interactions between Sirolimus (Rapamune) and other drugs
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.
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.
- Adenovirus Vaccine Type 4, Live
- Adenovirus Vaccine Type 7, Live
- Alefacept
- Amiodarone
- Bacillus of Calmette and Guerin Vaccine, Live
- Benazepril
- Berotralstat
- Boceprevir
- Capmatinib
- Captopril
- Ceritinib
- Clarithromycin
- Cobicistat
- Conivaptan
- Crizotinib
- Dengue Tetravalent Vaccine, Live
- Dronedarone
- Duvelisib
- Efavirenz
- Eluxadoline
- Enalapril
- Enalaprilat
- Enzalutamide
- Erdafitinib
- Etravirine
- Fluconazole
- Fosinopril
- Fosnetupitant
- Idelalisib
- Infliximab
- Influenza Virus Vaccine, Live
- Isavuconazonium Sulfate
- Itraconazole
- Ivosidenib
- Ketoconazole
- Lanreotide
- Larotrectinib
- Lasmiditan
- Lefamulin
- Letermovir
- Lisinopril
- Lorlatinib
- Lumacaftor
- Measles Virus Vaccine, Live
- Metoclopramide
- Mirabegron
- Moexipril
- Mumps Virus Vaccine, Live
- Netupitant
- Octreotide
- Pazopanib
- Perindopril
- Phenobarbital
- Poliovirus Vaccine, Live
- Quinapril
- Ramipril
- Ribociclib
- Rifampin
- Rotavirus Vaccine, Live
- Rubella Virus Vaccine, Live
- Saquinavir
- Selpercatinib
- Simeprevir
- Smallpox Vaccine
- St John's Wort
- Tacrolimus
- Telaprevir
- Telithromycin
- Tofacitinib
- Trandolapril
- Tucatinib
- Typhoid Vaccine, Live
- Varicella Virus Vaccine, Live
- Venetoclax
- Verapamil
- Vilazodone
- Voxelotor
- Yellow Fever Vaccine
- Zofenopril
- Zoster Vaccine, Live
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.
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