Sirolimus (Oral)

Sirolimus is used alongside other medications to help the body to accept a transplanted kidney. This medicine is also used as a treatment for lymphangioleiomyomatosis.

Overview

Sirolimus is a type of medication that is used in the process of a kidney transplantation, in order to combat any possible rejection. It is one of several medications used for this and is often used alongside corticosteroids. Sirolimus is a drug from the immunosuppressive agents family.

In the event that a patient receives any form of organ transplant, their bodies' white blood cells will act to reject or get rid of, the transplanted organ as the immune system sees it as a foreign item within the body. Sirolimus acts to prevent this by preventing the white blood cells from rejecting the transplanted organ.

As a very strong form of medication, Sirolimus can cause several potential side effects that can be very serious, including kidney problems. Due to the immunosuppressive nature of this medication, it may also cause the body's ability to fight infections to be reduced. Due to the seriousness of the potential side effects, it's important the patient and doctor discuss all the risks and benefits of Sirolimus prior to treatment.

In addition, Sirolimus can be used to treat lymphangioleiomyomatosis, which a rare lung disease that predominantly affects women of a childbearing age. This disorder mostly, but not exclusively, occurs in women and results in lung tumors - these tumors are not cancerous but potentially can affect breathing.

This medicine is available solely through a prescription.

Conditions Treated

Sirolimus is used as a preventative or treatment medication for the following:

  • To prevent the body from rejecting a transplanted kidney
  • Lymphangioleiomyomatosis

Type of Medicine

  • Tablet
  • Solution
  • Immunosuppressive agent

Side Effects

Alongside the required and defined effects of this medication, Sirolimus can also cause some additional unwanted side effects. Although only some, or none, of these effects, will occur, it is important to have a good understanding of any and all side effects that may result from this medication.

It is important for the patient to speak with their doctor or an emergency medical service urgently should any of these side effects present themselves while taking this medication:

  • Yellow skin and eyes
  • Yellow nails lacking a cuticle
  • White patches in the mouth or on/around the tongue
  • Weakness or heaviness of the legs
  • Vision changes
  • Unusual tiredness or weakness
  • Ulcers on the lips/in the mouth
  • Tremor
  • Tenderness, pain, swelling, warmth, skin discoloration, and prominent superficial veins over affected area
  • Swollen, painful, or tender lymph glands in neck, armpit, or groin
  • Swelling of the arms or legs
  • Sweating
  • Sudden, unexplained shortness of breath
  • Sudden, severe weakness/numbness in the arm or leg
  • Sudden loss of coordination
  • Sudden decrease in the amount of urine
  • Stomach pain or upset
  • Sores or white spots in the mouth
  • Sore throat
  • Slurred speech
  • Skin ulcer or sores
  • Severe, sudden headache
  • Severe vomiting
  • Severe constipation
  • Sensation of pins and needles
  • Runny nose
  • Ringing in the ears
  • Redness, pain, or swelling of the eye
  • Redness or swelling in the ear
  • Red or dark brown urine
  • Rash
  • Rapid heartbeat
  • Puffiness or swelling of the eyelids or the eyes, face, lips, or tongue
  • Prolonged bleeding from cuts
  • Pale skin
  • Pains in the stomach, side or abdomen
  • Painful cold sores or blisters on the lips, nose, eyes, or genitals
  • Pain in the chest, groin, or legs
  • Numbness or tingling around the lips, hands, or feet
  • New mole
  • Nausea or vomiting
  • Nasal congestion
  • Nails loose or detached
  • Muscle pain
  • Mole that leaks fluid or bleeds
  • Loss of voice
  • Loss of sexual ability, desire, drive, or performance
  • Large, hive-like swelling on the face, lips, eyelids, throat, tongue, hands, feet, legs, or sex organs
  • Large, flat, blue, or purplish patches in the skin
  • Lack of appetite
  • Itching, pain, redness, swelling, tenderness, or warmth on the skin
  • Increased menstrual flow or vaginal bleeding
  • Increased hunger
  • Hoarseness
  • Hives or itching
  • Headache
  • General feeling of discomfort or illness
  • Flushing or redness of the skin, especially on the face and neck
  • Fever
  • Fast, slow, or irregular heartbeat
  • Faintness or lightheadedness when standing
  • Facial hair growth in females
  • Eye pain
  • Extreme fatigue
  • Excessive tearing
  • Earache
  • Dry mouth
  • Drowsiness
  • Dizziness
  • Discharge from the eyes
  • Dilated neck veins
  • Difficulty with breathing or swallowing
  • Decreased vision
  • Decreased urine output
  • Deafness
  • Dark or bloody urine
  • Cough
  • Convulsions (seizures)
  • Confusion
  • Chills
  • Chest pain
  • Changes in skin color
  • Change in size, shape, or color of existing mole
  • Change in mental status
  • Burning, tingling, numbness, or pain in hands, arms, feet, or legs
  • Burning, dry, or itching eyes
  • Burning while urinating
  • Burning or stinging of the skin
  • Bruising
  • Bone pain
  • Body aches or pain
  • Blurred vision
  • Bloating
  • Bleeding from the gums or nose
  • Black or red, tarry stools
  • Backache
  • Anxiousness, unexplained
  • Accumulation of pus
  • Abnormal wound healing
  • Abdominal or stomach cramps or pain

Other side effects of Sirolimus can occur that in most cases do not require any form of medical attention. These effects may reduce during treatment as the body continues to adjust to the drug. A medical professional or doctor should be able to advise about methods to reduce or prevent some of these symptoms.

If any of the following conditions carry on longer than expected or are troublesome, it is important to contact your doctor as soon as possible:

  • Abnormal vision
  • Acne
  • 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
  • Constipation
  • Continuing ringing or buzzing or other noise in the ears
  • Cracked, dry, scaly skin
  • Crying
  • Decreased frequency of urination
  • Degenerative disease of the joint
  • Depersonalization
  • Diarrhea
  • Difficulty moving
  • Difficulty passing urine (dribbling)
  • Dysphoria
  • Ear pain
  • Enlarged abdomen/stomach
  • Euphoria
  • Excess air or gassiness
  • Excessive muscle tone, muscle tension or tightness
  • Fear
  • Feeling sad/empty
  • Hearing loss
  • Heartburn
  • Inability to have/keep an erection
  • Increase in heart rate
  • Increased hair growth, especially on the face
  • Increased urge to urinate during the night
  • Indigestion
  • Inflammation, redness, or swelling of the gums/mouth
  • Irritation in the mouth
  • Joint pain and/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
  • 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

In addition to the above side effects, as an immunosuppressant Sirolimus can also cause a reduction of blood cells that help to fight infection - which may lead to serious medical conditions which include but not limited to a severe brain infection, cancer, or a viral infection which can result in failure of a kidney transplant. It is critical that any signs of infection are monitored and identified as soon as possible, at which point the patient's doctor and emergency medical care should be notified.

Signs of infections can include:

  • Fever
  • Chills
  • Body aches

It is critical to let your doctor know if you have suffered from any unusual or allergic reaction to this type medicine or any other types medicines. It is also critical to inform your health care professional if you have other types of allergies, including allergies to foods, preservatives, dyes, or animals.

If the patient is experiencing any of the below symptoms and believes they have taken more of their medication than prescribed, then they may have taken an overdose.

It is critical request emergency medical support as soon as possible if any of the following symptoms are present:

  • Blurred vision
  • Diarrhea
  • Dizziness, faintness, lightheadedness when getting up
  • Indigestion
  • Pain or weakness in the hands or feet
  • Passing of gas
  • Stomach fullness or discomfort
  • Sweating
  • Trembling

Dosage

This medication should be taken exactly as directed by a medical professional. It is essential that the patient should not take more of it, take it more often, or take it for a more extended amount of time than was prescribed. Due to the strength of Sirolimus, each medication dosage is carefully decided by a doctor. Using too much medication can increase the risk of side effects, or using too little can lead to rejection of your transplanted kidney.

Usual Adult Dose for Organ Transplant (Rejection Prophylaxis)

For patients with low to moderate immunologic risk:

Body weight dosing levels:

Weight of less than 40 kg:

  • Loading dose: 3 mg/m2 on the first day
  • Maintenance: 1 mg/m2 once daily

Weight greater than or equal to 40 kg:

  • Loading dose: 6 mg orally on the first day
  • Maintenance: 2 mg orally once daily

For patients at high immunologic risk:

NOTE: these patients are defined as 'Black transplant recipients' and secondary or repeat renal transplant recipients who have lost a previous allograft for an immunologic reason, and patients defined as having high-panel reactive antibodies.

For patients who are receiving sirolimus alongside cyclosporine:

  • Loading Dose: Up to 15 mg on day one post-transplantation
  • Maintenance Dose: Beginning on day two, an initial maintenance dose of 5 mg/day. A trough level should be obtained between days five and seven, and the dosage of Sirolimus should be adjusted after.

Antibody induction therapy may be used. Once the sirolimus maintenance dose is adjusted, patients should continue on the new maintenance dose for at least 7 to 14 days before further dosage adjustment with concentration monitoring.

Usual Adult Dose for Pulmonary Lymphangioleiomyomatosis

  • Initial dose: 2 mg/day

Sirolimus whole blood trough should be measured in 10 to 20 days, with dosage adjustment to maintain levels between 5 and 15 ng/mL.

Usual Pediatric Dose for Organ Transplant - Rejection Prophylaxis

For patients with low-moderate immunologic risk:

Greater than 13 years old:

Body weight dosing levels:

Body weight of less than 40 kg:

  • Loading dose: 3 mg/m2 on first day
  • Maintenance: 1 mg/m2 once daily

Body weight greater than or equal to 40 kg:

  • Loading dose: 6 mg orally on the first day
  • Maintenance: 2 mg orally once daily

To help the patient to remember to take their medicine every time, it is recommended they get into a habit of taking Sirolimus each day at the same time. Doing so will help this medication to work better by maintaining a consistent level in the blood.

This medication can be taken both with or without food. The decision whether to take this medicine with food should be made at the start of treatment, as Sirolimus should then be taken this way for every single dose.

Never stop taking Sirolimus without confirming first with a doctor or medical professional who has full information about the medical situation the patient is in. It is possible that some transplanted patients will need to take this drug for the rest of their life, so the body cannot reject a transplant.

Sirolimus is often used alongside both a corticosteroid and cyclosporine (immunosuppressive agent) medication. When taken with these medicines, Sirolimus should be taken at minimum four hours after taking a cyclosporine modified solution (oral) or after taking cyclosporine modified capsules.

In some cases, when a patient has been taking Sirolimus alongside a cyclosporine medication between 2-4 months after their transplant, their doctor may decide to reduce and eventually stop the usage of cyclosporine, instead of increasing the dosage of Sirolimus. This is not the case for all patients, as those with certain conditions (such as black patients or those with a history of transplant rejection) are likely to need to continue taking cyclosporine as part of their treatment for up to a full year after the transplant.

When taking Sirolimus tablets, they should not be crushed, split or chewed. If the patient is struggling to take the tablet form of this medication, an oral solution is also available as an alternative. This can be discussed and prescribed by a relevant doctor.

Proper use of the oral liquid:

  • Open the bottle of solution and insert adapter tightly into the bottle.
  • Insert amber syringe (plastic needle) that comes with the bottle in order to draw the correct amount of medication from the bottle.
  • Empty the drug from the syringe into either a glass or plastic cup.
  • Mix the measured medicine with at minimum 60ml of water, or of orange juice. The mixture should then be stirred well and drunk immediately.
  • Add at least an additional 120ml of water or orange juice to the mixture, stir well, and consume it to avoid missing or not consuming any of the medication within the solution.
  • If a doctor has informed you that you should carry your medication, you can keep your daily dose of Sirolimus prepared in a tightly-capped syringe for up to 24 hours either at room temperature or inside the refrigerator. Each used syringe should be disposed of after use.

Should this medicine splash onto the skin, wash it with soap and water as soon as possible. If the solution gets in your eyes, you should rinse them with water immediately.

Interactions

Although certain medications shouldn't be used in conjunction at all, in some cases two different incompatible medicines may be used at the same time if the positives outweigh the risks. In all of these cases, it is important the patient discusses their medication with their doctor. When taking Sirolimus, it is especially key that your doctor or medical professional is aware if you are taking any of the drugs listed below or have taken them recently. The below interactions have been listed on the basis of their possible significance and are not all-inclusive of every interaction that may occur.

Using Sirolimus with any of the below medications is not recommended. A doctor may decide not to treat you with this medicine or may even alter some of the other medicines taken based on the usage of any of the following drugs:

  • Voriconazole
  • Ritonavir
  • Posaconazole
  • Mifepristone
  • Amifampridine

Using Sirolimus as a treatment alongside any of the following medications is in most cases not recommended, however, it may be required in some cases. If both of these drugs are prescribed in tandem, your doctor may be required to change the dose or the frequency you use both or one of the medicines.

  • Zofenopril
  • Yellow fever vaccine
  • Vilazodone
  • Venetoclax
  • Varicella virus vaccine
  • Typhoid vaccine
  • Trandolapril
  • Telithromycin
  • Telaprevir
  • Tacrolimus
  • St. John's Wort
  • Smallpox vaccine
  • Simeprevir
  • Secukinumab
  • Saquinavir
  • Rubella virus vaccine, live
  • Rotavirus vaccine, live
  • Rifampin
  • Ribociclib
  • Ramipril
  • Quinapril
  • Poliovirus vaccine, live
  • Pitolisant
  • Phenobarbital
  • Perindopril
  • Pazopanib
  • Mumps virus vaccine, live
  • Moexipril
  • Measles virus vaccine, live
  • Lumacaftor
  • Lisinopril
  • Ketoconazole
  • Itraconazole
  • Isavuconazonium sulfate
  • Influenza virus vaccine, live
  • Infliximab
  • Idelalisib
  • Guselkumab
  • Golimumab
  • Fosinopril
  • Fluconazole
  • Etravirine
  • Enzalutamide
  • Enalaprilat
  • Enalapril
  • Eluxadoline
  • Eliglustat
  • Efavirenz
  • Dronedarone
  • Crizotinib
  • Conivaptan
  • Cobicistat
  • Clarithromycin
  • Ceritinib
  • Captopril
  • Boceprevir
  • Blinatumomab
  • Benazepril
  • Bacillus of calmette and guerin vaccine, live
  • Amiodarone
  • Alefacept
  • Adenovirus vaccine type 7, live
  • Adenovirus vaccine type 4, live

Using Sirolimus at the same time of any of the below drugs can cause an increased risk of certain side effects, but prescription of both drugs may be the best treatment for the patient. If both medications are prescribed at the same time, discussing your medication choices with your doctor may be the best way to find out the right choice for your medical needs.

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

Interactions with Food/Tobacco/Alcohol

Certain medications cannot be used at/around the same time of eating food - or consumption of certain types of food as interactions may occur. In addition, using alcohol or tobacco with certain drugs can also cause interactions, both minor and serious, to occur. The following have been selected on the basis of their possible significance and are not all-inclusive of all possible interactions.

Using Sirolimus with any or all of the following can cause a risk of certain side effects, but taking the medication with the below may be unavoidable in some cases. If taken together regularly, your doctor may need to example your medication, and either correct the dose or how often you use Sirolimus.

  • Grapefruit Juice

Other Medical Problems

The presence of pre-existing or historical medical problems can affect the use of Sirolimus, and the results of the medication. Ensure that you tell your doctor if any of the following medical conditions apply to you, especially:

  • Skin cancer
  • Proteinuria
  • Peripheral edema
  • Lymphoma
  • Lung transplantation
  • Lung disease
  • Liver transplantation
  • Liver disease
  • Infection
  • Hyperlipidemia
  • Heart disease
  • Blood clotting problems
  • Ascites

Warnings

It is critical that your doctor is able to consistently check the progress and medical condition of you or your child at visits both regularly and often to ensure that this medicine is working properly. In addition, blood and urine tests might be required to check on the effects of the medication and how the condition of the patient is progressing.

Based on research, it is suggested that taking this medicine while you are pregnant may harm your unborn baby. It is important to take an effective form of birth control to keep from becoming pregnant, and to keep using it for at least 12 weeks after you stop taking this drug. If you think you have become pregnant during the course of this medicine, inform your doctor as soon as possible.

During the time that you are prescribed Sirolimus, it is critical to maintain an excellent level of dental hygiene and to see a dental professional regularly for cleaning of the teeth.

Both raw oysters and other shellfish can contain bacterias that may result in serious illnesses and even death. This is more likely to be an issue if these items are consumed by people with specific medical conditions, including those taking Sirolimus as a result of organ transplant.

Eating any form of raw shellfish based foods is generally not a problem for most people who are healthy. However, patients with any of the listed conditions may find themselves at higher risk:

  • Stomach problems
  • Organ transplantation
  • Corticosteroid use (long-term)
  • Liver disease
  • Immune disorders
  • Hemochromatosis
  • Excessive alcohol intake
  • Diabetes
  • Cancer

It is important not to eat any oysters/shellfish raw while you are undergoing treatment with Sirolimus. Be careful that oysters and seafood you do eat are fully cooked.

While you under treatment with Sirolimus, and following treatment with this medication, it is critical that you should consult your doctor before agreeing to take any immunizations (vaccinations). Choosing to take any immunizations without seeking the approval of your doctor may result in negative side effects. Sirolimus can act to lower resistance to many kinds of illness in your body, and due to this, there is a greater chance you can receive the form of infection that the immunization is designed to prevent. This is especially true of 'live' vaccines. In addition, any vaccines taken may not protect the patient as well during this time, making the patient still susceptible to disease.

Live vaccines include:

  • Zoster (shingles)
  • Yellow fever
  • Varicella (chickenpox)
  • Typhoid
  • Rubella (MMR)
  • Rotavirus
  • Polio
  • Nasal flu (influenza)
  • Mumps
  • Measles

Other persons who live in the patients' household should be careful to not take the oral polio vaccine, as there is a chance that they could pass the usually benign polio virus on to you. It is important to avoid other persons who may have taken this vaccine. Do not get close to them, and if possible do not remain in the same area with them for a long period. If these precautions cannot be taken, consider using a face mask that is protective and that covers both the nose and the mouth to prevent contraction of illness.

Treatment with Sirolimus can increase the risks of the patient getting other infections. If possible, avoid people who have colds or have had any other infections or illnesses. If you think that you or your child are are coming down with a cold, illness or other infection, inform your doctor as soon as possible.

This drug can also increase the risk of bleeding, as well as cause the delay in wound healing. It is recommended to stay away from any aggressive sports or any other situations that could result in being bruised, cut, or injured. It is important to brush and floss your teeth very carefully. Be careful when in situations that require sharp objects, including knives, razors and fingernail clippers.

Check with a medical professional immediately if either you or your child notice any of the following:

  • Unusual bleeding or bruising
  • Black, tarry stools
  • Blood in the urine or stools
  • Red spots on the skin

Sirolimus can cause serious forms of allergic reactions, especially when taken with certain medicines.

Contact a medical professional immediately if you experience any of the following symptoms after taking Sirolimus:

  • Trouble with breathing
  • Red, swollen skin
  • Large, hive-like swelling on the face, lips, eyelids, throat, tongue, hands, feet, legs, or sex organs
  • Itching
  • Chest tightness

Sirolimus can result in a greater risk of contracting cancer, in particular, skin cancer or cancer in the lymph glands (lymphoma).

The following is recommended when taking this medication:

  • Wear clothing that is protective, including but not limited to a hat and sunglasses
  • Stay out of direct sunlight
  • Do not use a sunlamp, tanning bed or booth
  • Apply a sunblock product that has an SPF of at least 15
  • Apply sunblock lip covering or stick that contains an SPF of at least 15

This medicine can also increase your cholesterol and the fats in the blood. If this occurs, a medical professional can give you some medicines that can lower the level of cholesterol and fats in the blood.

The medication may, in addition, increase the risk of the patient developing a rare and serious virus infection - BK virus-associated nephropathy (BKVAN). This virus can affect how your kidneys work, which can then and cause a transplanted kidney to fail.

Speak to your doctor as soon as you can if any of the following symptoms appear:

  • Weight gain
  • Vomiting
  • Unusual tiredness or weakness
  • Trouble with breathing
  • Swelling of the face, fingers, or lower legs
  • Nausea
  • Lower back or side pain
  • Loss of appetite
  • Increased thirst
  • Bloody urine
  • A decreased frequency or amount of urine

Sirolimus can also increase your risk of contracting a serious/rare brain infection named progressive multifocal leukoencephalopathy (PML).

Check with a medical professional right away if you are having more than one of the following symptoms:

  • Weakness in the legs
  • Vision changes
  • Memory loss
  • Loss of coordination
  • Difficulty speaking or understanding what others say
  • Confusion
  • Clumsiness

If you notice any new moles; including a change in size, color or shape of an existing mole; or a mole that has begun to leak blood or fluid, it's important to contact your doctor as soon as possible.

Storage

Keep this medication out of the reach of all pets and children at all times.

It is important not to keep any outdated medicine or medicine that is no longer needed.

Consult your medical professional on how you should properly dispose of any medicine you do not use.

If taking the oral tablets version of Sirolimus, store the container at room temperature in a, away from heat, moisture, and direct light.

For oral liquid, store this medication in the refrigerator. This medicine should be protected from direct light and moisture. Do not freeze. You can store the oral liquid at room temperature for a small period of time (not more than 15 days). If you can see a light haze or cloudiness within the bottle, leave Sirolimus oral liquid out at room temperature, and shake it until the haze disappears. Throw away any medicine that is unused after 30 days.

If you are using the Sirolimus oral liquid inside a disposable syringe, you can store a prepared and ready syringe in the carrying case you are given. Keep the case with a loaded syringe at consistent room temperature and use the medication inside the syringe within a day or 24 hours. Use each disposable syringe only a single time and then dispose of it appropriately.

Summary

Sirolimus is used with other preventative medications in order to aid the body in accepted a transplanted kidney. This medication is a part of a group of medicines known as immunosuppressive agents.

When a patient receives an organ transplant of any type, the body's white blood cells will actively try to get rid of (reject) the transplanted organ, as it sees the organ as something to be removed from the body. Sirolimus acts to prevent the white blood cells from rejecting the transplanted organ.

Sirolimus is a very strong medicine, and as such is only used in required situations such as for organ transplants. It can cause side effects that can be very serious, which may include brain infections or cancer. It may also reduce the body's ability to fight any infections, and can be particularly dangerous around people who have taken the polio vaccine recently.

Sirolimus is also used in the treatment lymphangioleiomyomatosis, a rare lung disease that affects women of childbearing age as a majority. Though this disorder happens mostly in women, it occurs across all ages and genders and can cause lung tumors that while they are not cancerous, they can negatively affect breathing.

 

Resources
Last Reviewed:
February 01, 2018
Last Updated:
April 27, 2018