Health Guide
Drug Guide

Sirolimus (Oral route)

Pronunciation:

sir-OH-li-mus

Brand Names:

Dosage Forms:

Warnings:

Oral route(Solution;Tablet)

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 for prophylaxis of organ rejection in patients receiving renal transplants, and they should have complete information requisite for the followup 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 was 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 such use is not recommended .

Classifications:

Therapeutic

Immune Suppressant

Uses of This Medicine:

Sirolimus is used together with other medicines to prevent the body from rejecting a transplanted kidney. It belongs to a group of medicines known as immunosuppressive agents.

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.

Sirolimus is also used to treat lymphangioleiomyomatosis, a rare lung disease that affects predominantly women of childbearing age.

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

Before Using This Medicine:

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.

Children

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 for prevention of kidney transplant rejection, and in children for treatment of lymphangioleiomyomatosis. Safety and efficacy have not been established in these age groups.

Older adults

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 and an adjustment in the dose for 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.

Other medicines

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.

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.

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.

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:

Proper Use of This Medicine:

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 a Medication Guide and patient 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 the same way every day. This means take it at the same time and take it consistently, either with or without food.

Do not change your dose or 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 kidney transplant.

Sirolimus is usually used along with a corticosteroid (cortisone-like medicine) and cyclosporine. Sirolimus should be taken 4 hours after cyclosporine modified oral solution 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 (eg, 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.

Swallow the tablet whole. Do not crush, break, or chew it. 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:

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.

You should not eat grapefruit or drink grapefruit juice while you are taking this medicine. Grapefruit and grapefruit juice may cause higher levels of sirolimus in the body. This could result in more unwanted effects.

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.

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 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 While Using This Medicine:

It is very important that your doctor check your or your child's progress 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.

Do not take clarithromycin, erythromycin, itraconazole, ketoconazole, rifabutin, rifampin, telithromycin, or voriconazole while you are being treated with this medicine, unless your doctor tells you to.

Using this medicine may increase your risk of getting skin cancer or cancer of the lymph system (lymphoma). Talk to your doctor if you have concerns about this risk.

This medicine may increase your risk of developing infections. Avoid being near people who are sick while you are using this medicine. Wash your hands often. Tell your doctor if you have any kind of infection before you start using this medicine. Tell your doctor if you have ever had an infection that would not go away or an infection that kept coming back.

Sirolimus may cause serious types of allergic reactions, including anaphylaxis. Anaphylaxis can be life-threatening and requires immediate medical attention. Call your doctor right away if you or your child has a rash, itching, large, hive-like swelling on the face, eyelids, lips, tongue, throat, hands, legs, feet, or sex organs, red, swollen skin, trouble breathing, trouble swallowing, or chest tightness while you are using this medicine.

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.

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 is 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 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.

This medicine may make your skin more sensitive to sunlight and can increase your risk of having skin cancer. Use a sunscreen when you are outdoors and avoid sunlamps and tanning beds.

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 (vaccines) without your doctor's approval. Sirolimus may lower your body's resistance and there is a chance you might get the infection the vaccine is meant to prevent. In addition, you should not be around other persons living in your household who receive live virus vaccines because there is a chance they could pass the virus on to you. Some examples of live vaccines include measles, mumps, influenza (nasal flu vaccine), poliovirus (oral form), rotavirus, and rubella. Do not get close to them and do not stay in the same room with them for very long. If you have questions about this, talk to your doctor.

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.

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.

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 (eg, St. John's wort) or vitamin supplements.

Side Effects of This Medicine:

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
chest pain
chills
confusion
convulsions (seizures)
cough
dark or bloody urine
deafness
decreased urine output
decreased vision
difficulty with breathing or swallowing
dilated neck veins
discharge from the eyes
dizziness
drowsiness
dry mouth
earache
excessive tearing
extreme fatigue
eye pain
facial hair growth in females
faintness or lightheadedness when getting up from lying or sitting position
fast, slow, or irregular heartbeat
fever
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
muscle pain
nasal congestion
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
runny nose
sensation of pins and needles
severe constipation
severe vomiting
severe, sudden headache
slurred speech
sore throat
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
tremor
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
Bloating
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
hives or itching
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
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 unexplained noise in the ears
cracked, dry, or scaly skin
crying
decrease in frequency of urination
degenerative disease of the joint
depersonalization
diarrhea
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
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 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.


Last Updated: 10/12/2016

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