SIROLIMUS (Systemic)
Some commonly used brand names are:
In the U.S.?
In Canada?
Another commonly used name is Rapamycin.
Category
Description
Sirolimus (sir-OH-li-mus) belongs toa group of medicines known as immunosuppressive agents. It is used to lowerthe body's natural immunity in patients who receive kidney transplants.
When a patient receives an organ transplant, the body's white blood cellswill try to get rid of (reject) the transplanted organ. Sirolimus works bypreventing the white blood cells from getting rid of the transplanted organ.
Sirolimus is a very strong medicine. It can cause side effects that canbe very serious, such as kidney problems. It may also reduce the body's abilityto fight infections. You and your doctor should talk about the good this medicinewill do as well as the risks of using it.
Sirolimus is available only with your doctor's prescription, in the followingdosage forms:
Oral- Oral solution (U.S. and Canada)
- Tablets (U.S.)
Before Using This Medicine
In deciding to use a medicine, therisks of taking the medicine must be weighed against the good it will do.This is a decision you and your doctor will make. For sirolimus, the followingshould be considered:
Allergies?Tell your doctor if you have ever had any unusual or allergicreaction to sirolimus. Also tell your health care professional if you areallergic to any other substances, such as foods, preservatives, or dyes.
Pregnancy?Sirolimus has not been studied in pregnant women. However, studiesin animals have shown that sirolimus causes problems in the fetus. It is veryimportant that an effective form of birth control be used before startingsirolimus therapy, during sirolimus therapy, and for 12 weeks after sirolimustherapy has stopped.
Breast-feeding?It is not known whether sirolimus passes into human breastmilk. However, because this medicine may cause serious side effects, breast-feedingmay not be recommended while you are receiving it. Discuss with your doctorwhether or not you should breast-feed while you are receiving sirolimus.
Other medicines?Although certainmedicines should not be used together at all, in other cases two differentmedicines may be used together even if an interaction might occur. In thesecases, your doctor may want to change the dose, or other precautions may benecessary. When you are taking sirolimus, it is especially important thatyour health care professional knows if you are taking any of the following:
- Carbamazepine (e.g., Tegretol) or
- Rifabutin (e.g., Mycobutin) or
- Rifampin (e.g., Rifadin) or
- Rifapentine (e.g., Priftin)
- St. John's wort?May decrease the effects of sirolimus by decreasingthe amount of sirolimus in the body
- Clarithromycin (e.g., Biaxin) or
- Cyclosporine (e.g. Neoral or Sandimmune) or
- Diltiazem (e.g., Cardizem) or
- Erythromycin (e.g., Akne-Mycin, Ery-Tab) or
- Itraconazole (e.g., Sporanox) or
- Ketoconazole (e.g., Nizoral)
- Telithromycin (e.g., Ketek) or
- Verapamil (e.g., Calan SR, Isoptin, Verelan) or
- Voriconazole (e.g., VFEND)?May increase the effects of sirolimusby increasing the amount of this medicine in the body
- Tacrolimus (e.g. Prograf)?May cause liver transplant rejectionor serious side effects in patients on sirolimus
Other medical problems?The presence of other medical problems may affect the use of sirolimus.Make sure you tell your doctor if you have any other medical problems, especially:
- Cancer or
- Hyperlipidemia (high amount of cholesterol and fats in the blood)?Sirolimuscan make these conditions worse
- Chickenpox (including recent exposure) or
- Herpes zoster (shingles)?Risk of severe disease affecting otherparts of the body
- Infection?Sirolimus decreases the body's ability to fight infection
- Liver disease?A lower dose of sirolimus may be needed in patientswith this condition
- Liver transplantation or
- Lung transplantation?Sirolimus is not recommended in liveror lung transplant patients
Proper Use of This Medicine
This medicine usually comes with patient informationor directions. Read them carefully and make sure you understand them beforetaking this medicine. If you have any questions, ask your health careprofessional.
Take this medicine only as directed by your doctor. Do not use more or less of it, and do not use it more often than yourdoctor ordered. The exact amount of medicine you need has been carefully workedout. Using too much will increase the risk of side effects, while using toolittle may lead to rejection of your transplanted kidney.
To help you remember to take your medicine, try to get into the habit oftaking it at the same time each day. This will help sirolimus work betterby keeping a constant amount in the blood.
Absorption of this medicine may be changed if you change your diet. Thismedicine should be taken consistently with respect to meals. You should notchange the type or amount of food you eat unless you discuss it with yourhealth care professional.
Do not stop taking this medicine without first checkingwith your doctor. You may have to take this medicine for the rest ofyour life to prevent your body from rejecting the transplant.
Sirolimus usually is used along with a corticosteroid (cortisone-like medicine)and cyclosporine (another immunosuppressive agent). Sirolimus should be taken4 hours after cyclosporine modified oral solution (Neoral) or cyclosporine modified capsules (Neoral).If you have any questions about this, ask your health care professional.
Mix sirolimus oral solution with at least 2 ounces (1/4 cup, 60 milliliters[mL]) of water or orange juice in a glass or plastic container. Stir the mixturewell and drink it immediately. Then, rinse the container with at least 4 ounces(1/2 cup, 120 mL) of additional water or orange juice, stir it well,and drink it to make sure that all of the medicine is taken.
Check with your doctor before you stop using cyclosporine when you havebeen taking sirolimus together with cyclosporine for 4 months after your transplant.Your doctor will tell you if you need to keep taking cyclosporine.
Dosing?The dose of sirolimuswill be different for different patients. Follow yourdoctor's orders or the directions on the label. The following informationincludes only the average doses of sirolimus. If yourdose is different, do not change it unless your doctor tells you to do so. If you have any questions about the proper dose of sirolimus, askyour doctor.
- For oral dosage form (oral solution ortablets):
- Adults and children 13 years of age and older weighing 88 pounds(40 kilograms) or more: The usual dose is 2 milligrams (mg) a day after aninitial one-time dose of 6 mg.
- For children 13 years of age and older who weigh less than 88 pounds(40 kilograms): The dose is based on body size. It is usually 1 mg per squaremeter of body surface area once a day after an initial one-time dose of 3mg per square meter of body surface area.
- For children up to 13 years of age: Use and dose must be determinedby your doctor.
Missed dose?If you miss a dose of sirolimus and remember it within 12hours, take the missed dose as soon as you remember. However, if it is almosttime for the next dose, skip the missed dose, go back to your regular dosingschedule, and check with your doctor. Do not double doses.
Storage?To store this medicine:
- Keep out of the reach of children.
- Store the oral liquid form in the refrigerator.
- Store tablets at room temperature.
- Protect from exposure to light.
- Keep the medicine from freezing.
- Do not keep outdated medicine or medicine no longer needed. Ask yourhealth care professional how you should dispose of any medicine you do notuse. Be sure that any discarded medicine is out of the reach of children.
Precautions While Using This Medicine
It is very important that your doctor check your progressat regular visits to make sure that this medicine is working properlyand to check for unwanted effects.
While you are taking sirolimus, it is important to maintain good dentalhygiene and see a dentist regularly for teeth cleaning.
Raw oysters or other shellfish may contain bacteriathat can cause serious illness and possibly death. This is more likely tobe a problem if these foods are eaten by patients with certain medical conditions. Even eating oysters from ?clean? water or good restaurantsdoes not guarantee that the oysters do not contain the bacteria. Eating rawshellfish is not a problem for most healthy people; however, patients withthe 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), excessalcohol intake (2 to 3 drinks or more per day), diabetes, stomach problems(including stomach surgery and low stomach acid), and hemochromatosis (aniron disorder). Do not eat raw oysters or other shellfishwhile you are taking sirolimus. Be sure oysters and shellfish are fully cooked.
While you are being treated with sirolimus, and after you stop treatmentwith it, it is important to see your doctor about theimmunizations (vaccinations) you should receive. Do not get any immunizationswithout your doctor's approval. Sirolimus may lower your body's resistanceand there is a chance you might get the infection the immunization is meantto prevent. In addition, other persons living in your household should nottake or have recently taken oral polio vaccine since there is a chance theycould pass the polio virus on to you. Also, avoid other persons who have takenthe oral polio vaccine. Do not get close to them, and do not stay in the sameroom with them for very long. If you cannot take these precautions, you shouldconsider wearing a protective face mask that covers the nose and mouth.
Treatment with sirolimus may also increase the chance of getting otherinfections. If you can, avoid people with colds or other infections. If youthink you are getting a cold or other infection, check with your doctor.
Grapefruits and grapefruit juice may increase the effects of sirolimusby increasing the amount of this medicine in your body. You should not eat grapefruit or drink grapefruit juice while you taking thismedicine.
Sirolimus may cause you to have a greater risk for getting skin cancer.When you begin taking this medicine:
- Stay out of direct sunlight, especially between the hours of 10:00a.m. and 3:00 p.m., if possible.
- Wear protective clothing, including a hat. Also, wear sunglasses
- Apply a sun block product that has a skin protection factor (SPF)of at least 15. Some patients may require a product with a higher SPF number,especially if they have a fair complexion. If you have any questions aboutthis, check with your health care professional.
- Apply a sun block lipstick that has an SPF of at least 15 to protectyour lips
- Do not use a sunlamp or tanning bed or booth.
Check with your doctor right away if you notice a new mole;a change in size, shape or color of an existing mole; or a mole that leaksfluid or bleeds.
Side Effects of This Medicine
Along with its needed effects, a medicine may cause someunwanted effects. Although not all of these side effects may occur, if theydo occur they may need medical attention.
Also, because of the way sirolimus acts on the body, there is a chancethat it may cause effects that may not occur until years after the medicineis used. These delayed effects may include certain types of cancer, such aslymphoma.
More common
Abdominal cramps or pain; accumulationof pus; anxiousness, unexplained; backache; bleeding from gums or nose; blindness; bloody or cloudy urine; blue lips and fingernails; blurred vision; body aches or pain; bonepain; bruising; burningwhile urinating; burning, dry, or itching eyes; burning or stinging of skin; burning,tingling, numbness, or pain in the hands, arms, feet, or legs; change in mental status; changes inskin color; chills; coldhands and feet; cold sweats; confusion; convulsions (seizures); cough; cough producing mucus; cough that sometimes produces a pink frothysputum; coughing up blood; dark or bloody urine; deafness; decreased urge to urinate; decreased urine output; decreased vision; difficult,fast, noisy breathing sometimes with wheezing; difficultyin breathing or swallowing; difficulty speaking; dilated neck veins; discharge from eye; dizziness; drowsiness; dry mouth; ear congestion; earache; excessive tearing; extreme fatigue; eye pain; facial hair growth in females; fainting; faintness or lightheadedness when gettingup from lying or sitting position; fast, slow, orirregular heartbeat; fatigue; feeling faint; feeling of warmth or heat; fever; flushed, dry skin; flushing or redness of skin, especially on face and neck; fractures; frequent urge to urinate; fruit-like breath odor; full or round face, neck, or trunk; increased menstrualflow or vaginal bleeding; increased hunger; increased sweating; increased thirst; increased urination; irregular breathing; irritability; itching, pain, redness, swelling, tenderness, warmth on skin; lab results that show problems with liver; large, flat, blue or purplish patches in the skin; lightheadedness; lack or loss of appetite; loss of consciousness; loss of sexualability, desire, drive, or performance; loss of voice; lower back or side pain; lump in abdomen; menstrual irregularities; mood changes; muscle cramps in hands,arms, feet, legs, or face; muscle pain; muscle wasting; nasal congestion; nausea or vomiting; noisy breathing; numbness or tingling around lips, hands, or feet; pain in chest, groin, or legs, especially the calves; pain, tenderness, swelling of foot or leg; painful blisters on trunk of body; painful cold sores or blisters on lips, nose, eyes, or genitals; painful or difficult urination; paleskin; paralysis; pinpointred spots on skin; pounding or racing heartbeat orpulse; prolonged bleeding from cuts; pus in urine; rapid heartbeat; rapid, shallow breathing; rash; red or dark brown urine; redness orswelling in ear; redness, pain, swelling of eye,eyelid, or inner lining of eyelid; ringing in theears; runny nose; sensationof pins and needles; severe constipation; severe vomiting; severe, sudden headache; slurred speech; sneezing; sore mouth or tongue; sore throat; sores or white spots on lips or in mouth; stabbing pain; stomachpain or upset; stomachache; sudden decrease in amount of urine; sudden loss ofcoordination; sudden, severe weakness or numbnessin arm or leg; sudden, unexplained shortness of breath; sweating; swelling offace, fingers, hands, ankles, feet, or lower legs; swollen glands; swollen, painful or tender lymphglands in neck, armpit, or groin; swollen, red, tenderarea of infection; tenderness, pain, swelling, warmth,skin discoloration, and prominent superficial veins over affected area; tightness in chest; tiredness; tremor; trouble breathing; ulcers on lips or in mouth; unusualbleeding or bruising; unusual tiredness or weakness; vision changes; weakness; weakness or heaviness of legs; weight gain; wheezing; white patches in mouth and/or on tongue
Less common
Bloating; change is size, shape or colorof existing mole; darkened urine; hoarseness; mole that leaks fluid or bleeds; new mole; pains in stomach, side orabdomen, possibly radiating to the back; skin ulceror soresRare
Weight gain, unusualUnknown frequency
Abnormal wound healing; hives; itching; large, hive-like swelling onface, eyelids, lips, tongue, throat, hands, legs, feet, sex organs; nails loose or detached; puffiness orswelling of the eyelids or around the eyes, face, lips, or tongue; swelling of arms or legs; troubled breathing; yellow nails lacking a cuticleOther side effects may occur that usually donot need medical attention. These side effects may go away during treatmentas your body adjusts to the medicine. However, check with your doctor if anyof the following side effects continue or are bothersome:
More common
Abdomen enlarged; abnormal vision; acne; belching; blistering, crusting, irritation, itching, or reddening of skin; bloated full feeling; burning feelingin chest or stomach; burning, crawling, itching,numbness, prickling, "pins and needles" or tingling feeling; constipation; continuing ring or buzzingor other unexplained noise in ears; cracked, dry,scaly skin; crying; decreasein frequency of urination; decrease in height; decreased interest in sexual intercourse; degenerative disease of the joint; depersonalization; diarrhea; difficulty inmoving; difficulty in passing urine [dribbling]; discouragement; dysphoria; ear pain; euphoria; excess air or gas in stomach or intestines; excessivemuscle tone, muscle tension or tightness; fear; feeling sad or empty; headache; hearing loss; heartburn; inability to have or keep an erection; increase in heart rate; increased hair growth, especiallyon the face; increased urge to urinate during thenight; indigestion; irritationin mouth; itching skin; joint pain or swelling; kidney pain; leg cramps; loss of bladder control; loss of energy or weakness; loss of interest or pleasure; loss of strength; lower abdominal pain; mental depression; muscle aches, pain, stiffness,or weakness; nervousness; pain; pain in back, ribs, arms, or legs; pain or burning in throat; pain or tendernessaround eyes and cheekbones; paranoia; passing gas; pelvic pain; quick to react or overreact emotionally; rapid breathing; rapidly changing moods; inflammation, redness, or swelling of gums or mouth; shaking or trembling; shivering; sleepiness; sunken eyes; swelling; swelling of the scrotum; tender, or enlarged gums; tendernessin stomach area; thickening of the skin; trouble concentrating; trouble in sleeping; waking to urinate at night; wrinkled skin
Other sideeffects not listed above may also occur in some patients. If you notice anyother effects, check with your doctor.
Developed: 04/20/2000
Revised: 04/19/2006
