0.5 mg, 1 mg, 2 mg coated tablets sirolimus
What Rapamune is and what it is used for
Rapamune contains the active substance sirolimus, which belongs to a group of medicines called immunosuppressive agents. It helps you keep your body’s immune system under control after a kidney transplant.
Rapamune is used in adults to prevent the body from rejecting a transplanted kidney and is usually combined with the immunosuppressive drugs corticosteroids and at the beginning of treatment (the first 2 to 3 months) with ciclosporin.
Rapamune is also used to treat patients with sporadic lymphangioleiomyomatosis (S-LAM) with moderate to severe lung disease or ongoing deterioration of lung function. S-LAM is a rare and progressive lung disease that mainly affects women of childbearing age. The most common symptom of S-LAM is shortness of breath.
What you need to know before using Rapamune
Do not take Rapamune
if you are allergic to sirolimus or any of the other ingredients of this medicine (listed in section 6).
Warnings and cautions
Talk to your doctor or pharmacist before taking Rapamune
- If you have any liver problems or have had a disease that may have affected your liver, tell your doctor. This may affect the dose of Rapamune prescribed by your doctor and may result in further blood sampling.
- Rapamune, like other immunosuppressive drugs, can lower the body’s ability to fight infections and may increase the risk of developing cancer of the lymph tissue or skin.
- if you have a BMI ( body mass index ) that is higher than 30 kg / m 2, this can affect your wound healing ability.
- if you are considered to be at high risk of rejection of a kidney transplant, for example, if you have previously lost a transplant.
Your doctor will take samples to check the amount of Rapamune in your blood. Your doctor will also take samples to check your kidney function, your blood fat levels ( cholesterol and/or triglycerides ), and possibly your liver function, during treatment with Rapamune.
Due to the increased risk of skin cancer, exposure to sunlight and ultraviolet (UV) light should be limited by wearing protective clothing and using sunscreen with a high sun protection factor.
Children and young people
There is limited experience with the use of Rapamune in children and adolescents under 18 years of age. The use of Rapamune is not recommended in this patient group.
Other medicines and Rapamune
Tell your doctor or pharmacist if you are taking, have recently taken, or might take any other medicines. Some medicines may interfere with the effect of Rapamune and therefore dose adjustment of Rapamune may need to be done. Your doctor or pharmacist must know if you are using any of the following remedies:
- other immunosuppressive agents.
- antibiotics or antifungal agents against infection, e.g. clarithromycin, erythromycin, telithromycin, troleandomycin, rifabutin, clotrimazole, fluconazole, itraconazole. Concomitant use of Rapamune with rifampicin, ketoconazole or voriconazole is not recommended.
- medicines for high blood pressure or heart problems, including nicardipine, verapamil, and diltiazem.
- medicines for epilepsy, including carbamazepine, phenobarbital, and phenytoin.
- medicines used to treat stomach ulcers or other gastrointestinal diseases such as cisapride, cimetidine, and metoclopramide.
- bromocriptine (used to treat Parkinson’s disease and various hormonal disorders), danazol (used to treat gynecological diseases), or protease inhibitors (eg for HIV and hepatitis C such as ritonavir, indinavir, boceprevir, and telaprevir).
- St. John’s wort ( Hypericum perforatum ).
- letermovir (antiviral medicine used to prevent cytomegalovirus diseases ).
Live vaccines should be avoided when Rapamune is used concomitantly. Before vaccination, tell your doctor or pharmacist that you are taking Rapamune.
The use of Rapamune may lead to elevated levels of cholesterol and triglycerides (blood fats) in the blood. This may require treatment. Drugs called statins or fibrates that are used to treat high cholesterol or triglycerides have been linked to an increased risk of muscle breakdown ( rhabdomyolysis ). You should tell your doctor if you are taking medicines to lower your blood fats.
Concomitant use of Rapamune with ACE inhibitors (a type of antihypertensive agent) may cause allergic reactions. Tell your doctor if you are taking other medicines that belong to this group of medicines.
Rapamune with food, drink, and alcohol
Rapamune should be taken consistently either with or without food. If you prefer to take Rapamune with a meal, always take it with a meal. If you prefer to take Rapamune without food, always take it without food. Food can affect the number of drugs that go into the bloodstream, by always taking your medication in the same way the levels of Rapamune in the blood are kept more stable.
Rapamune should not be taken with grapefruit juice.
Pregnancy, breastfeeding, and fertility
Rapamune should only be used during pregnancy if necessary. You must use effective contraception during treatment with Rapamune and 12 weeks after stopping treatment. If you are pregnant or breastfeeding, think you may be pregnant, or are planning to have a baby, ask your doctor or pharmacist for advice before taking this medicine.
It is not known if Rapamune passes into breast milk. Patients taking Rapamune should stop breastfeeding during treatment.
Decreased sperm counts have been associated with the use of Rapamune. This is usually normalized after stopping treatment with Rapamune.
Driving and using machines
Although Rapamune treatment is not expected to affect your ability to drive, you should talk to your doctor if you are unsure.
Rapamune contains lactose and sucrose
Rapamune contains 86.4 mg of lactose and up to 215.8 mg of sucrose. If you have been told by your doctor that you have an intolerance to some sugars, contact your doctor before taking this medicine.
How to take Rapamune
Always take this medicine exactly as your doctor has told you. Ask your doctor or pharmacist if you are unsure.
Your doctor will decide what dose of Rapamune to take and how often to take it. Follow the doctor’s instructions exactly and never change the dose yourself.
Rapamune should only be taken by mouth. The tablets must not be crushed, chewed, or divided. Tell your doctor if you have difficulty taking the tablet.
Several 0.5 mg tablets should not be taken instead of 1 mg or 2 mg tablets as the different strengths are not directly interchangeable.
Rapamune should always be taken with or without food.
Kidney transplantation
Your doctor will give you a starting dose of 6 mg as soon as possible after the kidney transplant. Then you must take 2 mg Rapamune every day until your doctor gives you other instructions. Your dose will be adjusted depending on the levels of Rapamune in your blood. Your doctor may need to take blood samples to measure Rapamune concentrations.
If you are also taking ciclosporin, both medicines should be taken about 4 hours apart.
It is recommended that Rapamune be used first in combination with ciclosporin and corticosteroids. After 3 months, your doctor may discontinue treatment with either Rapamune or ciclosporin, as it is not recommended that these medicines be taken together beyond this period.
Sporadic lymphangioleiomyomatosis (S-LAM)
Your doctor will give you 2 mg of Rapamune every day until your doctor tells you otherwise. Your dose will be adjusted according to how much Rapamune you have in your blood. Your doctor will need to take blood samples to measure your Rapamune concentration.
If you take more Rapamune than you should
If you have taken more medicine than you were prescribed, see a doctor or go to the hospital’s emergency department as soon as possible. Always carry the marked blister pack, even if it is empty.
If you forget to take Rapamune
If you forget to take Rapamune, take it as soon as you remember, but not if it is less than 4 hours until you take ciclosporin. Then continue to take your medication as usual. Do not take a double dose to make up for a forgotten dose, and make sure you always take Rapamune and ciclosporin at about 4-hour intervals. If you forget to take a dose of Rapamune tell your doctor.
If you stop taking Rapamune
Do not stop taking Rapamune unless your doctor tells you to, you can lose the transplant.
If you have any further questions on the use of this product, ask your doctor or pharmacist.
Possible side effects
Like all medicines, this medicine can cause side effects, although not everybody gets them.
Allergic reactions
Contact a doctor immediately if you experience symptoms such as swelling of the face, tongue, and/or throat (back of the mouth) and/or difficulty breathing ( angioedema ) or a severe skin inflammation where the skin is scaly (exfoliative dermatitis ). These may be symptoms of severe allergic reactions.
Kidney damage with low platelet count (thrombocytopenic purpura / hemolytic uremia syndrome)
Rapamune may increase the risk of kidney damage with low platelet counts and low red blood cell counts with or without rash (thrombocytopenic purpura / hemolytic uremia syndrome) when taken at the same time as medicines called calcineurin inhibitors (cyclosporine or tacrolimus). If you experience symptoms such as bruising or rash, changes in the urine or changes in behavior, or other symptoms that are severe, unusual, or long-lasting, contact your doctor.
Infection is
Rapamune reduces the body’s defense mechanisms. In case of infection, therefore, your body’s ability to fight infection will not be as good as usual. Therefore, if you take Rapamune, you may get more infections than usual, such as infections of the skin, mouth, stomach, intestines, lungs, and urinary tract. You should contact your doctor if you experience symptoms that are severe, unusual, or prolonged.
Frequency of side effects
Very common: may affect more than 1 user in 10
- Fluid accumulation around the kidney
- Swelling of the body including hands and feet
- Pain
- Fever
- Headache
- High blood pressure
- Stomach pain, diarrhea, constipation, nausea
- Low red blood cell count, low platelet count
- Elevated levels of fat in the blood ( cholesterol and/or triglycerides ), elevated blood sugar, low potassium levels in the blood, low levels of phosphate in the blood, elevated lactate dehydrogenase protein in the blood, elevated levels of creatinine in the blood
- Joint pain
- Acne
- Urinary tract infection
- Pneumonia and other bacterial, viral, and fungal infections
- Decreased number of anti-infective cells in the blood ( white blood cells )
- Diabetes
- Abnormal liver function tests, elevated AST and/or ALT (liver enzymes)
- Rash
- Elevated protein levels in the urine
- Menstrual disorders (such as missed, irregular, or heavy menstruation)
- Impaired healing ability (this may include rupture of surgical wounds or loosening of surgical stitches)
- Palpitation
- There is a general tendency for fluid to accumulate in various tissues
Common: may affect up to 1 in 10 users
- Infection (including life-threatening infection )
- Blood clots in the legs
- Blood clots in the lungs
- Cold sores
- Fluid accumulation in the abdomen
- Kidney damage with low platelet count and low red blood cell count, with or without skin rash (hemolytic uremia syndrome)
- Low levels of a type of white blood cell called a neutrophil
- Weakening of the bones in the body
- Inflammation that can lead to lung damage, fluid in the alveoli
- Nosebleed
- Skin cancer
- Kidney infection
- Cysts on the ovaries
- Accumulation of fluid in the pericardium, which in some cases can reduce the heart’s ability to pump blood
- Pancreatitis
- Allergic reactions
- Shingles
- Cytomegalovirus infection
Uncommon: may affect up to 1 in 100 people
- Lymphatic cancer (lymphoma / lymphoproliferative disease after transplantation), a combined reduction in the number of red blood cells, white blood cells, and platelets
- Bleeding from the lungs
- Protein in the urine, sometimes in larger amounts associated with side effects such as swelling
- Scarring of the kidneys, which may impair kidney function
- Accumulation of fluid in the tissues due to disturbance in the lymphatic system
- Low platelet count, with or without rash (thrombocytopenic purpura)
- Severe allergic reactions that can lead to flaky skin
- Tuberculosis
- Epstein-Barr virus infection
- Infectious diarrhea with Clostridium difficile
- Serious liver damage
Rare: may affect up to 1 in 1,000 people
- Protein storage in the air sacs of the lungs, can affect breathing
- Severe allergic reactions that may affect the blood vessels (see above for allergic reactions)
Has been reported: occurs in an unknown number of users
- Posterior reversible encephalopathy syndrome is a severe syndrome that affects the nervous system with the following symptoms: headache, nausea, vomiting, confusion, seizures, and loss of vision. If any of these occur together, consult your doctor
S-LAM patients had the same side effects as kidney transplant patients, with the addition of weight loss that can occur in up to 1 in 10 people.
How to store Rapamune
Keep this medicine out of the sight and reach of children.
Use before the expiry date which is stated on the carton after “EXP”: The expiry date refers to the last day of that month.
Do not store above 25 ° C.
Store the blister in the outer carton to protect it from light.
Medicines should not be disposed of via wastewater or household waste. Ask your pharmacist how to dispose of medicines no longer required. These measures will help to protect the environment.
Contents of the pack and other information
Content declaration
The active substance is sirolimus.
Each Rapamune 0.5 mg coated tablet contains 0.5 mg sirolimus.
Each Rapamune 1 mg coated tablet contains 1 mg sirolimus.
Each Rapamune 2 mg tablet contains 2 mg sirolimus.
The other ingredients are:
Tablet core: lactose monohydrate, macrogol, magnesium stearate, talc.
Tablet coating: macrogol, glycerol monooleate, shellac (pharmaceutical glaze), calcium sulfate, microcrystalline cellulose, sucrose, titanium dioxide, poloxamer 188, α-tocopherol, povidone, carnauba wax, printing ink (shellac, red iron oxide, propylene glycol one (E20) ammonium glycol (ammonia). The strengths 0.5 mg and 2 mg also contain yellow iron oxide (E172) and brown iron oxide (E172).
What the medicine looks like and the contents of the pack
Rapamune 0.5 mg is supplied as light brown, triangular-coated tablets marked “RAPAMUNE 0.5 mg” on one side.
Rapamune 1 mg is supplied as white, triangular-coated tablets marked “RAPAMUNE 1 mg” on one side.
Rapamune 2 mg is supplied as yellow-beige, triangular-coated tablets marked “RAPAMUNE 2 mg” on one side.
The tablets are supplied in blister packs of 30 and 100 tablets. Not all pack sizes may be marketed.
Marketing Authorization Holder and Manufacturer
Marketing Authorisation Holder:
Pfizer Europe MA EEIG
Boulevard de la Plaine 17
1050 Brussels
Belgium
Manufacturer:
Pfizer Ireland Pharmaceuticals
Little Connell
Newbridge
Co. Kildare
Ireland
Pfizer Manufacturing Deutschland GmbH
Operating office Freiburg
Mooswaldallee 1
79090 Freiburg
Germany
For any information about this medicinal product, please contact the local representative of the Marketing Authorization Holder.
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