Bula do remedy Rapamune

the package insert of the medicine Rapamune. Therapeutic class of Immunosuppressive agents. Active principles Sirolimo.

what For?

Rapamune drágea is indicated for prevention of organ rejection in transplanted kidney.

it is Recommended that it be used initially in treatment regimens with cyclosporine and corticosteroids.

Use adult and children above 13 years old – oral Use

Dosage

How to use?

Patients with Immunological Risk Low to Moderate

    the

  • Therapy with Rapamune) combined with cyclosporine:

In recipients of a first kidney transplant, one should administer a dose of attack of the Rapamune of 6 mg, a single time, followed by maintenance dose of 2 mg per day, daily, along with cyclosporine and steroids, two drugs that are used in accordance with the patient’s physician.

in These patients, cyclosporine can be taken between 2 and 4 months after renal transplantation in patients with immunological risk low to moderate and the dose of Rapamune should be increased according to the patient’s physician.

    the

  • Rapamune following withdrawal of cyclosporin – Referred to as the Maintenance Scheme of Rapamune:

Initially, patients should receive a therapy Rapamune in association with cyclosporine.

Between 1 and 4 months after transplantation, cyclosporine should be progressively discontinued over 4 to 8 weeks and the dose should be adjusted in order to obtain levels of concentrations minimum in whole blood.

The doctor of the patient should, at his discretion, adjust these doses.

High-Risk Patients Immune

    the

  • Therapy with Rapamune in combination:

it is recommended that Rapamune be used in association with tacrolimo and corticosteroids in the first year after transplant in high-risk patients.

For patients receiving Rapamune with tacrolimo, therapy with Rapamune should be initiated with a dose of attack of up to 10 mg on days 1 and 2 after transplantation.

With the beginning on day 3, a dose initial maintenance of 5 mg/day should be administered.

For patients receiving Rapamune with cyclosporine: a therapy with Rapamune should be initiated with a dose of attack of up to 15 mg on day 1 after the transplant.

With the beginning on day 2, a maintenance dose initial 5 mg/day should be administered.

it is Recommended that Rapamune be taken 4 hours after administration of cyclosporine.

This medicine can not be broken, opened or chewed.

Pharmacokinetics

How it works?

The sirolimo is an immunosuppressant (drug that inhibits the immune system) that, unlike other immunosuppressants, inhibits cell proliferation and antibody production.

The sirolimo binds to a protein called mTOR (Mammalian Target of Rapamycin), inhibiting its activity, and thus suppressing the proliferation of cells.

The time for the medicine to reach the maximum concentration in the blood is approximately 3 hours.

Side Effects

What are the evils that can cause me?

Like other medicines, Rapamune can have adverse effects.

However, since Rapamune is taken in combination with other medicines, adverse effects cannot always be attributed, with absolute certainty, to Rapamune.

Reaction very common: linfocele; swelling in the extremities of the body; fever, headache, hypertension (high blood pressure), abdominal pain; diarrhoea, constipation, nausea, particularly at higher doses: anaemia, decrease of cells coagulation of the blood – platelet count, hypertriglyceridemia (hiperlipemia); high cholesterol level; hipofosfatemia; hyperglycemia; hypokalemia (amount of potassium in the blood low); increase of the enzyme lactic (DHL); increase in creatinine (substance excreted in the urine which increase in the blood indicates that there is some problem in the functioning of the kidneys), arthralgia (joint pain), acne, urinary tract infection.

common Reaction: healing of wound abnormal; swelling; fungal infections, viral and bacterial; herpes simplex; sepsis, acceleration of the heartbeat; thromboembolism (the removal of blood clots from the blood vessels), venous (including pulmonary embolism – clogging a vein in the lung by a blood clot, deep vein thrombosis – the formation of a blood clot in a deep vein), stomatitis (inflammation of the mucous membrane of the mouth), ascites, leukopenia (reduction of the defense cells in the blood); decrease of a cell type of defense in the blood – neutrophils; purpura (spots caused by extravasation of blood into the skin) trombocitopênica thrombotic (obstruction of some type of vein or artery)/syndrome urêmica haemolytic anaemia, changes in liver function tests; aumentoda SGOT, increased SGPT (liver enzymes), accumulation of fluid, necrosis of bone (death of cells of the bone), nasal bleeding; pleural effusion; pneumonia; pneumonitis, rash (skin lesion), squamous cell carcinoma,carcinoma basal cell, pyelonephritis, proteinuria (increased protein in the urine/elimination of proteins in the urine), ovarian cysts, menstrual disorders (including amenorrhea – absence of menstruation and menorrhagia – menstruation long or intense).

Reaction uncommon: pericardial effusion (including hemodynamically significant effusions in children and adults), inflammation of the pancreas, lymphoma (cancer that originates in the lymph nodes: lymph nodes)/disorder linfoproliferativo post-transplant pancytopenia (decrease of all blood cells), hemorrhage (excessive loss of blood) in lung, melanoma, and nephrotic syndrome.

Reaction rare: lymphoedema, hypersensitivity reactions (allergic reaction), including anaphylactic reactions/anafilactoides (severe allergic reactions), swelling of the deeper parts of the skin or the mucosa, usually allergic in origin and vasculitis (inflammation of the wall of a blood vessel) hypersensitivity, have been associated with the administration of sirolimo, proteinose alveolar, exfoliative dermatitis (peeling of skin).

Contraindications

When should I not use?

Rapamune is contraindicated to persons with a known allergy to any of its components.

This medicine is contraindicated for children under 13 years of age.

Warnings and Precautions

what should I know before using?

Tell your doctor if you have or have had liver problems or any disease that may have affected this body, as this can change the dose of Rapamune.

The immunosuppression may cause increased susceptibility to infection and possible development of lymphoma.

Only physicians experienced in immunosuppressive therapy and in the treatment of transplant patients kidney should use Rapamune.

The physician responsible for maintenance therapy should have all the information necessary for the monitoring of the patient.

The immunosuppressive drugs might decrease the defense capacity of your body and can increase the risk of developing cancer of the lymphoid or skin.

patients should be advised that exposure to sun light and UV rays should only be done if they are wearing clothes that would protect them and if they are using a sunscreen with a high protection factor because of the increased risk of skin cancer.

Yet no studies have been conducted of the effects on ability to drive and operate machinery.

Therefore, the patients in the use of Rapamune should be advised to not drive vehicles or operate machinery.

Rapamune in pregnancy: tell your doctor the occurrence of pregnancy during treatment or after its completion. Inform your
doctor if you are breast-feeding.

it Is necessary to use effective method of contraception before the start, during and for 12 weeks after the end of treatment with Rapamune. In case of doubt, consult your doctor.

Drug Interactions

it is Not recommended the concomitant administration of Rapamune with inhibitors potent as ketoconazole, voriconazole, itraconazole, telithromycin or clarithromycin or inducers such as rifampin or rifabutin.

were Not observed in studies carried out on significant interactions of sirolimo with: acyclovir, atorvastatin, digoxin, glibenclamide (glyburide), nifedipine 0.3 mg norgestrel/0,03 mg ethinyl estradiol, methylprednisolone, sulfamethoxazole/trimetroprima and tacrolimo.

The immunosuppressive drugs can impair the response to vaccination.

During treatment with immunosuppressants, including Rapamune, vaccination may be less effective.

you Should avoid the administration of vaccines with live, attenuated microorganisms during treatment with Rapamune.

Among the examples of this type of vaccine are: measles, mumps, rubella, polio oral, BCG, yellow fever, varicella and typhoid attenuated.

The concomitant ingestion of food changes the bioavailability of the sirolimo after the administration of Rapamune tablets.

Therefore, you should opt for the administration of Rapamune consistently, either with or without food to minimize variability in the blood level.

The juice of grapefruit (grapefruit) reduces the metabolism of the drug mediated by CYP3A4 and potentially increase the contrafluxo of the drug of the enterócitos of the small intestine mediated by P-gp.

This juice should not be administered with Rapamune tablets.

Overdose

what to do if someone use a larger amount than is recommended?

If you have taken more Rapamune than you should, csee your doctor or go to a hospital immediately.

always Take with you the medicine bottle, even if it is empty.

experience with overdosage is limited.

In general, adverse effects of overdose are consistent with those mentioned in item – What are the evils that this drug can cause me?

Should be followed in the conduct of general support in all cases of overdosage.

based on the low water solubility and high binding rate of the sirolimo the erythrocytes and bound to plasma proteins, it is expected that the sirolimo is not dialyzable in significant amount.

what should I do when I forget to use this medicine?

If you forget to take Rapamune, take it as soon as you remember, unless you need to take your dose of cyclosporine during the next 4 hours.

in This case, do not take the missed dose of Rapamune but continue to take your medications as usual.

do Not take a double dose to make up for a missed dose, and always take Rapamune and cyclosporin with an interval of approximately 4 hours.