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► Afinitor (everolimus) - Medycyna Praktyczna

Afinitor (everolimus) - tablets

The name of the preparation Character; dose; package Manufacturer Price 100% Price after refund In which pharmacy?
Afinitor tablets; 10 mg; 30 tabl. Novartis Europharm b / d Check
Afinitor tablets; 5 mg; 30 tabl. Novartis Europharm b / d Check

Note: reimbursed drug prices are in line with the regulations in force from July 1, 2018.

The preparation contains the substance:everolimus

Prescription drug for proprietary use

What is Afinitor?

It is a medicine used in the treatment of cancer.

What does Afinitor contain and how does it work?

The active substance is everolimus, an anti-cancer drug from the group of protein kinase inhibitors. Protein kinases are enzymes that phosphorylate other proteins in the cell and thereby regulate their activity. In normal cells, the activity of protein kinases is strictly regulated, while in cancer cells it often gets out of control and is excessive. This causes disturbances in the functioning of many cellular pathways, and consequently leads to increased cell division and uncontrolled tumor growth. Inhibition, i.e. inhibition of excessive protein kinase activity, is the therapeutic target of the group of anticancer drugs in question. Everolimus inhibits mTOR protein kinase activity. This kinase not only controls cell division but also controls the synthesis of HIF transcription factors regulating the ability of the tumor to adapt to oxygen deficiency conditions and to the production of the factor responsible for the formation of tumor vasculature (vascular endothelial growth factor VEGF). Inhibition of mTOR kinase activity by everolimus not only limits the division of tumor cells but also reduces the level of HIF and VEGF proteins in the tumor or its environment which inhibits the development of tumor vasculature (anti-angiogenic effect). Used in the treatment of renal cell carcinoma.

When to use Afinitor?

The preparation is indicated for the treatment of patients with advanced renal cell carcinoma, whose disease progression occurred during or after anti-VEGF therapy (against the factor of vascular endothelial growth).

When not to use this preparation?

Unfortunately, even if there are indications to use the preparation, it can not always be used. You can not use the preparation if you are allergic (you are hypersensitive) to any of the ingredients of the preparation or to derivatives of rapamycin (sirolimus). Do not use during pregnancy. The use of the preparation is contraindicated during breast-feeding.

When should you use extreme caution when using Afinitor?

Certain diseases and other circumstances may constitute a contraindication to use or indication to change the dosage of the preparation. In certain situations, it may be necessary to carry out specific check-ups. Treatment may only be conducted under the supervision of an oncologist who has experience in the use of anticancer medicines.
Before and during the treatment, your doctor will prescribe lung X-ray examinations. The use of the preparation is associated with the risk of interstitial pneumonia or other forms of non-infectious pneumonia (non-infectious forms). Interstitial pneumonitis can be severe and in some cases can lead to death. Symptoms may include: shortness of breath, cough, fever, pleural effusion, hypoxia. If new or worsening respiratory symptoms occur, please consult your doctor immediately.Sometimes the severity of symptoms may require discontinuation of the preparation and treatment with corticosteroid s.
The preparation has an immunosuppressive effect, which means that it inhibits the immune response of the body. Therefore, the risk of bacterial, viral, fungal or protozoal infections, including opportunistic infections, increases. Infections may be local or systemic. Some of them may have a severe course and can lead to death. Before starting treatment, all existing infections should be cured. Any symptoms suggestive of infection should be immediately consulted with a doctor who will recommend appropriate treatment and if necessary discontinue administration.
The preparation may cause hypersensitivity reactions, including life-threatening Anaphylactic reactions . Symptoms may include: flushing, redness of the face, chest pain, shortness of breath, angioneurotic edema (swelling of the tongue, swelling of the airways that impede breathing). If you experience the first symptoms of the above hypersensitivity reactions, seek medical attention immediately.
The preparation may cause ulcers and oral inflammation. Local treatment is recommended; do not use mouthwash containing alcohol or hydrogen peroxide because they can exacerbate the symptoms. Antifungal drugs can only be used on the order of a doctor and only if a fungal infection has been diagnosed.
Your doctor will recommend periodic tests of kidney function, including blood urea and creatinine. The preparation may cause kidney problems, which may be supported by a decrease in the rate of creatinine excretion and its elevated concentration in the blood.
Your doctor will recommend regular blood Glucose tests (on an empty stomach). Treatment may lead to increased blood glucose which may require the use of antidiabetic agents (insulin or other hypoglycaemic agents). The first symptoms of an increase in blood glucose may be an increased thirst or an increase in urine volume and frequency of donation. If the above symptoms occur, please consult your doctor immediately.
Your doctor will prescribe a blood lipid control test before and during your treatment. During the treatment period, increased levels of triglycerides and cholesterol in the blood (hyperlipidemia, hypercholesterolemia) may occur, which may require appropriate treatment.
Your doctor will recommend regular haematological tests during your treatment because there is a risk of neutropenia (decreased neutrophil counts), lymphopenia (decreased lymphocyte counts), anemia and thrombocytopenia. Patients with thrombocytopenia are more likely to have haemorrhages (eg nosebleeds).
Hepatic impairment may increase exposure to everolimus. The preparation should not be used in patients with severe hepatic impairment.
Patients who are preparing for a major surgical procedure or in the perioperative period should be cautious, due to possible adverse effects of the preparation on the wound healing process. You should consult a doctor who will decide whether to stop treatment and possibly specify the time of cessation and the time to restart the treatment.
During the treatment period, the use of vaccines containing live microorganisms should be avoided, due to the risk of developing a serious vaccine reaction. Vaccination with other vaccines may be less effective due to the weakened immune response.
The use of preparations that strongly stimulate or inhibit the activity of the cytochrome P450 3A4 isoenzyme or P-glycoprotein (see below, where drug interactions with other drugs are discussed) should be avoided as they can cause a dramatic change in the concentration of everolimus and its metabolites in the blood.
The preparation may cause fertility problems. The preparation used during pregnancy may be toxic to the fetus and may cause birth defects in newborn babies.
Persons being treated with the preparation (both men and women) should absolutely consult a doctor about the use of effective contraception to prevent pregnancy during the treatment period.
Additional information about the other ingredients of the preparation:
The preparation contains lactose; people with galactose intolerance, lactase deficiency or malabsorption of glucose-galactose should not use this preparation.

Does this preparation affect the ability to drive vehicles?
No studies on the effects on the ability to drive and use machines / machines have been performed. Be cautious, especially if you feel tired during treatment.

Dosage of Afinitor

The preparation is in the form of tablets for oral use. The product should be taken at the same time of the day, regardless of the meal. The tablet should be swallowed whole (without chewing, breaking, chewing, etc.) with a glass of water. If you have any doubts regarding the use of the preparation, consult a physician. The doctor will select the dosage and determine the duration of treatment individually, depending on the indication and clinical situation. During the treatment, the doctor will adjust the dosage depending on the response to treatment and the severity of side effects.
Adults. 10 mg once daily, in case of severe or difficult to tolerate side effects your doctor may reduce the dose to 5 mg daily or treatment temporarily discontinued (eg for a week).
There is no data on the use of the preparation in children and adolescents under 18 years of age.
Elderly patients do not need to change their dosage.
There is no need to adjust the dose in patients with renal impairment. In patients with moderate hepatic impairment, the doctor will reduce the dose accordingly (usually up to 5 mg daily). There are no data on the use of this preparation in people with severe hepatic impairment and its use is not recommended in these patients.

Can Afinitor be used during pregnancy and breastfeeding?

During pregnancy, do not use any medicine without consulting your doctor!
It is very important that before using any medicine during pregnancy or breastfeeding, consult a physician and explain beyond any doubt the potential risks and benefits associated with the use of the drug. If you are pregnant or plan to become pregnant, please inform the doctor prescribing the prescription for this medicine. See also the warnings in the section "Take special care with the preparation?"
The preparation should not be used during pregnancy. The use of the preparation may pose a threat to the fetus.
The preparation is contraindicated during breast-feeding.

Can I use other preparations in parallel?

Tell your doctor about all medicines you have recently taken, including those that are over the counter.
Everolimus is metabolised by the cytochrome P450 3A4 isoenzyme and therefore preparations that strongly inhibit the activity of this isoenzyme (such as ketoconazole, posaconazole, itraconazol, voriconazole, nefazodone, ritonavir, atazanavir, nelfinavir, telithromycin, Clarithromycin ) may increase the concentration of everolimus and its metabolites in the blood and they may increase exposure (exposure) to everolimus; therefore, the use of these preparations is not recommended in parallel. The parallel use of agents moderately inhibiting CYP3A4 activity (such as Erythromycin , diltiazem, Verapamil , oral cyclosporine, Fluconazole , amprenavir, fosamprnavir) can only be undertaken with extreme caution. In addition, if you can not avoid using these medicines in parallel, your doctor may reduce the dose. Avoid consumption of grapefruit juice, which also inhibits CYP3A4 activity.
Drugs that potentiate the activity of the cytochrome P450 3A4 isoenzyme (such as rifampicin, Dexamethasone and other corticosteroids, phenytoin, carbamazepine, phenobarbital, efavirenz, nevirapine, St. John's wort) may reduce the concentration of everolimus and its metabolites in the blood and reduce the exposure to everolimus and its efficacy. actions; therefore, the use of these preparations is not recommended in parallel.
Caution should be exercised when using everolimus with drugs metabolised by the 2D6 isozyme (eg desipramine) or 3A4 cytochrome P450 because their concentration in blood may change as a result of changes in the activity of these isoenzymes.
Parallel administration of everolimus and drugs transported by P-glycoprotein may cause interaction.Everolimus may affect the blood concentration and the severity of side effects of the following drugs (and other substances transported by P-glycoprotein): vincristine, colchicine, Paclitaxel , Digoxin ; be careful.
During the treatment period, the use of live vaccines (eg nasal influenza vaccine, measles vaccinations, mumps, rubella, oral polio vaccine, BCG, yellow fever, chickenpox and typhoid fever [TY21]) should be avoided. Other vaccinations may be less effective due to the weakened immune response.

What side effects can occur?

Like all medicines, Afinitor can also cause side effects, although they will not occur in all patients who use this medicine. Remember that the expected benefits of using the drug are usually greater than the damage resulting from the occurrence of side effects.
Very often haematological abnormalities are possible: lymphopenia (decrease in the number of lymphocytes), neutropenia (decrease in neutrophil counts), thrombocytopenia, anemia (decrease in hemoglobin). Very common: infections (including opportunistic infections, sepsis, severe cases of reactivation of hepatitis B), increased blood glucose (hyperglycaemia), increased cholesterol and / or triglycerides in the blood, hypophosphatemia (reduction of inorganic phosphates in the blood) , anorexia, taste disturbance, pneumonia (including interstitial pneumonia), dyspnea, nosebleed, cough, stomatitis, diarrhea, mucositis, vomiting, nausea, increased liver enzymes AST and ALT, rash, dryness skin, pruritus, increased creatinine in the blood, fatigue, weakness, peripheral edema. Common: dehydration, insomnia, headache, conjunctivitis, eyelid edema, hypertension, hemoptysis, dry mouth, abdominal pain, dysphagia, indigestion, increased bilirubin, palmar plantar erythrodysaesthesia, erythema, skin exfoliation, changes in within the nails, seborrheic dermatitis, nail fragility, chest pain, fever. Uncommon: diabetes, congestive heart failure , haemorrhage, angioneurotic edema, impaired wound healing. Hypersensitivity reactions and potentially life threatening anaphylactic reactions may occur.

Other preparations on the Polish market containing everolimus

Certican (tablets)
Votubia (tablets)