Imatinib

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  1. Veenat 100 mg (Imatinib Mesylate)
    Veenat 100 mg (Imatinib Mesylate)
    80,00

Description

capsules solid gelatine, No. 0, white color. 

Pharmacological action

Antineoplastic agent, tyrosine kinase inhibitor. Imatinib effectively inhibits the enzyme Bcr-Abl-tyrosinekinase at the cellular level. Imatinib selectively inhibits proliferation and induces apoptosis in cell lines positive for VSG-AKI, as well as immature leukemic cells in chronic myeloid leukemia with positive Philadelphia chromosome (Ph+) and acute lymphoblastic leukemia. Imatinib selectively inhibits VSG - AN-positive colonies derived from blood cells from patients with chronic myeloid leukemia. In addition, imatinib is a potent inhibitor of the receptor tyrosine kinases for growth factor platelet (PDGF) and stem cell factor (SCF), c-Kit, and inhibits the cell-mediated response, mediated above-mentioned factors. In vitro, imatinib inhibits proliferation and induces apoptosis in stromal tumors of the gastrointestinal tract expressing Kit mutations.

Pharmacokinetics

Indications for use

- for the treatment of adults and children with newly diagnosed chronic myeloid leukemia with Philadelphia chromosome

- for the treatment of adults and children with Ph+ CML in the phase or blast crisis phase of acceleration, as well as for the treatment of chronic phase after failure of interferon-alpha therapy;

- for the treatment of adult patients with newly diagnosed acute lymphoblastic leukemia with the Philadelphia chromosome (Ph+ ALL) in the chemotherapy;

- for the treatment of adult patients with relapsing or refractory Ph+ ALL (as monotherapy);

- myelodysplastic/myeloproliferative diseases (MDS/MPD) adult patients related to the receptor activation and platelet growth factor;

- systemic mastocytosis (CM) with the absence of the D816V c-Kit mutation or in the absence of data on the mutational status of c-Kit in adult patients;

hypereosinophilic syndrome and/or chronic eosinophilic leukemia (HES/CEL) in adults; inoperable, recurrent ;

dermatofibrosarcoma (DFSP) in adults;

inoperable and/or metastatic stromal tumors of the gastrointestinal tract (GIST) in adults;

- adjuvant therapy after resection of GIST in adults.

Contraindications

Hypersensitivity to imatinib mesylate or to any component of the drug.

Children up to age 2 years.

Pregnancy and lactation.

Pregnancy and lactation

During therapy with imatinib women of reproductive age should use effective methods of contraception. In the case of use of imatinib during pregnancy the patient should be warned of the possibility of potential threats to the fetus.

Imatinib and its active metabolite can penetrate into breast milk in lactating women. The women taking imatinib should not breast-feeding.

Method of application and doses

It is recommended to take orally during eating with a full glass of water. Dose 400/600 mg is taken once per day, whereas the drug in a daily dose of 800 mg should use 400 mg 2 times a day, morning and evening.

Treatment can continue, if you do not show signs of exacerbation of the disease or undesirable toxicity.

The recommended dosage of imatinib:

In chronic myeloid leukemia: the recommended dose for the treatment of patients with XMJI in chronic phase is 400 mg daily, for patients with XMJI in the activation phase or blast crisis 600 mg per day.

In chronic myeloid leukemia patients in chronic phase of the disease increase the dosage from 400 mg to 600 mg or for patients in the activation phase or in blast crisis - an increase in dosage from 600 mg to 800 mg (400 mg twice a day) indicated only in the absence of severe side effects and in the absence not related to leukemia, neutropenia or thrombocytopenia. This increase in dose may be necessary in the following circumstances: disease progression (at any stage), the absence of a satisfactory hematological response after 3 months after the start of treatment, no cytogenetic response after 12 months of therapy, the loss of a previously achieved haematological and/or cytogenetic response.

In acute lymphoblastic leukemia Remmanuela dose for the treatment of patients with Ph+ OJIJI is 600 mg per day.

With myelodysplastic/myeloproliferative diseases Remmanuela dose for the treatment of patients with MDS/MPD is 400mg per day.

In systemic mastocytosis Remmanuela dose for the treatment of patients with SM with the absence of the D816V c-Kit mutation is 400 mg per day. For patients with SM associated with eosinophilia, a clonal hematological when pathology is associated with the synthesis of kinase FIPlLl-PDGFRa, the recommended dose is 100 mg per day. Increasing the dose from 100 mg to 400 mg may be considered in the absence of side effects and in the case of insufficient response to therapy.

When hypereosinophilia syndrome and/or chronic eosinophilic leukemia (HES/CEL) Remmanuela dose for the treatment of patients with HES/CEL is 400 mg per day. For patients who have an increased level of tyrosine kinase activity FIPlLl-PDGFRa, the recommended initial dose of 100 mg per day. Increasing the dose from 100 mg to 400 mg may be considered in the absence of side effects and in the case of insufficient response to therapy.

When wybuchowa dermatofibrosarcoma (DFSP) the recommended starting dose of imatinib in adult patients with DPSP is 400 mg/day. If necessary, increase the dose to 800 mg per day.

In the stromal tumors of the gastrointestinal tract (GIST): the recommended dose for the treatment of patients with inoperable and/or metastatic GIST is 400 mg per day. Dose increase from 400 mg to 600 and 800 mg may be considered for patients in whom there are no side reactions, or if response to treatment is not effective enough.

The recommended dose for adjuvant treatment of adult patients after resection of GIST is 400 mg per day. The optimal duration of adjuvant therapy has not been established.

Dosing in special populations: :/a

Children .

Clinical experience on the use of imatinib,teh.delenia-children under 2 years suffering from chronic myeloid leukemia, not available. Experience in use of the drug for the treatment of children for other reasons is not practically available.

Calculation of dosage regimen in children older than 2 years is based on the body surface area (mg/m2). The recommended dose of 260 mg/m2 per day in the chronic phase XMJ1 and 340 mg/m2 per day when XMJ1 in the phase of acceleration, respectively. The total daily dose in children must not exceed the equivalent dose for adults is 400 mg and 600 mg. Treatment should be scheduled once a day or alternative divided into two doses - one morning, another in the evening.

Patients with abnormal liver function

Since imatinib is metabolized mainly in the liver, patients with minor, moderate impaired hepatic function you should assign the minimum recommended dose of 400 mg/day or less, depending on the recommended dose for treatment of the indication. In patients with severe liver dysfunction the recommended dose below 100 mg/day, increase by 100 mg/day to 400 mg/day acceptable in the absence of side effects.

Patients with impaired renal function

A significant highlight of imatinib and its metabolites is via the kidneys does not occur. Patients with impaired renal function or patients on dialysis, drug administered in minimum initial dose of 400 mg. However, when treating this category of patients should be used with caution. In case of intolerance the dose can be reduced. With good tolerability and lack of effectiveness dose can be increased.

Dosing in special cases

Modify dosage in hepatotoxicity and other pathological reactions non-hematologic in nature.

In case of severe non-hematologic adverse reactions (such as severe liver disease or fluid retention) it is necessary to discontinue Imatinib until the disappearance of these phenomena, after which the treatment can be resumed in accordance with the shown reaction.

If you raise the level of bilirubin 3 times above the upper limit of normal or elevated liver transaminases more than 5 times, receiving Imatinib must be suspended until then, until the bilirubin concentration does not decrease to a level that exceeds the upper limit of normal no more than 1.5 times, and the level of hepatic transaminases is not reduced to a level that exceeds the upper limit of normal no more than 2.5 times. After that, treatment with imatinib may be continued at a reduced daily dose. For adults the dose is reduced from 400 to 300 mg or from 600 to 400 mg, or from 800 to 400 mg per day. For children - from 260 to 200 mg/m2 / day or from 340 to 260 mg/ m2 per day. Hematologic adverse reaction


Side effects

In the expanded stage chronic myeloid leukemia or gastrointestinal stromal tumours, patients may have multiple related violations, making assessment of side effects due to a number of symptoms associated with concomitant diseases, their progression and reception of various drugs.

In General, imatinib is well tolerated long-term daily oral administration in patients with XMJI, including in children. Most patients had side effects, usually mild to moderate expressed. The discontinuation of the drug because of side reactions were observed in less than 5% of patients.

The most common adverse events associated with drug intake were mild nausea, vomiting, diarrhea, myalgia, muscle cramps, rash, which were easily controlled. It has often been noted primarily peripheral edema periorbital areas, or edema of the lower extremities. However, they rarely had a pronounced and well to diuretic therapy; in some patients, the swelling took place after lowering the dose of imatinib.

Various adverse events such as pleural effusion, ascites, pulmonary edema and rapid weight gain peripheral edema with or without them can be generally classified as fluid retention.

Adverse events are listed below by organ and systems, indicating the frequency of their occurrence.

Determination of the frequency very often (1/10), often (from 1/100 to 1/10), infrequently (from 1/1000 to 1/100), rare (1/10000 to 1/1000), very rare (1/10000).

Infectious and parasitic diseases: rarely, herpes simplex, herpes zoster, nasopharyngitis, pneumonia, sinusitis, cellulitis, infections of the upper respiratory tract, influenza, infections of the urinary tract, gastroenteritis, sepsis; rarely fungal infections.

Violations by the blood and lymphatic system: very often - neutropenia, thrombocytopenia, anemia; often - pancytopenia, febrile neutropenia; rare - thrombocythemia, lymphopenia, depression of bone marrow function, eosinophilia, lymphadenopathy; rare - hemolytic anemia.

Violations of metabolism and nutrition: often - anorexia; rarely, hypokalaemia, increased appetite, hypophosphatemia, decreased appetite, dehydration, gout, hyperuricemia, hyperglycemia, hypercalcemia, hyponatremia; rarely hyperkalemia, hypomagnesemia.

Mental disorders: often - insomnia, rarely - depression, decreased libido, anxiety; rare - confusion.

Disorders of the nervous system: very often - headache, often - dizziness, paresthesia, impaired taste sensation, hypesthesia; rare - headache, drowsiness, loss of consciousness, peripheral neuropathy, memory impairment, sciatica, syndrome "restless" legs, tremor, bleeding in the brain; rarely increased intracranial pressure, convulsions, optic neuritis.

Violations of the organ of vision: often - swelling of the eyelids, increased tearing, conjunctival hemorrhage, conjunctivitis, dry eyes, blurred vision; rarely, irritation in eyes, eye pain, orbital edema, hemorrhages in sclera, hemorrhage into the retina, blepharitis, macular edema, rarely - cataracts, glaucoma, of papilloedema.

Violations of the organ of hearing and labyrinth disorders: infrequent - vertigo, tinnitus, hearing loss.

Disorders of the heart: rarely palpitation, tachycardia, congestive heart failure, pulmonary edema; rare - arrhythmia, atrial fibrillation, cardiac arrest, myocardial infarction, angin

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