Philachromin capsules 100mg, 120pcs

Composition

Per capsule: Active ingredient: Imatinib mesylate 119.5 mg, based on imatinib 100 mgcomotive substances: Microcrystalline cellulose 92 mg Crospovidone 15 mg colloidal silicon dioxide 1.5 mg Magnesium stearate 2 mg Capsule composition: capsule body: titanium dioxide – 2%, gelatin – up to 100%; capsule cap: indigo carmine – 0.3%, titanium dioxide-1%, iron oxide yellow-1.7143%, gelatin – up to 100%.

Pharmacological action

Imatinib selectively inhibits the enzyme Veg-Abl-tyrosine kinase, which is formed when a region of the Veg gene (breakpoint cluster region) and the proto-oncogene Abl (Abelson) merge at the cellular level.

Imatinib selectively suppresses proliferation and causes apoptosis of cell lines expressing Veg-Abl-tyrosine kinase, as well as immature leukemia cells in chronic Philadelphia chromosome-positive myeloid leukemia and acute lymphoblastic leukemia. In patients with chronic myeloid leukemia, imatinib selectively inhibits Veg-Abl-positive colonies and has antitumor activity in monotherapy.

Imatinib selectively inhibits Veg-Abl-positive colonies obtained from blood cells of patients with chronic myeloid leukemia.

Activation of platelet growth factor receptors or the tyrosine kinase Abl fragment can cause the development of both myelodysplastic/myeloproliferative diseases, as well as hypereosinophilic syndrome and chronic eosinophilic leukemia and bulging dermatofibrosarcoma.

Activation of the c-Kit tyrosine kinase receptor and platelet growth factor receptors may underlie the pathogenesis of systemic mastocytosis.

Imatinib inhibits cell signaling and cell proliferation resulting from dysregulation of platelet and stem cell growth factors, the c-Kit receptor, and the Abl tyrosine kinase fragment.

Imatinib inhibits proliferation and induces apoptosis of gastrointestinal stromal tumor cells expressing tyrosine kinase with a c-Kit receptor mutation.

Indications

• First detected Philadelphia chromosome-positive (Ph+) chronic myeloid leukemia in children and adults.

• Philadelphia chromosome positive (Ph+) chronic myeloid leukemia in the chronic phase with failure of previous interferon alpha therapy or in the acceleration phase, or blast crisis in children and adults.

• Newly diagnosed Philadelphia chromosome-positive (Ph+) acute lymphoblastic leukemia in adult patients in combination with chemotherapy.

• Recurrent or refractory acute lymphoblastic leukemia Philadelphia chromosome positive (Ph+) in adult patients as monotherapy.

• Myelodysplastic / myeloproliferative diseases associated with gene rearrangements of the platelet growth factor receptor in adult patients.

• Systemic mastocytosis in adult patients with no D816V c-Kit mutation or unknown c-Kit mutation status.

• Hypereosinophilic syndrome and / or chronic eosinophilic leukemia in adult patients with positive or negative abnormal FIP1L1-PDGRF alpha-tyrosine kinase.

• Adjuvant therapy of gastrointestinal stromal tumors (GISO) positive for c-Kit (CD 117) in adult patients.

• Inoperable and / or metastatic malignant gastrointestinal stromal tumors (GIST) positive for c-Kit (CD 117) in adult patients.

• Inoperable, recurrent and / or metastatic bulging dermatofibrosarcoma in adult patients.

Contraindications

• Hypersensitivity to the Active ingredient or any other component of the drug..
• Children under 2 years of age (efficacy and safety have not been established).
• Pregnancy and lactation.

With caution

Caution should be exercised when prescribing to patients with severe hepatic insufficiency, severe renal impairment, cardiovascular disease, or risk factors for heart failure, as well as when undergoing a regular hemodialysis procedure.

Side effects

When taking the drug, such undesirable effects from organs and systems are possible:

the onset of nausea, vomiting, liver function disorders (increased activity of “hepatic” transaminases and alkaline phosphatase, hyperbilirubinemia).

neutropenia, thrombocytopenia, anemia, pancytopenia.

fluid retention in the body — weight gain, superficial edema, local or widespread edema, pleural and / or pericardial effusion, ascites, pulmonary edema, edema of the periorbital region, rarely of the extremities, impaired renal function.

CHF.

Muscle spasm.

Interaction

An increase in the concentration of imatinib, the main substance of Filachromin in blood plasma, is possible with the simultaneous use of Filachromin FS together with such drugs as ketoconazole, itraconazole, erythromycin, clarithromycin.

Reduction of the drug in blood plasma is possible when taken simultaneously with: dexamethasone, rifampicin, antiepileptic drugs such as: carbamazepine, oxcarbazepine, phenytoin, phenobarbital, phosphenytoin, primidone or drugs based on St. John’s wort.

Caution is recommended when imatinib is co-administered with cyclosporine and pimozide.

When used concomitantly with warfarin, it is possible to increase the prothrombin time. When co-administered with coumarin derivatives, short-term monitoring of prothrombin time is necessary at the beginning and end of imatinib therapy, as well as when changing the dosage regimen of imatinib. Alternatively, the use of low molecular weight heparin derivatives should be considered.

When imatinib is combined with chemotherapeutic drugs, in high doses, transient hepatotoxicity may develop in the form of increased liver transaminase activity and hyperbilirubinemia.

How to take, course of use and dosage

The recommended daily dose of filachromin in remission is 400 mg, in the acute stage and in the blast crisis-600 mg. Dosage in case of disease progression can be adjusted: in the remission stage – up to 600 mg / day, in the acute stage and in case of blast crisis – up to 800 mg/day (400 mg 2 times a day).

In case of impaired liver function (an increase in the bilirubin concentration by 3 times compared to the initial value, the activity of “liver” transaminases — by 5 times), treatment is stopped until the values of the indicators decrease to 1.5 and 2.5, respectively. In this case, treatment is resumed, reducing the dose from 400 to 300 mg and from 600 to 400 mg.

In blast crisis, and in the acute stage (the dosage regimen of 600 mg/day) in the case of reduction of neutrophils less than 500/µl, platelets less than 100 thousand/µl, treatment should be stopped; to differentiate the cause of the cytopenia, conduct a bone marrow biopsy; if cytopenia is not associated with leukemia, the dose of imatinib was reduced to 400 mg; if cytopenia persists for the next 2 weeks, reduce the dose to 300 mg; if cytopenia lasts for about 4 weeks, treatment should be stopped until recovery of blood counts (neutrophil — not less than 1 thousand/µl platelet — not less than 200 thousand/µl), and then resume at a reduced dose of 300 mg/day.

Form of production

Solid gelatin capsules No. 1, white body, dark green lid

The contents of capsules are powder or powder with granules from white to yellow with a brownish tinge of color

Active ingredient

Imatinib

Conditions of release from pharmacies

By prescription

Dosage form

Capsules

Description

Children as prescribed by a doctor, Adults as prescribed by a doctor

Indications

Cancer