Description
Latin name
Philachromin
Pharmacological action of
Imatinib selectively inhibits the Ber-Abl tyrosine kinase enzyme, which is formed by the fusion of a portion of the Ber gene (breakpoint cluster region) and the Abl proton oncogen (Abelson) at the cellular level.
Imatinib selectively inhibits proliferation and induces apoptosis of cell lines expressing Ber-Abl tyrosine kinase, as well as immature leukemia cells in chronic myelogenous leukemia with Philadelphia positive chromosome and in acute lymphoblastic leukemia. In patients with chronic myelogenous leukemia, imatinib selectively inhibits Ber-Abl-positive colonies and has antitumor activity during monotherapy.
Imatinib selectively inhibits Ber-Abl-positive colonies, obtained from blood cells of patients with chronic myelogenous leukemia.
Activation of receptors for platelet growth factors or the Abl tyrosine kinase fragment can cause both myelodysplastic / myeloproliferative diseases and hypereosinophilic syndrome and chronic eosinophilic leukemia and swelling dermatofibrosarcoma.
Activation of the tyrosine kinase c-Kit 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, c-Kit receptor, and Abl tyrosine kinase fragment.
Imatinib inhibits proliferation and induces apoptosis of gastrointestinal stromapoma tumor cells, expressing tyrosine kinase with c-Kit receptor mutation.
Contraindications
Hypersensitivity to the active substance or any other component of the drug. .
Children under 2 years of age (efficacy and safety not established).
Pregnancy and lactation.
Caution
Use with caution in patients with severe liver failure, severe renal impairment, cardiovascular disease or in the presence of risk factors for heart failure, as well as during regular hemodialysis procedures.
Composition
For one capsule:
Active ingredient: srdlkat mini 119.5 mg, calculated on imatinib 100 mg
Excipients:
Microcrystalline cellulose 92 mg
Crospovidone 15 mg
Silicon dioxide colloidal 1.5 mg
Magnesium stearate 2 mg
Capsule composition:
capsule body:
titanium dioxide – 2%, gelatin – up to 100% cap %, titanium dioxide – 1%, yellow iron oxide – 1.7143%, gelatin – up to 100%.
Dosage and administration of
Recommended daily dose of filachromine in remission – 400 mg, in the acute stage and in blast crisis – 600 mg. The dosage for the progression of the disease can be adjusted: in the remission stage – up to 600 mg / day, in the acute stage and in blast crisis – up to 800 mg / day (400 mg 2 times a day).
In case of impaired liver function (an increase in the concentration of bilirubin 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 doses from 400 to 300 mg and from 600 to 400 mg.
In blast crisis and in the stage of exacerbation (dosing regimen – 600 mg / day) in the case of a decrease in neutrophils of less than 500 / Ојl, platelets – less than 100 thousand / Ојl, treatment is stopped to differentiate the cause of cytopenia, a bone marrow biopsy is performed if cytopenia is not associated with leukemia the dose of imatinib is reduced to 400 mg if cytopenia persists for the next 2 weeks, the dose is reduced to 300 mg if cytopenia lasts up to 4 weeks, treatment is stopped until blood counts are restored (neutrophils – at least 1 thousand / Ојl, platelets – at least 200 thousand ./mcl), and then renewed in a reduced dose – 300 mg / day.
Side effects of
When taking the drug, such unwanted effects from organs and systems are possible:
The onset of nausea, vomiting, impaired liver function (increased activity of “liver” 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, less commonly extremities, impaired renal function.
CHF.
muscle spasm.
Drug interaction
An increase in the concentration of imatinib, the main substance of Filachromin in the blood plasma, is possible with the simultaneous use of Filachromin FS together with such drugs as: ketoconazole, itraconazole, erythromycin, clarithromycin.
Decrease in the drug in blood plasma, possible while taking it with: dexamethasone, rifampicin, antiepileptic drugs, such as: carbamazepine, oxcarbazepine, phenytoin, phenobarbital, fosphenytoin, primidone or drugs based on St. John’s wort.
Caution recommended while using imatinib and cyclosporin and pimozide.
With simultaneous use with warfarin, an increase in prothrombin time is possible. With simultaneous administration with coumarin derivatives, short-term monitoring of prothrombin time at the beginning and at the end of imatinib therapy, as well as when changing the dosage regimen of imatinib, is necessary. Alternatively, the use of low molecular weight heparin derivatives should be considered.
When combining imatinib with chemotherapeutic drugs in high doses, transient hepatotoxicity may develop in the form of increased liver transaminases and hyperbilirubinemia.
Active ingredient
Imatinib
Dosage form
capsule
