Filachromin

2024 Author: Rachel Wainwright | [email protected]. Last modified: 2023-12-15 07:39

Filachromin: instructions for use and reviews

1. Release form and composition
2. Pharmacological properties
3. Indications for use
4. Contraindications
5. Method of application and dosage
6. Side effects
7. Overdose
8. Special instructions
9. Application during pregnancy and lactation
10. Use in childhood
11. In case of impaired renal function
12. For violations of liver function
13. Use in the elderly
14. Drug interactions
15. Analogs
16. Terms and conditions of storage
17. Terms of dispensing from pharmacies
18. Reviews
19. Price in pharmacies

Latin name: Philachromin

ATX code: L01XE01

Active ingredient: imatinib (Imatinib)

Manufacturer: JSC Pharmstandard-UfaVITA (Russia); LLC "Nativa" (Russia)

Description and photo update: 2019-08-07

Prices in pharmacies: from 2099 rubles.

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Filachromin is an antineoplastic agent.

Release form and composition

The drug is available in the form of capsules: hard gelatinous, size No. 3 (dosage 50 mg) or No. 1 (dosage 100 mg), with a white body and a dark green lid; contents - powder (granules may be present) from white to brownish-yellow color (capsules in a dosage of 50 mg: 30 pcs. in polymer bottles, in a cardboard box 1 bottle; 10 pcs. in a cell contour packaging, in a cardboard box 3 packages; capsules in a dosage of 100 mg: 24, 36, 48, 96, 120 and 180 pcs. in polymer bottles, in a cardboard box 1 bottle; 6 and 12 pcs. in blister contour packages, in a cardboard box 4, 6, 8, 16, 20 or 30 packs of 6 capsules, 2, 3, 4, 8, 10 or 15 packs of 12 capsules Each pack also contains instructions for the use of Filachromin).

Composition of 1 capsule:

active substance: imatinib (in the form of imatinib mesylate) - 50 or 100 mg;
auxiliary components: colloidal silicon dioxide, crospovidone, microcrystalline cellulose, magnesium stearate;
capsule shell: body - gelatin, titanium dioxide; cap - gelatin, titanium dioxide, indigo carmine dye, iron oxide yellow dye.

Pharmacological properties

Pharmacodynamics

Imatinib, the active substance of Filachromin, is an inhibitor of protein tyrosine kinase. Selectively inhibits the enzyme BCR-ABL-tyrosine kinase, which is formed at the fusion at the cellular level of the BCR gene region (Breakpoint Cluster Region) and the ABL proto-oncogene (Abelson). The drug selectively inhibits proliferation. It causes apoptosis (death) of cell lines expressing BCR-ABL-tyrosine kinase and immature leukemia cells in patients with chronic myeloid leukemia with positive Philadelphia chromosome and in patients with acute lymphoblastic leukemia.

In chronic myeloid leukemia, imatinib selectively suppresses BCR-ABL-positive colonies and has an antitumor effect when administered alone.

Activation of receptors for platelet growth factors and c-Kit (kit2c75) FITC (c-Kit receptor tyrosine kinase) may be the basis for the pathogenesis of systemic mastocytosis.

Due to the activation of receptors for platelet growth factors or ABL-fragment of tyrosine kinase, the development of both myelodysplastic syndromes / myeloproliferative diseases and chronic eosinophilic leukemia, hypereosinophilic syndrome, bulging dermatofibrosarcoma is possible.

Imatinib inhibits cell proliferation and signal transduction in cells due to dysregulation of the activity of stem cell platelet growth factors, ABL tyrosine kinase fragment and c-Kit receptor.

Filachromin inhibits proliferation, induces apoptosis of gastrointestinal stromal tumor cells that express tyrosine kinase with a mutation of the c-Kit receptor.

Pharmacokinetics

absorption: after oral administration, imatinib is characterized by high bioavailability - about 98%. The simultaneous intake of food with a significant fat content, in comparison with taking the capsule on an empty stomach, slightly reduces the degree and rate of absorption. The AUC (area under the concentration-time curve) varies by a factor of 40-60%;
distribution: about 95% of the received dose is associated with plasma proteins (mainly with acidic α-glycoproteins and albumin, to a small extent with lipoproteins);
metabolism: imatinib is metabolized in the liver to form N-demethylated piperazine derivative - the main circulating metabolite, the pharmacological activity of which in vitro is similar to that of imatinib;
excretion: after a single dose, most of the drug is excreted as metabolites within 7 days, of which 68% is excreted by the intestines and 13% by the kidneys. The share of unchanged imatinib accounts for approximately 25% of the dose, including 20% excreted by the intestines, 5% by the kidneys. The half-life (T _1/2) is ~ 18 hours.

With repeated administration of Filachromin 1 time per day, the pharmacokinetic characteristics of the drug do not change. The equilibrium concentration (C _ss) exceeds the initial value by 1.5–2.5 times.

Pharmacokinetics in special cases:

gender: differences in the pharmacokinetics of imatinib were not found in female and male patients;
body weight: with an increase in the patient's body weight, the clearance value of the drug increases, but there is no need to adjust the dose;
advanced age: in patients over 65 years of age, the volume of distribution (Vd) of the drug increases slightly (~ 12%), but no change in the dosage regimen is required;
children's age: in children and adolescents under 18 years of age, as in adults, the drug is rapidly absorbed after oral administration. Cumulation of imatinib was noted with repeated use;
liver function: in patients with impaired hepatic function, an increase in serum concentrations of the drug is possible;
renal function: in patients with mild to moderate functional impairment of the kidneys [creatinine clearance (CC)> 30 ml / min], the exposure of imatinib in plasma increases by approximately 1.5-2 times, which corresponds to an increase in the content of acidic α-glycoproteins (the main plasma proteins binding to imatinib). No relationship was found between the severity of renal impairment and drug exposure.

Indications for use

For adults and children:

newly diagnosed chronic myeloid leukemia (CML), positive for the Philadelphia chromosome (Ph +);
Ph-positive CML in the chronic phase with the ineffectiveness of previous therapy with interferon-α, as well as in the phase of acceleration or blast crisis.

Additionally for adults:

newly diagnosed acute lymphoblastic leukemia (ALL), positive for the Philadelphia chromosome (Ph +) - in combination with chemotherapy;
refractory or recurrent Ph-positive ALL - as monotherapy;
myelodysplastic syndromes / myeloproliferative diseases (MDS / MPD) associated with gene rearrangements of the platelet growth factor receptor;
recurrent, metastatic and / or inoperable protruding dermatofibrosarcoma (WDFS);
hypereosinophilic syndrome (HES) and / or chronic eosinophilic leukemia (CEL) with positive or negative abnormal FIP1L1-PDGRF α-tyrosine kinase;
systemic mastocytosis (SM) in the absence of D816V c-Kit mutation or unknown c-Kit mutation status;
metastatic and / or inoperable gastrointestinal stromal tumors (GIST), positive for c-Kit (CD 117);
GIST positive for c-Kit (CD 117) - adjuvant therapy.

Contraindications

Absolute:

children under 2 years old;
period of pregnancy and lactation;
increased sensitivity to the active or any auxiliary component contained in the capsule composition.

Filachromin is used with caution in cardiovascular diseases and the presence of a risk of heart failure, severe renal impairment, severe liver failure, as well as during regular hemodialysis procedures.

Filachromin, instructions for use: method and dosage

Filachromin is indicated for oral administration: the capsules should be swallowed whole with plenty of water (1 glass) with meals. Daily doses of up to 600 mg should be taken at a time, 800 mg should be divided into two equal doses, in the morning and in the evening.

For patients who have difficulty swallowing whole capsules (including children), the capsules can be opened and the contents diluted with water or apple juice. The suspension prepared in this way cannot be stored, therefore it should be prepared right before taking it.

Standard dosage regimens for Filachromin for different indications:

CML in adults: the daily dose in the chronic phase is 400 mg, in the phase of acceleration and blast crisis - 600 mg. If there are no side effects not associated with leukemia and neutropenia / thrombocytopenia, the dose, if necessary, can be increased to 600 or 800 mg in patients with the disease in the chronic phase, to 800 mg in the phase of acceleration and blast crisis. The indicated dose increase may be necessary in the following cases: disease progression (regardless of the stage), the absence of a satisfactory hematological response after 3 months of therapy, the absence of a cytogenetic response after 12 months of treatment, the loss of a previously achieved hematological and / or cytogenetic response;
CML in children from 2 years: in a daily dose of chronic and accelerated phase is 340 mg / m ² (but not more than 600 mg) in 1 or 2 divided doses;
inoperable and / or metastatic GIST: 400 mg per day. If necessary, the dose can be increased to 600 or 800 mg (with insufficient response, but no adverse reactions);
adjuvant therapy GIST, MDS / MPZ, HES / HEL: 400 mg per day;
HES / HEL and SM due to abnormal FIP1L1-PDGFR α-tyrosine kinase: initial daily dose of 100 mg. With insufficient effectiveness, it is possible to increase the dose to 400 mg per day, provided that there are no side effects;
CM in the absence of D816V c-Kit mutation, CM with unknown mutational status in case of insufficient effectiveness of previous therapy: 400 mg per day;
ALL with (Ph +): 600 mg per day;
recurrent, metastatic and / or inoperable VDFS: 800 mg per day.

Treatment is advisable for the entire period of maintaining the clinical effect and the absence of signs of disease progression. The optimal duration of adjuvant therapy has not been established.

For patients with concomitant liver dysfunction (of any severity), the recommended daily dose of Filachromin is 400 mg. If toxic effects develop, the dose is reduced.

Patients with concomitant renal impairment of mild to moderate severity should begin treatment with a daily dose of 400 mg. The experience of using imatinib in severe functional disorders of the kidneys and hemodialysis is limited, so the initial dose is 400 mg once a day. In case of poor tolerance of Filachromin, a dose reduction is possible, if the effect is insufficient, an increase.

Dose adjustment for the development of non-hematological adverse reactions

In the event of any serious non-hematological effect developing while using Filachromin, therapy should be suspended. The decision to resume the course of treatment is made by the doctor.

Patients who have an increase in the concentration of bilirubin and the activity of hepatic transaminases in the blood serum, respectively, 3 and 5 times compared with those with congenital adrenal hyperplasia (CAH), treatment is suspended until the first indicator reaches a value of less than 1.5 × VGKN, the second - 2.5 × VGKN. Reception of Filachromin is resumed with a lower daily dose: in adults, the daily dose of 400 mg is reduced to 300 mg, 600 mg to 400 mg, 800 mg to 600 mg; in children - the dose of 340 mg / m ^{2 is} reduced to 260 mg / m ².

Dose adjustments for serious hematological adverse reactions

In case of thrombocytopenia or neutropenia, depending on their severity, reduce the dose or temporarily cancel Filachromin.

Recommendations for dose reduction depending on the indications and the severity of neutropenia / thrombocytopenia:

SM and HES / CEL due to abnormal FIP1L1-PDGFR α-tyrosine kinase (the initial dose of imatinib was 100 mg): if the absolute neutrophil count <1000 / μL and / or the platelet count <50,000 / μL decreases, Filachromin should be canceled until the absolute number is restored neutrophils to values ≥ 1500 / μl and platelets ≥ 75,000 / μl. The therapy is resumed at the dose that was used before the temporary discontinuation of the drug;
CML in the chronic phase of children and adults, SM and HES / CEL, MDS / MPD, malignant GIST in adults (at the initial stage of imatinib dose therapy in adults is 400 mg, in children - 340 mg / m ²): the reduction in the absolute number of Neutrophil count <1000 / μL and / or platelet count <50 000 / μL Filachromin should be discontinued until the absolute neutrophil count is restored to ≥ 1500 / μL and platelets ≥ 75,000 / μL and therapy should be resumed at the dose that was used until the drug was temporarily discontinued. In the case of a repeated decrease in neutrophils / platelets to the indicated values, the treatment is temporarily stopped, as indicated above, and then resumed in a reduced dose - 300 mg in adults, 260 mg / m ² in children;
CML in accelerated phase and blast crisis of adults and children with ALL with (Ph +) in adults (initial dose of imatinib in adults - 400 mg, in children - 340 mg / m ²): the reduction in absolute neutrophil count <500 / ul, and / or platelet count <10,000 / μL after one or more months of treatment, it should be established (bone marrow examination) whether cytopenia is associated with leukemia. If not associated, the current dose of Filachromin is reduced to 400 mg in adults, to 260 mg / m ² in children. If cytopenia persists within 2 weeks, the dose of the drug is reduced to 300 mg in adults, to 200 mg / m ²in children. In the case when cytopenia still persists over the next 4 weeks, and the association of its development with leukemia is not confirmed, Filachromin is canceled until the absolute number of neutrophils reaches ≥ 1000 / μl and platelets ≥ 20,000 / μl. Resume treatment with the drug at a dose of 300 mg in adults and 260 mg / m ² in children;
recurrent, metastatic and / or inoperable VDFS (at the initial stage of therapy, the dose of imatinib was 800 mg): with a decrease in the absolute number of neutrophils <1000 / μl and / or the number of platelets <50,000 / μl, Filachromin should be canceled until the absolute number of neutrophils is restored to ≥ 1500 / μL and platelets ≥ 75,000 / μL and resume therapy at 600 mg. In the event of a repeated decrease in neutrophils / platelets to the indicated values, the treatment is temporarily stopped, as indicated above, and resumed at a reduced dose of 400 mg.

Side effects

The following are the registered side effects that occurred more often than single observations (the frequency is defined as follows: very often -> 10% of appointments, often -1-10%, infrequently - 0.1-1%, rarely - 0.01– 0.1%, very rarely - <0.01%):

infectious diseases: infrequently - sinusitis, nasopharyngitis, infectious processes in the upper respiratory tract, influenza, pneumonia ¹, urinary tract infections, herpes zoster, herpes simplex, sepsis, gastroenteritis, inflammation of the subcutaneous tissue; rarely - mycoses;
on the part of the vessels and heart: infrequently - hemorrhages ¹, increased or decreased blood pressure, tachycardia, palpitations, impaired capillary permeability, thrombosis / embolism, flushing ², congestive heart failure ³, pulmonary edema; rarely - cold extremities, hematomas, Raynaud's syndrome, angina pectoris, arrhythmias, atrial fibrillation, pericarditis, atrial fibrillation, cardiac tamponade, myocardial infarction, pericardial effusion, sudden cardiac arrest;
from the nervous system: very often - headache ²; often - taste disturbances, hypesthesia, paresthesia, dizziness; infrequently - drowsiness, migraine, memory impairment, peripheral neuropathy, fainting, tremor, restless legs syndrome (Wittmaak-Ekbom syndrome), sciatica, cerebral edema, hemorrhagic stroke; rarely - optic neuritis, increased intracranial pressure, convulsions;
from the organs of the chest, mediastinum, respiratory system: often - cough, shortness of breath, nosebleeds; infrequently - pharyngitis, pain in the throat / larynx, pleural effusion ³, interstitial pneumonia, acute respiratory failure; rarely - pulmonary hypertension, pleural pain, pleurisy, pulmonary fibrosis, pulmonary hemorrhage;
on the part of the connective and musculoskeletal tissue: very often - musculoskeletal pain ⁴ (including bone pain, myalgia, arthralgia, muscle spasms, convulsions); often - swelling in the joints; infrequently - stiffness of joints and muscles, sciatica; rarely - myopathy, arthritis, muscle weakness, avascular necrosis of the femoral head, rhabdomyolysis (acute necrosis of skeletal muscles);
from the gastrointestinal tract: very often - abdominal pain ⁴, dyspepsia, diarrhea, nausea, vomiting, reflux esophagitis; often - dryness of the oral mucosa, stomatitis, ulceration of the oral mucosa, flatulence, bloating, constipation, pancreatitis, gastritis; infrequently - cheilitis, belching, dysphagia, melena, pancreatitis, stomach ulcer, gastrointestinal bleeding ⁴, ascites, tumor necrosis; rarely - intestinal inflammation, colitis, diverticulitis, intestinal obstruction (paralytic, obstructive);
from the liver and biliary tract: often - increased activity of liver enzymes; infrequently - hyperbilirubinemia, jaundice, hepatitis; rarely - liver failure ⁵, liver necrosis ⁵;
from the urinary tract and kidneys: infrequently - hematuria, frequent urination, pain in the kidney, renal failure, acute renal failure;
from the side of metabolism: often - anorexia; infrequently - increased or decreased appetite, hypokalemia, hypercalcemia, hyponatremia, hypophosphatemia, hyperuricemia, dehydration, gout, hyperglycemia; rarely - hypomagnesemia, hyperkalemia;
from the lymphatic system and blood: very often - anemia, neutropenia, thrombocytopenia; often - febrile neutropenia, pancytopenia; infrequently - lymphadenopathy, lymphopenia, thrombocytopenia, eosinophilia, inhibition of bone marrow hematopoiesis; rarely - hemolytic anemia;
from the organ of hearing: infrequently - tinnitus, hearing loss;
on the part of the organ of vision: often - dryness of the conjunctiva, increased lacrimation, conjunctivitis, hemorrhage under the conjunctiva, edema of the eyelids, blurred vision; infrequently - eye pain, eye irritation, blepharitis, macular edema, orbital edema, retinal hemorrhages, papillary edema; rarely - edema of the optic nerve head, glaucoma, cataracts, vitreous hemorrhage;
psyche: often - insomnia; infrequently - anxiety, depression, decreased libido; rarely - confusion of consciousness;
from the endocrine and reproductive systems: infrequently - nipple pain, breast enlargement, gynecomastia, menstrual irregularities, menorrhagia, scrotal edema, erectile dysfunction, decreased potency, sexual dysfunction; very rarely - bleeding from an ovarian cyst in women;
from the subcutaneous tissues and skin: very often - skin rash, dermatitis, periorbital edema, eczema; often - dry skin, itching, night sweats, facial puffiness, alopecia, erythema, eyelid edema, photosensitivity reactions; infrequently - urticaria, petechiae, bullous rash, exfoliative dermatitis, ecchymosis, hypopigmentation / hyperpigmentation of the skin, folliculitis, increased sweating, psoriasis, bruising, hypotrichosis, urticaria, purpura, nail damage, mild hematoma; rarely - vesicular rash, lichen planus, lichenoid keratosis, discoloration of nails, acute generalized exanthemic pustulosis, angioedema, Stevens-Johnson syndrome, leucoclastic vasculitis, erythema multiforme, acute febrile neutrophilic dermatosis (Sweet's syndrome); very rarely - toxic epidermal necrolysis;
neoplasms (benign, malignant, unspecified): rarely - tumor disintegration syndrome;
others: very often - increased fatigue, weight gain, fluid retention in the body, edema; often - trembling, chills, fever, weight loss, weakness, anasarca; infrequently - chest pain, general malaise, increased concentration of creatinine, alkaline phosphatase, creatine phosphokinase and lactate dehydrogenase in the blood serum; rarely - an increase in amylase activity in blood plasma; very rarely - anaphylactic shock.

Explanation of notes:

¹ Hemorrhages (hematomas, hemorrhages) and pneumonia most often occur in patients with CML in the phase of acceleration and blast crisis, as well as in patients with inoperable and / or metastatic malignant GIST.

² Headache and hot flashes are more common in patients with a diagnosis of inoperable and / or metastatic malignant GIST.

³ Side effects from the heart (including congestive heart failure) and pleural effusion in patients with CML in the phase of acceleration and blast crisis are observed more often than in the chronic phase.

⁴ Musculoskeletal pain / cramps, abdominal pain, gastrointestinal bleeding usually predominate in patients receiving Filachromin due to malignant inoperable and / or metastatic GIST.

⁵ There are separate reports on the development of liver failure and liver necrosis.

The side effect profile of imatinib is similar in patients receiving the drug for different indications.

The most common negative effects of Filachromin are passing abdominal pain, diarrhea, mild nausea, vomiting, myalgia, muscle cramps, fatigue, skin rashes, peripheral edema (mainly in the lower extremities and periorbital region). All these symptoms are easily relieved.

In patients with GIST and CML in the advanced stage, it is difficult to assess the side effects of imatinib, since they may develop multiple concomitant disorders, manifested by various symptoms.

It is known that in adults and children with CML, with long-term daily intake of imatinib, the drug is generally well tolerated. At a certain stage of therapy, the majority of them experience some kind of undesirable reactions, which are usually mild or moderate.

Intratumoral bleeding is characteristic only in the group of patients with malignant GIST, and myelosuppression is less common in them. The profile of the occurrence of side effects is similar when taking Filachromin both in a daily dose of 400 mg and 800 mg.

Combined phenomena such as rapid weight gain, ascites, pleural effusion, and pulmonary edema (sometimes with peripheral edema) can qualify as fluid retention. To eliminate them, temporary discontinuation of imatinib and the use of diuretics are usually sufficient. However, in some cases, such phenomena can reach a serious and even life-threatening degree.

Overdose

Overdose in adults

A patient with CML in the blast crisis phase when taking imatinib in a daily dose of 1200–1600 mg for 1–10 days had the following symptoms: decreased appetite, diarrhea, abdominal pain, nausea, vomiting, fatigue, headache, muscle cramps, swelling joints, edema, erythema, skin rash, pancytopenia, thrombocytopenia.

Taking Filachromin in a daily dose of 1800–3200 mg (the highest dose was 3200 mg per day for 6 days) caused gastrointestinal pain, myalgia, weakness, and increased concentrations of creatine phosphokinase and bilirubin in the blood.

There is one known case when a patient took a single dose of 6400 mg. He had facial edema, abdominal pain, nausea, vomiting, increased liver transaminase activity, and a decrease in the number of neutrophils.

A single dose of 8,000-10,000 mg of imatinib caused gastrointestinal pain and vomiting.

Overdose in children and adolescents

A single dose of 400 mg of imatinib caused a 3-year-old child to vomit, diarrhea, and anorexia. Another 3-year-old child had diarrhea and a decrease in white blood cell count after a single dose of 980 mg.

Treatment

The antidote for imatinib is unknown. Conducting symptomatic therapy is shown. Careful medical supervision of patients is recommended. The outcome of an overdose is generally favorable.

special instructions

Filachromin can only be prescribed by a doctor with experience in the use of anticancer drugs.

In case of opening the capsules, care should be taken: avoid accidental inhalation of the powder, avoid contact with the skin and mucous membranes of the eyes. After opening the capsule, it is recommended to wash your hands immediately.

During the period of therapy, especially for patients with liver diseases, regular monitoring of liver function and a clinical blood test is shown.

Careful medical supervision of patients with heart disease is recommended, including regular determination of body weight, since imatinib can cause severe fluid retention, in some cases with a severe course, up to death. In case of a sudden rapid increase in body weight, it is necessary to conduct an examination, if necessary, cancel Filachromin and / or prescribe a diuretic.

In rare cases, patients with heart disease and hypereosinophilic syndrome develop left ventricular failure or cardiogenic shock at the beginning of anticancer therapy. These conditions require the cancellation of Filachromin, they are usually stopped by the introduction of systemic glucocorticosteroids (GCS) and the implementation of measures aimed at maintaining blood circulation.

In patients with malignant GIST, bleeding from the gastrointestinal tract and from the tumor is possible. Depending on the anatomical localization of the tumor, both intra-abdominal and intrahepatic bleeding occur.

Patients with MDS / MPZ and a high level of eosinophils are shown electrocardiogram and determination of serum troponin concentration. In case of deviations from the norm at the beginning of treatment for 1-2 weeks, simultaneously with imatinib, prophylactic administration of systemic corticosteroids (at a dose of 1-2 mg / kg) is possible.

Less than 3% of patients with CML show a significant increase in bilirubin and transaminase levels (the duration of such episodes is on average 1 week). In this case, a decrease in the dose of Filachromin or its temporary cancellation is required.

Patients who have undergone thyroidectomy and are receiving replacement therapy with levothyroxine sodium, during anticancer therapy, should periodically determine the concentration of thyroid-stimulating hormone, since there is a risk of hypothyroidism.

Influence on the ability to drive vehicles and complex mechanisms

Given the likelihood of side effects from the organ of vision and the nervous system (for example, blurred vision, dizziness, fainting), during the period of treatment, all patients are advised to observe precautions when performing potentially dangerous tasks.

Application during pregnancy and lactation

To date, there is no data on the clinical use of imatinib in pregnancy. It was found that the drug has a toxic effect on human reproductive function, however, the probable risks for the fetus are still unknown. In this regard, the use of Filachromin is contraindicated for pregnant women, except in cases of vital necessity.

Women of reproductive age are recommended to use reliable contraceptives during the period of therapy and for at least 3 months after its completion.

Imatinib and its metabolites can be excreted in breast milk in small amounts. If during lactation antineoplastic therapy is required, breastfeeding should be discontinued.

Pediatric use

The drug Filachromin is not used to treat children under 2 years of age, since its safety and efficacy have not been established in this age group of patients.

With impaired renal function

Filachromin should be used with caution for the treatment of patients with concomitant severe renal impairment and patients undergoing regular hemodialysis procedures. The initial recommended dose is 400 mg, if necessary, it is further adjusted: it is increased if the effect is insufficient or reduced if the therapy is poorly tolerated.

For violations of liver function

Filachromin should be used with caution for the treatment of patients with concomitant severe hepatic impairment. The recommended daily dose is 400 mg. It should be reduced if toxic effects develop.

Use in the elderly

No dosage adjustment is required.

Drug interactions

In the case of the combined use of high doses of chemotherapeutic drugs, the development of transient hepatotoxicity (increased activity of hepatic transaminases, the development of hyperbilirubinemia) is possible.

When combining imatinib with chemotherapy regimens with potentially hepatotoxic effects, careful monitoring of hepatic function is required.

With the simultaneous use of drugs that inhibit the CYP3A4 isoenzyme of cytochrome P ₄₅₀ (for example, erythromycin, itraconazole, ketoconazole, clarithromycin), an increase in the plasma concentration of imatinib is possible. Take special care.

In the case of joint administration of drugs that induce CYP3A4 (for example, dexamethasone, rifampicin, drugs based on St. John's wort, antiepileptic drugs - carbamazepine, oxcarbazepine, phenobarbital, phenytoin, primidone, phosphenytoin), it is possible to accelerate the metabolism of imatinib and reduce its concentration.

Imatinib, due to inhibition of CYP3A4, increases the level of simvastatin in the blood. Care must be taken when prescribing CYP3A4 substrate drugs with a narrow range of therapeutic concentrations (pimozide, cyclosporine) in combination. Imatinib is capable of increasing serum levels of other drugs metabolized by CYP3A4: dihydropyridines, triazolo-benzodiazepines, calcium channel blockers, most HMG-CoA reductase inhibitors, including statins.

In vitro, the drug inhibits CYP2C19 and CYP2C9, as well as O-glucuronidation of paracetamol. There is a known case of development of acute liver failure with a fatal outcome in a patient taking paracetamol simultaneously with imatinib. In this regard, special care is required.

In vitro, imatinib inhibits the CYP2D6 isoenzyme at the same concentrations as it inhibits CYP3A4. It must be assumed that the effects of concomitantly used drugs, which are a substrate of CYP2D6, may be enhanced.

Imatinib, applied at 400 mg 2 times a day simultaneously with metoprolol (a substrate of the CYP2D6 enzyme), slightly reduced the metabolism of the latter, which was accompanied by an increase in its Cmax and AUC by about 21%. However, the intensification of the effects was of a moderate nature, so no dose adjustment was required.

In patients receiving warfarin, imatinib may increase prothrombin time. If it is necessary to use coumarin derivatives, at the beginning and at the end of taking imatinib, as well as when changing its dose, prothrombin time should be monitored. Alternatively, it is recommended to consider the appointment of low molecular weight heparin derivatives.

Analogs

Filachromin's analogs are Albitinib, Bozulif, Vargatef, Giotrif, Gleevec, Dasatinib, Zelboraf, Imbruvika, Imatib, Imvek, Inlita, Caprelsa, Xalkori, Neopax, Ninlaro, Risarg, Stivarga, Tayverblot, Tafinblarisso, Erwin

Terms and conditions of storage

Storage conditions recommended by the manufacturer: temperature - no more than 25 ° С, place - protected from light, out of reach of children.

Shelf life of the drug: 2 years.

Terms of dispensing from pharmacies

Dispensed by prescription.

Reviews about Filachromin

Reviews of Filachromin are rare, which is probably due to serious indications for which it is prescribed. This drug is a domestic analogue of the well-known Swiss drug Gleevec. Patients respond positively to this generic: it is tolerated no worse than the original, the effectiveness is similar, and the cost is an order of magnitude lower.

There are reports of the development of side effects, which are usually mild and do not require discontinuation of treatment.

The price of Filachromin in pharmacies

On average, the price of Filachromin for a pack of 120 capsules of 100 mg is 6399 rubles.

Filachromin: prices in online pharmacies

Drug name

Price

Pharmacy

Filachromin 100 mg capsules 120 pcs.

RUB 2099

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Filachromin capsules 100mg 120 pcs.

2292 RUB

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Maria Kulkes Medical journalist About the author

Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".

Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!