Imatinib is a pharmaceutical in the fight against tumors in patients who can not be operated. It is prescribed as a targeted cytotoxic in chemotherapy.
A new generation drug with selective action against leukocytes that underwent genetic changes.
Composition, form and packaging
The preparation has an active substance with the same name of the preparation. The amount of active ingredient in tablets and capsules varies from 50 mg to 400.
Imatinib with 50 mg of active ingredient includes additional ingredients to facilitate absorption and dissolution of the mesylate( one of the forms of imatinib):
- hydroxypropylcellulose low-substituted( formulator) - 65.2 mg;
- low molecular weight polyvinylpyrrolidone in insoluble form( intestinal sorbent) - 0.285 mg;
- sodium carboxymethyl starch( thickener) - 21 mg;
- pyrogenic silicon dioxide in the form of a colloid( intestinal sorbent) - 1.9 mg;
- magnesium salt of stearic acid( excipient) - 1,035 mg.
To form the coating, the tablets are impregnated with iron oxides of yellow( 6.84 mg) and red( 0.36 mg) color( opadrai red and yellow).
Tablets with 50 mg of the active substance are brown in color with an orange tinge. Cardboard packaging includes 3 cellular plates of 10 tablets each. The shape of the tablets is round, with bulges on both sides and engraved "50".
Tablets with 100 and 400 mg of active substance are engraved on the surface with an indication of the amount of active substance. The quantitative and qualitative composition of the auxiliary substances has differences with tablets with 50 mg of mesylate.
Low molecular weight polyvinylpyrrolidone is found in two forms: crospovidone and povidone K30.As a sorbent in the intestine is used a soluble substance( biological analogue of silicon dioxide) - croscarmellose sodium. For better compression of the tablet substances, lactose is used that is dehydrated.
As a thickener, talc is included. As a dye of the tablet shell, opadrai red( E172), titanium dioxide, ethanediol polymer, hypromellose and talc are used. The color of the tablets with 100 and 400 mg of active ingredient is also brown, but with a pink tinge.
Tablets are distinguished by engraving, packed in blisters of 10 pieces or a can of polymeric materials. The number of tablets in the pot with 400 mg or 100 mg of active ingredient varies from 10 to 180( a total of 12 quantitative variants).
Imatinib Capsule includes 100 mg of mesylate, colloidal silica, crospovidone, magnesium stearate, dehydrated lactose. Packed gelatin capsules in the top ten in blisters. Number of blisters in a carton - 3 pieces.
Manufacturer
Packing, number of tablets in a honeycomb plate, the number of plates in the package may vary depending on the manufacturer.
More often than not the Russian pharmaceutical market includes domestic producers( Ozon OO and Biocad), Chinese( Shijiazhuang Ilin Pharmaceutical Co., Ltd.), the Republic of Belarus( Akademfarm RPMU), Israeli company TEVA.
Indications for use
Imatinib is used in the following cases:
- metastasis, recurrence or inability to perform surgery for dermatofibrosarcoma in patients of mature and advanced age;
- mastazatirovanii or the impossibility of carrying out the operation of malignant neoplasms on the organs of the digestive system in patients of mature and advanced age;
- in the presence of the Philadelphia chromosome with myelodic leukemia, which occurred for the first time in adult and pediatric patients;
- with insufficient effect of treatment with interferon α of chronic myeloid leukemia during exacerbation or progressing stage in patients of childhood and adulthood;
- lymphoblastic leukemia in the acute phase in patients of childhood and adulthood with chemotherapeutic treatment( with the existing Philadelphia chromosome);
- is a monotherapeutic agent in the treatment of relapses or refractory forms of acute lymphoblastic leukemia in adult patients;
- for cytopenic phenomena and the probability of degeneration of dysplastic processes into acute leukemia in adult patients;
- for fat-cell leukemia, if there is no mutation associated with the replacement of aspartic acid with 2-amino-3-butanoic acid at position 816( alternative - no mutation data) in adult patients;
- chronic eosinophilic leukemia in adult patients;
- additional treatment after removal of gastrointestinal stromal tumor.
Contraindications
Imatinib is not used only if hypersensitivity to one of the substances( active or supplemental) is detected. Hepatic impairment after taking Imtinib can intensify, so the dosage in this case is trying to pick up the minimum.
No contraindications for infants and toddlers are available.
Mechanism of action
Imatinib has a pronounced effect on malignant neoplasms. The pathological enzyme protein tyrosine kinase, produced by the disease, is inhibited by the drug.
Pathological development of the enzyme begins with the chronic form of myeloid leukemia in the mutation of the 22nd chromosome, which in medicine is known as the "Philadelphia chromosome".
The inhibition of protein tyrosine kinase inhibits the growth of platelets and stem cells. Imatinib is able to inhibit the process of cell death to apoptotic bodies and the proliferation of malignant cells of the digestive system.
Imatinib bioavailability is not lower than 98%.After ingestion, the active substance Imatinib immediately begins to be absorbed and reaches a maximum concentration in the blood after 3 hours. Delivered to target cells in a bound state with plasma proteins.
The half-life of the active substance is 18 hours, but the metabolic intermediates produced in the liver disintegrate within 40 hours. Approximately 2/3 of the metabolites are excreted by the digestive system, 1/3 by the kidneys.
The half-life of imatinib in the liver occurs with the participation of the enzymes of the Cytochrome P450 system( CYP3A4, CYP13A2, etc.).
Instructions for use Imatinib
Imatinib is used once a day by the oral route. Reception time is arbitrary. When taking the drug you need a sufficient amount of fluid - at least 0.2 liters. It is better to combine the drug with one of the daily meals.
Patients of adult age in the stage of recovery take 400 mg Imatinib per day. If a recurrence of hematologic parameters or a clinical progress is detected, the daily dose is increased by 1.5 times.
In the acute or crisis stage of leukemia, it is recommended to maintain a daily dose of 600 mg. In the absence of pronounced side effects and the progress of the disease, the drug intake is recommended to be divided into 400 mg twice a day during meals.
For pediatric patients, the dosage is selected based on 2 rules:
- the maximum daily dose for children should not exceed the standard dose for adults( 400 mg);
- the exact dosage is in direct proportion to the surface area of the child's body( mg / m2).
Side effects of
- Myalgia can be seen from the musculoskeletal system. Sometimes there are muscle spasms and cramps.
- On the part of the digestive system, a disorder accompanied by nausea and vomiting, diarrhea.
- On the skin of some patients, rash and hyperemic areas may be noted.
- Extremities are sometimes swollen.
Overdose
Experience with the use of an antitumor drug is few.
Imatinib over 600 mg administered for several days resulted in accumulation of fluid in the abdominal cavity, increase in the blood of creatinine, transaminases and bilirubin in the liver. With the abolition of Imatinib, hematological and clinical symptoms disappeared.
Experimental administration of a dose equivalent to 1600 mg per day for animals caused muscle cramps. Seizures disappeared after drug withdrawal.
Special instructions
For acute hepatic impairment, the drug should be temporarily discontinued. During the treatment, the liver is monitored continuously.
No data on the inability to use the drug for renal impairment.
The slight deterioration in vision accompanying Imatinib's reception, dizziness, creates an obstacle for driving a car.
Drug Interaction
Sharing Paracetamol increases the effectiveness of both drugs, which should be considered when choosing the dose of Imatinib. Cyclosporine and Warfarin, other inhibitors of one form of the enzyme reductase are more effective when taken together with Imatinib.
Erythromycin and Clarithromycin increase the blood levels of Imatinib, while Dexamethasone and Phenobarbital decrease.
Reviews
For side effects, patients respond to forums with the same share of positive and negative, since the effect of the drug is not the same on different organisms.
Price in Russia
Imatinib with a dosage of 100 mg has an initial cost of 17500 rubles( 30 tablets).Preparations with a higher dosage are more expensive.
The maximum cost is Imatinib capsules - 74600 rubles.
Analogues of Imatinib
Analogs of Imatinib are Imagliv, Neopox, Genfatinib, etc.
Synonyms of drug
Synonyms of medication are the trademarks under which Imatinib is known: Helvec, Zelboraf, Vovrient, etc.
Conditions for dispensing from pharmacies
The drug is dispensed only by prescription.
Storage conditions and shelf life
Imatinib and its analogs are stored in locations inaccessible to children. Storage conditions are preferable: no more than 25 degrees, in places protected from direct sunlight, with low humidity.
Imatinib is available for use for 24 months.