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Tape
Antineoplastic antineoplastic Tasignon based on protein kinase inhibitor nilotinib.
Indications of the tape
Apply Tacos in the following cases:
- for treatment for the first time of the detected chronic course of myeloid leukemia in adults with characteristic chromosomal translocation;
- for treatment for the first time of the detected chronic and accelerated course of myeloid leukemia in adults with characteristic chromosomal translocation, as well as with habituation or hypersensitivity to the previous therapeutic regimen (including, in particular, imatinib treatment).
Release form
It is produced in a capsized form:
- dense capsules 150 mg are the reddish forms with an inscription black color NVR and BCR;
- dense capsules 200 mg are yellowish forms with the inscription red in color NVR and TKI.
Capsules contain a powdery substance of a whitish-yellowish hue.
The blister plate contains four capsules of 150 mg each, or four or four capsules of 200 mg each. A pack of cardboard holds 2-7 blister plates.
Active ingredient of Tasigne is nilotinib g / x monohydrate.
Pharmacodynamics
Tasign is a potent drug that inhibits the activity of Abl oncoprotein Bcr-Abl acting in successive generations of cellular structures and primary positive for the Philadelphia chromosome of leukemia-affected cells.
Taxon forms a dense bond in the ATP binding zone, forming the strongest inhibitor of Bcr-Abl, and continues to be active against 32 mutant imatinib-resistant Bcr-Abl species.
As a result of biological and chemical activity, Tasex selectively inhibits proliferative changes and induces apoptosis processes in successive cell generations and in primary positive leukemia-affected cells isolated from patients with chronic myeloid leukemia.
Taposignificantly affects, or does not affect the vast number of protein kinases, including serine protein kinase. The only exception is platelet FR, receptor tyrosine kinase activity and efrinoreceptor kinases: Tazosin inhibits them at the level observed after oral administration of the therapeutic dose of the drug.
Pharmacokinetics
Limit content of Taws in the blood is observed for 3 hours after oral administration of the capsules. Absorption may be about 30%. When you use Taksi in conjunction with food, the maximum content of the drug in the blood rises. With the use of Tasign in half an hour or 2 hours after meals, the bioavailability of the medication is increased by 29 or 15%, respectively. Absorption of Tacos may be disturbed in patients undergoing gastrectomy surgery or partial gastrectomy.
The binding to plasma proteins may be about 98%.
The basic ways of metabolism of Tasign are the processes of oxidation and hydrooxidation. The main ingredient in the blood serum is nilotinib.
After a single-dose dose, more than 90% of the drug is excreted throughout the week, with mostly caloric masses.
The expected half-life, calculated to determine the kinetic properties of the multiple Tasigne techniques, was 17 hours.
Exposure of the active ingredient of Tasigne in a state of equilibrium is considered dose-dependent. The equilibrium is reached most often on the eighth day. The increase in serum exposure of nilotinib between the intake of the initial dose and the onset of equilibria was twice taken once a day, or 3.8-fold when taking Tasox twice a day.
Use of the tape during pregnancy
Studies have proven the reproductive toxicity of Tasign, therefore, this medication can not be used to treat pregnancy: there is a high risk of complications for the fetus.
Patients of childbearing age in the treatment of Tasign should use reliable contraceptives. Their use continues for two weeks after the end of therapy.
Experiments on animals have shown that Tasea enters the breast milk. For this reason, do not use this medication during the entire period of breastfeeding.
Contraindications
Specialists do not advise appointing Taksi:
- during pregnancy;
- at thoracal feeding;
- in pediatrics (children under 18 years);
- with a shortage of lactase, with disturbed absorption of glucose-galactose, with galactose hypersensitivity;
- with a tendency to allergies to Taxon.
Relative contraindications are:
- decompensated and severe heart damage;
- complicated liver pathology;
- pancreatitis.
Side effects of the tape
Tapox therapy may be accompanied by some side effects:
- infectious complications in the form of folliculitis, pharyngitis, pneumonia, herpes, thrush, gastroenteritis;
- cutaneous papilloma;
- thrombocytopenia, anemia, neutropenia;
- dysfunction of the thyroid gland;
- emaciation, electrolyte exchange disorders, diabetes mellitus, impaired appetite;
- pain in the head, dizziness, neuropathy, trembling in the limbs, migraine;
- sleep disturbances, anxiety, depressive conditions;
- hemorrhage into the retina, conjunctivitis, impairment of visual function;
- vertigo;
- heart rhythm disorders, angina pectoris, tachycardia, increased blood pressure, disruption of blood coagulation;
- shortness of breath, bleeding from the nose, chest pain, pulmonary edema;
- nausea, upset of the chair, pain in the stomach, thirst, jaundice;
- hyperhidrosis, redness and rash on the skin, impaired pigmentation, the appearance of blisters and cysts on the skin;
- pain in the muscles and joints, pain in the hands and feet;
- disturbances of urination;
- pain behind the sternum, erectile dysfunction, enlargement of the mammary glands;
- a feeling of fatigue, swelling, fever, hot flashes.
Dosing and administration
Capsulated medication Tasone is recommended for admission twice a day (once in 12 hours), 2 hours after eating. After taking the capsules, you can not eat more than sixty minutes.
Tapos are washed down with water, not crushing or emptying the capsules. The exception is patients who have problems with swallowing food: they are allowed to dilute the powder from the capsules in 1 tsp. Apple puree.
If the patient accidentally misses taking Taksi, then no additional capsule should be taken: the next prescribed dosage of Tasigne is taken.
Before the start of therapy, the patient is required to carry out an ECG and determine the quantitative content of potassium and magnesium in the bloodstream.
The standard amount of Tasign is determined in a dosage of 300 mg of medication twice a day - 2 capsules with a dosage of 150 mg. If the doctor prescribed 400 mg twice a day, then use capsules with a dosage of 200 mg.
The duration of the Tasigna is determined by the clinical effect of the drug.
Overdose
There are information about several cases of deliberate overdose of Taksin, as well as cases of combination of a drug with alcoholic beverages or other drugs. In the listed situations, symptoms such as neutropenia, emetic seizures and loss of strength were noted. The liver and heart were not controlled. The death of patients after episodes of an overdose was not noted.
If there is a suspicion that the patient receives too much of Tasign, it is recommended to perform a thorough diagnosis of the functionality of the body, then prescribe symptomatic and supportive therapy.
Interactions with other drugs
- Medicamental substances that can increase the concentration of Thyssin in the blood serum:
- imatinib;
- ketoconazole, voriconazole, ritonavir, intraconazole, telithromycin, clarithromycin.
- Medicinal substances that lower the concentration content of Taxol in the blood serum:
- inducers of the isoenzyme CYP3A4 (phenytoin, phenobarbital, rifampicin, carbamazepine, preparations of St. John's wort).
- It is allowed to prescribe a tasone in combination with warfarin, the anti-coagulation properties of which do not suffer. The use of taoxa with midazolam leads to a slight increase in the concentration of the latter, but the degree of metabolism of midazolam did not change.
- Tazsone is not prescribed in combination with antiarrhythmic drugs, which include amiodarone, sotalol, quinidine, procainamide, as well as with preparations that detect quality of the QT interval (pimozide, methadone, chloroquine, clarithromycin, etc.).
- It is not recommended to take Taxos with food, as this leads to an increase in the serum concentration of nilotinib.
- It is not recommended to take Tasigne with grapefruit juice and medicines that inhibit the isoenzyme CYP3A4.