Geftinat Gefitinib (Geftinat – Gefitinib) from Natco Pharm. Description of the drug.
Geftint Geftinat (Gefitinib 250mg – Gefitinib 250mg) description of the drug and Geftinat Geftinib 250mg price in India.
* Brand name: Geftinat
* Active ingredients: Gefitinib 250 mg
- Manufacturer: NATCO
- Country of origin: India
* Package: 250mg (30 tablets)
Gefitinib is a selective inhibitor of epidermal growth factor receptors tyrosine kinase, the expression of which is observed in many solid tumors inhibits the growth of various lines of human tumor cells, metastasis and angiogenesis, as well as accelerates tumor cell apopto.sis, increases antitumor activity of chemotherapy drugs, radiation and hormonal therapy
1 tablet contains 250 mg of gefitinib;
Auxiliary substances: lactose, microcrystalline cellulose, sodium croscarmellose, sodium lauryl sulfate, polyvinylpyrrolidone K-30, magnesium stearate E-5, polyethylene glycol 300, titanium dioxide, iron oxide red, iron oxide yellow.
Antineoplastics funds (inhibitor proteincontaining). ATC code L01XX31.
Gefitinib is a selective inhibitor of epidermal growth factor receptors tyrosine kinase, the expression of which is observed in many solid tumors inhibits the growth of various lines of human tumor cells, metastasis and angiogenesis, as well as accelerates tumor cell apoptosis, increases antitumor activity of chemotherapy drugs, radiation and hormonal therapy.
After ingestion absorbed relatively slowly. Bioavailability is 59%. Food intake does not affect bioavailability. With pH of gastric juice above 5, bioavailability of gefitinib decreases by 47%. A steady state of plasma concentration (Css) is achieved after taking 7-10 doses. Regular use of the drug 1 time a day leads to an increase in the concentration of 2-8 times compared with a single reception. Time to reach the maximum concentration in blood plasma (TCmax) – 3-7 hours. The volume of gefitinib distribution at Css-1400 l, which indicates the extensive distribution of the drug in the tissues. Communication with plasma proteins (albumin and alpha 1-glycoprotein) – about 90%. Undergoes oxidative metabolism by the enzyme CYP3A4 of cytochrome P450. In vitro slightly inhibits the enzyme CYP2D6. The metabolism of gefitinib happens 3 ways: the metabolism of N – propellerdriven group, demethylation metaxylene group on chinazoline part and oxidative dephosphorylation galogenirovannami phenyl groups. The main metabolite, which is determined in the blood plasma, the Pro – desmethylation, which has 14 times less pharmacological activity compared with gefitinib relative to the cell growth stimulated by epidermal growth factor, which suggests that a significant impact on the clinical activity of gefitinib unlikely. Total clearance of gefitinib – about 500 ml / min. the elimination half-life (T1 / 2) – 41 hours Excreted mainly in faeces; the renal output of less than 4% of the administered dose. With moderate hepatic insufficiency, pharmacokinetics does not change significantly. In severe liver failure due to metastases in the liver Css is similar to that, as in normal liver function.
Locally advanced or metastatic non-small cell lung cancer, refractory to chemotherapy regimens containing platinum derivatives and docetaxel.
Method of application and doses
Inside, 250 mg 1 time per day regardless of the meal. Tablet Getinfo 250 can be dissolved in 100 ml of drinking (non-carbonated) water. Other liquids cannot be used. For the correct dissolution, it is necessary to lower the tablet into the water without kneading, stirring until completely dissolved (about 10 minutes) and immediately drink the resulting solution. Pour another 1/2 Cup of water, washing the walls and drink the resulting solution. The solution can be prescribed through naso-gastral probe.
Most often (20%) are observed such adverse reactions when taking Getinfo 250: diarrhea, skin (including acne) rash, itching, dry skin. Of course appear during the first month of the drug and, as a rule, reversible. 8% of patients had serious adverse reactions (3 to 4 degrees of severity according to the General toxicity criteria), but only 1% of patients stopped therapy due to adverse reactions.
Very often (more than 10%); often (more than 1 and less than 10%); not often (more than 0.1 and less than 1%); rarely (more than 0.01 and less than 0.1%); very rarely (less than 0.01%).
From the hematopoietic organs: often-hematuria, nasal bleeding; not often-hypocoagulation and / or an increase in the frequency of bleeding during warfarin administration.
From the digestive system: very often-diarrhea (in some cases expressed), nausea often – vomiting, anorexia, stomatitis, dehydration, asymptomatic increase in the activity of “hepatic” transaminases; rarely – pancreatitis.
On the part of the organ of vision: often – conjunctivitis, blepharitis; rare – reverse erosion of the cornea, impaired the growth of eyelashes.
From the respiratory system: rarely – interstitial pneumonia (3 – 4 degrees of toxicity, up to death).
From the skin: very often – a rash (pustular), itching, dry skin against the background of erythema; often – nail changes, alopecia is very rare – toxic epidermal necrolysis and multiform exudative erythema.
very rarely-angioneurotic edema, urticaria.
Hypersensitivity, pregnancy, lactation, childhood and adolescence (safety and efficacy are not established.
Symptoms: increased frequency and severity of adverse reactions, mainly diarrhea and skin rashes. Treatment is symptomatic. The antidote is unknown.
Be wary appoint Getint 250 idiopathic pulmonary fibrosis, interstitial pneumonia, pneumoconiosis, post-radiation pneumonia, pneumonitis the drug (marked by elevated levels of mortality from these diseases during the treatment of prepart) the increased activity of “liver” transaminases.
On the background of treatment with 250 Geminatum been cases of interstitial lung disease (including fatalities). With an increase in symptoms such as shortness of breath, cough, fever, the use of the drug should be discontinued immediately and the survey. If the patient confirms the presence of interstitial pulmonary disease, the drug is stopped and prescribed appropriate treatment.
Against the background of treatment, there was an asymptomatic increase in liver transaminases, in connection with which it is necessary to periodically monitor liver function. In marked elevation of transaminases use Getinfo 250 should be discontinued.
Patients taking warfarin should regularly monitor the prothrombin time.
With the appearance of any symptoms on the part of the visual organs or with the development of severe or prolonged diarrhea, nausea, vomiting or anorexia, the patient should immediately consult a do When using Getinfo 250 in combination with radiotherapy as first-line therapy in children with brainstem glioma or incompletely remote with glioma of supratentorial localization were reported 4 cases (one fatal) hemorrhage in the brain. Another case of cerebral hemorrhage was observed in a child with Ependymoma during monotherapy with gefitinib. In patients with small cell lung cancer in the treatment Geminata 250 similar side effects were recorded.
Women of childbearing age and men should use reliable contraceptive methods during treatment and at least 3 months after treatment.
During the reception, Pettinato 250 care must be taken when driving and when working with equipment.
Interaction with other drugs
Getint 250 enhances the neutropenia caused by the use of Vinorelbine. Rifampin (potent inducer of CYP3A4) reduces the AUC of gefitinib by 83%. Itraconazole (CYP3A4 enzyme inhibitor) increases AUC (area under the concentration / hour curve) of gefitinib by 80%, which can be clinically significant. Medicines significantly and for a long time increase the pH of gastric contents, reduce the AUC of gefitinib by 47%. Drugs-inducers of CYP3A4 isoenzyme (phenytoin, carbamazepine, barbiturates, St. John’s wort tincture) can increase metabolism and reduce the concentration of gefitinib in blood plasma, which can lead to a decrease in its effectiveness. Concomitant administration with metoprolol (a substrate for CYP2D6) led to a slight increase (by 35%) in the concentration of metoprolol, which is not clinically significant.
Store in a dry, protected from light place at temperature not exceeding 250 C. the Drug should be stored out of reach of children.