A Geftinat tablet has an active component called Gefitinib, used for lung cancer like non-small cell lung cancer. Gefitinib is an EGFR inhibitor, acts by interfere with signal transduction of epidermal growth factor receptor in tumor cells. Gefitinib is active only in cancer with mutated and hyper active EGFR. Gefitinib is classified as a prime discriminating inhibitor of epidermal growth factor receptors tyrosine kinase domain.
Geftinat tablets are used in non-small cell lung cancer as a first line therapy, in which cancer cells have EGFR like exon 19 deletions or exon 21 substitution mutations.
The suggested dosage of Geftinat tablets is 250mg should be administered orally as a single dose. The missed dose should not be taken within 12 hours of next dose
Stop the Geftinat therapy, if patients have any of the following effects such as;
Elevation of ALT & AST levels;
Severe ocular disorders like keratitis
High skin reactions
Acute upraising or aggravation of pulmonary symptoms like cough, fever, dyspnea
Brand Name :Geftinat
Active component : Gefitinib
Manufactured by :Natco pharma
Strength : 250mg
Packing : Pack of 30 Tablets.
The safety and effectiveness of Gefitinib in metastatic NSCLC whose cancer cell have EGFR alteration other than 19 deletions and exon 21 substitution mutations has not been established.
Geftinat tablets are administered orally by taking with or without food. If patients are unable to take the tablets through mouth, must disperse tablets in a 4 to 8 ounces of water and mix it well, then drink the liquid immediately or taken via naso-gastric tube.
Tumor cells asserted epidermal growth factor receptors on their cell surface, present in both active and cancer infected cells. These receptors complicated in advancement of cell growth and production. Some epidermal growth factor receptors have exciting mutations (changes) within non small cell lung cancer cells which are supposing to encourage cancer cell growth, restrict the apoptosis, which may raise angiogenic factors and develop metastasis process. Geftinat enclose Gefitinib causes erratic prohibition of tyrosine kinase and provoke abnormality of EGFR, block the autophosphorylation of tyrosine debris similar with receptor, via inhibition of following signaling and blockade EGFR dependent multiplication.
• Gastrointestinal perforation
• Interstitial lung disease
• Ulcerative keratitis
• Severe liver damage
Oral bioavailability: 60% Peak plasma concentration time: 3 to 7 hours
Volume of distribution: 1400L Human plasma protein bound: 90%
Geftinat is metabolized by hepatic, utilizing CYP3A4 Metabolism is occurring by undergoing biotransformation; • Metabolism of N-propoxymorpholino group • Methoxy substituent on quinazoline demethylation occur • Halogenated phenyl group undergoes oxidative defluorination An active metabolite of Gefitinib: O desmethyl Gefitinib by CYP2D6
Geftinat is metabolized by liver and eliminated through feces and urine. Half life period: 48 hours Steady state plasma concentration time: 10 days Elimination through; Feces: 86%; urine: less than 4%
Geftinat with strong CYP3A4 inducers: Reduction of AUC of Gefitinib by 83%. Geftinat with CYP3A4 inhibitor: Increase in AUC of Gefitinib by 80%. Geftinat with gastric regulators: Reduction in AUC of Gefitinib by 47%. Metoprolol (CYP2D6 substrate) with Geftinat: Increase in risk by 30%, preferred on day 15 of Gefitinib treatment with stable tumors.
Geftinat tablet combined with strong CYP3A4 inducers like phenytoin, rifampicin, or tricyclic depressant may leads to decreasing the plasma concentration of Gefitinib because of increasing the metabolism. To avoid this problem, while concomitant with these drugs, the dosage of Geftinat is increased to 500mg, maintained by 250mg for 7 days after stopping the CYP3A4 inducers. Co administration of Geftinat with strong CYP3A4 inhibitors like itraconazole causes elevating the plasma concentration of Gefitinib due to decreasing in metabolism. Geftinat combined with gastric regulator, causes depletion of plasma concentration of Gefitinib. Gastric regulators like proton pump inhibitors, H2 receptors antagonist, or antacids. Geftinat tablets are taken 12 hours after the last dose or 12 hours earlier to proton pump inhibitors; Geftinat tablets taken at 6 hours after or earlier to the dose of H2 receptor antagonist or antacids. Geftinat with warfarin leads to produce hemorrhage, to avoid this problem patients monitored frequently for prothrombin time alteration.
The adverse effect of geftinat tablets;
Liver toxicity, Gastrointestinal perforation, Severe diarrhea, Bullous & expoliative skin disorders, Ocular disorders, Interstitial lung disease.
Interstitial lung disease:
Geftinat therapy is discontinued and immediately examine for ILD in any patients who have acute respiratory problems.
Patient getting Geftinat therapy, accidentally elevate AST & ALT levels and increased bilirubin levels leads to cause hepatotoxicity and to rescue from this condition discontinue the therapy.
Stop the Gefitinib therapy permanently.
Discontinue the Gefitinib therapy
Ocular disorders like corneal erosion, aberrant eyelash growth may occur during the therapy of Geftinat. To avoid this problem discontinue the Geftinat therapy.
Skin disorders like Stevens Johnson’s syndrome, epidermal necrolysis & Erythema multiforme formed during the therapy. Geftinat therapy should be suspended or break off.
Embryo fetal toxicity:
Gefitinib produce fetal harm, like fetotoxicity and neonatal death. Not recommended this therapy in pregnant women and use effective contraception methods.
Headache, Diarrhea, Fatigue, Respiratory failure occurs due to pneumonia & pulmonary embolism, Mucosal inflammation, tongue ulceration, eye irritation, eyelid Pruritus, edema, Elevation of AST, ALT, Proteinuria, Hemorrhagic cystitis, Cutaneous vasculitis , Nausea, Vomiting, Skin reactions, Nail disorders, Stomatitis, Loss of appetite, Conjunctivitis, Blepharitis, Dry eye.
The safety and effectiveness of Gefitinib has not been evaluated in pediatric patients and geriatric with the age of 65 years and above.
Breast feeding should not be suggested in lactating period.
There is no particular therapy evaluated for over dosage condition of Gefitinib. If over dosage occurs in a patients receiving therapy, must compensate with adequate supportive therapy and investigate the signs and symptoms of toxicity due to over dosage.
Geftinat tablet is a chemo medicine; it is used only under the supervision of medical oncologist. If patient fail to take the dose of Gefitinib must consult with certain medical adviser and take the missed dose. Otherwise the missed dose should not be taken within 12 hours of following dose. In this condition, skip the missed dose and follow the regular schedule.
Pregnancy category: D Geftinat produces fetal harm, even to death. Geftinat tablets should not be recommended in pregnancy period; sometimes it may leads to miscarriage.
Geftinat tablet container should be stored in room temperature at 20oC to 25oC (68oF to 77oF). Geftinat container should be keep away from light, heat and moisture.
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