A Gefticip 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.
Gefticip tablets are used in non-small cell lung cancer as a first line therapy, in which ncancer cells have EGFR like exon 19 deletions or exon 21 substitution mutations. Gefticip tablets limitation in usage; 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.
The suggested dosage of Gefticip tablets is 250mg should be administered orally as a single dose. The missed dose should not be taken within 12 hours of next dose.
Gefticip 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.
Oral bioavailability: 60% Peak plasma concentration time: 3 to 7 hours
Volume of distribution: 1400L Human plasma protein bound: 90%
Gefticip 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
Gefticip 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%
Stop the Gefticip 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.
Gastrointestinal perforation, Interstitial lung disease, Ulcerative keratitis, Severe liver damage.
In concomitant with strong CYP3A4 inducers, the dosage is increased to 500mg; continue the Gefticip therapy with 250mg after cessation of strong CYP3A4 inducers
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. Gefticip 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.
Gefticip 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 Gefticip is increased to 500mg, maintained by 250mg for 7 days after stopping the CYP3A4 inducers. Co administration of Gefticip with strong CYP3A4 inhibitors like itraconazole causes elevating the plasma concentration of Gefitinib due to decreasing in metabolism. Gefticip combined with gastric regulator, causes depletion of plasma concentration of Gefitinib. Gastric regulators like proton pump inhibitors, H2 receptors antagonist, or antacids. Gefticip tablets are taken 12 hours after the last dose or 12 hours earlier to proton pump inhibitors; Gefticip tablets taken at 6 hours after or earlier to the dose of H2 receptor antagonist or antacids. Gefticip with warfarin leads to produce hemorrhage, to avoid this problem patients monitored frequently for prothrombin time alteration.
Gefticip with strong CYP3A4 inducers: Reduction of AUC of Gefitinib by 83%. Gefticip with CYP3A4 inhibitor: Increase in AUC of Gefitinib by 80%. Gefticip with gastric regulators: Reduction in AUC of Gefitinib by 47%. Metoprolol (CYP2D6 substrate) with Gefticip: Increase in risk by 30%, preferred on day 15 of Gefitinib treatment with stable tumors.
Patient getting Gefticip therapy, accidentally elevate AST & ALT levels and increased bilirubin levels leads to cause hepatotoxicity and to rescue from this condition discontinue the therapy.
Embryo fetal toxicity:
Gefitinib produce fetal harm, like fetotoxicity and neonatal death. Not recommended this therapy in pregnant women and use effective contraception methods.
Stop the Gefitinib therapy permanently.
Discontinue the Gefitinib therapy
Ocular disorders like corneal erosion, aberrant eyelash growth may occur during the therapy of Gefticip. To avoid this problem discontinue the Gefticip therapy.
Skin disorders like Stevens Johnson’s syndrome, epidermal necrolysis & Erythema multiforme formed during the therapy. Gefticip therapy should be suspended or break off.
Interstitial lung disease:
Gefticip therapy is discontinued and immediately examine for ILD in any patients who have acute respiratory problems.
Breast feeding should not be suggested in lactating period.
The safety and effectiveness of Gefitinib has not been evaluated in pediatric patients and geriatric with the age of 65 years and above.
Gefticip 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 Gefticip produces fetal harm, even to death. Gefticip tablets should not be recommended in pregnancy period; sometimes it may leads to miscarriage.
Gefticip tablet container should be stored in room temperature at 20oC to 25oC (68oF to 77oF). Gefticip container should be keep away from light, heat and moisture.
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