Xefta 250mg (Gefitinib)
Description of Xefta 250mg (Gefitinib 250mg)
Xefta 250mg (Gefitinib 250mg) tablets are categorized as kinase inhibitor, which exhibits anti-cancer activity by undergoing mechanism like protein kinase inhibition, the main ingredient which is used as Gefitinib Iressa. Xefta 250mg (Gefitinib 250mg) contains an active compound known as Gefitinib Iressa which is chemically known as anilinoquinazoline which contains anti-neoplastic effects. Xefta 250mg (Gefitinib 250mg) is a FDA approved product, manufactured by Natco pharma.
INDICATIONS of Xefta 250mg (Gefitinib 250mg)
Xefta 250mg (Gefitinib 250mg) is considered as first line therapy in non-small cell lung carcinoma in metastatic stage, tumor cell containing epidermal growth factor receptors like exon 19 deletion or exon 21 substitution mutations which is identified by FDA approved test.
MECHANISM OF ACTION of Xefta 250mg (Gefitinib 250mg)
Cancer cells expressed epidermal growth factor receptors on their cell surface, occurred in both healthy and cancer infected cells. These receptors involved in development of cell growth and multiplication. Some epidermal growth factor receptors have stimulating mutations (changes) within non small cell lung cancer cells which are providing encouragement to cancer cell growth, blockade of apoptosis occurs, which may elevates angiogenic factors and promoting metastasis process. Xefta 250mg (Gefitinib 250mg) containing Gefitinib causes unstable inhibition of tyrosine kinase and triggering variation of EGFR, hindering the autophosphorylation of tyrosine debris related with receptor, through prohibits following signaling and blockade EGFR dependent multiplication
ADME OF ACTION of Xefta 250mg (Gefitinib 250mg)
The mean bioavailability of Gefitinib Iressa is 60% The peak plasma concentration time of Gefitinib is reaches within 3 to 7 hours after drug intake Gefitinib Iressa is distributed throughout the body and causes steady state volume of distribution in 1400L The human plasma protein bound of Gefitinib is occurs as 90%. The metabolism of Gefitinib Iressa is occurs through hepatically, by using CYP3A4. Three sections of biotransformation occurs in metabolism of Gefitinib includes as; 1. Metabolism of N-propoxymorpholino group 2. Methoxy substituent on quinazoline demethylation occur 3. Halogenated phenyl group undergoes oxidative defluorination The major active metabolite of Gefitinib is O desmethyl Gefitinib which is formed by CYP2D6 metabolism. Gefitinib Iressa is cleared away with the help of liver, with half life elimination occurring within 48 hours. The steady state plasma concentration is accomplished within 10 days after daily single dose. The elimination of Gefitinib Iressa is occurs through feces with the range of 86% and renal elimination also occurred with less than 4%. Drug- Drug interaction causing alteration in pharmacokinetic properties: Co administration of Xefta 250mg (Gefitinib 250mg) with strong CYP3A4 inducers like rifampicin causes reduction in mean AUC of Gefitinib Iressa by 83%. Concurrent use of Xefta 250mg (Gefitinib 250mg) tablet with CYP3A4 inhibitor like itraconazole leads to elevation of AUC by 80%. Co administration of drugs which affecting gastric pH like ranitidine with sodium bicarbonate, which may causes decreasing the AUC by 47%. Metoprolol is a substrate of CYP2D6, increasing the exposure by 30% which is given on day 15 Gefitinib therapy with solid tumors.
SIDE EFFECTS of Xefta 250mg (Gefitinib 250mg)
The major adverse effect of Xefta 250mg (Gefitinib 250mg) tablets occurs as; Liver toxicity, Gastrointestinal perforation, Severe diarrhea, Bullous & expoliative skin disorders, Ocular disorders, Interstitial lung disease.
The most common side effects are; Headache, Diarrhea, Fatigue, Respiratory failure occurs due to pneumonia & pulmonary embolism, Nausea, Vomiting, Skin reactions, Nail disorders, Stomatitis, Loss of appetite,, Conjunctivitis, Blepharitis, Dry eye, Mucosal inflammation, tongue ulceration, eye irritation, eyelid Pruritus, edema, Elevation of AST, ALT, Proteinuria, Hemorrhagic cystitis, Cutaneous vasculitis .
PRECAUTION of Xefta 250mg (Gefitinib 250mg)
Interstitial lung disease: In this case, Xefta 250mg (Gefitinib 250mg) therapy is discontinue and rapidly examine for ILD in any patients who have acute respiratory problems. Liver toxicity: Patient receiving Xefta 250mg (Gefitinib 250mg) tablets have a chance to elevate AST & ALT levels and increased bilirubin levels cause hepatotoxicity and to recover from this condition discontinue the therapy. Gastrointestinal perforation: For this condition, stop the therapy permanently. Persistent diarrhea: Discontinue the therapy with Xefta 250mg (Gefitinib 250mg) Ocular disorders: Ocular disorders like corneal erosion, aberrant eyelash growth may occur during the therapy of Xefta 250mg (Gefitinib 250mg), discontinue the Xefta 250mg (Gefitinib 250mg) therapy. Skin disorders: It includes Stevens Johnson’s syndrome, epidermal necrolysis & Erythema multiforme formed during the therapy. In this case, Xefta 250mg (Gefitinib 250mg) therapy should be postponed or discontinued. Embryo fetal toxicity: Gefitinib causes fetal harm, like fetotoxicity and neonatal death. Avoid this therapy in pregnant women and use effective contraception methods.
DRUG INTERACTION of Xefta 250mg (Gefitinib 250mg)
Strong CYP3A4 inducers:
In combination with Xefta 250mg (Gefitinib 250mg) tablets causes increasing the metabolism of Gefitinib Iressa and reducing the plasma concentration of Gefitinib. In this condition the dosage of Xefta 250mg (Gefitinib 250mg) is increased to 500mg and followed by 250mg for 7 days after stopping the CYP3A4 inducers like phenytoin, rifampicin or tricyclic anti depressants.
Strong CYP3A4 inhibitors:
Concurrent use with Xefta 250mg (Gefitinib 250mg) tablets leads to cause decreasing the metabolism of Gefitinib Iressa and increasing the plasma concentration of Gefitinib. Avoid this concomitant otherwise monitor the patients frequently who are receiving this combinational therapy.
Drugs increasing gastric pH:
Co administration of Xefta 250mg (Gefitinib 250mg) tablets with proton pump inhibitors, antacids or histamine H2 receptor antagonist may leads to decrease the plasma concentration of Gefitinib. Xefta 250mg (Gefitinib 250mg) tablets are administered 12 hours after the last dose or 12 hours before the dose of proton pump inhibitors; Xefta 250mg (Gefitinib 250mg) should be taken 6 hours after or before the dose of H2 receptor antagonist or antacids. While taking warfarin in Xefta 250mg (Gefitinib 250mg) therapy causes increased risk of hemorrhage. To avoid this life threatening condition, patient should be monitored periodically for alteration in prothrombin time.
OVERDOSAGE of Xefta 250mg (Gefitinib 250mg)
There is no distinct therapy for over dosage of Gefitinib Iressa, if over dosage occurs provide supportive care and monitor the patients frequently for the signs and symptoms of over dosage of Gefitinib.
PREGNANCY of Xefta 250mg (Gefitinib 250mg)
Pregnancy category: D Xefta 250mg (Gefitinib 250mg) tablets should not be recommended during pregnancy period Xefta 250mg (Gefitinib 250mg) causes fetal harm, even to death. Xefta 250mg (Gefitinib 250mg) causes miscarriage during pregnancies in some population.
LACTATION of Xefta 250mg (Gefitinib 250mg)
Breast feeding should not be recommended.
GERIATIC of Xefta 250mg (Gefitinib 250mg)
The safety of the drug Gefitinib Iressa should not be evaluated in geriatric patients with the age of 65 years and above.
DOSAGE of Xefta 250mg (Gefitinib 250mg)
The usual prescribed dosage of Xefta 250mg (Gefitinib 250mg) tablets are 250mg should be given orally as a single dose by administering with or without food continuously. If patient feel difficult for swallow the tablets, must immerse the tablets with 4 to 8 ounces of water and mix it well for relatively 15 minutes. Take the solution immediately through naso-gastric tube.
STORAGE of Xefta 250mg (Gefitinib 250mg)
The storage of Xefta 250mg (Gefitinib 250mg) tablet container should be kept at 20℃ to 25℃ (68℉ to 77℉). Protect the container from moisture, heat and light.
MISSED DOSE of Xefta 250mg (Gefitinib 250mg)
if a single dose is missed, have the drug probably soon Next dose time reaches then leave the missed dose and continue the regular schedule Please consult with the doctor.
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