GEFTINAT
Drug profile of Geftinat
Geftinat 250mg tablets are cipla manufactured product which is endorsed by FDA with anti-neoplastic activity.
Geftinat 250mg containing active constituent known as Gefitinib is an inhibitor of epidermal growth factor receptor.
Geftinat 250mg is only powerful in tumor cells which get mutated & uncontrolled EGFR.
Geftinat 250mg is also characterized as single transduction inhibitor by intercede with EGFR. Geftinat 250mg Tablets is active against tyrosine kinase protein.
Chemically Gefitinib 250mg Tablets is categorized as anilinoquinazoline with anti-tumor activity.
Geftinat 250mg is pharmacologically classified as;
Anti-neoplastic agent
Epidermal growth factor signal transduction inhibitor
Tyrosine kinase inhibitor
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| GEFTINAT |
Brand name: Geftinat
Active substance: Gefitinib
Strength: 250mg
Mfg: Cipla
Pack: 30 tablets in a container
Classified as: EFGR inhibitor, kinase inhibitor or Anti-neoplastic agent
Prescribing information of Geftinat
Geftinat tablets are therapeutically indicated in the conditions like;
Non small cell lung cancer only suggested after the failure of therapies with platinum based compounds & docetaxel chemotherapies.
In adults, Geftinat is used for the treatment of long lasting advanced stage of non small cell lung cancer.
Geftinat is a first line therapy; used in NSCLC patients with EFGR exon 19 deletions or exon 21 mutations.
The potency of Gefitinib has not been evaluated completely in advanced NSCLC with EGFR exon 19 deletions or exon 21 mutations.
Mechanism of Geftinat
Geftinat containing Gefitinib expels anti-tumor activity.
Gefitinib works by prohibiting tyrosine kinase phosphorylation occurs intracellularly which is related to cell surface receptors.
Gefitinib acts on cell surface of tumors by interfering with signal transduction by epidermal growth factor receptor.
This signal transfer is responsible for tumor cell division, blockade of apoptosis & elevating the production of angiogenic factors which is inducing metastasis.
Finally the inhibition of signal transduction stops all these functions of tumor cells leads to lyses.
Absorption
The absorption of Geftinat occurs gradually and reaches peak plasma levels within 3 to 7 hours.
Food does not interfere with absorption, no chances occur in bioavailability
Distribution
Gefitinib is widely distributed in the body; the apparent volume of distribution is 1400L
Gefitinib is largely bound to human plasma protein with the range of 90%.
Metabolism
Gefitinib 250mg is a P-gp substrates, it undergoes metabolism hepatically with the help of CYP3A4.
During metabolism, biotransformation occurs it is follows as;
ü N-propoxymorpholino-group metabolism
ü Methoxy-substituent on the quinazoline demethylation
ü Halogenated phenyl group Oxidative defluorination.
Excretion
Elimination of Gefitinib 250mg occurs through;
86% through feces;
Less than 4% through urine
Gefitinib is cleared out by liver at first, reaches half life time in 48 hours.
The steady state levels reaches within 10 days.
When to take the Geftinat tablets
Geftinat 250mg tablets should be taken with or without food.
If patient fail to administer Geftinat 250mg tablet orally, tablet should be dissolved with 4 to 8 ounces of water and drink it or administer through naso gastric tube immediately after dispersion.
Dosage regimens of Geftinat
The usual prescribed dose of Geftinat 250mg tablets are 250mg tablet should be administered orally as a single dose until unpleasant toxicities occurs.
Dose alteration;
In some serious cases, the dose of Geftinat 250mg should be altered for reducing the adverse effects related to Geftinat
Conditions like;
Acute out breaking or aggravation of pulmonary syndromes like cough, fever, dyspnea
Increasing level of AST & ALT
Severe grade III diarrhea
Severe skin reactions
Severe ocular disorders
Postpone the therapy until improvement of these effects to grade II
Discontinue the treatment;
Geftinat tablets should be stopped under the conditions like;
ü Interstitial lung disease
ü Gastrointestinal perforation
ü Ulcerative keratitis
ü Hepatic damage
Dose variation occurs in drug interaction
While concurrent use of Geftinat with strong CYP3A4 inducers, the dose of Geftinat is increased to 500mg daily taken as a single dose and continue to take 250mg for 7 days after CYP3A4 inducers discontinuation.
In pediatric:
Geftinat tablets potency and effectiveness has not been identified in pediatric patients who are less than 18 years of age.
In hepatic impaired patients, the plasma concentration of Gefitinib gets elevated.
In renal impaired patients, dosage adjustment should not be suggested in CrCl >20ml/min.
Elder patients have poor liver & kidney mechanism, no dosage adjustment should be provided.
Geftinat caused side effects
Diarrhea
Skin reactions like rashes, Pruritus, dry skin, acne
Loss of weight
Anorexia
Conjunctivitis
Corneal erosion
Hemorrhage, Hematuria & Epistaxis
Nausea
Dehydration
Dry mouth
Elevation of AST & ALT
Nail disorders
Alopecia
Anaphylactic reactions
Increase in creatinine value
Proteinuria
Asthenia
Cystitis
Pyrexia
Drug - drug interaction of Geftinat
The major drug interaction occurs in Gefitinib therapy;
Geftinat combined with strong CYP3A4 inducers like rifampicin, anti-convulsants causes elevating the Gefitinib metabolism and depletes the Gefitinib concentration.
To avoid this problem, the dose of Geftinat should be increased to 500mg then continue the therapy with 250mg as a single dose after the discontinuation of CYP3A4 inducers drugs.
Geftinat tablets co administered with strong CYP3A4 inhibitors causes diminishing the Gefitinib metabolism leads to increase the plasma concentration.
Geftinat should not be co administered with gastric regulator drugs, causes reduction in plasma concentration of Gefitinib.
Administration of Geftinat tablets should be taken with the dosing interval of 6 hours after or before the H2 receptor antagonist.
Administration of Geftinat tablets should be taken with the dosing interval of 12 hours after or before the proton pump inhibitors.
Geftinat tablets combined with warfarin causes hemorrhage, to overcome this adverse patient’s prothrombin time or INR value must be monitored.
Geftinat combined with CYP2D6 substrate like metoprolol causes increasing the exposure of metoprolol.
Food drug interaction of Geftinat
Grape fruit juice should not be taken while patient receiving Geftinat tablets.
Citric acid, ascorbic acid containing fruits should not be taken.
This is because which will alter the absorption of Gefitinib.
Possible contraindications of Geftinat
Geftinat is contraindicated to pregnancy & lactating women
Some hypersensitivity reactions may produce due to patients contraindicated to the component of Geftinat tablets.
Safety measures of Geftinat
Valuation of epidermal growth factor receptor mutation status occurs frequently in the patients for better effectiveness. This is also used to prevent false negative or false positive identifications.
Pulmonary toxicity like interstitial lung disease, cough, and pulmonary edema may occur during the therapy, to avoid these risk cases postpone or discontinue the treatment with Geftinat tablets.
Gefitinib did not produce any genetic defects. Carcinogenesis, mutagenesis or fertility impairment may occur. Avoid getting pregnancy during the therapy with Geftinat.
Patient with Lapp lactose deficiency, galactose intolerance, or glucose-galactose malabsorption should not take this medication due to presence of lactose in Gefitinib
Abnormalities occurred in Hepatic function test like elevating bilirubin, AST & ALT causes liver injuries leads to death. This may prevent by frequent LFT analysis.
Patients should know the precaution in case of;
Diarrhea, nausea, vomiting may leads to dehydration must get medical advice
Geftinat with NSAIDS causes GI perforations
Severe ocular disorders like keratitis, conjunctivitis may occur
Ulcerative keratitis
For all these following risk factors, Geftinat tablets should be discontinued and take supportive measures.
Pregnancy and lactation
Pregnancy category of Gefitinib D
Geftinat tablets should not be prescribed for pregnancy condition
Breast feeding should not be allowed, contraindicated
Storage and handling
Geftinat tablet container should be kept in cool & dry place with controlled temperature of 20oC to 25oC.
Protect the container from moisture, heat & light
Missed dose
Patients do not take the missed dose of Gefitinib within 12 hours of next dosing schedule.
Patient should skip the missed dose
Over dosage
There is no special treatment for over dosage of Gefitinib is applicable.
In case of over dosage, patient must be provided with supportive measures.
Due to over dosage, patient may suffer with severe diarrhea, skin reactions.
Avoid missed dose.
In this condition discontinue the Geftinat therapy
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