Geftinat (Gefitinib 250mg)
Geftinat tablets correspond to tyrosine kinase inhibitor. Geftinat containing an active component known as Gefitinib, which is pharmacologically categorized as, Epidermal growth factor receptor tyrosine kinase inhibitor.
Geftinat tablet indicated for
The therapeutic indication of Geftinat tablet is first line treatment in advanced non-small cell lung carcinoma.
The major demerit of Geftinat,
The potency and safeness of Gefitinib has not been evaluated in advanced non-small cell lung cancer patients, whose cancer cells have EGFR variation apart from exon 19 deletion or exon 21 altering variation.
Geftinat tablets pharmacological action
Geftinat tablets are anti-cancer drug, which is involved in mechanism for exhibiting anti-tumor activity against tumor cells.
Gefitinib exhibits its action by inhibiting epidermal growth factor receptor which is present on cell surface of cancer cells. These receptors are used for signaling transduction which is essential for cancer replication.
Hence the obstruction of receptors causing prohibition of multiplication, angiogenesis and induce apoptosis.
Geftinat tablets ADME properties
Bioavailability: 60%, not naturally varied by food; gastric pH alter the bioavailability of Gefitinib. If pH level is >5, causes reduced by 47%.
Peak plasma concentration time: 3 to 7hours
Volume of distribution for Gefitinib is 1400 to 1600L
Human plasma protein bound: 90%
Metabolism occurs through hepatically, producing an active metabolite O-desmethyl Gefitinib
Elimination occurs via <4% in urine; 86% in feces
The half-life period of Gefitinib 30.5 hours to 41 hours
Clearance value of Gefitinib 500ml/min
Geftinat tablets dosage and administration
The usual dosage of Geftinat tablets; one tablet 250mg should be taken as a single dose.
Geftinat tablets should be administered with or without food.
Patients fail to take through mouth,
Geftinat tablets should be dispersed in water with the quantity of 4 to 8 ounces
After completely dissolves, immediately drink it or administered through nasogastric tube.
Withheld the Geftinat tablets in the conditions like:
- Outbreak or aggravation of pulmonary symptoms
- Elevation of ALT & AST levels
- Higher worsening of diarrhea
- Skin reactions
Discontinue the Geftinat tablets during the conditions:
- Severe worsening of hepatic impairment
- Gastrointestinal perforation
- Ulcerative keratitis
- Interstitial lung disease
While combining strong CYP3A4 inducers with Geftinat tablets, the dosage of Geftinat should be varied 500mg of Geftinat should be recommended and continue with 250mg of Geftinat tablets for seven days after stopping the strong CYP3A4 inducers.
Geftinat should not be combined with gastric regulators while combining with proton pump inhibitors should be taken 12 hours after or before the dose of PPI; with H2 receptor antagonist 6 hours after or before the dose of H2 receptor antagonist.
Geftinat tablets overdosage
There is no special treatment preferred for the over dosage condition of Gefitinib. In case of over dosage providing patients with specific supportive measures and monitor the signs and symptoms periodically.
Geftinat tablets interact with some drugs
Geftinat combines with CYP3A4 inducers causes increasing in metabolism of Gefitinib leads to decrease the plasma concentration of Gefitinib
Geftinat combines with CYP3A4 inhibitors causes decreasing the metabolism of Gefitinib lead to increase the plasma concentration of Gefitinib
Geftinat combines with drugs regulating the gastric pH causes reducing the plasma concentration of Gefitinib
Geftinat combines with warfarin causes increasing the adverse bleeding effects, this may avoid by monitoring the prothrombin time or INR level of patients frequently.
During Geftinat therapy, grape fruit juice should not be taken causes elevation of plasma concentration of Gefitinib.
Geftinat tablets side effects
- Severe atrial fibrillation
- QT prolongation
- Peripheral edema
- Loss of body weight
- Dry skin
- Erythema multiforme
- Exfoliative dermatitis
- Nail disorders
- Increasing AST & ALT
- Abdominal pain
- Interstitial lung disease
- GI perforation
Geftinat tablets precautions
In interstitial lung disease: If patients acquiring ILD withheld or discontinue the Geftinat tablets immediately.
In hepatotoxicity: In case of elevation of AST & ALT levels, causing liver toxicity, to avoid this condition discontinue the therapy with Gefitinib.
In GI perforation: Permanently discontinue the therapy.
In diarrhea: Withheld or discontinue the therapy
Ocular disorders: In case of ocular disorders, treatment should be withheld or stop permanently.
Bullous & exfoliative skin disorders: In this condition, Geftinat tablet should be withhold or discontinue if possible.
Embryo fetal damage: Using Geftinat tablets in pregnancy conditions, causes fetal harm. Avoid this usage during pregnancy and lactation
Geftinat tablets treatment usage in
Pregnancy category of Gefitinib D; it should not be used in pregnancy.
Milk feeding should not be recommended
Geftinat tablets missed dose
Geftinat tablets should not be taken within 12 hours of next dose.
In case of missed dose occurred in patients, must be consult with medical oncologist.
Storage condition of Geftinat
Store the drug at 200C – 250C.
Keep away from children’s
- Trade name Geftinat
- Substance Gefitinib 250mg
- Manufacturer Natco Pharma Limited
- Packaging 30 tablets
- Country of origin India