Gefticip (Gefitinib 250mg)
Gefticip tablets correspond to the tyrosine kinase inhibitor,
Gefticip containing an active component known as Gefitinib, which is pharmacologically categorized as;
Epidermal growth factor receptor tyrosine kinase inhibitor.
Gefticip tablet indicated for
The therapeutic indication of Gefticip tablet is first line treatment in advanced non-small cell lung carcinoma.
The major demerit of Gefticip;
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.
Gefticip tablets pharmacological action
Gefticip 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.
Gefticip 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
Gefticip tablets dosage and administration
The usual dosage of Gefticip tablets; one tablet 250mg should be taken as a single dose.
Gefticip tablets should be administered with or without food.
Patients fail to take through mouth;
Gefticip tablets should be dispersed in water with the quantity of 4 to 8 ounces
After completely dissolves, immediately drink it or administered through the nasogastric tube.
Withheld the Gefticip tablets in the conditions like:
- Outbreak or aggravation of pulmonary symptoms
- Elevation of ALT & AST levels
- Higher worsening of diarrhea
- Skin reactions
Discontinue the Gefticip tablets during the conditions:
- Severe worsening of hepatic impairment
- Gastrointestinal perforation
- Ulcerative keratitis
- Interstitial lung disease
While combining strong CYP3A4 inducers with Gefticip tablets, the dosage of Gefticip should be varied 500mg of Gefticip should be recommended and continue with 250mg of Gefticip tablets for seven days after stopping the strong CYP3A4 inducers.
Gefticip 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.
Gefticip tablets overdosage
There is no special treatment preferred for the overdosage condition of Gefitinib. In case of overdosage providing patients with specific supportive measures and monitor the signs and symptoms periodically.
Gefticip tablets interact with some drugs
Gefticip combines with CYP3A4 inducers causes increasing in metabolism of Gefitinib leads to decrease the plasma concentration of Gefitinib
Gefticip combines with CYP3A4 inhibitors causes decreasing the metabolism of Gefitinib lead to increase the plasma concentration of Gefitinib
Gefticip combines with drugs regulating the gastric pH causes reducing the plasma concentration of Gefitinib
Gefticip combines with warfarin causes increasing the adverse bleeding effects, this may avoid by monitoring the prothrombin time or INR level of patients frequently.
During Gefticip therapy, grape fruit juice should not be taken causes elevation of plasma concentration of Gefitinib.
Gefticip 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
Gefticip tablets precautions
In interstitial lung disease: If patients acquiring ILD withheld or discontinue the Gefticip 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, Gefticip tablet should be withhold or discontinue if possible.
Embryo fetal damage: Using Gefticip tablets in pregnancy conditions, causes fetal harm. Avoid this usage during pregnancy and lactation
Gefticip tablets treatment usage in
Pregnancy category of Gefitinib D; it should not be used in pregnancy.
Milk feeding should not be recommended
Gefticip tablets missed Dose
Gefticip 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 Gefticip
Store the drug at 200C – 250C.
Keep away from children’s
- Trade name Gefticip
- Substance Gefitinib 250mg
- Manufacturer Cipla Limited
- Packaging 30 tablets
- Country of origin India