Dosage adjustment
- Elevation of ALT & AST levels;
- Stop the Geftinat therapy, if patients have any of the following effects such as;
- High skin reactions
- Severe ocular disorders like keratitis
- Acute upraising or aggravation of pulmonary symptoms like cough, fever, dyspnea
Geftinat 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.
Administration
- 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.
- Geftinat tablets are administered orally by taking with or without food.
- If patients are unable to take the tablets through mouth,
Geftinat tablets works as
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. Tumor cells asserted epidermal
growth factor receptors on their cell surface, present in both active and cancer infected cells.
prohibition of tyrosine kinase and provoke abnormality of EGFR, block the autophosphorylation
oftyrosine debris similar with receptor, via inhibition of following signaling and blockade EGFR
dependent multiplication.
Geftinat therapy should be discontinuing forever; in case of
• Gastrointestinal perforation
• Interstitial lung disease
• Ulcerative keratitis
• Severe liver damage
Pharmacokinetics
Absorption :
Oral bioavailability: 60% Peak plasma concentration time: 3 to 7 hours
Distribution:
Volume of distribution: 1400L Human plasma protein bound: 90%
Metabolism:
Geftinat 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
Excretion:
Geftinat 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%
Drug- Drug interaction causing variation in
pharmacokinetic properties
Geftinat with strong CYP3A4 inducers: Reduction of AUC of Gefitinib by 83%. Geftinat with
CYP3A4 inhibitor:
Increase in AUC of Gefitinib by 80%. Geftinat with gastric regulators: Reduction in AUC of
Gefitinib by 47%. Metoprolol (CYP2D6 substrate) with Geftinat: Increase in risk by 30%,
preferred on day 15 of Gefitinib treatment with stable tumors.
drug interaction
Geftinat tablet combined with strong CYP3A4 inducers like phenytoin, rifampicin, or tricyclic
depressant may leads to decreasingthe plasma concentration of Gefitinib because of increasing
the metabolism. To avoid this problem, while concomitant with these drugs,the dosage of Geftinat
is increased to 500mg, maintained by 250mg for 7 days after stopping the CYP3A4 inducers.
Co administration of
Geftinat with strong CYP3A4 inhibitors like itraconazole causes
elevating the plasma concentration of Gefitinib due to decreasing in metabolism.
Geftinat combined with gastric regulator, causes depletion of plasma concentration of Gefitinib.
Gastric regulators like proton pump inhibitors, H2 receptors antagonist, or antacids.
Geftinat tablets are taken 12 hours after the last dose or 12 hours earlier to proton pump inhibitors;
Geftinat tablets taken at 6 hours after or earlier to the dose of H2 receptor antagonist or antacids.
Geftinat with warfarin leads to produce hemorrhage, to avoid this problem patients monitored
frequently for prothrombin time alteration.
Geftinat tablets producing unwanted effects
The adverse effect of geftinat tablets;
Liver toxicity, Gastrointestinal perforation, Severe diarrhea,Bullous & expoliative skin disorders,
Ocular disorders, Interstitial lung disease.
Warning and precaution of Geftinat tablets
Interstitial lung disease:
Geftinat therapy is discontinued and immediately examine for ILD in any patients who have
acute respiratory problems.
Liver toxicity:
Patient getting Geftinat therapy, accidentally elevate AST & ALT levels and increased bilirubin
levels leads to cause hepatotoxicity and to rescue from this condition discontinue the therapy.
Gastrointestinal perforation:
Stop the
Gefitinib therapy permanently.
Persistent diarrhea:
Discontinue the Gefitinib therapy
Ocular disorders:
Ocular disorders like corneal erosion, aberrant eyelash growth may occur during the therapy
of
Geftinat. To avoid this problem discontinue the Geftinat therapy.
Skin disorders:
Skin disorders like Stevens Johnson’s syndrome, epidermal necrolysis & Erythema multiforme
formed during the therapy.
Geftinat therapy should be suspended or break off.
Embryo fetal toxicity:
Gefitinib produce fetal harm, like fetotoxicity and neonatal death. Not recommended this therapy
in pregnant women and use effective.contraception methods.
Common side effects
Headache, edema, Elevation of AST,ALT, Proteinuria, Hemorrhagic cystitis, Cutaneous vasculitis ,
Nausea, Diarrhea, Fatigue, Respiratory failure occurs due top neumonia & pulmonary embolism,
Mucosal inflammation, tongueulceration, eye irritation, eyelid Pruritus,Vomiting, Skin reactions,
Nail disorders, Stomatitis, Loss of appetite,Conjunctivitis, Blepharitis, Dry eye.
Pediatric and geriatric
The safety and effectiveness of
Gefitinib has not been evaluated inpediatric patients and geriatric
with the age of 65 years and above.
Lactation
Breast feeding should not be suggested in lactating period.
Over dosage
There is no particular therapy evaluated for over dosage condition of Gefitinib. If over dosage
occurs in a patients receiving therapy, must compensate with adequate supportive therapy and
investigate the signs and symptoms of toxicity due to over dosage.
Missed dose
Geftinat 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.
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