Friday, December 7, 2018

GEFTICIP - 250MG

GEFTICIP - 250MG

About Gefticip

A Gefticip tablet has an active component called Gefitinib, used for lung cancer like non-small cell lung cancer. Gefitinib is an EGFR inhibitor, acts by interfere with signal transduction of epidermal growth factor receptor in tumor cells. Gefitinib is active only in cancer with mutated and hyper active EGFR. Gefitinib is classified as a prime discriminating inhibitor of epidermal growth factor receptors tyrosine kinase domain.

Gefticip tablets Indication

Gefticip tablets are used in non-small cell lung cancer as a first line therapy, in which ncancer cells have EGFR like exon 19 deletions or exon 21 substitution mutations. Gefticip 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.

Dosage management of Gefticip tablets

The suggested dosage of Gefticip tablets is 250mg should be administered orally as a single dose. The missed dose should not be taken within 12 hours of next dose.

Administration

Gefticip tablets are administered orally by taking with or without food. If patients are unable to take the tablets through mouth, 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.

Pharmacokinetics

Absorption :
Oral bioavailability: 60% Peak plasma concentration time: 3 to 7 hours
Distribution:
Volume of distribution: 1400L Human plasma protein bound: 90%
Metabolism:
Gefticip 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:
Gefticip 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%.

Dosage adjustment

Stop the Gefticip therapy, if patients have any of the following effects such as; Elevation of ALT & AST levels; Severe ocular disorders like keratitis, High skin reactions, Acute upraising or aggravation of pulmonary symptoms like cough, fever, dyspnea.
Gefticip therapy should be discontinuing forever; in case of Gastrointestinal perforation, Interstitial lung disease, Ulcerative keratitis, Severe liver damage.
Strong CYP3A4 inducers

In concomitant with strong CYP3A4 inducers, the dosage is increased to 500mg; continue the Gefticip therapy with 250mg after cessation of strong CYP3A4 inducers
Gefticip tablets Mechanism

Tumor cells asserted epidermal growth factor receptors on their cell surface, present in both active and cancer infected cells. 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. Gefticip enclose Gefitinib causes erratic prohibition of tyrosine kinase and provoke abnormality of EGFR, block the autophosphorylation of tyrosine debris similar with receptor, via inhibition of following signaling and blockade EGFR dependent multiplication.

Drug interaction

Gefticip tablet combined with strong CYP3A4 inducers like phenytoin, rifampicin, or tricyclic depressant may leads to decreasing the plasma concentration of Gefitinib because of increasing the metabolism. To avoid this problem, while concomitant with these drugs, the dosage of Gefticip is increased to 500mg, maintained by 250mg for 7 days after stopping the CYP3A4 inducers. Co administration of Gefticip with strong CYP3A4 inhibitors like itraconazole causes elevating the plasma concentration of Gefitinib due to decreasing in metabolism. Gefticip combined with gastric regulator, causes depletion of plasma concentration of Gefitinib. Gastric regulators like proton pump inhibitors, H2 receptors antagonist, or antacids. Gefticip tablets are taken 12 hours after the last dose or 12 hours earlier to proton pump inhibitors; Gefticip tablets taken at 6 hours after or earlier to the dose of H2 receptor antagonist or antacids. Gefticip with warfarin leads to produce hemorrhage, to avoid this problem patients monitored frequently for prothrombin time alteration.

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