Gefitinib

Cytostatic · Tyrosine kinase inhibitor

Indications

Locally advanced or metastatic non-small cell lung cancer with activating mutations of EGFR-TK.

Dosage

Adults: 250 mg once daily. Children: Not recommended.

Adverse Effects

Anorexia, GI upsets, interstitial lung disease (discontinue), haemorrhage, eye infections, dry eye, dry mouth, abnormal LFTs, skin reactions, nail disorders, alopecia, raised creatinine, proteinuria, cystitis, asthaenia, pyrexia. Reports of GI perforation.

Risk Factor (Pregnancy/Lactation)

Pregnancy: Contraindicated in pregnancy. Lactation: Contraindicated or not recommended. Precautions: Moderate to severe hepatic impairment, renal impairment (CrCl = 20 mL/min), CYP2D6 poor metabolisers. Risk factors for GI perforation. Monitor liver function. Interrupt treatment and evaluate patient who develop unexplained pulmonary symptoms. Advise patients to report eye symptoms or severe or persistent GI upset or anorexia.

Interactions

Phenytoin, carbamazepine, rifampicin, barbiturates, St. John's Wort and other CYP3A4 inducers. Azole antifungals, macrolides, protease inhibitors and other CYP3A4 inhibitors. Warfarin, PPIs, H2 antagonists, antacids, vinorelbine.

Advice to Patient

Take with or without meals. Disperse tablet in half glass of non-carbonated water. Do not take with any other liquid. Do not crush it. Drop tablet in water, and stir for about 10 minutes. Drink it immediately. Rinse the glass with another half glass of water and drink. Liquid may also be administered through nasogastric tube. Do not take antacids 2 hours before or after taking this medication. Contact prescriber if there is chest pain, cough, difficulty in breathing, wheezing, severe constant diarrhoea, skin rash, eye pain, change in vision, eye infection, joint pain, weakness. Periodic laboratory tests are required during treatment. Take sufficient amount of fluids (2-3 litres per day) to maintain hydration, unless restricted by the prescriber.

Pharmacokinetics

Absorption: Slow. Metabolism: Hepatic. Bioavailability: 60%. Half-life elimination: 41-48 hrs. Time to peak, plasma: Oral: 3-7 hrs. Excretion: Faeces (mainly; 86%). Urine (<4%).

Brands with this active ingredient

• Gefiton
• Gefticip

Compiled by Healify Pharmacy from published drug references. How we compile it →

Always consult a pharmacist or doctor.