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GEFTICIP

GEFITINIB · by A. J. MIRZA

ANTINEOPLASTICS Tyrosine kinase inhibitor A. J. MIRZA

Composition

Tab: Gefitinib 250 mg.

Indications & Dosage

Treatment of locally advanced or metastatic non-small cell lung cancer with activating mutations of epidermal growth factor receptor: Adult: 250 mg once daily.

Contraindications

Hypersensitivity to the drug

Precautions

Severe renal or hepatic impairment, monitor LFTs, monitor for pulmonary toxicity, interrupt treatment and evaluate patient who develop pulmonary symptoms, risk factor for GI perforation. Ensure adequate contraception. Diarrhoea; withhold treatment if severe, low gastric pH (reduced absorption), electrolyte disturbances. During treatment if patients present with acute or worsening signs and symptoms suggestive of keratitis should be referred promptly to an opthalmology specialist. Treatment should be interupted or discontinued if ulcerative keratitis is diagnosed.

Interactions

Antacids, Antiarrhythmics (dronedarone), Antiepileptics (carbamazepine, fosphenytoin, phenobarbital, phenytoin, primidone), Antifungals, azoles, Aprepitant, Bosentan, Calcium channel blockers (diltiazem, verapamil), Cobicistat, Anticoagulant, Crizotinib, Efavirenz, Enzalutamide, H2 receptor antagonists, HIV-protease inhibitors (atazanavir, darunavir, fosamprenavir, indinavir , lopinavir, ritonavir, saquinavir, tipranavir), Idelalisib, Imatinib, Macrolides (clarithromycin, erythromycin), Netupitant, Nevirapine, Nilotinib, Proton pump inhibitors, Rifampicin, St Johns Wort

Pregnancy

Positive evidence of risk: Avoid

Lactation

Contraindicated. Discontinue breast-feeding

Side Effects

Alopecia, anorexia, asthenia, bone-marrow suppression, blepharitis, conjunctivitis, diarrhoea, vomiting, dry eye, dry mouth, dry skin, epistaxis, haematuria, interstitial lung disease (discontinue), proteinuria, pruritus, acne, pyrexia, rash, skin reactions, corneal erosion, pancreatitis, nausea, oral mucositis. Rare: Hepatitis, toxic epidermal necrolysis, hyperuricaemia, thromboembolism, tumour lysis syndrome.