Generic Name: Gefitinib 250mg
Company Name: Beacon Pharmaceuticals Limited
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Indications
Gefinix 250 is a medication used to treat non-small cell lung cancer. It is used in patients whose cancer has spread to other parts of their bodies, who have abnormal epidermal growth factor receptor (EGFR) genes, and who have not previously received cancer treatment. Gefinix 250 can be taken with or without food, but for best results, take it at the same time every day. You should continue to take it for as long as your doctor recommends.
Pharmacology
Gefitinib binds to and inhibits the adenosine triphosphate (ATP)-binding site of the epidermal growth factor receptor (EGFR) tyrosine kinase. The function of the EGFR tyrosine kinase in activating the Ras signal transduction cascade is thus prevented, and malignant cells are suppressed as a result. Gefitinib is the first and only EGFR tyrosine kinase inhibitor that is also known as Her1 or ErbB-1. EGFR is overexpressed in the cells of certain types of human carcinomas, such as lung and breast cancer. Overexpression inappropriately activates the apoptotic Ras signal transduction cascade, resulting in uncontrolled cell growth.
Dosage & Administration
The recommended dose of Gefitinib is 250 mg orally once daily with or without food until disease progression or unacceptable toxicity. Do not take a missed dose within 12 hours of the next dose.
Interaction
Use of CYP3A4 inducers (e.g., rifampicin, phenytoin, carbamazepine, barbiturates) along with gefitinib may lower serum levels. Potent CYP3A4 inhibitors may raise plasma concentrations (e.g. itraconazole, ketoconazole). Warfarin can cause an increase in INR or bleeding. Metoprolol levels in the blood may rise. Vinorelbine-induced neutropenia may be exacerbated. Drugs that change stomach pH can cause decreased plasma levels and possibly reduced efficacy (e.g. PPIs, H2-receptor antagonists).
Contraindications
Hypersensitivity. Lactation.
Side Effects
The following adverse reactions have been reported with Gefitinib across NSCLC trials: nausea (18%), asthenia (17%), pyrexia (9%), alopecia (4.7%), hemorrhage (including epistaxis and hematuria) (4.3%), dry mouth (2%), dehydration (1.8%), allergic reactions including angioedema and urticaria (1.1%), elevations in blood creatinine (1.5%), and pancreatitis (0.1%).
Pregnancy & Lactation
D is the pregnancy category. Although there is evidence of human fetal danger, the advantages of usage in pregnant women may outweigh the risk (e.g., if the drug is needed in a life-threatening situation or for a serious disease for which safer drugs cannot be used or are ineffective).
Precautions & Warnings
Patients with idiopathic pulmonary fibrosis, new or worsening pulmonary or eye symptoms. Renal and hepatic dysfunction Pregnancy. Parameters for monitoring Regularly check your liver function, prothrombin time, and INR. Lactation Unknown; not recommended if distributed in
Storage Conditions
Store between 20-25° C.
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