Gabisof

Gabisof

gefitinib

Manufacturer:

Khandelwal Lab

Distributor:

Ni Lay Naing
Full Prescribing Info
Contents
Gefitinib.
Description
Each film-coated tablet also contains the following excipients: Red and yellow iron oxides and titanium dioxide.
Action
Pharmacotherapeutic Group: Antineoplastic, signal transduction inhibitor.
Pharmacology:
Gefitinib may inhibit activity of many tyrosine kinases associated with transmembrane cell surface receptors, including those associated with epidermal growth factor receptor (EGFR-TK). This effect ultimately blocks cell growth and reproduction. Epidermal growth factor receptor is expressed on cell surface of many normal cell and cancer cell, including those in colon, lung, head and neck.
Pharmacokinetics:
Gabisof is metabolized in the liver. It peaks in 3-7 hrs and achieves steady-state plasma concentrations in 10 days. Elimination half-life (t½) is 48 hrs. It is excreted primarily in feces.
Indications/Uses
Locally advanced or metastatic non-small cell lung cancer after failure of platinum-based and docetaxel chemotherapies.
Dosage/Direction for Use
Adults: 250 mg once daily.
Dosage Modification:
Gabisof is administered on continuous schedule over 28 days. It is given for 14 days on and 14 days off in patients with poorly tolerated diarrhea and adverse skin reaction.
If patient experiences acute onset or worsening of pulmonary symptoms (eg, dyspnea, cough and fever), discontinue Gabisof and initiate appropriate treatment. Discontinue drug if interstitial lung disease is confirmed.
Patient Receiving Acute CYP3A4 Inducers (eg, Rifampin or Phenytoin): 500 mg once daily in the absence of severe adverse reactions.
Administration: Do not crush or break film-coated tablets. Tablets can be dispersed only in half-glass of non-carbonated drinking water. Drop tablet into water without crushing it and stir until it disperses. Have patient drink immediately, then rinse glass with water and drink again.
Gabisof may be given by nasogastric tube if patient cannot swallow.
Overdosage
Symptoms: Anticipated overdose effects include increased frequency and severity of some adverse reactions mainly diarrhea and rash.
Treatment: Provide symptomatic treatment. In particular, manage severe diarrhea appropriately.
Contraindications
Hypersensitivity to Gabisof or to any of its components.
Warnings
Gabisof should be used only in cancer patients who have already taken it and whose physicians believe it is benefiting them. New patients should not receive it; large study found that it did not extend life.
Pulmonary Toxicity: In the event of acute onset or worsening of pulmonary symptoms (dyspnea, cough, fever), Gefitinib therapy should be interrupted and a prompt investigation of these symptoms should occur. If interstitial lung disease is confirmed, gefitinib should be discontinued and the patient should be treated appropriately.
Use in pregnancy: Pregnancy Category D: Gefitinib may cause fetal harm when administered to a pregnant woman. There are no adequate and well-controlled studies in pregnant women using gefitinib. If gefitinib is used during pregnancy or if the patient becomes pregnant while receiving Gabisof, she should be apprised of the potential hazard to the fetus or potential risk for loss of the pregnancy.
Special Precautions
Use cautiously in hepatic impairment, cardiac disease, severe renal impairment and pregnancy or breastfeeding. Safety and efficacy in children have not been established.
Monitor international normalized ratio (INR) or prothrombin time regularly in patients receiving warfarin.
Observe closely for interstitial lung disease; incidences are 1% with 1/3 of cases considered fatal.
Inform patient that Gabisof may cause nausea, anorexia, vomiting or persistent diarrhea. Advise patient to report these symptoms promptly if they persist.
Advise patient to report eye irritation. Instruct patient to consume adequate fluids, especially if diarrhea occurs.
Advise patient to promptly report new or worsening pulmonary symptoms eg, dyspnea, cough and fever.
Advise women with childbearing potential to use effective contraception.
Use in lactation: Caution breastfeeding patient not to breastfeed during therapy.
Use In Pregnancy & Lactation
Use in pregnancy: Pregnancy Category D: Gefitinib may cause fetal harm when administered to a pregnant woman. There are no adequate and well-controlled studies in pregnant women using gefitinib. If gefitinib is used during pregnancy or if the patient becomes pregnant while receiving Gabisof, she should be apprised of the potential hazard to the fetus or potential risk for loss of the pregnancy.
Use in lactation: Caution breastfeeding patient not to breastfeed during therapy.
Adverse Reactions
Eye, Ear, Nose and Throat (EENT): Conjunctivitis.
Gastrointestinal: Diarrhea, nausea, vomiting, anorexia.
Skin: Rash, acne, dry skin.
Drug Interactions
Drug-Drug: CYP3A4 Inducers (eg, Rifampin, Phenytoin): Increased gefitinib metabolism and decreased plasma concentration.
CYP3A4 Inhibitors (eg, Ketoconazole, Itraconazole): Decreased gefitinib metabolism and increased plasma concentration.
Histamine2-Receptor Antagonists (eg, Ranitidine, Cimetidine): Decreased gefitinib plasma concentration.
Warfarin: Increased INR, bleeding events.
Drug-Diagnostic Tests: Alkaline Phosphatase (ALP), Alanine transaminase (ALT), Aspartate transaminase (AST), Serum Bilirubin: Possible increase.
Storage
Protect from light and moisture.
ATC Classification
L01XE02 - gefitinib ; Belongs to the class of protein kinase inhibitors, other antineoplastic agents. Used in the treatment of cancer.
Presentation/Packing
FC tab 250 mg x 10's.
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