GEFITINIB

Description: Gefitinib is a synthetic anilinoquinazoline which inhibits the intracellular phosphorylation of numerous tyrosine kinases associated w/ transmembrane cell surface receptors found on both normal and cancer cells. With this inhibition, the growth of cancer cells are slowed down.

Pharmacokinetics:

Absorption: Slowly absorbed. Bioavailability: Approx 60%. Time to peak plasma concentration: 3-7 hr.

Distribution: Volume of distribution: 1400 L. Plasma protein binding: Approx 90%.

Metabolism: Undergoes extensive hepatic metabolism via CYP3A4 and CYP2D6 isoenzymes; O-desmethylgefitinib (major metabolite).

Excretion: Via faeces (86% as metabolites), urine (<4%). Elimination half-life: Approx 41-48 hr.

Gefitinib treats lung cancer by slowing or stopping the growth of cancer cells. It blocks a certain protein (an enzyme called tyrosine kinase).

How to use gefitinib

Take gefitinib by mouth once daily, with or without food, or as directed.

Medications which reduce or completely block stomach acid (e.g., proton pump inhibitors/PPIs, H2 blockers, antacids) may decrease the absorption of gefitinib. This could decrease the effectiveness of gefitinib. Consult your doctor or pharmacist if you are taking any of these medications.

Use this medication regularly in order to get the most benefit from it. To help you remember, use it at the same time each day.

Gefitinib has rarely caused very serious (possibly fatal) liver disease. Get medical help right away if you develop symptoms of:

  • liver disease
  • including stomach/abdominal pain
  • extreme fatigue
  • dark urine
  • yellowing eyes/skin

Gefitinib has also rarely caused very serious (possibly fatal) holes in the wall of the stomach or intestines. Get medical help right away if you develop:

  • stomach/abdominal pain
  • black/bloody stools
  • vomit that looks like coffee grounds

Notify your doctor or pharmacist immediately if any of these side effects persist or worsen:

  • Diarrhea
  • Rash
  • Acne
  • Nausea
  • Vomiting
  • loss of appetite
  • nail problems
  • hair loss
  • red/sore mouth or throat
  • unusual weakness

Persistent nausea, vomiting, diarrhea, or loss of appetite may result in a serious loss of body water (dehydration) and kidney problems. Contact your doctor promptly if you notice any symptoms of dehydration.

Tell your doctor immediately if any of these unlikely but serious side effects occur:

  • unusual bleeding (coughing up blood, blood in urine)
  • eye irritation/pain
  • swelling of the ankles/feet

Gefitinib may cause rare (possibly fatal) lung disease (interstitial lung disease-ILD). Tell your doctor immediately if you develop trouble breathing, cough or fever.

If you have persistent diarrhea or skin rashes contact your doctor. Your doctor may temporarily stop gefitinib (for up to 14 days) which may help reverse those side effects. Treatment is then resumed with the same dosage.

An allergic reaction to this drug is unlikely, but seek immediate medical attention if it occurs. Symptoms of an allergic reaction include:

  • severe rash
  • itching/swelling (especially of the face/tongue/throat)
  • dizziness
  • Trouble breathing

This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.

Precautions

Before taking this medication, tell your doctor or pharmacist if you are allergic to it; or if you have any other allergies. Talk to your pharmacist for more details.

Before using this medication, tell your doctor or pharmacist your medical history, especially of:

  • lung disease (e.g., pulmonary fibrosis)
  • severe kidney disease, eye problems
  • stomach/intestinal ulcers
  • other stomach/intestinal problems (such as diverticulitis, blockage, bowel disease)
  • smoking
  • cancer that has spread to the bowels

Gefitinib is not recommended for use during pregnancy. It may cause harm to an unborn baby. Consult your doctor for more details.

It is not known whether this drug passes into breast milk. Due to the potential risk to the infant, breast-feeding while using gefitinib is not recommended.

 

Interactions

Before using this medication, tell your doctor or pharmacist of all prescription and nonprescription products you may use, especially of:

  • “blood thinners” (warfarin)
  • drugs which reduce stomach acid (e.g., ranitidine, cimetidine, famotidine, omeprazole, lansoprazole, rabeprazole)
  • certain liver enzyme inhibitors (CYP 3A4 inhibitors such as ketoconazole, itraconazole, erythromycin, clarithromycin)
  • vinorelbine
  • NSAIDs (such as ibuprofen, naproxen)
  • corticosteroids (such as prednisone)

Your dosage of gefitinib may need to be increased if you are using some liver enzyme inducer medications such as rifamycins (e.g., rifampin, rifabutin), St. John’s wort or phenytoin. Consult your doctor or pharmacist for more details.

This document does not contain all possible interactions. Therefore, before using this product, tell your doctor or pharmacist of all the products you use. Keep a list of all your medications with you, and share the list with your doctor and pharmacist.

Overdose

If overdose is suspected, contact a poison control center or emergency room immediately. Symptoms of overdose may include: severe/persistent diarrhea, severe skin rash.

Notes

Do not share this medication with others.

Laboratory and/or medical tests (such as kidney/liver function tests) should be performed periodically to monitor your progress or check for side effects. Consult your doctor for more details.

Missed Dose

If you miss a dose, use it as soon as you remember. If it is less than 12 hours before the next dose, skip the missed dose and resume your usual dosing schedule. Do not double the dose to catch up.

Storage

Store at room temperature between 68 and 77 degrees F (20-25 degrees C) away from light and moisture. Do not store in the bathroom. Keep all medicines away from children and pets.

Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company for more details about how to safely discard your product.

 

Brands

Available Brands

Iressa [ AstraZeneca ]

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