IMATINIB

COMMON BRAND NAME(S): Gleevec

GENERIC NAME(S): IMATINIB MESYLATE

 

Description: Imatinib is a tyrosine kinase inhibitor that blocks proliferation and induces apoptosis in BCR-ABL positive cell lines, as well as fresh leukaemic cells from Philadelphia chromosome positive CML. Imatinib also inhibits receptor kinases for platelet-derived growth factor (PDGF) and stem cell factor (SCF), c-kit, PDGF- and SCF-mediated cellular events.
Pharmacokinetics: 
Absorption: Rapidly and well absorbed from the GI tract. Mean bioavailability: Approx 98%. Time to peak plasma concentration: 2-4 hr.
Distribution: Plasma protein binding: Approx 95%.
Metabolism: Primarily via CYP3A4 isoenzyme and to a lesser extent via CYP1A2, CYP2D6, CYP2C9 and CYP2C19 isoenzymes. N-demethylated piperazine derivative (active metabolite).
Excretion: Via faeces (68%) and urine (13%) w/in 7 days; excreted mostly as metabolites, w/ 25% as unchanged drug. Elimination half-life: Approx 18 hr (imatinib); approx 40 hr (N-demethylated piperazine derivative).

This medication is used to treat  acute lymphoblastic leukemia, chronic myeloid leukemia, gastrointestinal stromal tumors, and myelodysplastic/myeloproliferative diseases that works by stopping or slowing the growth of cancer cells (tumors) and by causing cancer cells to die.

 

How to use imatinib

Take this medication by mouth with a meal and a full glass of water (8 ounces or 240 milliliters), usually once or twice daily or as directed by your doctor. Do not crush the tablets. The US manufacturer recommends that if you have trouble swallowing the tablets whole, you may dissolve your dose in a glass of water or apple juice. The amount of liquid will vary depending on your dose. Consult your doctor or pharmacist for more detailed instructions. Stir the mixture well until the tablet(s) dissolve, and drink immediately.

 

The dosage is based on your medical condition and response to treatment. In children, the dosage is based on body size. Do not increase your dose or take this medication more often than prescribed. Your condition will not improve any faster, and the risk of serious side effects may be increased.

 

Avoid eating grapefruit or drinking grapefruit juice while using this medication unless your doctor or pharmacist says you may do so safely. Grapefruit can increase the chance of side effects with this medicine. Ask your doctor or pharmacist for more details.

 

Since this drug can be absorbed through the skin and lungs and may harm an unborn baby, women who are pregnant or who may become pregnant should not handle this medication or breathe the dust from the tablets.

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

 

  • Upset stomach
  • Nausea
  • Vomiting
  • Diarrhea
  • Headache
  • joint pain
  • muscle cramps/pain
  • dizziness
  • blurred vision
  • drowsiness

 

 

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

 

  • easy bruising/bleeding
  • fast/pounding heartbeat
  • extreme tiredness
  • sudden/unexplained weight gain
  • swelling (especially of lower legs/the area around eyes)
  • increasing trouble breathing (shortness of breath)

 

 

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

 

  • black/bloody stools
  • dark urine
  • stomach/abdominal pain
  • vomit that looks like coffee grounds
  • yellowing eyes/skin

 

 

This medication can lower the body’s ability to fight an infection.

 

Imatinib sometimes causes tumor lysis syndrome. This is from the side effects due to rapid destruction of cancer cells.

 

A very serious allergic reaction to this drug is rare.

 

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

Precautions

 

  • Allergic reaction to this medication
  • Patients with medical history of:
    • bleeding problems
    • heart problems (e.g., heart failure)
    • kidney problems
    • liver problems
  • This drug may make you dizzy or drowsy or cause blurred vision
  • Do not have immunizations/vaccinations without the consent of your doctor
  • avoid contact with people who have recently received oral polio vaccine or flu vaccine inhaled through the nose
  • Tell your doctor or dentist that you are using this medication before having surgery
  • This medication may slow down a child’s growth
  • The elderly may be more sensitive to the side effects of this drug (e.g., swelling)
  • routine heart test (LV ejection fraction) in the elderly before treatment
  • women who are pregnant or who may become pregnant should not handle this medication or breathe the dust from the tablets
  • This medication is not recommended for use during pregnancy
  • Consult your doctor before breast-feeding

Consult your doctor regarding the precautions mentioned above.

 

Interactions

 

This drug should not be used with warfarin because very serious interactions may occur.

 

Tell your doctor or pharmacist before starting imatinib if you are currently using the medication listed above.

 

Before using this medication, tell your doctor or pharmacist of all prescription and nonprescription/herbal products you may use, especially of Levothyroxine or drugs affecting liver enzymes that remove imatinib from your body such as:

 

  • azole antifungals including itraconazole/ketoconazole
  • HIV protease inhibitors including ritonavir/saquinavir
  • macrolide antibiotics including erythromycin, cimetidine, rifamycins including rifampin/rifabutin
  • corticosteroids including dexamethasone
  • John’s wort
  • certain anti-seizure medicines including carbamazepine/phenytoin

 

 

This drug can slow down the removal of other drugs from your body by affecting certain liver enzymes, such as:

 

  • Acetaminophen
  • Cyclosporine
  • Midazolam
  • Nifedipine
  • Sildenafil
  • simvastatin

 

 

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 muscle cramps, dark urine, abdominal swelling.

 

Notes

Do not share this medication with others.

 

Laboratory and/or medical tests (such as complete blood count, liver function tests, body weight) 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, take it as soon as you remember. If it is near the time of 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 at 77 degrees F (25 degrees C) away from light and moisture. Brief storage between 59-86 degrees F (15-30 degrees C) is permitted. Do not store in the bathroom. Keep all medications 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

Glivec [ Novartis Healthcare ]

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