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Home :: Drugs ::Imatinib
Imatinib - Learn about Imatinib Side Effects and Precautions
Imatinib Information
The pharmacology action of Imatinib is that it
imatinib inhibits proliferation and induces apoptosis in BCR-ABL positive cell lines as well as fresh leukemic cells from Philadelphia chromosome-positive (Ph+) chronic myeloid leukemia (CML). Imatinib inhibits tumor growth of BCR-ABL transfected murine myeloid cells and BCR-ABL positive leukemia lines derived from CML patients in blast crisis. It also inhibits the receptor tyrosine kinases for platelet-derived growth factor (PDGF) and stem cell factor (SCF), c-Kit, and inhibits PDGF- and SCF-mediated cellular events.
Imatinib is used treatment of newly diagnosed adult patients with Ph+ CML in chronic phase; patients with Ph+ CML in blast crisis, accelerated phase, or in chronic phase after failure of interferon-alpha treatment; children with Ph+ chronic phase CML whose disease has recurred after stem cell transplant or who are resistant to interferon-alpha therapy; treatment of gastrointestinal stromal tumors (GIST).
on coagulopathies (DIC); prevention of postoperative deep venous thrombosis (DVT), and PE.
| Imatinib Class |
Protein-tyrosine kinase inhibitor |
| HowImatinib Supplied |
Gleevec Tablets 100 mg , Tablets 400 mg
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| Brand Name : |
Imatinib |
Interaction and Contraindication of Imatinib
Interaction of Imatinib -
Acetaminophen: Increased risk of hepatotoxicity.
Drugs that induce CYP3A4 (eg, carbamazepine, dexamethasone, phenobarbital, phenytoin, rifampin, St. John's wort): Decreased imatinib concentrations and antineoplastic efficacy.
Drugs that inhibit CYP3A4 (eg, clarithromycin, erythromycin, itraconazole, ketoconazole): Increased imatinib concentrations and toxicity.
Drugs metabolized by CYP3A4 (eg, calcium channel blockers, cyclosporine, dihydropyridine, pimozide, simvastatin, triazolobenzodiazepines): Imatinib may reduce metabolism, resulting in increased concentrations and toxicity.
Warfarin: Because warfarin is metabolized by CYP2C9 and CYP3A4, patients who require anticoagulation should receive low-molecular weight or standard heparin. |
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Contraindication of Imatinib -
Standard considerations.
Side Effects o f Imatinib
Here are the list of some common side effects ofImatinib :
- Fatigue (48%); headache (36%); asthenia (21%); anorexia (17%); dizziness (16%); insomnia (14%); depression (13%); anxiety (12%); CNS hemorrhage (9%); paresthesia (1% to 10%).
- Rash (47%); pruritus (14%); alopecia, dry skin (1% to 10%).
- Nasopharyngitis (27%); pharyngolaryngeal pain (17%); lacrimation (11%); conjunctivitis, vision blurred (1% to 10%).
- Nausea (73%); diarrhea (60%); vomiting (58%); abdominal pain (37%); dyspepsia (27%); flatulence (23%); constipation (16%); taste disturbance (14%); GI hemorrhage (8%); abdominal distention, gastroesophageal reflux, mouth ulceration (1% to 10%).
- Hemorrhage (53%); anemia (42%); thrombocytopenia (31%); neutropenia (27%).
Precaution and Warning while taking Imatinib
The precaution and warnings of Imatinib drug is as follows:
- Review dosing schedule with patient.
- Advise patient that dose may be changed, or medication temporarily stopped, based upon results of lab tests, development of side effects, and response to therapy.
- Advise patient to take prescribed dose with food and large glass of water to minimize GI irritation.
- Advise patient if unable to swallow tablets that the tablets may be dispersed in a glass of water or apple juice. Instruct patient to place required number of tablets in a glass with appropriate volume of beverage (eg, 2 oz for 100 mg tablet, 6 oz for 400 mg tablet) and stir with a spoon until the tablets have disintegrated. Instruct patient that suspension must be swallowed immediately after complete disintegration of the tablets.
- Caution patient to avoid grapefruit and grapefruit juice while taking imatinib.
- Advise patient that if a dose is missed to take it as soon as possible; however, if patient is close to the next dose to skip the missed dose and take the next dose at the regularly scheduled time. Caution patient not to double the dose to catch up.
- Advise patient to immediately report any of the following to their health care provider: skin rash; swelling of the feet, ankles, legs, or around the eyes; rapid weight gain; bloating; shortness of breath or difficulty breathing; fever, chills, or other signs of infection; sore throat; persistent nausea, vomiting, or appetite loss; bleeding; unusual bruising.
- Advise patient that drug may cause dizziness and to use caution while driving or performing other tasks requiring mental alertness and coordination until tolerance is determined.
- Advise patient that medication may cause photosensitivity (sensitivity to sunlight or ultraviolet light) and to avoid unnecessary exposure to sunlight or tanning lamps, use sunscreens, and wear protective clothing until tolerance is determined.
- Caution women of childbearing potential to avoid becoming pregnant while being treated.
- Advise women to notify health care provider if pregnant, planning to become pregnant, or breastfeeding.
How to store Imatinib
- Administer doses of 400 to 600 mg as a single daily dose. Administer 800 mg dose as 400 mg bid.
- In children, medication can be administered as a single daily dose or may be split into 2 doses (once in the morning and once in the evening).
- If patient is unable to swallow film-coated tablets, the tablets may be dispersed in a glass of water or apple juice. Place required number of tablets in a glass with appropriate volume of beverage (eg, 50 mL for 100 mg tablet, 200 mL for 400 mg tablet) and stir with a spoon until the tablets have disintegrated. Immediately have patient swallow the suspension.
- Store tablets at controlled room temperature (59° to 86°F). Protect from moisture.
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