GLEEVEC (Imatinib)

What is this medication? 

GLEEVEC (Imatinib)
Antineoplastic Agent, BCR-ABL Tyrosine Kinase Inhibitor

GLEEVEC (Imatinib) is indicated for the treatment of acute lymphoblastic leukemia, aggressive systemic mastocytosis, chronic myeloid leukemia, dermatofibrosarcoma protuberans, gastrointestinal stromal tumor, hypereosinophilic syndrome and/or chronic eosinophilic leukemia, myelodysplastic/myeloproliferative diseases.

How does this medication work? 

Imatinib inhibits Bcr-Abl tyrosine kinase, the constitutive abnormal gene product of the Philadelphia chromosome in chronic myeloid leukemia (CML). Inhibition of this enzyme blocks proliferation and induces apoptosis in Bcr-Abl positive cell lines as well as in fresh leukemic cells in Philadelphia chromosome positive CML. Also inhibits tyrosine kinase for platelet-derived growth factor (PDGF), stem cell factor (SCF), c-Kit, and cellular events mediated by PDGF and SCF.

How should I take this medication? 

Oral: Take 100-600mg once or twice daily.

How to Take: Should be administered with a meal and a large glass of water. For daily dosing ≥800 mg, the 400 mg tablets should be used to reduce iron exposure. Tablets may be dispersed in water or apple juice (using ~50 mL for 100 mg tablet, ~200 mL for 400 mg tablet); stir until dissolved and administer immediately. Doses ≤600 mg may be given once daily; 800 mg dose should be administered as 400 mg twice daily.

You Need to Avoid: Avoid grapefruit juice.  Do not crush tablets.  Avoid skin or mucous membrane contact with crushed tablets; if contact occurs, wash thoroughly. Avoid exposure to crushed tablets.

What should I watch for while using this medication?

Before starting GLEEVEC (Imatinib) make sure your physician is aware of any allergies or medications you currently take, if you have liver disease, have had gastric surgery, kidney disease, or thyroid disease.  Imatinib has been associated with bone marrow suppression (i.e. thrombocytopenia, neutropenia, anemia), cardiovascular disease (i.e. ischemic events, cardiac fluid retention, conduction abnormalities), dermatologic toxicity, fluid retention, hemorrhage, hepatotoxicity, nephrotoxicity, GI toxicity, and tumor lysis syndrome.

Imatinib is associated with a moderate emetic potential; antiemetics may be recommended to prevent nausea and vomiting.

What if I miss a dose?

If you miss a dose of medication, try to take it as soon as possible. However, if it is almost time for your next dose, take only that scheduled dose. Do not take double or extra doses.

How should I store this medication?

Keep out of the reach of children at all times. Store at room temperature, 59 to 86° F (15 to 30° C). Protect from light.  Keep the container tightly closed. Properly dispose of any unused medication after the expiration date.

What are the possible side effects of using this medication? 

Edema, facial edema, peripheral edema, chest pain, headache, fatigue, pain, dizziness, insomnia, depression, taste disorder, rigors, anxiety, paresthesia, chills, skin rash, dermatitis, pruritis, night sweats, alopecia, diaphoresis, fluid retention, increased lactate dehydrogenase, weight gain, decreased serum albumin, hypokalemia, diarrhea, nausea, vomiting, abdominal pain, anorexia, dyspepsia, flatulence, abdominal distention, constipation, upper abdominal pain, stomatitis, hematologic disturbances, increased liver enzymes, infections, influenza, muscle cramps, musculoskeletal pain, muscle spasm, arthralgia, myalgia, asthenia, back pain, limb pain, ostealgia, periorbital edema, increased lacrimation, eyelid edema, blurred vision, increased serum creatinine, fever.

Note this is not a complete list of side effects for GLEEVEC (Imatinib), only common ones.