Imatinib, Gleevec
Description: Antineoplastic Agent, BCR-ABL Tyrosine Kinase Inhibitor
CSA NA – FDA Approved – REMS (N) – Can Ship
How Does It 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 a platelet-derived growth factor (PDGF), stem cell factor (SCF), c-Kit, and cellular events mediated by PDGF and SCF.
Indications For Use
Acute Lymphoblastic Leukemia, Aggressive Systemic Mastocytosis, Chronic Myeloid Leukemia, Dermatofibrosarcoma Protuberans, Gastrointestinal Stromal Tumor, Hypereosinophilic syndrome and/or chronic eosinophilic leukemia, Myelodysplastic/Myeloproliferative diseases.
Precautions
Before starting Imatinib, Gleevec makes 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, Gleevec 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 tumour lysis syndrome.
Imatinib is associated with a moderate emetic potential; antiemetics may be recommended to prevent nausea and vomiting
Usual Dosing
Oral: 100-600mg once or twice daily
Pharmacist Tips On Using
How to Take: This 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
Side Effects
Edema, facial edema, peripheral edema, chest pain, headache, fatigue, pain, dizziness, insomnia, depression, taste disorder, rigours, 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 Imatinib, Gleevec only common ones.
Frequently Asked Questions
Why would my physician prescribe a medication with such serious side effects?
Your physician takes the most recent clinical guidelines to make evidence-based decisions on what medication is appropriate in which situations. Your current medications, your allergies, age, cost of medication, comorbid conditions and many other factors will further complicate or limit which medications are appropriate. This medication is used for certain forms of cancer and your physician has determined the benefits outweigh the risks. Furthermore, they will be monitoring your bloodwork and symptoms closely to avoid many of the serious side effects and will keep you on the lowest effective dosage for the shortest amount of time possible.