Drug Index

Imatinib

 
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Mechanism :

Imatinib mesylate is a protein-tyrosine kinase inhibitor that inhibits the BCR-ABL tyrosine kinase, the constitutive abnormal tyrosine kinase created by the Philadelphia chromosome abnormality in chronic myeloid leukemia (CML). It inhibits proliferation and induces apoptosis in BCR-ABL positive cell lines as well as fresh leukemic cells from Philadelphia chromosome positive chronic myeloid leukemia.


Indication :

• Philadelphia chromosome positive chronic phase CML

• Philadelphia chromosome positive (Ph+) ALL


Contraindications :

Contraindicated in patients with hypersensitivity to imatinib or to any other component.


Dosing :

Above 1 year: 340 mg/sqm/day orally; Max: 600 mg/day.

Below 1 year: Safety and efficacy not established.


Adverse Effect :

Muscle cramps, nausea and vomiting, edema, diarrhea, myalgia, musculoskeletal pain, rash, bone marrow suppression, nasopharyngitis, dyspepsia, cough, abdominal pain.


Interaction :

Ketoconazole, Itraconazole, Erythromycin, Clarithromycin, substances that inhibit the Cytochrome P450 Isoenzyme (CYP3A4) activity: May increase imatinib plasma concentrations.
Inducers of CYP3A4 (e.g., Dexamethasone, Phenytoin, Carbamazepine, Rifampin, Phenobarbital): May decrease imatinib plasma concentrations.


07/17/2019 20:33:51 Imatinib
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