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Imatinib Mesylate- Drug Interactions, Dosage, Side Effects, indications, Uses and Precautions

Look for Drugs and Conditions

Imatinib Mesylate

Imatinib Mesylate

It is a protein-tyrosine kinase inhibitor that inhibits Bcr-Abl tyrosine kinase. It is also an inhibitor of the receptor tyrosine kinases for platelet derived growth factor and stem cell factor, C-kit, and inhibits their mediated cellular events.

Indications

Philadelphia chromosome positive chronic myeloid leukemia (CML). Kit (CD117) positive unresectable and/or metastatic malignant gastrointestinal stromal tumors (GIST).


Dosage

To be administered orally with a meal and a large glass of water. Range of dosage to be adjusted according to therapeutic response and adverse effects. Chronic Phase CML: 400mg-600mg/day. Accelerated Phase or blast crisis CML : 600mg-800mg/day (400mg twice daily). Unresectable and/or metastatic malignant GIST: 400mg-600mg/day.


Contra-Indications

Hypersensitivity.


Special Precautions

Dose adjustment/reduction or treatment interruption is recommended if a severe adverse effect develops. Paediatric : Safety and efficacy have not been established under the age of 18-years of age. Pregnancy : Safety is not established. Lactation : Safety is not established. Elderly : Safe


Side Effects

Nausea, vomiting, diarrhoea, abdominal pain, rash, edema, and muscle cramps. Local or generalised fluid, retention and rapid weight gain. Cytopenias. Hepatotoxicity.


Drug Interactions

Ketoconazole, itraconazole, erythromycin, and clarithromycin may increase plasma concentration of imatinib, while dexamethasone, phenytoin, carbamazepine, rifampicin, phenobarbital may decrease the plasma concentration of imatinib. It will increase plasma concentration of triazolo-benzodiazepines, dihydropyridine, calcium channel blcokers, certain HMG-CoA reductase inhibitors etc. Warferin.


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