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.



Renal Dose :

Dose in Renal Impairment GFR (mL/min)
20-50Dose as in normal renal function
10-20Dose as in normal renal function.
<10Dose as in normal renal function.

Dose in Patients undergoing Renal Replacement Therapies
CAPDUnlikely to be dialysed. Dose as in normal renal function
HDUnlikely to be dialysed. Dose as in normal renal function
HDF/High fluxUnlikely to be dialysed. Dose as in normal renal function
CAV/VVHDUnknown dialysability. Dose as in GFR=10–20 mL/min

Hepatic Dose :

Mild to moderate hepatic impairment: No adjustment necessary
Severe hepatic impairment: Reduce dose by 25%
Hepatotoxicity during therapy
If elevations of bilirubin >3 times upper limit of normal (ULN) or liver transaminases >5 times ULN: withhold treatment until bilirubin <1.5 times ULN and transaminases <2.5 times ULN. Resume treatment at a reduced dose as follows: If current dose 340 mg/m2/day, reduce dose to 260 mg/m2/day. Maximum daily dose range:300 to 400 mg/day
07/29/2020 00:26:40 Imatinib
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