৳ 100/unit
Pack: ৳ 100
৳ 100/unit
Pack: ৳ 100
At a glance
Imatinib is a tyrosine kinase inhibitor used for the treatment of chronic myeloid leukemia (CML), acute lymphocytic leukemia (ALL), and gastrointestinal stromal tumors (GIST).
Indications
- Newly diagnosed Ph+ CML (chronic phase)
- Ph+ CML (blast crisis, accelerated phase, or after interferon-alpha therapy failure)
- Relapsed or refractory Ph+ ALL (adults)
- Newly diagnosed Ph+ ALL (pediatric, in combination with chemotherapy)
- MDS/MPD (with PDGFR gene re-arrangements)
- Aggressive systemic mastocytosis (without D816V c-Kit mutation)
- Hypereosinophilic syndrome/eosinophilic leukemia (with FIP1L1-PDGFRα fusion kinase)
- Unresectable, recurrent and/or metastatic dermatofibrosarcoma protuberans
- Kit (CD117) positive unresectable and/or metastatic malignant GIST
- Adjuvant treatment of GIST (after complete gross resection)
Pharmacology
Imatinib is a small molecule protein-tyrosine kinase inhibitor that potently inhibits the activity of the Bcr-Abl tyrosine kinase (TK), as well as several receptor TKs. It is well absorbed after oral administration with absolute bioavailability of 98%. Plasma protein binding is approximately 95%. CYP3A4 is the major enzyme responsible for metabolism. Imatinib elimination is predominately in the feces, mostly as metabolites.
Dosage
Adult Dose (Oral):
- Ph+ CML CP: 400 mg/day
- Ph+ CML AP or BC: 600 mg/day
- Ph+ ALL: 600 mg/day
- MDS/MPD: 400 mg/day
- ASM: 100 mg/day or 400 mg/day
- HES/CEL: 100 mg/day or 400 mg/day
- DFSP: 800 mg/day (400 mg twice daily)
- GIST (metastatic/unresectable): 400 mg/day
- GIST (adjuvant): 400 mg/day × 3 years
Child Dose (Oral):
- Ph+ CML CP: 340 mg/m2/day (max 600 mg/day)
- Ph+ ALL: 340 mg/m2/day (max 600 mg/day)
Hepatic Impairment: Severe: Reduce dose by 25%
Side effects
Common Side Effects:
- Abdominal pain
- Diarrhea
- Fatigue
- Muscle cramp
- Musculoskeletal pain
- Nausea
- Rash
- Vomiting
Serious: Fluid retention and edema, hematologic toxicity, congestive heart failure, hepatotoxicity, hemorrhage, tumor lysis syndrome, hypothyroidism
Use in pregnancy
Use in Pregnancy: Unsafe; definite evidence of risk to developing baby; if used during pregnancy or patient becomes pregnant, apprise of potential hazard to fetus; effective contraception required during treatment and for 15 days after stopping.
Pregnancy Category: D — always consult a doctor before taking during pregnancy.
Precautions & warnings
Precautions:
- Imatinib may affect your ability to drive (dizziness, blurred vision)
- Fluid retention and edema: Monitor weight regularly
- Cytopenias: Weekly CBC for first month, biweekly for second month
- Hepatotoxicity: Monitor liver function before and monthly during treatment
- Monitor patients with cardiac disease or risk factors
- Apprise pregnant women of potential harm to fetus
Overdose effects
Overdose: 1200-1600 mg: nausea, vomiting, diarrhea, rash; 1800-3200 mg: weakness, myalgia; 6400 mg (single dose): nausea, vomiting, abdominal pain, pyrexia; 8-10 g (single dose): vomiting, gastrointestinal pain; provide symptomatic supportive treatment.
Storage conditions
Store below 30°C, in a cool and dry place; keep away from light; keep out of reach of children.