Makindo Medical Notes

🚨 Urgent medical attention is required if the patient develops fever >38 °C, chills, breathlessness, or uncontrolled bleeding (nose, mouth, vagina, or rectum >15 min).

💊 About: Always check the BNF link here

• Imatinib is a tyrosine kinase inhibitor (TKI), used primarily in chronic myeloid leukaemia (CML) and GIST.
• It revolutionised outcomes in CML by turning a previously fatal disease into a chronic, controllable condition.

⚙️ Mode of Action

• Selective inhibitor of tyrosine kinases (BCR-ABL, PDGFR, c-KIT).
• Blocks the BCR-ABL fusion protein produced by the Philadelphia chromosome → halts abnormal myeloid proliferation.
• Also inhibits c-KIT signalling in Gastrointestinal Stromal Tumours (GISTs).

🩺 Indications & Typical Dosage (verify with BNF)

• Chronic Myeloid Leukaemia (CML): Ph+ CML in chronic, accelerated, or blast phase; oral route (OD or BD depending on phase).
• Acute Lymphoblastic Leukaemia (ALL): For Ph+ relapsed/refractory cases (usually with chemotherapy).
• Myelodysplastic / Myeloproliferative Diseases (MDS/MPD): With PDGFR rearrangements.
• GIST: For unresectable, metastatic, or recurrent c-KIT positive GISTs.
• 💊 Usual dose: 400 mg OD PO (CML, GIST); up to 600–800 mg daily in advanced phases (split BD).

⚖️ Interactions

• Metabolised by CYP3A4 → interactions with inhibitors (ketoconazole, clarithromycin) and inducers (rifampicin, carbamazepine).
• May increase levels of warfarin, ciclosporin, and statins → monitor closely.

⚠️ Cautions

• Monitor FBC regularly → risk of cytopenias.
• Check U&E and LFTs during therapy.
• Use caution in hepatic or renal impairment.
• Pregnancy: teratogenic potential – avoid unless benefits outweigh risks.

⛔ Contraindications

• Severe hepatic impairment.
• Known hypersensitivity to imatinib or excipients.

❗ Side Effects

• 🩸 Haematological: pancytopenia, neutropenia, thrombocytopenia, anaemia.
• 🤢 GI: nausea, vomiting, diarrhoea, abdominal pain.
• 💧 Fluid retention: periorbital oedema, ankle swelling, pleural/pericardial effusions (rare).
• 💪 Musculoskeletal: cramps, myalgia, bone pain.
• 🩹 Dermatological: rash, pruritus.
• 🌡️ Constitutional: fever, fatigue.