Company: Rowex Ltd.
Legal category: Prescription. Hi tech reimbursable. Sport permitted.
Active ingredient: Imatinib (as mesilate) 100mg, 400mg.
Description: Very dark yellow to brownish orange, round or ovaloid, biconvex film-coated tablets marked with NVR or 400 on one side and SA or SL on either side of score line on reverse, respectively.
Presentation: 100mg-60, €470.86; 400mg-30, €941.72.
Indications: Newly diagnosed Philadelphia chromosome (bcr-abl) positive (Ph+) chronic myeloid leukaemia (CML) when bone marrow transplantation not considered as first line treatment. Ph+ CML in chronic phase after failure of interferon-alpha therapy, or in accelerated phase or blast crisis. Newly diagnosed Philadelphia chromosome positive acute lymphoblastic leukaemia (Ph+ ALL) integrated with chemotherapy. Adults only: Relapsed or refractory Ph+ ALL as monotherapy; myelodysplastic/ myeloproliferative diseases (MDS/MPD) associated with platelet-derived growth factor receptor (PDGFR) gene re-arrangements; advanced hypereosinophilic syndrome (HES) and/or chronic eosinophilic leukaemia (CEL) with FIP1L1-PDGFRa rearrangement; unresectable dermatofibrosarcoma protuberans (DFSP) and recurrent and/or metastatic DFSP when not eligible for surgery.
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: Kit, the receptor for stem cell factor (SCF) coded for by the c-Kit protooncogene, the discoidin domain receptors (DDR1 and DDR2), the colony stimulating factor receptor (CSF-1R) and the platelet-derived growth factor receptors alpha and beta (PDGFR-alpha and PDGFR-beta). It also inhibits cellular events mediated by activation of these receptor kinases.
Dosage: Adult: Take with meal and large glass of water, if unable to swallow may disperse in glass of still water or apple juice. CML: Chronic phase, 400mg once daily; accelerated phase or blast crisis, 600mg once daily. May consider increasing dose to up to 800mg/day (maximum) as 400mg twice daily (morning and evening) in certain circumstances (see SPC). Ph+ ALL (supervise): 600mg once daily until disease progression. MDS/MPD: 400mg once daily. HES/CEL: 100mg once daily, may increase to 400mg if tolerated and response insufficient. Continue as long as patient benefits. DFSP: 800mg/day. Dose adjustments: See SPC. Hepatic impairment: 400mg daily, reduce if not tolerated. Renal impairment, dialysis (caution): Initially 400mg daily, increase/reduce if tolerated/not tolerated, respectively. Elderly: As per adults. Children: CML: Chronic or advanced phase, 340mg/m2 once daily dose or split (morning and evening); may consider increasing dose to 570mg/m2 daily in certain circumstances (see SPC); maximum 800mg total dose. Under 2 years, no experience. Ph+ ALL: 340mg/m2 (maximum 600mg total dose). Under 1 year, no experience. MDS/MPD, DFSP, HES/CEL: Under 18 years, not recommended.
Contraindications: Hypersensitivity to the active substance or to any of the excipients. Pregnancy (unless clearly necessary), lactation.
Special precautions: Evaluate renal function (closely monitor during therapy) prior to initiation, correct clinically significant dehydration and high uric acid levels prior to initiation, assess risk/benefit of HES/CEL patients prior to initiation. Hepatitis B reactivation may occur (consult expert if positive for serology prior to initiation or if HBV infection occurs during treatment); closely monitor carriers during therapy and for several months following discontinuation. Caution: Severe renal impairment, cardiac dysfunction. Cardiac disease (monitor for cardiac failure). Monitor liver enzymes (especially in patients with hepatic impairment, also monitor peripheral blood counts). Severe fluid retention (weigh patients regularly). Thyroidectomy patients undergoing levothyroxine replacement (closely monitor thyroid-stimulating hormone levels). Monitor for gastrointestinal (GI) haemorrhage (consider discontinuation). Closely monitor growth in children. Perform complete blood counts regularly. Cytopenias may occur in CML patients; may need to suspend or reduce dose. Driving/using machines (caution).
Drug interactions: Avoid: Strong CYP3A4 inducers, coumarin derivatives (use low-molecular-weight or standard heparin instead). Caution: CYP3A4 substrates, inducers, and inhibitors, paracetamol (with high dose Imatinib), CYP2D6 substrates with a narrow therapeutic window, levothyroxine, L-asparaginase.
Adverse drug reactions: Neutropenia (including febrile), thrombocytopenia, anaemia, pancytopenia, anorexia, insomnia, headache, dizziness, paraesthesia, taste disturbance, hypoaesthesia, fluid retention, oedema (including eyelid, face, periorbital), increased lacrimation, conjunctival haemorrhage, conjunctivitis, dry eye, blurred vision, flushing, haemorrhage, dyspnoea, epistaxis, cough, GI disorders, increased hepatic enzymes, dermatitis/ eczema/ rash, pruritus, dry skin, erythema, alopecia, night sweats, photosensitivity reaction, muscle spasm and cramps, pain (bone, musculoskeletal including myalgia), arthralgia, joint swelling, fatigue, weakness, pyrexia, anasarca, chills, rigors, increased/ decreased weight.
Full prescribing information and references available from Rowex Ltd. Telephone: 1800 304400. Fax: (027) 50417. E-mail: rowex@rowa-pharma.ie
The post Imatinib Rowex appeared first on Irish Medical Times.