Ferasiro

Deferasirox

Chronic Fe overload due to blood transfusions (transfusional hemosiderosis) in adults & ped patients ≥2 yr & nontransfusion-dependent thalassemia syndrome in patients ≥10 yr.

Transfusional Fe overload Initially 14 mg/kg daily, may be adjusted in steps of 3.5-7 mg/kg daily every 3-6 mth. Patient receiving packed RBC >14 mL/kg/mth Initially 21 mg/kg daily, may be increased to 28 mg/kg daily. Maintenance of body Fe level Patient receiving packed RBC <7 mL/kg/mth Initially 7 mg/kg daily. Nontransfusion-dependent thalassemia syndrome Initially 7 mg/kg daily, may be adjusted in steps of 3.5-7 mg/kg daily every 3-6 mth. Max: 14 mg/kg daily. Patient in whom liver Fe conc was not assessed & serum ferritin ≤2,000 mcg/L Not to exceed 7 mg/kg daily.

May be taken with or without food: Swallow whole w/ some water. For patients w/ swallowing difficulty, crush tab & sprinkle full dose on soft food (eg, yogurt, apple sauce/puree) & consume immediately.

Hypersensitivity. Concomitant use w/ other Fe chelator therapies. Patients w/ estimated CrCl <60 mL/min.

Discontinue use if any severe cutaneous ARs eg, SJS, TEN, DRESS is suspected or hypersensitivity reactions occur. Interrupt therapy if metabolic acidosis develops; proteinuria, glycosuria, renal tubulopathy or Fanconi syndrome & unexplained cytopenia occurs. Not recommended in patients w/ short life expectancy eg, high-risk myelodysplastic syndromes. Patients w/ platelet counts <50,000/mm³ (50 x 10⁹/L); signs & symptoms of GI ulceration & haemorrhage; blood disorders; cardiac dysfunction. Monitor serum creatinine, CrCl, plasma cystatin C prior to initiation, wkly during 1st mth & mthly thereafter; serum transaminases, bilirubin & alkaline phosphatase prior to initiation, every 2 wk during 1st mth & mthly thereafter; serum ferritin mthly. Perform auditory & ophth testing prior to initiation & annually thereafter. Ensure adequate hydration & acid-base balance. Long-term use. Concomitant use w/ medicinal products depressing renal function; substances w/ known ulcerogenic potential eg, NSAIDs, corticosteroids or oral bisphosphonates; anticoagulants. May affect ability to drive & use machines. Not recommended in severe hepatic impairment (Child-Pugh class C). Pre-existing renal & chronic hepatic conditions; renal impairment. Women of childbearing potential should use effective contraception. Not to be used during pregnancy. Not recommended during lactation. Monitor body wt, height & sexual development prior to initiation & annually thereafter in childn. Elderly.

Increased blood creatinine. Headache; diarrhoea, constipation, vomiting, nausea, abdominal pain & distension, dyspepsia; increased transaminases; rash, pruritus; proteinuria.

Decreased exposure & efficacy w/ potent UGT inducers (eg, rifampicin, carbamazepine, phenytoin, phenobarb, ritonavir), ciclosporin, simvastatin, hormonal contraceptives, bepridil, ergotamine. Reduced exposure w/ cholestyramine. Decreased midazolam exposure. Increased AUC & C_max of repaglinide, theophylline, CYP1A2-metabolised substances w/ narrow therapeutic index eg, clozapine, tizanidine. Low affinity for Al & Al-containing antacids. Increased GI toxicity w/ NSAIDs including high-dose ASA, corticosteroids, oral bisphosphonates. Increased GI haemorrhage w/ anticoagulants. Increased AUC of busulfan. Not to be combined w/ other Fe chelator therapies. Increased C_max w/ high-fat meal.

Antidotes & Detoxifying Agents

V03AC03 - deferasirox ; Belongs to the class of iron chelating agents. Used in the management of chronic iron overload associated with blood transfusion.

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