Deferiprone
Deferiprone.JPG

Deferiprone

CLINICAL USE

Orally administered chelator:Treatment of transfusional iron overload

DOSE IN NORMAL RENAL FUNCTION

25 mg/kg 3 times daily. Maximum 100 mg/kg daily

PHARMACOKINETICS

  • Molecular weight                           :139.2
  • %Protein binding                           :No data
  • %Excreted unchanged in urine     : 15 – see Other Information
  • Volume of distribution (L/kg)       :1.55–1.73
  • half-life – normal/ESRD (hrs)      :2–3/Unknown

    DOSE IN RENAL IMPAIRMENT

    GFR (mL/MIN)

  • 20 to 50     : Dose as in normal renal function
  • 10 to 20     : Give 50% of dose and monitor
  • <10           : Give 50% of dose and monitor

    DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

  • CAPD                :Unknown dialysability. Dose as in GFR <10 mL/min
  • HD                     :Dialysed. Dose as in GFR <10 mL/min
  • HDF/high flux   :Dialysed. Dose as in GFR <10 mL/min
  • CAV/VVHD      :Dialysed. Dose as in GFR 10 to 20 mL/min

    IMPORTANT DRUG INTERACTIONS

    Potentially hazardous interactions with other drugsNone known

    ADMINISTRATION

    Reconstition

    Route

    Oral

    Rate of Administration

    Comments

    OTHER INFORMATION

    Deferiprone is hepatically metabolised (>85%) to predominantly glucuronide conjugates (no chelating activity). Deferiprone, the glucuronide conjugates, and deferiprone-complexed iron are cleared principally by the kidney, with 80% of the dose recovered in the urineSide effects include reversible neutropenia, agranulocytosis, musculoskeletal and joint pain, subclinical ototoxicity, plus case reports of systemic vasculitis and fatal SLECan cause subnormal serum zinc levels Reddish-brown discolouration of the urine reported in 40% of thalassaemia patients undergoing deferiprone therapyDeferiprone removed aluminium in vitro from blood samples of 46 patients undergoing chronic haemodialysis. Only patients with serum aluminium concentrations >80 mcg/mL were included. Deferiprone removed the aluminium faster and more effectively from higher molecular weight proteins than desferrioxamine. (Canteros-Piccotto MA, Fernández-Martin JL, Cannata-Ortiz MJ, et al. Effectiveness of deferiprone (L1) releasing the aluminium bound to plasma proteins in chronic renal failure.



    See how to identify renal failure stages according to GFR calculation

    See how to diagnose irreversible renal disease

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