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.

Tags: post-by-auto-php