Desferrioxamine mesilate

CLINICAL USE

Chelating agent:Acute iron poisoning Chronic iron or aluminium overload

DOSE IN NORMAL RENAL FUNCTION

SC/IV: Initially 500 mg then 20–60 mg/ kg/day 3–7 times a week. Exact dosages should be determined for each individualIM: 0.5–1 g daily as 1 or 2 injections, maintenance dose as per responseOral: acute iron poisoning: 5–10 g should be dissolved in 50–100 mL waterAluminium overload in

HD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :: (IV) 5 mg/kg weekly over last hour of dialysisPD: (SC, IM, IV, IP) 5 mg/kg weekly before the final exchange of the day

PHARMACOKINETICS

Molecular weight &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :656.8

%Protein binding &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :

<10 &nbsp &nbsp &nbsp &nbsp &nbsp :

%Excreted unchanged in urine &nbsp &nbsp : 22

Volume of distribution (L/kg) &nbsp &nbsp &nbsp :2–2.5

half-life – normal/ESRD (hrs)&nbsp &nbsp &nbsp :6/–

DOSE IN RENAL IMPAIRMENT

GFR (mL/MIN)

20 to 50 &nbsp &nbsp : Dose as in normal renal function

10 to 20 &nbsp &nbsp : Dose as in normal renal function

<10 &nbsp &nbsp &nbsp &nbsp &nbsp : Dose as in normal renal function

DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

CAPD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp:Dialysed. Treatment of aluminium overload: 1 g once or twice each week prior to final exchange of the day by slow

IV infusion

, IM, SC or IP

HD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :Dialysed. Treatment of aluminium overload: 1 g once each week administered during the last hour of dialysis as a slow

IV infusion

HDF/high flux &nbsp :Dialysed. Treatment of aluminium overload: 1 g once each week administered during the last hour of dialysis as a slow

IV infusion

CAV/VVHD &nbsp &nbsp &nbsp:Dialysed. Dose schedule unknown. Metal chelates will be removed by dialysis

IMPORTANT DRUG INTERACTIONS

Potentially hazardous interactions with other drugsAvoid prochlorperazine, methotrimeprazine (prolonged unconsciousness)Do not administer with blood

ADMINISTRATION

Reconstition

Dissolve contents of one vial (500 mg) in 5 mL of water for injection =10% solution. If for IV administration, the 10% solution can be diluted with sodium chloride 0.9%, glucose 5% or glucose/sodium chloride

Route

IV, SC (bolus or continuous infusion), IM, IP, oral

Rate of Administration

IV (acute overdose): Maximum 15 mg/kg/ hour. Reduce after 4–6 hours so that total dose does not exceed 80 mg/kg/24 hoursSC: Infuse over 8–24 hours. Local irritation may occur

Comments

The urine may appear orange/red in patients treated with desferrioxamine for severe iron intoxicationSC infusion is about 90% as effective as IV administration, which is now the route of choice in transfusion-related iron overloadIM injection is less effective than SC

OTHER INFORMATION

Studies suggest that during

HD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp : only a small amount of plasma desferrioxamine crosses the dialysis membraneContraindicated in patients with severe renal disease except those on dialysis100 mg desferrioxamine mesilate can bind 4.1 mg Al3+Desferrioxamine may predispose to development of infection with Yersinia speciesIn haemodialysis patients treated with desferrioxamine post dialysis, the half-life has been found to be extended to 19 hours between dialysis sessionsdesferrioxamine mesilate.dEsFErrioXAMinE MEsiLATE 219Anecdotally, escalating doses of up to 2 g, 3 times a week have been successfully used for iron overload in patients on haemodialysisIn treatment of acute iron poisoning, effectiveness of treatment is dependent on an adequate urine output. If oliguria or anuria develop, PD or

HD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp : may be necessary

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