pentamidine isethionate.txt

CLINICAL USE

Antibacterial agent:Pneumocystis treatment and prophylaxis Visceral leishmaniasis Cutaneous leishmaniasis Trypanosomiasis

DOSE IN NORMAL RENAL FUNCTION

Pneumocystis: Treatment: Nebuliser: 600 mg daily for —3 weeks; IV: 4 mg/kg/day for at least 14 days Prophylaxis: 300 mg monthly or —150 mg every 2 weeksVisceral leishmaniasis: 3–4 mg/kg on alternate days to a maximum of 10 doses (deep IM)Cutaneous leishmaniasis: 3–4 mg/kg once or twice weekly (deep IM)Trypanosomiasis: 4 mg/kg daily, or alternate days to a total of 7–10 doses (deep IM or IV)

PHARMACOKINETICS

Molecular weight &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :592.7

%Protein binding &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :69

%Excreted unchanged in urine &nbsp &nbsp : <5

Volume of distribution (L/kg) &nbsp &nbsp &nbsp :3–4

half-life – normal/ESRD (hrs)&nbsp &nbsp &nbsp :6–9/9

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 : Depending on severity of infection: 4 mg/kg/day IV for 7–10 days, then on alternate days to complete minimum 14 doses, OR, 4 mg/kg on alternate days to complete minimum 14 doses

DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

CAPD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp:Not dialysed. Dose as in GFR <10 mL/min

HD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :Not dialysed. Dose as in GFR <10 mL/min

HDF/high flux &nbsp :Unknown dialysability. Dose as in GFR <10 mL/min

CAV/VVHD &nbsp &nbsp &nbsp:Unknown dialysability. Dose as in GFR 10 to 20 mL/min

IMPORTANT DRUG INTERACTIONS

Potentially hazardous interactions with other drugs

Anti-arrhythmics: increased risk of ventricular arrhythmias with amiodarone – avoid concomitant use

Antibacterials: increased risk of ventricular arrhythmias with moxifloxacin and parenteral erythromycin – avoid concomitant use with moxifloxacin

Antidepressants: increased risk of ventricular arrhythmias with tricyclics

Antipsychotics: increased risk of ventricular arrhythmias with amisulpride and phenothiazines – avoid concomitant use with amisulprideIvabradine: increased risk of ventricular arrhythmias

ADMINISTRATION

Reconstition

IV: 300 mg with 3–5 mL water for injection IM: 300 mg with 3 mL water for injection Inhalation: 600 mg with 6 mL water for injection

Route

IV, IM, nebulised

Rate of Administration

Over at least 1 hour

Comments

Dilute calculated dose in 50–250 mL sodium chloride 0.9% or glucose 5%Pentamidine isetionate.570 PEnTAMidinE isETionATE

OTHER INFORMATION

Monitor patients closely Patient must be lying down when drug is administeredIf given by

IV infusion

, patient should be monitored closely: heart rate, blood pressure, blood glucoseIV prophylaxis (unlicensed): 4–5 mg/kg over a minimum of 1 hour every 4 weeksNebulise over 20 minutes using Respigard II or other suitable nebuliser, oxygen flow rate 6–10 L/minute5 mg nebulised salbutamol may be given prior to pentamidine nebulisation to reduce risk of bronchospasm. Do not mix together in nebuliserMay produce reversible impairment of renal functionRenal clearance accounts for <5% of the plasma clearance of pentamidine.

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