iloprost

CLINICAL USE

Prostacyclin analogue:Treatment of pulmonary hypertension Relief of pain, promotion of ulcer-healing and limb salvage in patients with severe peripheral arterial ischaemia (unlicensed product)

DOSE IN NORMAL RENAL FUNCTION

Pulmonary hypertension: Nebulised: 2.5–5 mcg per inhalation —session 6 to 9 times per dayIV: Usually 1–8 ng/kg/min, but can —use higher doses (up to 25 ng/kg/min) according to responseSevere peripheral arterial ischaemia: Dose is adjusted according to —individual tolerability within the range of 0.5–2 ng/kg/min over 6 hours daily

PHARMACOKINETICS

Molecular weight :360.5

%Protein binding :≈60

%Excreted unchanged in urine : <5

Volume of distribution (L/kg) :0.6–0.8

half-life – normal/ESRD (hrs) :0.3–0.5/Unchanged

DOSE IN RENAL IMPAIRMENT

GFR (mL/MIN)

20 to 50 : Dose as in normal renal function

10 to 20 : Dose as in normal renal function

<10 : Dose as in normal renal function

DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

CAPD :Unknown dialysability. Dose as in normal renal function

HD :Unknown dialysability. Dose as in normal renal function

HDF/high flux :Unknown dialysability. Dose as in normal renal function

CAV/VVHD :Unknown dialysability. Dose as in normal renal function

IMPORTANT DRUG INTERACTIONS

Potentially hazardous interactions with other drugs

Anticoagulants: enhanced anticoagulant effect and increased risk of bleeding with heparin, coumarins and phenindione, as iloprost inhibits platelet aggregationIncreased risk of bleeding with NSAIDs, aspirin, clopidogrel, eptifibatide and tirofiban

ADMINISTRATION

Reconstition

Dilute 0.1 mg with 500 mL sodium chloride 0.9% or glucose 5%. Final concentration = 0.2 micrograms iloprost/mL

Route

Nebulised,

IV infusion

via peripheral vein or central venous catheter

Rate of Administration

Infuse 0.1 mg over 6 hours daily (see below)

Comments

Treatment should be started at an infusion rate of 10 mL/hour for 30 minutes, which corresponds to a dose of 0.5 nanograms/kg/minute for a patient of 65 kgThen increase dose in steps of 10 mL/hour every 30 minutes up to a rate of 40 mL/hour (50 mL/hour if patient’s body weight is more than 75 kg)If side effects occur (e.g. headache, nausea, or an undesired drop in BP), infusion rate should be reduced until the tolerable dose is found; if side effects are severe, infusion should be interruptedFor rest of the treatment period, continue with dose found to be tolerated in the first 2–3 days

OTHER INFORMATION

BP and heart rate must be measured at the start of the infusion and after every increase in doseDuration of treatment is up to 4 weeks. Shorter treatment periods (3–5 days) are often sufficient in Raynaud’s phenomenonIloprost infusions can also be used to control blood pressure during a scleroderma hypertensive crisisFor fluid-restricted patients, dilute 0.1 mg iloprost with 50 mL sodium chloride 0.9%, and run at a rate of 1–4 mL/hourToxic by inhalation, contact with skin, and if swallowed.

See how to identify renal failure stages according to GFR calculation

See how to diagnose irreversible renal disease

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