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.

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