Brand name: Aurlumyn
Drug class: Vasodilating Agents, Miscellaneous

Medically reviewed by Drugs.com on Feb 10, 2025. Written by ASHP.

Introduction

Vasodilator and platelet-aggregation inhibitor; synthetic analog of prostacyclin (PGI₂).

Uses for Iloprost (Frostbite)

Frostbite

Treatment of severe frostbite in adults to reduce the risk of digit amputations. Effectiveness established in young, healthy adults who suffered frostbite at high altitudes.

The American Burn Association and the Wilderness Medical Society have published clinical practice guidelines on treatment of frostbite. Goals of treatment include decreasing ischemia, inflammation, and coagulation, and restoring blood flow to prevent irreversible ischemia.

The Wilderness Medical Society recommends consideration of IV iloprost as first-line therapy for grade 3 or 4 frostbite less than 72 hours after injury, when tissue plasminogen activator (tPA) is contraindicated, and in settings where tPA infusion is considered risky or evacuation to a treatment facility will be delayed. The American Burn Association states that no recommendation can be made on the use of iloprost for reducing the risk of amputations; additional larger studies are needed.

Iloprost (Frostbite) Dosage and Administration

General

Pretreatment Screening

• Monitor vital signs prior to the start of the infusion and with every dose increase.

• Monitor BP. Correct hypotension prior to administration of iloprost.

Patient Monitoring

• Monitor vital signs during infusion.

• Monitor BP.

Administration

IV Administration

Administer as a continuous IV infusion (after dilution) over 6 hours each day for up to a maximum of 8 consecutive days.

Administer via a peripheral line or peripherally inserted central catheter using an infusion pump. Use an infusion set with an in-line 0.22- or 0.2-micron filter.

The infusion pump should (1) be able to deliver rates of 0.1 to 99.9 mL per hour, (2) adjust infusion rates with increments of 0.1 mL per hour, (3) be accurate to within 5% of the programmed rate, and (4) be positive pressure-driven (continuous or pulsatile). The reservoir and infusion line set should be made of PVC.

Avoid inadvertent administration of a bolus dose. Do not flush catheter without withdrawing residual drug from the catheter system. Discard any unused portion.

Dilution

Use aseptic technique to prepare the infusion solution.

Dilute only using 0.9% sodium chloride injection. Do not dilute or mix with any other parenteral medications or solutions.

Withdraw 1 mL (100 mcg) of iloprost solution from the vial and transfer into a PVC infusion bag containing 100 mL of 0.9% sodium chloride injection to provide a final concentration of 1 mcg/mL (1000 ng/mL).

Iloprost can be added to commercially available infusion bags labeled as containing 100 mL of 0.9% sodium chloride injection.

Gently mix by slowly inverting IV bag. Do not shake.

Rate of Administration

Infusion rates may be calculated using the following formula:

Infusion rate (mL/hr)=[dose (ng/kg/min) x weight (kg) x 60 min/hr]/final concentration of iloprost (1000 ng/mL)

Dosage

Adults

Severe Frostbite

IV Infusion

Dosage is based on actual patient body weight (kg).

Start initial infusion on day 1 at a rate of 0.5 ng/kg/minute and increase in increments of 0.5 ng/kg/minute every 30 minutes based on tolerability up to a maximum of 2 ng/kg/minute.

Repeat dose titration steps on day 2 and day 3.

From day 4 onward, start infusion at the highest tolerated dose from previous day, and adjust rate as needed, based on tolerability.

Dosage Modification for Toxicity

If a dose-limiting adverse reaction (e.g., headache, flushing, jaw pain, myalgia, nausea, vomiting) occurs during administration at the starting dosage, discontinue infusion; may attempt re-initiation of the infusion after the event resolves or is treated.

If a dose-limiting adverse reaction occurs that cannot be tolerated by the patient, then decrease the dosage in a stepwise manner by 0.5 ng/kg/min every 30 minutes, until a tolerated dosage is reached.

If the infusion is stopped at any point for a dose-limiting adverse event, the infusion can be reinitiated at a previously tolerated dose/infusion rate once the event has resolved; maximum tolerated dose should be maintained for the remaining 6-hour daily infusion.

Special Populations

Hepatic Impairment

Patients with moderate or severe hepatic impairment (Child-Pugh Class B or C): initiate infusion at 0.25 ng/kg/minute for 30 minutes, then continue titration in 0.5 ng/kg/minute increments every 30 minutes according to tolerability to a maximum dosage of 2 ng/kg/minute.

Renal Impairment

Patients with renal impairment with eGFR <30 mL/minute: initiate and titrate dosing per recommended dosage. If patient cannot tolerate starting dosage of 0.5 ng/kg/minute, dosage can be decreased to 0.25 ng/kg/minute. For patients requiring intermittent hemodialysis, consider iloprost administration after the end of hemodialysis. Alternatively, hemodialysis can be started at least 1 hour after the end of iloprost infusion.

Geriatric Patients

Select dosage with caution.

Cautions for Iloprost (Frostbite)

Contraindications

• None

Warnings/Precautions

Hypotension

Iloprost is a systemic vasodilator and may cause symptomatic hypotension.

Correct hypotension prior to administration and monitor vital signs during administration.

Consider temporary discontinuation of concomitant vasodilator or other antihypertensive medications while administering iloprost to reduce potential additive hypotensive effects. Consider down-titration or discontinuation of therapy if hypotension persists despite discontinuation of other antihypertensives and fluid resuscitation.

Specific Populations

Pregnancy

No available data with iloprost injection during pregnancy to evaluate for a drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes. Limited cases of inhaled iloprost use during pregnancy have not identified a drug-associated risk of adverse maternal or fetal outcomes.

Lactation

No data on presence of iloprost in human milk, effects on the breastfed infant, or effects on milk production. Advise women not to breastfeed during treatment with iloprost.

Females and Males of Reproductive Potential

No human data on the effect of iloprost on reproductive potential. Animal studies indicate iloprost does not impact fertility.

Pediatric Use

Safety and efficacy not established.

Geriatric Use

Insufficient experience in patients ≥65 years of age to determine whether they respond differently than younger patients.

Hepatic Impairment

Mean clearance reduced by approximately 50% in Child-Pugh Class B hepatic impairment. In patients with moderate or severe hepatic impairment (Child-Pugh Class B or C), use a lower starting dosage of 0.25 ng/kg/minute.

Renal Impairment

Systemic exposure substantially higher in patients with kidney failure receiving intermittent hemodialysis than in those not requiring dialysis.

In patients with renal impairment (eGFR <30 mL/minute), dosage can be lowered to 0.25 ng/kg/minute if starting dosage of 0.5 ng/kg/minute is not tolerated. For patients requiring intermittent hemodialysis, consider iloprost administration after the end of hemodialysis. Alternatively, hemodialysis can be started at least 1 hour after the end of the infusion.

Common Adverse Effects

Most common adverse effects include headache, flushing, palpitations/tachycardia, nausea, vomiting, dizziness, hypotension.

Drug Interactions

CYP isoenzymes play only a minor role in metabolism; metabolized principally via β-oxidation.

Specific Drugs

Iloprost (Frostbite) Pharmacokinetics

Distribution

Plasma Protein Binding

Approximately 60% protein-bound, primarily to albumin.

Elimination

Metabolism

Metabolized principally via β-oxidation of the carboxyl side chain.

Main metabolite is tetranor-iloprost, which is found in the urine in free and conjugated form.

Elimination Route

Excreted in urine (68%) and feces (12%).

Half-life

Half-life is 20 to 30 minutes.

Stability

Storage

Parenteral

Injection concentrate

Unopened vials are stable until date indicated on package when stored at 20–25ºC (excursions permitted between 15–30ºC). Keep in carton and do not expose to direct sunlight. Do not freeze.

Diluted solutions can be stored at room temperature (20–25°C) for up to 4 hours, if not used immediately.

Actions

• Synthetic analog of prostacyclin PGI₂.

• Pharmacologic actions include vasodilation and inhibition of platelet aggregation.

Advice to Patients

• Advise patients that iloprost can decrease BP, so dizziness may occur during drug administration. Patients should stand up slowly when getting out of a chair or bed.

• Advise patients to inform their clinician of existing or contemplated concomitant therapy, including prescription and OTC drugs and dietary or herbal supplements, as well as any concomitant illnesses.

• Advise patients to inform their clinician if they are or plan to become pregnant or plan to breast-feed.

• Inform patients of other important precautionary information.

Additional Information

The American Society of Health-System Pharmacists, Inc. represents that the information provided in the accompanying monograph was formulated with a reasonable standard of care, and in conformity with professional standards in the field. Readers are advised that decisions regarding use of drugs are complex medical decisions requiring the independent, informed decision of an appropriate health care professional, and that the information contained in the monograph is provided for informational purposes only. The manufacturer’s labeling should be consulted for more detailed information. The American Society of Health-System Pharmacists, Inc. does not endorse or recommend the use of any drug. The information contained in the monograph is not a substitute for medical care.

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

Iloprost is obtained through specialty distributors. Contact manufacturer or consult the Aurlumyn™ website at [Web] for specific availability information.

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