Iloprost
Pulmonary arterial hypertension drugs (endothelin receptor antagonists and prostacyclins)
Pulmonary arterial hypertension drugs (endothelin receptor antagonists and prostacyclins)
A prostacyclin analogue: inhaled for pulmonary arterial hypertension, and given intravenously for severe frostbite.
Quick facts
- Group
- Pulmonary arterial hypertension drugs (endothelin receptor antagonists and prostacyclins)
- Target
- Prostacyclin receptor (IP receptor)
- Used for
- Pulmonary arterial hypertension · Severe frostbite
- Key effects
- Flushing and headache · Cough · Nausea
- Monitor
- Blood pressure and dizziness
- ATC
- B01AC11
No doses: the clinician sets them by the current guideline.
Mechanism of action
No structure with iloprost on the IP receptor is available: the figure shows treprostinil, a prostacyclin analogue that occupies the same site of the human IP receptor (cryo-EM, with its G protein).
Iloprost is a stable synthetic analogue of prostacyclin. It activates the IP receptor on vascular smooth muscle, which raises cyclic AMP and relaxes the vessel; it also inhibits platelet aggregation. Inhaled, it acts mainly on the pulmonary arteries and lowers pulmonary vascular resistance with less systemic vasodilation than intravenous prostacyclin. Given intravenously, it dilates small vessels in frostbitten tissue.
- Iloprost activates the prostacyclin (IP) receptor
- Gs raises cyclic AMP in vascular smooth muscle
- Pulmonary arteries dilate; platelets aggregate less
- Pulmonary vascular resistance falls while the effect lasts
Indications
- Pulmonary arterial hypertension (inhaled) Pulmonary hypertension and cor pulmonale →
- Severe frostbite (intravenous) Frostbite →
Adverse effects
Common
- Flushing and headache
- Cough
- Jaw muscle pain or tightness
- Nausea, vomiting and dizziness
- Blurred vision, trouble sleeping and tongue pain (inhaled)
Contraindications
- Hypersensitivity to iloprost
- Caution with low blood pressure, asthma, COPD or a lung infection
- Caution in liver or kidney disease
Key interactions
- Vasodilators and antihypertensives
- Additive fall in blood pressure
- Anticoagulants and antiplatelet drugs
- Iloprost inhibits platelets; bleeding risk may add up
What is monitored
- Blood pressure and dizziness
- Breathing and wheeze after inhalation
- Heart rhythm during intravenous infusion
Administration and safety
- Inhaled only through its own nebuliser system, at least two hours apart, and not mixed with other medicines
- The solution is not swallowed; skin or eye contact is rinsed with water
- The nebuliser is kept away from others, especially pregnant women and infants; a backup system is kept
- Intravenous iloprost for frostbite is infused by staff over several hours a day
Pregnancy and breastfeeding
Data in pregnancy are limited; pulmonary hypertension itself carries high risk in pregnancy, and use is decided with the specialist. Breastfeeding is avoided during intravenous treatment.
Nursing care
- Check blood pressure and teach to rise slowly to avoid fainting
- Teach correct nebuliser use and cleaning
- Teach to report wheeze, breathing difficulty or pink frothy sputum at once
- Inhaled iloprost has been discontinued in the US; product availability depends on the country
Pharmacokinetics
- Absorption
- Inhaled by nebuliser (pulmonary hypertension) or intravenous infusion (frostbite)
- Metabolism
- Little CYP-dependent metabolism
- Onset and duration
- A single inhalation acts for a short time, so it is inhaled several times a day
Test yourself
Think of the answer, then tap the question to see it.
Why is inhaled iloprost given several times a day?
The effect of a single inhalation is short-lived.
What is the advantage of inhaling a prostacyclin analogue in pulmonary hypertension?
It acts mainly on the pulmonary vessels, with less systemic vasodilation and hypotension.
Which non-pulmonary emergency is an indication for intravenous iloprost?
Severe frostbite.
Which two adverse effects are shared by the prostacyclin class?
Headache and jaw pain (also flushing).
Connections
Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.
Sources: Iloprost Oral Inhalation: MedlinePlus Drug Information (MedlinePlus (U.S. National Library of Medicine), 2026); Iloprost Injection: MedlinePlus Drug Information (MedlinePlus (U.S. National Library of Medicine), 2026); ATCDDD - ATC/DDD Index (WHO Collaborating Centre for Drug Statistics Methodology, 2026).
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Representative model, for educational purposes only.