[Durgical](https://durgical.com/en/) › [DurgiPedia](https://durgical.com/en/durgipedia/) › [Pharmacology](https://durgical.com/en/pharmacology/) › [Pulmonary arterial hypertension drugs (endothelin receptor antagonists and prostacyclins)](https://durgical.com/en/pharmacology/classes/pulmonary-arterial-hypertension-drugs/) › Iloprost

# 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.

Updated Nov 1, 2026

## Quick facts

**Group**
[Pulmonary arterial hypertension drugs (endothelin receptor antagonists and prostacyclins)](https://durgical.com/en/pharmacology/classes/pulmonary-arterial-hypertension-drugs/)

**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.

On this page

- The basics Mechanism of action
- Indications
- Adverse effects
- Pharmacokinetics
- Memory aid

- Safety Contraindications
- Key interactions
- What is monitored
- Administration and safety
- Pregnancy and breastfeeding
- Nursing care

- Study Test yourself

- Connections Connections

## Mechanism of action

◎**Prostacyclin receptor (IP receptor)**Iloprost

ⓘ 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).

**Target in 3D:** Prostacyclin receptor (IP receptor). PDB structure 8X7A (RCSB PDB, public domain). [View the structure at RCSB PDB](https://www.rcsb.org/structure/8X7A) · Drag to rotate · pinch to zoom

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 →](https://durgical.com/en/conditions/pulmonary-hypertension-and-cor-pulmonale/)
- Severe frostbite (intravenous) [Frostbite →](https://durgical.com/en/conditions/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)

### Serious (rare, important)

- Fainting and low blood pressure, especially on standing or exercise
- Bronchospasm, wheeze and breathing difficulty
- Changes in heart rhythm (intravenous)

## 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

## Memory aid

ILOprost: Inhaled Little and Often (short-acting), IV for Ice (frostbite).

## 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).

[Add to my cards (4)](https://durgical.app/estudiar/?add=/en/pharmacology/iloprost/)

[More Pharmacology questions →](https://durgical.com/en/practice/?f=pharmacology)

## Connections

## Related drugs 4

- [Epoprostenol](https://durgical.com/en/pharmacology/epoprostenol/)
- [Treprostinil](https://durgical.com/en/pharmacology/treprostinil/)
- [Selexipag](https://durgical.com/en/pharmacology/selexipag/)
- [Bosentan](https://durgical.com/en/pharmacology/bosentan/)

## Related conditions 2

- [Pulmonary hypertension and cor pulmonale](https://durgical.com/en/conditions/pulmonary-hypertension-and-cor-pulmonale/)
- [Frostbite](https://durgical.com/en/conditions/frostbite/)

[← Back to the class: Pulmonary arterial hypertension drugs (endothelin receptor antagonists and prostacyclins)](https://durgical.com/en/pharmacology/classes/pulmonary-arterial-hypertension-drugs/)

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](https://medlineplus.gov/druginfo/meds/a612032.html) (MedlinePlus (U.S. National Library of Medicine), 2026); [Iloprost Injection: MedlinePlus Drug Information](https://medlineplus.gov/druginfo/meds/a625114.html) (MedlinePlus (U.S. National Library of Medicine), 2026); [ATCDDD - ATC/DDD Index](https://atcddd.fhi.no/atc_ddd_index/?code=B01AC11) (WHO Collaborating Centre for Drug Statistics Methodology, 2026).

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Representative model, for educational purposes only.

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