Epoprostenol
Pulmonary arterial hypertension drugs (endothelin receptor antagonists and prostacyclins)
Pulmonary arterial hypertension drugs (endothelin receptor antagonists and prostacyclins)High alert
An error with this medicine can cause serious harm: double checks and protocols are used.
Synthetic prostacyclin given as a continuous intravenous infusion for severe pulmonary arterial hypertension; it acts for only minutes.
Quick facts
- Group
- Pulmonary arterial hypertension drugs (endothelin receptor antagonists and prostacyclins)
- Target
- Prostacyclin receptor (IP receptor)
- Used for
- Pulmonary arterial hypertension
- Key effects
- Flushing and headache · Jaw pain · Nausea
- Monitor
- Blood pressure · Catheter site for infection
- ATC
- B01AC09
No doses: the clinician sets them by the current guideline.
Mechanism of action
No structure with epoprostenol 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).
Epoprostenol is prostacyclin (PGI2) itself. It activates the IP receptor on pulmonary artery smooth muscle, a Gs-coupled receptor that raises cyclic AMP; protein kinase A lowers intracellular calcium and relaxes the vessels, and cAMP also slows smooth-muscle growth. It dilates both pulmonary and systemic arteries, increases cardiac output and inhibits platelet aggregation. It is hydrolysed in blood within minutes.
- Epoprostenol (prostacyclin) binds the IP receptor of vascular smooth muscle
- Gs activates adenylyl cyclase and cyclic AMP rises
- Calcium falls: pulmonary and systemic arteries relax
- Pulmonary resistance falls and platelets aggregate less
Indications
- Pulmonary arterial hypertension (WHO group 1), especially advanced disease, to improve exercise capacity Pulmonary hypertension and cor pulmonale →
Adverse effects
Common
- Flushing and headache
- Jaw pain
- Nausea, vomiting and diarrhoea
- Musculoskeletal pain and flu-like symptoms
- Anxiety and nervousness
Contraindications
- Heart failure due to severe left ventricular systolic dysfunction
- Pulmonary oedema
- Hypersensitivity to epoprostenol or related compounds
Key interactions
- Diuretics, antihypertensives and other vasodilators
- Additive fall in blood pressure
- Anticoagulants and antiplatelet drugs
- Higher bleeding risk
- Digoxin
- Digoxin levels may rise, important in patients prone to toxicity
What is monitored
- Blood pressure, heart rate and symptoms at every dose change
- Infusion pump function and line patency
- Catheter site for infection; temperature
- Signs of rebound: sudden breathlessness, dizziness, weakness
Administration and safety
- Continuous intravenous infusion through a central venous catheter with an ambulatory pump
- Never mixed with other parenteral medicines or solutions, before or during the infusion
- The infusion must never be stopped or its rate reduced abruptly
- Aseptic technique for reconstitution, line changes and catheter care
- Some formulations are sensitive to light and temperature; preparation follows the product's instructions
Pregnancy and breastfeeding
Limited reports have not shown a clear drug-related risk; untreated pulmonary arterial hypertension carries serious risks for mother and fetus.
Nursing care
- Treat any pump alarm or line problem as an emergency: even a brief interruption can cause rebound
- Do not give other drugs or fluids through the epoprostenol line
- Check blood pressure and heart rate after every rate change
- Inspect the catheter site and watch for fever
- Teach the patient and family pump care, sterile technique and what to do if the infusion stops
Pharmacokinetics
- Metabolism
- Rapid spontaneous hydrolysis at blood pH plus enzymatic breakdown, to inactive products
- Elimination
- Metabolites mainly in urine
- Half-life
- A few minutes in human blood
- Onset and duration
- Within minutes; the effect also wears off within minutes if the infusion stops
Test yourself
Think of the answer, then tap the question to see it.
Why is epoprostenol given as a continuous infusion?
It is hydrolysed in blood within minutes; only a continuous central infusion keeps its effect.
What happens if the epoprostenol pump stops?
Rebound pulmonary hypertension can develop quickly, with breathlessness, dizziness and collapse.
Which receptor and second messenger does epoprostenol use?
The prostacyclin IP receptor, coupled to Gs, which raises cyclic AMP.
Which are two typical side effects of prostacyclin therapy?
Flushing, headache, jaw pain, diarrhoea or nausea.
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: DailyMed - EPOPROSTENOL injection, powder, lyophilized, for solution (DailyMed (U.S. National Library of Medicine), 2026); Epoprostenol: MedlinePlus Drug Information (MedlinePlus (U.S. National Library of Medicine), 2026); RCSB PDB - 8X7A: Treprostinil bound Prostacyclin Receptor G protein complex (RCSB Protein Data Bank, 2024).
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Representative model, for educational purposes only.