Treprostinil
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.
A longer-acting prostacyclin analogue for pulmonary arterial hypertension, given by subcutaneous or intravenous infusion, inhaled or by mouth.
Quick facts
- Group
- Pulmonary arterial hypertension drugs (endothelin receptor antagonists and prostacyclins)
- Target
- Prostacyclin receptor (IP receptor)
- Used for
- Pulmonary arterial hypertension · Inhaled form
- Key effects
- Headache and flushing · Jaw pain · Oedema
- Monitor
- Blood pressure · Infusion site pain and reaction
- ATC
- B01AC21
No doses: the clinician sets them by the current guideline.
Mechanism of action
The figure shows treprostinil bound to the human prostacyclin (IP) receptor coupled to its G protein (cryo-EM).
Treprostinil is a stable analogue of prostacyclin. Like epoprostenol it activates the IP receptor, raises cyclic AMP and relaxes pulmonary and systemic arteries, and it inhibits platelet aggregation. It lasts much longer than epoprostenol, which allows subcutaneous infusion, inhalation and oral tablets as well as intravenous use.
- Treprostinil binds the prostacyclin IP receptor
- Gs raises cyclic AMP in vascular smooth muscle
- Pulmonary arteries relax and platelets aggregate less
- Pulmonary resistance falls and exercise symptoms ease
Indications
- Pulmonary arterial hypertension (WHO group 1), to reduce symptoms on exercise Pulmonary hypertension and cor pulmonale →
- Patients who need to move from epoprostenol to another prostacyclin
- Inhaled form: pulmonary hypertension associated with interstitial lung disease
Adverse effects
Common
- Pain and reaction at the subcutaneous infusion site
- Headache and flushing
- Jaw pain
- Diarrhoea and nausea
- Oedema; cough and throat irritation with the inhaled form
Contraindications
- No absolute contraindications in the injection label
- Caution with low blood pressure, bleeding risk and liver impairment
Key interactions
- CYP2C8 inhibitors (gemfibrozil) or inducers (rifampicin)
- Raise or lower treprostinil exposure; the regimen is adjusted
- Anticoagulants and antiplatelet drugs
- Higher bleeding risk
- Antihypertensives, diuretics and other vasodilators
- Additive fall in blood pressure
What is monitored
- Blood pressure and symptoms after each dose change
- Infusion site pain and reaction (subcutaneous) or catheter site and temperature (intravenous)
- Signs of bleeding
- Exercise capacity and breathlessness
Administration and safety
- Continuous subcutaneous infusion is preferred; a central intravenous line is used if the site reaction is not tolerated
- Must not be stopped or reduced abruptly; pump problems are treated as urgent
- Strict aseptic technique with central lines because of bloodstream infection risk
- Inhaled and oral forms exist for selected patients
Pregnancy and breastfeeding
Human data are limited; untreated pulmonary arterial hypertension carries serious risks for mother and fetus, and the specialist team decides.
Nursing care
- Inspect subcutaneous infusion sites and help manage site pain
- For intravenous use, inspect the catheter and report fever promptly
- Check blood pressure and watch for bleeding
- Teach pump care and what to do if the infusion stops
Pharmacokinetics
- Absorption
- Subcutaneous infusion is almost completely absorbed; also given intravenously, inhaled or orally
- Metabolism
- Liver, mainly by CYP2C8
- Elimination
- Mostly in urine, as metabolites
- Half-life
- About 4 hours after subcutaneous infusion
Test yourself
Think of the answer, then tap the question to see it.
What advantage does treprostinil have over epoprostenol?
It is more stable and longer acting, so it can be given subcutaneously, inhaled or by mouth as well as intravenously.
What is the most common adverse effect of subcutaneous treprostinil?
Pain and reaction at the infusion site.
Which serious complication is linked to intravenous treprostinil through a central line?
Bloodstream infection and sepsis.
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 - TREPROSTINIL injection, solution (DailyMed (U.S. National Library of Medicine), 2025); Treprostinil Oral Inhalation: 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.