Treprostinil
REMODULIN
What it isProstacyclin analog; pulmonary arterial hypertension.
Why this oneIt can be given subcutaneously, intravenously, by inhalation or orally, the widest route range of the prostacyclins.
What limits itInfusion-site pain is often severe with the subcutaneous route. Headache, jaw pain and diarrhea; abrupt interruption causes rebound.
FDA-approved for
- pulmonary arterial hypertension (2002)
FDA label
Read the full label on DailyMed ↗
| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| Pulmonary arterial hypertension (WHO Group 1) | Treprostinil-naïve adults | 26.5 mcg (2 breaths) 3–5x/day | 79.5–106 mcg QID | 848 mcg/day (studied) |
| PAH — transition from treprostinil inhalation solution (Tyvaso) | Adults | 26.5–159 mcg per transition table (3–5x/day) | 79.5–106 mcg QID | 848 mcg/day (studied) |
Titration Increase by 26.5 mcg per dose each week as tolerated
Renal No dosage adjustment required; not cleared by dialysis
Hepatic Uptitrate slowly (clearance reduced up to 80% in mild-to-moderate insufficiency); not studied in severe insufficiency
Instructions
- Oral inhalation only; do not swallow the capsules
- Use only with the provided inhaler
- Inhale contents of each capsule in 2 breaths
- If a scheduled dose is missed, resume as soon as possible at the usual dose
Cautions
- Symptomatic hypotension (pulmonary and systemic vasodilator)
- Increased bleeding risk (inhibits platelet aggregation)
- Dose adjustment may be needed with CYP2C8 inhibitors (e.g., gemfibrozil) or inducers (e.g., rifampin)
- Acute bronchospasm (higher risk in asthma/COPD/airway hyperreactivity)
Adverse reactions
- Cough
- Headache
- Throat irritation
- Dizziness
- Diarrhea
- Chest discomfort
- Nausea
Pregnancy Limited case reports insufficient; animal studies without adverse effects in rats but malformations in rabbits; PAH itself increases maternal/fetal mortality
Lactation No data on presence in human milk or effects on the breastfed infant
NO BOXED WARNINGS
Principal riskSevere infusion-site pain subcutaneously
Cost, est. cash$1,000–$20,000/month
Generic entry2017
Classes and tags
Clinical profile
Legacy pregnancy categoryUnknown / historical label unavailable
Defining liabilityGenerally tolerated at therapeutic doses; clinically important risks are agent-specific and increase with interactions or organ impairment.
Mechanism of action: Treprostinil ballicule
