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What class of medication is epoprostenol?

3 min read

Globally, an estimated 192,000 people had pulmonary arterial hypertension (PAH) in 2021. For those with this condition, a key question is, what class of medication is epoprostenol? Epoprostenol belongs to the prostacyclin analog class, serving as a powerful vasodilator.

Quick Summary

Epoprostenol is a prostacyclin analog, a potent vasodilator, and a platelet aggregation inhibitor used to treat pulmonary arterial hypertension (PAH) by relaxing blood vessels in the lungs.

Key Points

  • Classification: Epoprostenol is a prostacyclin analog, which is a type of prostaglandin, and also functions as a vasodilator and platelet aggregation inhibitor.

  • Primary Indication: It is primarily used to treat pulmonary arterial hypertension (PAH) to improve exercise capacity and slow symptom progression.

  • Mechanism of Action: Epoprostenol works by directly dilating pulmonary and systemic arteries and inhibiting the clumping of platelets.

  • Administration: Due to an extremely short half-life of 3-6 minutes, it must be administered via a continuous intravenous infusion.

  • Critical Risk: Abruptly stopping or interrupting the epoprostenol infusion can cause severe rebound pulmonary hypertension and can be fatal.

  • Brand Names: Common brand names for epoprostenol are Flolan and Veletri.

  • Proven Survival Benefit: It is the only medication for PAH that has been shown to improve survival in randomized, controlled trials.

In This Article

Understanding Epoprostenol's Role in Pharmacology

Epoprostenol is a synthetic form of prostacyclin, a natural body substance. It's classified as a prostacyclin analog, falling under prostaglandins and vasodilators. Approved in 1995, it was the first FDA-approved therapy for pulmonary arterial hypertension (PAH). PAH involves narrowed lung blood vessels, increasing pressure and straining the heart. Epoprostenol combats this by widening these vessels and preventing platelet clumping, improving blood flow and reducing heart strain.

Mechanism of Action

Epoprostenol, derived from arachidonic acid, has two main effects:

  1. Potent Vasodilation: Relaxes and widens pulmonary and systemic arteries, lowering high blood pressure in the pulmonary arteries.
  2. Inhibition of Platelet Aggregation: Prevents platelets from forming clots, which can block narrowed lung vessels.

Its short half-life of 3-6 minutes necessitates continuous intravenous infusion via a pump and central catheter. Stopping the infusion can cause a dangerous and potentially fatal rebound in pulmonary hypertension.

Primary Medical Use: Pulmonary Arterial Hypertension (PAH)

Epoprostenol treats WHO Group 1 PAH, enhancing exercise ability and slowing symptom progression. It's a first-line option for advanced disease (NYHA Class IV) due to its proven survival benefit in trials. It improves hemodynamics, functional class, and exercise tolerance in various forms of PAH.

Administration

Initial treatment often occurs in a hospital setting to carefully manage potential side effects and adjust the administration rate. Long-term use requires meticulous care of the pump and catheter to prevent infections. Brand names include Flolan and Veletri. Veletri is stable at room temperature, which differs from Flolan.

Common Side Effects and Risks

Side effects, often dose-related extensions of its vasodilatory action, include flushing, headache, jaw pain, nausea, vomiting, diarrhea, hypotension, and musculoskeletal pain. Catheter-related infections are a significant risk with long-term use. Abrupt discontinuation is extremely dangerous, potentially causing rapid, severe worsening of PAH.

Comparison of Prostacyclin Pathway Therapies

Epoprostenol is one of several drugs targeting the prostacyclin pathway, with different administration methods and properties.

Medication Class/Mechanism Route of Administration Half-Life Key Features
Epoprostenol Prostacyclin Analog Continuous IV Infusion ~3-6 minutes First approved PAH therapy; proven survival benefit; requires pump and central line.
Treprostinil Prostacyclin Analog IV, Subcutaneous, Inhalation, Oral ~3-4 hours More stable with a longer half-life, allowing for more administration options including oral tablets (Orenitram) and inhalation (Tyvaso).
Iloprost Prostacyclin Analog Inhalation ~20-25 minutes Administered via a nebulizer multiple times daily; localized effect on the lungs can minimize systemic side effects.
Selexipag Selective IP Prostacyclin Receptor Agonist Oral Metabolite: ~7.9 hours An oral medication that works on the same receptor as prostacyclin but is not a prostacyclin analog; allows for twice-daily dosing.

Conclusion

Epoprostenol, a prostacyclin analog, vasodilator, and platelet aggregation inhibitor, is vital for severe PAH treatment. It dilates pulmonary arteries and prevents clotting, extending life and improving hemodynamics and exercise capacity in advanced PAH. Despite challenges like its short half-life and the risks of continuous IV infusion, its survival benefit confirms its crucial role. Ongoing development of other prostacyclin pathway drugs with alternative delivery methods continues to broaden treatment possibilities.


For further reading on prostacyclin analogs, see the National Center for Biotechnology Information's article on the topic: Prostacyclin Analogs - LiverTox - NCBI Bookshelf

Disclaimer: This information is for general knowledge and should not be taken as medical advice. Consult with a healthcare professional before starting any new supplement regimen.

Frequently Asked Questions

The main brand names for epoprostenol are Flolan® and Veletri®.

Epoprostenol must be infused continuously because it has a very short half-life in the body, estimated to be between 3 and 6 minutes. If the infusion is stopped, the drug is eliminated very quickly, leading to a rapid and dangerous return of high blood pressure in the lungs.

Epoprostenol is primarily used to treat pulmonary arterial hypertension (PAH), a condition of high blood pressure in the arteries of the lungs. It helps improve the ability to exercise and slows the worsening of symptoms.

The most common side effects are related to its vessel-widening properties and include flushing (redness of the skin), headache, jaw pain, nausea, vomiting, diarrhea, dizziness, and muscle or bone pain.

Yes, it is extremely dangerous. Suddenly stopping epoprostenol can cause a rebound effect where pulmonary hypertension rapidly worsens, which can be fatal. Any changes to the dose must be done under a doctor's supervision.

Epoprostenol works in two main ways: it is a potent vasodilator that relaxes and widens the narrowed blood vessels in the lungs, and it inhibits platelet aggregation, which prevents blood cells from clumping together and forming clots. Both actions help to reduce pressure and improve blood flow.

Flolan and Veletri are both brand names for epoprostenol. A key difference is their formulation and stability. The original Flolan formulation needs to be kept cold with ice packs during infusion, while Veletri is stable at room temperature.

No, epoprostenol cannot be taken orally. Due to its very short half-life and instability, it must be administered as a continuous intravenous infusion.

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Medical Disclaimer

This content is for informational purposes only and should not replace professional medical advice.