Pharmacokinetic evaluation of continuous intravenous epoprostenol

Importance of the field: Prostacyclin is the main arachidonic acid metabolite and its decrease has been proven to be important in the pathophysiology of the pulmonary arterial hypertension (PAH). Epoprostenol has been the first analog of prostacyclin to be approved for the treatment of PAH and despite the development of therapeutic options, the last recommendations of European Societies of Cardiology and Pulmonology maintain it as the first choice therapy for severe patients in the WHO functional class IV. In this review, we focus on pharmacokinetics of epoprostenol characterized by its instability in aqueous biological fluids and compare its pharmacokinetics with other stable analogs of prostacyclin. Moreover, pharmacodynamics, clinical efficacy and safety of epoprostenol were studied. Areas covered in this review: A literature search and review of the studies published on epoprostenol were carried out using the MEDLINE database. What the reader will gain: The paper provides the reader with information on epoprostenol pharmacokinetics and comparison with other analogs of prostacyclin. This paper also provides data on pharmacodynamics, clinical efficacy, safety and tolerability of epoprostenol. Take home message: Despite epoprostenol's short half-life and complicated delivery system, this treatment remains the first choice therapy for severe PAH patients.