Epoprostenol (epoprostenol sodium (glycine))
Last reviewed · Source: First Databank (FDB) drug data
Overview
Epoprostenol (PGI2, PGX, prostacyclin), a naturally occurring prostaglandin, is a short-acting vasodilator and platelet-aggregation inhibitor.
Epoprostenol sodium (PGI2, PGX, prostacyclin), the synthetic salt of a naturally occurring prostaglandin, possesses the pharmacologic actions (e.g., vasodilation of pulmonary and systemic arterial vascular beds, inhibition of platelet aggregation) of endogenous prostacyclin, a naturally occurring prostaglandin and arachidonic acid metabolite. Epoprostenol, a short-acting vasodilating agent and a platelet-aggregation inhibitor, produces dose-related increases in cardiac index and stroke volume and dose-related decreases in pulmonary vascular resistance, total pulmonary resistance, and mean systemic arterial pressure.
In animals, epoprostenol reduces right and left ventricular afterload and increases cardiac output and stroke volume as a result of the drug's vasodilatory effects. Studies have shown that cardiac effects of the drug are dose dependent; low doses of epoprostenol may cause a vagally mediated bradycardia while high doses of the drug cause a reflex tachycardia secondary to direct vasodilation and hypotension. Epoprostenol and synthetic prostacyclin analogs may have antiproliferative effects, including inhibition of fibromuscular proliferation of the intima of precapillary arteries which may be involved in the pathogenesis of pulmonary hypertension.
Major effects on cardiac conduction have not been reported. Additional pharmacologic effects of epoprostenol observed in animals include bronchodilation, inhibition of gastric acid secretion, and decreased gastric emptying.
Since epoprostenol is unstable at pH values below 10.2-10.8 (for Flolan(R)) and 11-13 (for the Veletri(R) preparation), oral administration is not possible and continuous IV administration is necessary, because of the drug's short half-life (about 6 minutes). Administration of the drug is complex, because of the requirements for continuous IV infusion (using permanent indwelling catheters), drug reconstitution by patients, operation of infusion pump, and protection from light. The benefits of epoprostenol therapy in patients with pulmonary arterial hypertension (e.g., improvement in survival, exercise capacity, and quality of life assessments) and the logistical issues associated with drug's administration have led to the development of more stable synthetic prostacyclin analogs with similar pharmacologic actions and less complicated routes of administration (e.g., iloprost by oral inhalation, treprostinil by continuous subcutaneous infusion).
Epoprostenol is rapidly hydrolyzed at neutral pH in plasma and also undergoes enzymatic degradation. Chemical assays with sufficient sensitivity and specificity to assess the in vivo pharmacokinetics of epoprostenol in humans are not currently available. Epoprostenol is metabolized to 2 major metabolites, 6-keto-PGF1alpha (formed by spontaneous degradation) and 6,15-diketo-13,14-dihydro-PGF1alpha (formed by enzymatic degradation), which appear to have minimal pharmacological activity based on laboratory animal data.
In addition, 14 minor metabolites have been isolated from urine. Following IV administration of radiolabeled epoprostenol in adults, 82 and 4% of the total radioactivity was recovered in urine and feces, respectively, over 7 days.
USES: This medication is used to treat high blood pressure in the lungs (pulmonary arterial hypertension). It helps to increase your ability to exercise and improve symptoms such as shortness of breath and tiredness. It works by relaxing and widening the blood vessels (arteries) in the lungs and other parts of the body so that blood can flow more easily.
This medication belongs to a class of drugs known as vasodilators.
Generic name: epoprostenol sodium (glycine)
Pronunciation: (E-poe-PROST-en-ol)
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
Today’s intelligence on Epoprostenol
Indications
The following indications are listed for Epoprostenol:
- Pulmonary Arterial Hypertension
Also known as: Hypertensive Pulmonary Arterial Disease, Pulmonary Hypertensive Arterial Disease.
Dosing
Dosage of epoprostenol sodium is expressed in terms of epoprostenol. There is considerable interindividual variability in patient response to epoprostenol and dosage must be individualized. Dosage should be carefully titrated until therapeutic effect is achieved or adverse effects become intolerable.
Epoprostenol sodium is administered by continuous IV infusion via a central venous catheter with a portable controlled-infusion device. A peripheral IV catheter may be used temporarily to administer the infusion until central venous access is established. Consult the manufacturer's labeling for ambulatory infusion-device specifications.
Delivery system malfunctions (e.g., infusion-device failure, occluded catheter) may result in inadvertent overdosage or underdosage. To avoid potential interruptions in drug delivery secondary to equipment malfunction, patients should have access to a back-up IV infusion device and infusion sets. A multi-lumen catheter should be considered for patients who routinely receive other IV drugs.
Epoprostenol also has been administered by oral inhalation (via nebulization+ through the ventilator circuit) in patients with acute respiratory distress syndrome (ARDS)+ receiving mechanical ventilation.
Store unopened vials of Flolan(R) powder for injection at room temperature (15-25degreesC), in the carton, and protect from light. Store unopened vials of the sterile diluent for Flolan(R) at room temperature (15-25degreesC). Do not freeze the diluent.
Store vials of Veletri(R) at controlled room temperature (20-25degreesC); store in the carton and do not expose to direct sunlight.
No dosing information is available for this tab.
No dosing information is available for this tab.
Drug interactions
During clinical trials, epoprostenol sodium was used concomitantly with anticoagulants, cardiac glycosides, diuretics, oral vasodilators, and supplemental oxygen.
There are no contraindication interactions for this drug.
There are no severe interactions for this drug.
There are no moderate interactions for this drug.
Contraindications
*Long-term use in patients with CHF due to severe left ventricular systolic dysfunction.
*Long-term use in patients who develop pulmonary edema during initial dosage titration (Veletri(R) only).
*Known hypersensitivity to epoprostenol or structurally related drugs.
There are no contraindication contraindications for this drug.
There are no severe contraindications for this drug.
There are no moderate contraindications for this drug.
Adverse reactions
The most common adverse reactions reported among patients treated with Flolan(R) include dizziness, jaw pain, headache, musculoskeletal pain, and nausea/vomiting.
The most common adverse reactions reported among patients initiating treatment with Veletri(R) include nausea/vomiting, headache, hypotension, flushing, chest pain, anxiety, dizziness, bradycardia, dyspnea, abdominal pain, musculoskeletal pain, and tachycardia. The most common adverse reactions reported among patients receiving chronic dosing of Veletri(R) include headache, jaw pain, flushing, diarrhea, nausea/vomiting, flu-like symptoms, and anxiety/nervousness.
There are no severe adverse reactions for this drug.
There are no less severe adverse reactions for this drug.
Precautions
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Safety and efficacy of epoprostenol have not been established in pediatric patients.
A drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes has not been demonstrated in limited data from case reports and case series describing epoprostenol use during pregnancy. Untreated pulmonary arterial hypertension (PAH) in pregnancy increases the risk for maternal heart failure, stroke, preterm delivery, and maternal and fetal death.
It is not known whether epoprostenol is distributed into milk. The developmental and health benefits of breast-feeding should be considered along with the mother's clinical need for epoprostenol and any potential adverse effects on the breast-fed child from the drug or from the underlying maternal condition.
Select an initial dosage in geriatric patients with caution (usually at the low end of the dosage range) and titrate carefully because of age-related decreases in hepatic, renal, and/or cardiac function and concomitant disease and drug therapy.
Clinical studies of epoprostenol sodium did not include sufficient numbers of patients 65 years of age or older to determine whether geriatric patients respond differently than younger patients. Other reported clinical experience has not identified differences in responses between geriatric and younger patients. In general, titrate dosage carefully in geriatric patients. Consider the greater frequency of decreased hepatic, renal, and/or cardiac function and of concomitant disease and drug therapy observed in the elderly.
ICD codes
No ICD codes are available for this drug.
Formulary status
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Last reviewed · Source: First Databank (FDB) drug data
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