Epoprostenol

Table of contents

  • Brand Names
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Genes that may be involved
  • Drug Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

Europe

Austria: Flolan; Belgium: Flolan; Czech Republic: Flolan; Denmark: Flolan; Estonia: Flolan; France: Flolan; Greece: Flolan; Ireland: Flolan; Italy: Flolan; Luxembourg: Flolan; Malta: Flolan; Netherlands: Flolan; Poland: Flolan; Spain: Flolan; UK: Flolan.

North America

Canada: Flolan; USA: Epoprostenol, Flolan.

Asia

Japan: Flolan.

Drug combinations

Chemistry

Epoprostenol: C~20~H~32~O~5~. Mw: 352.47. (1) Prosta-5,13-dien-1-oic acid, 6,9-epoxy-11,15-dihydroxy-, (5Z,9α,11α,13E,15S)-; (2)(Z)-(3aR,4R,5R,6aS)-Hexahydro-5-hydroxy-4-[(E)-(3S)-3-hydroxy-1-octenyl]-2H-cyclopenta[b]furan-Δ^2,Δ^-valeric acid. CAS-35121-78-9 (1979).

Epoprostenol Sodium: C~20~H~31~NaO~5~. Mw: 374.45. Prosta-5,13-dien-1-oic acid, 6,9-epoxy-11,15-dihydroxy-, sodium salt, (5Z,9α,11α,13E,15S)-. CAS-61849-14-7 (1980).

Pharmacologic Category

Vasodilating Agents, Miscellaneous; Prostacyclin; Prostaglandin. (ATC-Code: B01AC09).

Mechanism of action

Epoprostenol, a naturally occurring prostaglandin, is a short-acting vasodilating agent and a platelet-aggregation inhibitor. This effect results from its activation of intracellular adenylate cyclase and the resultant increase in cAMP concentrations within the platelets.

Therapeutic use

Treatment of idiopathic pulmonary arterial hypertension and pulmonary hypertension associated with the scleroderma spectrum of disease.

Pregnancy and lactiation implications

Safety and efficacy during labor, vaginal delivery, or cesarean section not established. Unknown whether epoprostenol is distributed into milk. Use with caution in nursing women.

Unlabeled use

Contraindications

Hypersensitivity to epoprostenol or to structurally-related compounds. Chronic use in CHF due to severe left ventricular systolic dysfunction. Patients who develop pulmonary edema during dose initiation.

Warnings and precautions

Avoid abrupt discontinuance or sudden large reductions in infusion rates (may result in symptoms associated with rebound pulmonary hypertension, including dyspnea, dizziness, and asthenia). Risk of pulmonary thromboembolism or systemic embolism associated with the permanent indwelling central venous catheter. Some patients with primary pulmonary hypertension developed pulmonary edema during dosing adjustment (may be associated with pulmonary veno-occlusive disease). Use with caution in risk factors for bleeding. During chronic use, unless contraindicated, anticoagulants should be co-administered to reduce risk of thromboembolism. Chronic continuous I.V. infusion of epoprostenol via a chronic indwelling central venous catheter associated with local infections and serious blood stream infections.

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