Country: Canada
Language: English
Source: Health Canada
EPOPROSTENOL (EPOPROSTENOL SODIUM)
SANDOZ CANADA INCORPORATED
B01AC09
EPOPROSTENOL
0.5MG
POWDER FOR SOLUTION
EPOPROSTENOL (EPOPROSTENOL SODIUM) 0.5MG
INTRAVENOUS
100
Prescription
VASODILATING AGENTS
Active ingredient group (AIG) number: 0133040001; AHFS:
CANCELLED PRE MARKET
2021-04-21
_Epoprostenol for Injection Page 1 of 35_ PRODUCT MONOGRAPH PR EPOPROSTENOL FOR INJECTION Epoprostenol Sodium 0.5 mg or 1.5 mg per vial VASODILATOR Sandoz Canada Inc. Date of Revision: December 6, 2018 110 rue de Lauzon Boucherville, QC, Canada J4B 1E6 Control Number: 221995 _Epoprostenol for Injection Page 2 of 35_ PR EPOPROSTENOL FOR INJECTION Epoprostenol Sodium 0.5 mg or 1.5 mg per vial ACTION AND CLINICAL PHARMACOLOGY Epoprostenol sodium, also known as prostacyclin, PGI 2 or PGX, a metabolite of arachidonic acid, is a naturally occurring prostaglandin. Epoprostenol has two major pharmacological actions: (1) direct vasodilation of pulmonary and systemic arterial vascular beds, and (2) inhibition of platelet aggregation. In animals, the vasodilatory effects of epoprostenol reduce right and left ventricular afterload and increase cardiac output and stroke volume. The effect of epoprostenol on heart rate in animals varies with dose. At low doses, there is vagally mediated bradycardia, but at higher doses, epoprostenol causes reflex tachycardia in response to direct vasodilation and hypotension. No major effects on cardiac conduction have been observed. Additional pharmacologic effects of epoprostenol in animals include bronchodilation, inhibition of gastric acid secretion, and decreased gastric emptying. PHARMACOKINETICS ABSORPTION/DISTRIBUTION: Epoprostenol is rapidly hydrolyzed at neutral blood pH and is also subject to enzymatic degradation. No available chemical assay is sufficiently sensitive and specific to assess the _in vivo_ human pharmacokinetics of epoprostenol. Animal studies using tritium-labelled epoprostenol have indicated a high clearance (93 mL/min/kg), small volume of distribution (357 mL/kg), and a short half-life (2.7 minutes). During infusions in animals, steady- state plasma concentrations of tritium-labelled epoprostenol were reached within 15 minutes and were proportional to infusion rates. METABOLISM: Tritium-labelled epoprostenol has been administered to humans in order to identify the Read the complete document