EPOPROSTENOL SODIUM- epoprostenol sodium injection, powder, for solution
STERILE DILUENT- water injection
Teva Parenteral Medicines, Inc.
DESCRIPTION
Epoprostenol sodium for injection is a sterile sodium salt formulated for intravenous (IV) administration. Each vial of epoprostenol sodium for injection contains epoprostenol sodium equivalent to either 0.5 mg (500,000 ng) or 1.5 mg (1,500,000 ng) epoprostenol, 3.76 mg glycine, 2.93 mg sodium chloride, and 50 mg mannitol. Sodium hydroxide may have been added to adjust pH.
Epoprostenol (PGI2 , PGX, prostacyclin), a metabolite of arachidonic acid, is a naturally occurring prostaglandin with potent vasodilatory activity and inhibitory activity of platelet aggregation.
Epoprostenol is (5Z,9?,11?,13E ,15S)-6,9-epoxy-11,15-dihydroxyprosta-5,13-dien-1-oic acid.
Epoprostenol sodium has a molecular weight of 374.45 and a molecular formula of C20 H31 NaO5 . The structural formula is:
Chemcial structure for epoprostenol sodium
(click image for full-size original)
Epoprostenol sodium for injection is a white to off-white powder that must be reconstituted with STERILE DILUENT for epoprostenol sodium for injection. STERILE DILUENT for epoprostenol sodium for injection is supplied in glass vials containing 50 mL of 94 mg glycine, 73.3 mg sodium chloride, sodium hydroxide (added to adjust pH), and Water for Injection, USP.
The reconstituted solution of epoprostenol sodium for injection has a pH of 11.0 to 11.8 and is increasingly unstable at a lower pH.
CLINICAL PHARMACOLOGY
General
Epoprostenol has 2 major pharmacological actions: (1) direct vasodilation of pulmonary and systemic arterial vascular beds, and (2) inhibition of platelet aggregation. In animals, the vasodilatory effects 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.
