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PubChem
Name: Alprostadil
PubChem Compound ID: 10499025
Description: A potent vasodilator agent that increases peripheral blood flow.
Molecular formula: C20H34O5
Molecular weight: 364.522 g/mol
DrugBank
Identification
Name: Alprostadil
Name (isomeric): DB00770
Drug Type: small molecule
Description: A potent vasodilator agent that increases peripheral blood flow.
Brand: Alprox-TD, Edex, Befar, Prink, Alprostadil Prostoglandin E1, Prostaglandin E1, l-Prostaglandin E1, Topiglan, Prostin VR, Prostin VR Pediatric, Alista, Femprox, Muse, Caverject, PGE1
Brand name mixture: Caverject Sterile Powder - Kit 11.9mcg /Vial(Alprostadil + Water), Caverject Sterile Powder - Kit 23.2mcg/Vial(Alprostadil + Water)
Category: Vasodilator Agents, Fibrinolytic Agents, Platelet Aggregation Inhibitors
CAS number: 745-65-3
Pharmacology
Indication: For palliative, not definitive, therapy to temporarily maintain the patency of the ductus arteriosus until corrective or palliative surgery can be performed in neonates who have congenital heart defects and who depend upon the patent ductus for survival. Also for the treatment of erectile dysfunction due to neurogenic, vasculogenic, psychogenic, or mixed etiology.
Pharmacology:
Alprostadil (prostaglandin E1) is produced endogenously to relax vascular smooth muscle and cause vasodilation. In adult males, the vasodilatory effects of alprostadil on the cavernosal arteries and the trabecular smooth muscle of the corpora cavernosa result in rapid arteriolar inflow and expansion of the lacunar spaces within the corpora. As...
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Mechanism of Action:
Alprostadil causes vasodilation by means of a direct effect on vascular and ductus arteriosus (DA) smooth muscle, preventing or reversing the functional closure of the DA that occurs shortly after birth. This is because, as a form of prostaglandinE1 (PGE1) it has multiple effects on blood flow. This results in increased pulmonary or systemic blood ...
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Absorption: The absolute bioavailability of alprostadil has not been determined.
Protein binding: Bound in plasma primarily to albumin (81% bound) and to a lesser extent alpha-globulin IV-4 fraction (55% bound).
Biotransformation: Alprostadil must be infused continuously because it is very rapidly metabolized. As much as 80% of the circulating alprostadil may be metabolized in one pass through the lungs, primarily by beta- and omega-oxidation.
Route of elimination: Alprostadil must be infused continuously because it is very rapidly metabolized. As much as 80% of the circulating alprostadil may be metabolized in one pass through the lungs, primarily by β- and ω-oxidation. The metabolites are excreted primarily by the kidney, and excretion is essentially complete within 24 hours after administration.
Half Life: 5 to 10 minutes (after a single dose), in healthy adults and neonates.
Toxicity: Oral, mouse: LD50 = 186 mg/kg; Oral, rat: LD50 = 228 mg/kg. Apnea, bradycardia, pyrexia, hypotension, and flushing may be signs of drug overdosage.
Affected organisms: Humans and other mammals

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