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Prostaglandin E1
Systematic (IUPAC) name
7-[(1R,3R)-3-hydroxy-2-[(1 E,3S)-3-hydroxyoct-1-en-1-yl]-5-oxocyclopentyl]heptanoic acid
Identifiers
CAS number 745-65-3
ATC code C01EA01 G04BE01
PubChem 149351
DrugBank APRD00785
Chemical data
Formula C 20H34O5  
Mol. mass 354.481 g/mol
Pharmacokinetic data
Bioavailability  ?
Metabolism  ?
Half life  ?
Excretion  ?
Therapeutic considerations
Pregnancy cat.  ?
Legal status
Routes  ?
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Prostaglandin E1 (PGE1) is pharmaceutically known as Alprostadil.[1] It is used as a drug in the treatment of erectile dysfunction[2] and has vasodilatory properties.

Sexual dysfunction

Alprostadil is sold in the United States as urethral suppositories, under the brand name MUSE [3] (Medicated Urethral Suppository for Erection) by Vivus. It is also sold in injectable form as Caverject and Edex.

Muse delivers alprostadil as a penile suppository, inserted into the urethra, at least ten minutes before the erection will be needed. Caverject and Edex are similarly fast-acting, but are actually injected directly into the corpus cavernosum of the penis.

NexMed is developing transdermal formulations—Alprox-TD(R) for men with erectile dysfunction and Femprox(R) for female sexual arousal disorder. Alprox-TD(R) has been selling in China and in Hong Kong since October 2001 and April 2002, respectively. Two Phase III studies have been completed for this product, and the Company is seeking regulatory approval in the U.S., Canada and Europe. [4]

It is also available as a generic. The major cost is that it must be mixed by a compounding pharmacy and the alprostadil is sometimes difficult to get. There are different formulations (bi-mix, trimix) which may include papaverine and/or phentolamine. A sample mix might be papaverine 30 mg, phentolamine 2 mg, & alprostadil 20 mcg
As a generic, it is much less expensive than the pre-packaged injectables. For one thing, it is premixed (must be kept refrigerated) so one only loads the syringe with the quantity needed.

Other uses

Aprostadil is also used in maintaining a patent ductus arteriosus in the newborn. This is primarily useful when there is threat of premature closure of the ductus arteriosus in an infant with ductal-dependent congenital heart disease, including cyanotic lesions (e.g., pulmonary atresia/stenosis, tricuspid atresia/stenosis, transposition of the great arteries) and acyanotic lesions (e.g., coarctation of the aorta, hypoplastic left heart syndrome, critical aortic stenosis, interrupted aortic arch).

References

  1. ^ Cawello W, Leonhardt A, Schweer H, Seyberth HW, Bonn R, Lomeli AL (September 1995). "Dose proportional pharmacokinetics of alprostadil (prostaglandin E1) in healthy volunteers following intravenous infusion". British journal of clinical pharmacology 40 (3): 273–6. PMID 8527291.  
  2. ^ Harding LM, Adeniyi A, Everson R, Barker S, Ralph DJ, Baranowski AP (December 2002). "Comparison of a needle-free high-pressure injection system with needle-tipped injection of intracavernosal alprostadil for erectile dysfunction". International journal of impotence research 14 (6): 498–501. doi:10.1038/sj.ijir.3900916. PMID 12494285. http://dx.doi.org/10.1038/sj.ijir.3900916.  
  3. ^ MUSE
  4. ^ Fain Hughes (2007-10-29). "NEXM: Dutton Sees Strong Speculative Buy and 12-Month Price Double". http://www.tradingmarkets.com/.site/news/Stock%20News/722371/. Retrieved 2007-11-01.  







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