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In
late 1980's, many papers were published o n the potential
of Alprostadil (prostaglandin E1) in the
treatment of male erectile dysfunction. Since then the
compound has been recognized as an important
pharmacological agent for this indication.
The demand for Alprostadil is expected to increase significantly
resulting from this new use. There now exist and many
are still under development for various means of
application including intracavernous, topical
(transdermal
or intra-urethral), and needle-less injection.
According
to recent survey of urologists, intracavernosal
injection is the most effective route for treating
erectile dysfunction, while intraurethral application
and oral therapy are the safest1.
Pharmacology:
A wide variety of pharmacological
effects of Alprostadil are vasodilation, inhibition of
platelet aggregation, and stimulation of intestinal and
uterine smooth muscle. Alprostadil induces erection by
relaxation of trabecular smooth muscle and by dilation
of cavernosal arteries.
In
vitro, Alprostadil has been shown to cause
dose-dependent smooth muscle relaxation in isolated
corpus cavernosum and corpus spongiosum preparations.
In
human studies using Doppler duplex ultrasonography,
administration of Alprostadil resulted in an increase in
peak systolic flow velocities.
Applications:
1.
Cardiovascular
disorders:
Maintaining the patency of the
ductus arteriosus in neonates with congenital heart
disease until surgery is possible2.
2.
Peripheral
vascular disease:
Alprostadil can be
administered by intra-arterial or intravenous infusion3.
3.
Erectile
Dysfunction:
Intracavernous injection4,
intra-urethral application5 and non-invasive
delivery systems including topical and needle-less
applications6.
Proprietary Names:
Befarâ,
Caverjectâ,
Edexâ,
Lipleâ,
Minprogâ,
MUSEâ,
Palusâ,
Prostandinâ,
Prostavasinâ,
Prostinâ
VR, Prostineâ
VR, Prostivasâ,
Sutineâ,
Topiglan®.
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Everlight’s
Alprostadil can be supplied as:
¨
Bulk Active Pharmaceutical Ingredient
¨
Alprostadil
alpha-cyclodextrin (3% w/w)
¨
Alprostadil 500mcg/ml injection @ 5 x 1ml ampoules
Specs
are available upon request.
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※
Sales to countries without patent issues only ※
1)
Script No. 2431 April 23rd 1999 p24
2) Silove ED, et al. Arch Dis Child 1985; 60: 1025-30
3) Martin MFR and Tooke JE, ibid. 1982; 285: 1688
4)
Ishii N, et al. J Urol (Baltimore) 1988; 141: 323-5
5)
Padma-Nathan H, et al. J N Engl J Med 1997; 336: 1-7
6)
Watkinson AC, et al. Int J Pharm 1992; 83: 171-175
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