In late 1980's, many papers were published on 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®.

 

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.

      Sales to countries without patent issues only

References

 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

 

 

前列腺素原料药

 

Alprostadil(PG E1)

先天性心脏动脉阻塞之治疗 

Misoprostol

消炎镇痛剂所造成的胃及十二指肠溃疡之治疗及预防 

Cloprostenol Sodium 

动物妊娠末期的催生

Dinoprostone (PG E2)

人工引产

Latanoprost

Epoprostenol Sodium (PGI2)

治疗青光眼

治疗肺动脉高压

心血管原料药

 

Felodipine

抗高血压

中间体

     NEPA/NEPA-NCA

心血管药ACE抑制剂中间体

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