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Silodosin
Systematic (IUPAC) name
1-(3-hydroxypropyl)-5-[(2R)-({2-[2-[2-(2,2,2-trifluoroethoxy)phenoxy]ethyl}amino)propyl]indoline-7-carboxamide
Identifiers
CAS number 160970-54-7
ATC code G04CA04
PubChem 5312125
Chemical data
Formula C25H33F3N3O4 
Mol. mass 495.534 g/mol
SMILES eMolecules & PubChem
Pharmacokinetic data
Bioavailability 32%
Protein binding 97%
Metabolism Hepatic glucuronidation (UGT2B7-mediated); also minor CYP3A4 involvement
Half life 13±8 hours
Excretion Renal and fecal
Therapeutic considerations
Pregnancy cat. B(US) Not for use in women
Legal status Prescription only
Routes Oral

Silodosin is an α1-adrenoceptor antagonist with high uroselectivity. [1]

Contents

History

Silodosin received its first marketing approval in Japan in May 2006 under the tradename Urief, which is jointly marketed by Kissei Pharmaceutical Co., Ltd. and Daiichi Sankyo Pharmaceutical Co., Ltd.

Kissei licensed the US, Canadian, and Mexican rights for silodosin to Watson Pharmaceuticals, Inc. in 2004.

On February 12, 2008, Watson announced that the New Drug Application submitted to the United States Food and Drug Administration for silodosin has been accepted for filing. FDA approved this drug on October 9th, 2008.[2] Silodosin is marketed under the tradename Rapaflo.

Pharmacology

Since Silodosin is a highly selective inhibitor of the α1A adrenergic receptor, it causes practically no orthostatic hypotension (in contrast to other α1 blockers). On the other side, the high selectivity seems to cause more problems with ejaculation.[3]

As alpha 1A-adrenoceptor antagonists are being investigated as a means to male birth control due to their ability to inhibit ejaculation but not orgasm, a trial with 15 male volunteers was conducted. While silodosin was completely efficacious in preventing the release of semen in all subjects, 12 out of the 15 patients reported mild discomfort upon orgasm. The men also reported the psychosexual side effect of being strongly dissatisfied by their lack of ejaculation.[4] Despite the incidence of side effects, the drug still appears to be a promising candidate for a male oral contraceptive drug.

References

External links








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