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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2012/12/14 15:16:35」(JST)

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Silodosin (trade names Rapaflo (USA), Silodyx (Europe), Rapilif (India), Silodal (India), Urief (Japan)) is a medication for the symptomatic treatment of benign prostatic hyperplasia. It acts as an α₁-adrenoceptor antagonist with high uroselectivity (selectivity for the prostate).^[1]

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 trade names Rapaflo in the US and Silodyx in Europe.^[3] and Rapilif in India (Ipca Urosciences)

Pharmacology

Since silodosin has high affinity for the α_1A 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.^[4]

As α_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.^[5]

References

^ Yoshida M, Homma Y, Kawabe K (December 2007). "Silodosin, a novel selective alpha 1A-adrenoceptor selective antagonist for the treatment of benign prostatic hyperplasia". Expert Opin Investig Drugs 16 (12): 1955–65. doi:10.1517/13543784.16.12.1955. PMID 18042003. http://www.expertopin.com/doi/abs/10.1517/13543784.16.12.1955.
^ "Drugs.com, Watson Announces Silodosin NDA Accepted for Filing by FDA for the Treatment of Benign Prostatic Hyperplasia". http://www.drugs.com/nda/silodosin_080212.html. Retrieved 2008-02-13.
^ European Medicines Agency: Assessment report for Silodyx
^ Schubert-Zsilavecz, M, Wurglics, M, Neue Arzneimittel 2008/2009
^ Kobayashi K, Masumori N, Kato R, Hisasue S, Furuya R, Tsukamoto T. (December 2009). "Orgasm is preserved regardless of ejaculatory dysfunction with selective alpha1A-blocker administration.". Int J Impot Res. 21 (5): 306. doi:10.1038/ijir.2009.27. PMC 2834370. PMID 19536124. //www.ncbi.nlm.nih.gov/pmc/articles/PMC2834370/.

External links

Watson Pharm., Inc.- Press Release
Rapaflo Official Site

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UpToDate Contents

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1. 前立腺肥大症の内科的治療 medical treatment of benign prostatic hyperplasia
2. 男性における下部尿路症状 lower urinary tract symptoms in men
3. 男性性機能不全の治療 treatment of male sexual dysfunction
4. 男性の尿失禁 urinary incontinence in men
5. 患者情報：前立腺肥大症（BPH）（詳細） benign prostatic hyperplasia bph beyond the basics

English Journal

Appropriateness of oral drugs for long-term treatment of lower urinary tract symptoms in older persons: results of a systematic literature review and international consensus validation process (LUTS-FORTA 2014).

Oelke M1, Becher K2, Castro-Diaz D3, Chartier-Kastler E4, Kirby M5, Wagg A6, Wehling M7.
Age and ageing.Age Ageing.2015 Jun 23. pii: afv077. [Epub ahead of print]
AIM: we aimed to systematically review drugs to treat lower urinary tract symptoms (LUTS) regularly used in older persons to classify appropriate and inappropriate drugs based on efficacy, safety and tolerability by using the Fit fOR The Aged (FORTA) classification.METHODS: to evaluate the efficacy,
PMID 26104505

Intraoperative floppy iris syndrome associated with silodosin.

Ipekci T1, Akin Y2, Hoscan B1, Tunckiran A1.
Acta ophthalmologica.Acta Ophthalmol.2015 Jun;93(4):e306. doi: 10.1111/aos.12549. Epub 2014 Aug 31.
PMID 25175780

Selecting the right α-blocker: is silodosin your best option?

Lavigueur-Blouin H1, Bhojani N.
BJU international.BJU Int.2015 May;115(5):677-8. doi: 10.1111/bju.12961.
PMID 25885559

Japanese Journal

症例報告 Silodosinにより重篤な薬物性肝障害を惹起した1例

野村憲弘,伊藤敬義,金田祥明 [他]
肝臓 55(11), 670-676, 2014-11
NAID 40020275047

Silodosinにより重篤な薬物性肝障害を惹起した1例

野村憲弘,伊藤敬義,金田祥明,司馬信一,保母貴宏,林隆広,佐藤雅,佐久間大,江口潤一,三田村圭太郎,出口義雄,松川正明,斎藤光次,井上晴洋
肝臓 55(11), 670-676, 2014
… 63歳男性．前立腺肥大症に対して選択的α1a遮断薬（Silodosin 8 mg）及び漢方薬（ツムラ八味地黄丸®7.5 g）を前医から処方され服用していた．服用開始14日後より褐色尿を自覚し，同27日後の血液検査にてT.Bil 10.6 mg/dl，AST 2,707 IU/L，ALT 3,035 IU/Lと肝障害を認め，当院へ紹介され入院となった．肝炎ウィルス，自己免疫疾患関連マーカーは陰性，過度の飲酒歴はなく，薬物性肝障害を疑った．入院後I度肝性脳症出現し，プロト …
NAID 130004705846

Silodosin versus naftopidil in Japanese patients with lower urinary tract symptoms associated with benign prostatic hyperplasia : A randomized multicenter study

SHIRAKAWA Toshiro,HARAGUCHI Takahiro,SHIGEMURA Katsumi,MORISHITA Shinichi,MINAYOSHI Kohji,MIYAZAKI Jiro,YAMADA Yuji,MIYAKE Hideaki,TANAKA Kazushi,FUJISAWA Masato
International journal of urology 20(9), 903-910, 2013-09-01
NAID 10031195892

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リンク元

「シロドシン」

Silodosin
Systematic (IUPAC) name
	1-(3-hydroxypropyl)-5-[(2R)-({2-[2-[2-(2,2,2-trifluoroethoxy)phenoxy]ethyl}amino)propyl]indoline-7-carboxamide
Clinical data
Pregnancy cat.	B (US) Not for use in women
Legal status	℞ Prescription only
Routes	Oral
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
Identifiers
CAS number	160970-54-7
ATC code	G04CA04
PubChem	CID 5312125
IUPHAR ligand	493
ChemSpider	4471557
UNII	CUZ39LUY82
ChEMBL	CHEMBL24778
Synonyms	KAD-3213, KMD-3213
Chemical data
Formula	C25H32F3N3O4
Mol. mass	495.534 g/mol
	SMILES FC(F)(F)COc3ccccc3OCCN[C@H](C)Cc1cc2c(c(c1)C(=O)N)N(CC2)CCCO;
	InChI InChI=1S/C25H32F3N3O4/c1-17(30-8-12-34-21-5-2-3-6-22(21)35-16-25(26,27)28)13-18-14-19-7-10-31(9-4-11-32)23(19)20(15-18)24(29)33/h2-3,5-6,14-15,17,30,32H,4,7-13,16H2,1H3,(H2,29,33)/t17-/m1/s1 ; Key:PNCPYILNMDWPEY-QGZVFWFLSA-N ;
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　　[★]

英: silodosin
商: ユリーフ Urief

[pmid18042003-1] Yoshida M, Homma Y, Kawabe K (December 2007). "Silodosin, a novel selective alpha 1A-adrenoceptor selective antagonist for the treatment of benign prostatic hyperplasia". Expert Opin Investig Drugs 16 (12): 1955–65. doi:10.1517/13543784.16.12.1955. PMID 18042003. http://www.expertopin.com/doi/abs/10.1517/13543784.16.12.1955.

[2] "Drugs.com, Watson Announces Silodosin NDA Accepted for Filing by FDA for the Treatment of Benign Prostatic Hyperplasia". http://www.drugs.com/nda/silodosin_080212.html. Retrieved 2008-02-13.

[3] European Medicines Agency: Assessment report for Silodyx

[4] Schubert-Zsilavecz, M, Wurglics, M, Neue Arzneimittel 2008/2009

[pmid19536124-5] Kobayashi K, Masumori N, Kato R, Hisasue S, Furuya R, Tsukamoto T. (December 2009). "Orgasm is preserved regardless of ejaculatory dysfunction with selective alpha1A-blocker administration.". Int J Impot Res. 21 (5): 306. doi:10.1038/ijir.2009.27. PMC 2834370. PMID 19536124. //www.ncbi.nlm.nih.gov/pmc/articles/PMC2834370/.

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silodosin