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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2017/08/04 15:23:08」(JST)

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Silodosin (trade names Rapaflo (USA), Silodyx (Europe and South Africa), Rapilif (India), Silodal (India), Urief (Japan), Thrupas (South Korea), Urorec (Russia)) 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).

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.

FDA approved silodosin on October 9, 2008.^[1] Silodosin is marketed under the trade names Rapaflo in the US and Silodyx in Europe.^[2]

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 be the cause of silodosin's typical side effect of loss of seminal emission.^[3]

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.^[4]

References

^ "Drugs.com, Watson Announces Silodosin NDA Accepted for Filing by FDA for the Treatment of Benign Prostatic Hyperplasia". Retrieved 2008-02-13.
^ European Medicines Agency: Assessment report for Silodyx
^ Kobayashi, K; Masumori, N; Kato, R; Hisasue, S; Furuya, R; Tsukamoto, T (2009). "Orgasm is preserved regardless of ejaculatory dysfunction with selective α1A-blocker administration". International Journal of Impotence Research. 21 (5): 306–310. PMC 2834370 . doi:10.1038/ijir.2009.27.
^ 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): 306–10. PMC 2834370 . PMID 19536124. doi:10.1038/ijir.2009.27.

External links

Official site

English Journal

[Multi-center trial on the early effects of silodosin on lower urinary tract symptoms associated with benign prostatic hyperplasia].

Ogawa T, Uemura H, Sano F, Hoshino K, Kita K, Hayashi N, Kagota M, Murakami T, Makiyama K, Miyoshii Y, Nakaigawa N, Yao M, Shimura H, Furuhata A, Fujikawa N, Shioi K, Ueki T, Hara Y, Saitou K, Kawakami S, Satomi Y, Hattori Y, Teranishi J, Kondo K, Kishida T, Saito K, Noguchi K, Fuji H, Yamaguchi T, Kinoshita Y, Nomura S, Yoshida M, Sakai N, Terao H, Matsumoto T, Umemoto S, Ogo Y, Kobayashi K, Noguchi S, Asakura T, Kohdaira T, Iguchi K, Izumi K, Hirano M, Kanno H, Takahashi T, Nukui F, Mokuo Y, Muraoka K, Osada Y, Funahashi M, Kitami K, Sugiura S, Ohta J, Miura T, Ishibashi Y, Masuda M, Komiya A, Suwa Y, Hashiba T, Mitaka K, Kobayashi M, Ohsaka K, Futoshi T, Tsuchiya T, Iwasaki A, Yamashita Y, Matsuzaki J, Kubota Y.SourceThe Department of Urology, Yokohama City Univercity Graduate School of Medicine.
Hinyokika kiyo. Acta urologica Japonica.Hinyokika Kiyo.2008 Dec;54(12):757-64.
Silodosin (URIEF), a new so-called 3rd generation alpha-1 blocker, is widely expected to be effective and useful for lower urinary tract symptoms (LUTS) associated with benign prostatic hyperplasia (BPH), due to its high specificity to alpha-1A receptor. We evaluated the efficacy of Silodosin, on 18
PMID 19174997

[Pharmacological and clinical profile of silodosin (URIEF Cap. 2 mg, 4 mg)].

Kobayashi M, Shimizu T.Sourcemamoru_kobayashi@pharm.kissei.co.jp
Nihon yakurigaku zasshi. Folia pharmacologica Japonica.Nihon Yakurigaku Zasshi.2006 Oct;128(4):259-68.
PMID 17038792

Japanese Journal

シロドシン口腔内崩壊錠(ユリーフOD錠)の臨床製剤学的評価

製剤機械技術学会誌 = Journal of pharmaceutical machinery and engineering 24(5), 483-491, 2015
NAID 40020682742

PP-128 シロドシンによる排尿障害の治療 : Urief Dose-Up and QOL Study(前立腺肥大症/薬物療法・診断1,一般演題ポスター,第97回日本泌尿器科学会総会)

日本泌尿器科学会雑誌 100(2), 348, 2009
NAID 110007229304

前立腺肥大症に伴う排尿障害に対するシロドシンの服用後早期効果に関する多施設共同臨床研究(SELECTIVITY)--Silodosin Early Effectiveness and Safety Multi Center Trial in Yokohama

泌尿器科紀要 54(12), 757-764, 2008-12
NAID 120001178146

Related Pictures

Urief (Silodosin) 4 mg – Ampuh Untuk Masalah Prostat & Batu Saluran Kemih | Tara URIEF TABLETS 4mg：50tablets｜Pharmacy Global Prostate Enlargement - Urief Sildosin Tablets Exporter from Mumbai Drug Express - Online Drug Shop - Urief Jual URIEF SILODOSIN 4MG di lapak Apotik Medica Station ranto_situmorang Jual URIEF 4 MG BOX di lapak sanjayakusuma sanjayakusuma816 臺北榮民總醫院藥物外觀辨識系統

★リンクテーブル★

リンク元

「シロドシン」

Silodosin
Clinical data
Pregnancy; category	US: B (No risk in non-human studies); Not approved for use in women;
Routes of; administration	Oral
ATC code	G04CA04 (WHO);
Legal status
Legal status	In general: ℞ (Prescription only);
Pharmacokinetic data
Bioavailability	32%
Protein binding	97%
Metabolism	Hepatic glucuronidation (UGT2B7-mediated); also minor CYP3A4 involvement
Biological half-life	13±8 hours
Excretion	Renal and fecal
Identifiers
	IUPAC name 1-(3-hydroxypropyl)-5-[(2R)-({2-[2-[2-(2,2,2-trifluoroethoxy)phenoxy]ethyl}amino)propyl]indoline-7-carboxamide;
Synonyms	KAD-3213, KMD-3213
CAS Number	160970-54-7 ;
PubChem CID	5312125;
IUPHAR/BPS	493;
ChemSpider	4471557 ;
UNII	CUZ39LUY82;
ChEMBL	CHEMBL24778 ;
Chemical and physical data
Formula	C25H32F3N3O4
Molar mass	495.534 g/mol
3D model (JSmol)	Interactive image;
	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

[1] "Drugs.com, Watson Announces Silodosin NDA Accepted for Filing by FDA for the Treatment of Benign Prostatic Hyperplasia". Retrieved 2008-02-13.

[2] European Medicines Agency: Assessment report for Silodyx

[3] Kobayashi, K; Masumori, N; Kato, R; Hisasue, S; Furuya, R; Tsukamoto, T (2009). "Orgasm is preserved regardless of ejaculatory dysfunction with selective α1A-blocker administration". International Journal of Impotence Research. 21 (5): 306–310. PMC 2834370 . doi:10.1038/ijir.2009.27.

[pmid19536124-4] 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): 306–10. PMC 2834370 . PMID 19536124. doi:10.1038/ijir.2009.27.

v t e Drugs used in benign prostatic hyperplasia (G04C)
5α-Reductase inhibitors	Dutasteride Epristeride Finasteride
Alpha blockers (α₁)	Alfuzosin Doxazosin Silodosin Tamsulosin Terazosin
Herbals	Pygeum africanum Saw palmetto extract
Other	Gestonorone caproate Mepartricin Osaterone acetate Oxendolone

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Urief