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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2015/10/30 14:49:51」(JST)

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Tamsulosin (rINN) (/tæmˈsuːlɵsɨn/ or /tæmsʉˈloʊsɨn/) is an α_1aadrenergic receptor antagonist used in the symptomatic treatment of benign prostatic hyperplasia (BPH). Tamsulosin was developed by Yamanouchi Pharmaceuticals (now part of Astellas Pharma) and was first marketed in 1996 under the trade name Flomax, and also under the name Omnic.

Tamsulosin is used in the treatment of difficult urination, a common symptom of enlarged prostate. Tamsulosin, and other medications in the class called alpha blockers, work by relaxing bladder neck muscles and muscle fibers in the prostate itself and make it easier to urinate.^[1]

The U.S. patent for Flomax expired in October 2009.^[2] The U.S. Food and Drug Administration (FDA) approved generic Flomax in March 2010.^[3]

Mechanism

Tamsulosin is a selective α₁ receptor antagonist that has preferential selectivity for the α_1A receptor in the prostate versus the α_1B receptor in the blood vessels.^[4]

When alpha 1 receptors in the bladder neck and the prostate are blocked, this causes a relaxation in smooth muscle and therefore less resistance to urinary flow. Due to this, the pain associated with BPH can be reduced.

Selective action of tamsulosin in alpha 1A/D receptors is controversial and over three quarters of tamsulosin registered human studies are unpublished.^[5]

Clinical uses

Flomax 0.4 MG Oral Capsule

Tamsulosin is primarily used for benign prostatic hyperplasia, but can also assist the passage of kidney stones by the same mechanism of smooth muscle relaxation via alpha antagonism.^[6]^[7] Tamsulosin is also used as adjunct treatment of acute urinary retention. Multiple studies have shown patients will void more successfully after catheter removal if they are taking tamsulosin vs. placebo. Patients taking tamsulosin are also less likely to need re-catheterization.^[8]^[9]^[10] An additional use for tamsulosin is its use in medical expulsive therapy for some cases of nephrolithiasis.

Adverse effects

Immunologic: Higher risk of allergic reaction in those with sulfa allergies.^[11]
Ophthalmologic: Patients taking tamsulosin are prone to a complication known as floppy iris syndrome during cataract surgery. Adverse outcomes of the surgery are greatly reduced by the surgeon's prior knowledge of the patient's history with this drug, and thus having the option of alternative techniques.^[12]
Severe hypotension.^[13]^[14]

Tamsulosin has also affected sexual function in men. It can cause males to experience retrograde ejaculation.^[15] In males, retrograde ejaculation occurs when the fluid to be ejaculated, which would normally exit the body via the urethra, is redirected to the urinary bladder. Normally, the bladder sphincter contracts and the ejaculate goes to the urethra, the area of least pressure. In retrograde ejaculation, this sphincter does not function properly. This side effect can be mitigated by exercising the sphincter muscle; this is done by practicing a pumping action during ejaculation and urination - some semen fluid can then be ejaculated.

Clinical comparison

Although prostate specific, it does not have the prostate apoptotic effects of other prostate drugs such as the 5 alpha-reductase inhibitors such as dutasteride and finasteride.^{[citation needed]}

Use in combination therapy

The results of the CombAT (Combination of Avodart and Tamsulosin under the brand name Duodart) trial in 2008 demonstrated that treatment with the combination of dutasteride (Avodart) and tamsulosin provides greater symptom benefits compared to monotherapy with either agent alone for treatment of benign prostatic hyperplasia. ^[16] The CombAT trial became the medication Jalyn. It was approved by the FDA on June 14, 2010.^[17] This combination can be useful as it can take up to six months for any symptomatic relief to be found by 5-alpha-reductase inhibitors such as dutasteride compared to alpha-1 receptor blockers which can provide relief in some cases within 48 hours.^[18]

Brand names

Tamsulosin was first marketed in 1996 under the trade name Flomax. It is now marketed by various companies under licence, including Boehringer-Ingelheim and CSL. Tamsulosin hydrochloride extended-release capsules are marketed under the trade names Urisurge(India), Flomax, Flomaxtra, Contiflo XL,bestflo, Urimax and Pradif,^[19] although generic, non-modified-release capsules are still approved and marketed in many countries (such as Canada). In Mexico, it is marketed as Secotex and as Harnal D in Japan and Indonesia.^[20] In Egypt,^[21] Italy and Iceland, it is marketed under the trade name Omnic by Astellas Pharma Europe. The largest manufacturer of tamsulosin, drug substance, is Synthon.

References

^ http://www.mayoclinic.com/health/prostate-gland-enlargement/DS00027/DSECTION=treatments-and-drugs
^ "Flomax – Big Patent Expirations of 2010". February 10, 2010. Retrieved 14 January 2012.
^ "FDA Approves First Generic Tamsulosin to Treat Enlarged Prostate Gland" (Press release). U.S. Food and Drug Administration (FDA). March 2, 2010.
^ Shen, Howard (2008). Illustrated Pharmacology Memory Cards: PharMnemonics. Minireview. p. 13. ISBN 1-59541-101-1.
^ http://www.bmj.com/content/347/bmj.f6320/rr/698284. Missing or empty |title= (help)
^ http://www.renalandurologynews.com/tamsulosin-aids-stone-expulsion/article/193855/
^ http://www.prnewswire.com/news-releases/study-shows-use-of-tamsulosin-or-nifedipine-helps-patients-to-clear-ureteral-stone-fragments-faster-and-reduces-rate-of-recurrence-54518887.html
^ Lucas MG, Stephenson TP, Nargund V (February 2005). "Tamsulosin in the management of patients in acute urinary retention from benign prostatic hyperplasia". BJU Int. 95 (3): 354–7. doi:10.1111/j.1464-410X.2005.05299.x. PMID 15679793.
^ Jeong IG, You D, Yoon JH, et al. (February 2014). "Impact of tamsulosin on urinary retention following early catheter removal after robot-assisted laparoscopic radical prostatectomy: A prospective randomized controlled trial". Int. J. Urol. 21 (2): 164–8. doi:10.1111/iju.12225. PMID 23906190.
^ PharmacistAnswers Tamsulosin & Catheterization Retrieved February 12, 2014.
^ "Tamsulosin (Oral Route) - Before Using". Mayo Clinic. Retrieved 5 June 2015.
^ Medscape, Good Cataract Surgery Outcomes Possible in Intraoperative Floppy Iris Syndrome Due to Tamsulosin.
^ Bird, ST; Delaney, JA; Brophy, JM; Etminan, M; Skeldon, SC; Hartzema, AG (Nov 5, 2013). "Tamsulosin treatment for benign prostatic hyperplasia and risk of severe hypotension in men aged 40-85 years in the United States: risk window analyses using between and within patient methodology.". BMJ (Clinical research ed.) 347: f6320. doi:10.1136/bmj.f6320. PMID 24192967.
^ Ramirez, J (Nov 5, 2013). "Severe hypotension associated with α blocker tamsulosin.". BMJ (Clinical research ed.) 347: f6492. doi:10.1136/bmj.f6492. PMID 24192968.
^ "Tamsulosin Side Effects". Drugs.com. Retrieved 2011-04-27
^ Roehrborn CG, Siami P, Barkin J, et al. (February 2008). "The effects of dutasteride, tamsulosin and combination therapy on lower urinary tract symptoms in men with benign prostatic hyperplasia and prostatic enlargement: 2-year results from the CombAT study". J. Urol. 179 (2): 616–21; discussion 621. doi:10.1016/j.juro.2007.09.084. PMID 18082216.
^ http://www.accessdata.fda.gov/drugsatfda_docs/nda/2010/022460Orig1s000Approv.pdf
^ Australian Medicines Handbook
^ Dr. Sandro Magnanelli; Dr.ssa Ada Maria Vetere. "Pradif 0,4 Mg Capsule Rigide A Rilascio Prolungato". Torrinomedica.it. Retrieved 15 November 2012.
^ "Drugs.com Database".
^ "Novartis hits Astellas with transplant drug generic". Reuters. 11 August 2009. Retrieved 11 August 2009.

External links

Tamsulosin – information from USP DI Advice for the Patient
Flomax (drugs.com) – U.S. product information
Product label U.S. Food and Drug Administration (FDA)
Flomax (Official Site)^{[dead link]} – Official Site

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. 男性の尿失禁 urinary incontinence in men
3. 男性における下部尿路症状 lower urinary tract symptoms in men
4. 尿管結石のマネージメント management of ureteral calculi
5. 男性の性交時痛 male dyspareunia

English Journal

Effect of medical expulsive therapy on the health-related quality of life of patients with ureteral stones: a critical evaluation.

Eryildirim B1, Sahin C, Tuncer M, Sabuncu K, Cetinel C, Tarhan F, Sarica K.
International urology and nephrology.Int Urol Nephrol.2015 Jun 30. [Epub ahead of print]
PURPOSE: To evaluate the possible effects of medical expulsive therapy (MET) on the health-related quality of life (HRQOL) of the patients under watchful waiting for ureteral stones.PATIENTS AND METHODS: A total 120 patients with ureteral stones were included into this study program. Patients were d
PMID 26122118

The beneficial effect of alpha-blockers for ureteral stent-related discomfort: systematic review and network meta-analysis for alfuzosin versus tamsulosin versus placebo.

Kwon JK1, Cho KS2, Oh CK3, Kang DH4, Lee H5, Ham WS6, Choi YD7, Lee JY8.
BMC urology.BMC Urol.2015 Jun 24;15:55. doi: 10.1186/s12894-015-0050-5.
BACKGROUND: This study was carried out a network meta-analysis of evidence from randomized controlled trials (RCTs) to evaluate stent-related discomfort in patients with alfuzosin or tamsulosin versus placebo.METHODS: Relevant RCTs were identified from electronic databases. The proceedings of approp
PMID 26104313

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

Japanese Journal

自律神経疾患の治療の進歩

神経治療学 33(4), 542-545, 2017
NAID 130005398471

高血圧と前立腺肥大症を有する男性患者の下部尿路症状に対するサブタイプ非選択的ならびに選択的 α1遮断薬の後ろ向き比較検討

臨床薬理 48(1), 1-7, 2017
NAID 130005331768

過活動膀胱を有する前立腺肥大症患者に対する薬物治療の臨床的検討: クロスオーバー法を用いた比較検討

泌尿器科紀要 = Acta urologica Japonica 62(7), 341-347, 2016-07
NAID 120005829357

Related Pictures

★リンクテーブル★

リンク元	「タムスロシン」「α受容体遮断薬」
拡張検索	「tamsulosin hydrochloride」

「タムスロシン」

Tamsulosin
Systematic (IUPAC) name
	(R)-5-(2-{[2-(2-ethoxyphenoxy)ethyl]amino}propyl)-2-methoxybenzene-1-sulfonamide
Clinical data
Trade names	Flomax
AHFS/Drugs.com	monograph
MedlinePlus	a698012
Licence data	US FDA:link
Pregnancy; category	AU: B2; US: B (No risk in non-human studies);
Legal status	AU: Prescription Only (S4); UK: Prescription-only (POM); US: ℞-only;
Routes of; administration	oral
Pharmacokinetic data
Bioavailability	100% (oral)
Metabolism	hepatic
Biological half-life	9–13 hours
Excretion	76% renal
Identifiers
CAS Registry Number	106133-20-4
ATC code	G04CA02
PubChem	CID: 129211
IUPHAR/BPS	488
DrugBank	DB00706
ChemSpider	114457
UNII	G3P28OML5I
KEGG	D08560
ChEBI	CHEBI:9398
ChEMBL	CHEMBL836
Chemical data
Formula	C20H28N2O5S
Molecular mass	408.51
	SMILES CCOc1ccccc1OCCN[C@@H](C)Cc1ccc(OC)c(c1)S(=O)(=O)N ;
	InChI InChI=1S/C20H28N2O5S/c1-4-26-17-7-5-6-8-18(17)27-12-11-22-15(2)13-16-9-10-19(25-3)20(14-16)28(21,23)24/h5-10,14-15,22H,4,11-13H2,1-3H3,(H2,21,23,24)/t15-/m1/s1 ; Key:DRHKJLXJIQTDTD-OAHLLOKOSA-N ;
(what is this?) (verify)

　　[★]

英: tamsulosin
化: 塩酸タムスロシン tamsulosin hydrochloride、タムスロシン塩酸塩
商: ウロスロール、タムスロン、ハラナシン、ハルスロー、ハルタム、ハルナール、パルナック、ハルリーブ、ハロネロール、リストリーム
関: αアドレナリン受容体遮断薬、アドレナリン受容体; その他の泌尿生殖器官及び肛門用薬

分類

αアドレナリン受容体遮断薬

選択的α1受容体拮抗薬

作用機序

前立腺に存在するα_1A受容体を介して作用

薬理作用

下部尿路平滑筋弛緩作用が強い。
血圧は下げない

適応

前立腺肥大に伴う排尿障害

添付文書

ハルナールD錠0.1mg／ハルナールD錠0.2mg

http://www.info.pmda.go.jp/go/pack/2590008F1026_1_08/2590008F1026_1_08?view=body

「α受容体遮断薬」

　　[★]

英: α adrenergic receptor blocker α-adrenergic blocking agent, α-adrenoceptor blocking agent
同: αアドレナリン受容体遮断薬、α遮断薬 α-blocker, α-blockade

非選択的α受容体拮抗薬

選択的α₁受容体拮抗薬

選択的α₂受容体拮抗薬

ヨヒンビン yohimbine

「tamsulosin hydrochloride」

　　[★] 塩酸タムスロシン、タムスロシン塩酸塩、タムスロシン

[1] ttp://www.mayoclinic.com/health/prostate-gland-enlargement/DS00027/DSECTION=treatments-and-drugs

[2] "Flomax – Big Patent Expirations of 2010". February 10, 2010. Retrieved 14 January 2012.

[3] "FDA Approves First Generic Tamsulosin to Treat Enlarged Prostate Gland" (Press release). U.S. Food and Drug Administration (FDA). March 2, 2010.

[pharmnemonics-4] Shen, Howard (2008). Illustrated Pharmacology Memory Cards: PharMnemonics. Minireview. p. 13. ISBN 1-59541-101-1.

[5] ttp://www.bmj.com/content/347/bmj.f6320/rr/698284. Missing or empty |title= (help)

[6] ttp://www.renalandurologynews.com/tamsulosin-aids-stone-expulsion/article/193855/

[7] ttp://www.prnewswire.com/news-releases/study-shows-use-of-tamsulosin-or-nifedipine-helps-patients-to-clear-ureteral-stone-fragments-faster-and-reduces-rate-of-recurrence-54518887.html

[8] Lucas MG, Stephenson TP, Nargund V (February 2005). "Tamsulosin in the management of patients in acute urinary retention from benign prostatic hyperplasia". BJU Int. 95 (3): 354–7. doi:10.1111/j.1464-410X.2005.05299.x. PMID 15679793.

[9] Jeong IG, You D, Yoon JH, et al. (February 2014). "Impact of tamsulosin on urinary retention following early catheter removal after robot-assisted laparoscopic radical prostatectomy: A prospective randomized controlled trial". Int. J. Urol. 21 (2): 164–8. doi:10.1111/iju.12225. PMID 23906190.

[10] PharmacistAnswers Tamsulosin & Catheterization Retrieved February 12, 2014.

[11] "Tamsulosin (Oral Route) - Before Using". Mayo Clinic. Retrieved 5 June 2015.

[12] Medscape, Good Cataract Surgery Outcomes Possible in Intraoperative Floppy Iris Syndrome Due to Tamsulosin.

[13] Bird, ST; Delaney, JA; Brophy, JM; Etminan, M; Skeldon, SC; Hartzema, AG (Nov 5, 2013). "Tamsulosin treatment for benign prostatic hyperplasia and risk of severe hypotension in men aged 40-85 years in the United States: risk window analyses using between and within patient methodology.". BMJ (Clinical research ed.) 347: f6320. doi:10.1136/bmj.f6320. PMID 24192967.

[14] Ramirez, J (Nov 5, 2013). "Severe hypotension associated with α blocker tamsulosin.". BMJ (Clinical research ed.) 347: f6492. doi:10.1136/bmj.f6492. PMID 24192968.

[15] "Tamsulosin Side Effects". Drugs.com. Retrieved 2011-04-27

[Roehrborn2008-16] Roehrborn CG, Siami P, Barkin J, et al. (February 2008). "The effects of dutasteride, tamsulosin and combination therapy on lower urinary tract symptoms in men with benign prostatic hyperplasia and prostatic enlargement: 2-year results from the CombAT study". J. Urol. 179 (2): 616–21; discussion 621. doi:10.1016/j.juro.2007.09.084. PMID 18082216.

[17] ttp://www.accessdata.fda.gov/drugsatfda_docs/nda/2010/022460Orig1s000Approv.pdf

[18] Australian Medicines Handbook

[19] Dr. Sandro Magnanelli; Dr.ssa Ada Maria Vetere. "Pradif 0,4 Mg Capsule Rigide A Rilascio Prolungato". Torrinomedica.it. Retrieved 15 November 2012.

[20] "Drugs.com Database".

[21] "Novartis hits Astellas with transplant drug generic". Reuters. 11 August 2009. Retrieved 11 August 2009.

匿名

検索

案内

案内

tamsulosin

Wikipedia preview

wiki en

Contents

Mechanism

Clinical uses

Adverse effects

Clinical comparison

Use in combination therapy

Brand names

References

External links

UpToDate Contents

English Journal

Japanese Journal

Related Pictures

★リンクテーブル★

「タムスロシン」

分類

作用機序

薬理作用

適応

添付文書

「α受容体遮断薬」

非選択的α受容体拮抗薬

選択的α₁受容体拮抗薬

選択的α₂受容体拮抗薬

「tamsulosin hydrochloride」

匿名

検索

案内

tamsulosin

Wikipedia preview

wiki en

Contents

Mechanism

Clinical uses

Adverse effects

Clinical comparison

Use in combination therapy

Brand names

References

External links

UpToDate Contents

English Journal

Japanese Journal

Related Pictures

★リンクテーブル★

「タムスロシン」

分類

作用機序

薬理作用

適応

添付文書

「α受容体遮断薬」

非選択的α受容体拮抗薬

選択的α1受容体拮抗薬

選択的α2受容体拮抗薬

「tamsulosin hydrochloride」

選択的α₁受容体拮抗薬

選択的α₂受容体拮抗薬