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a complex consisting of an organic base in association with hydrogen chloride

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2016/03/07 16:34:29」(JST)

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Tamsulosin (rINN) (/tæmˈsuːləsən/^[1]) is an α_1a adrenergic 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.^[2]

The U.S. patent for Flomax expired in October 2009.^[3] The U.S. Food and Drug Administration (FDA) approved generic Flomax in March 2010.^[4]

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.^[5]

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tamsulosin in alpha 1A/D receptors is controversial and over three quarters of tamsulosin registered human studies are unpublished.^[6]

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.^[7]^[8] 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.^[9]^[10]^[11] 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.^[12]
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.^[13]
Severe hypotension.^[14]^[15]

Tamsulosin has also affected sexual function in men. It can cause males to experience retrograde ejaculation.^[16] 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.^[17] The CombAT trial became the medication Jalyn. It was approved by the FDA on June 14, 2010.^[18] 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.^[19]

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,^[20] 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 and as Harnal Orca in Thailand.^[21] In Egypt,^[22] Italy and Iceland, it is marketed under the trade name Omnic by Astellas Pharma Europe. The largest manufacturer of Tamsulosin, drug substance, is Synthon BV (The Netherlands).

References

^ "Tamsulosin". Merriam-Webster Dictionary.
^ "Benign prostatic hyperplasia (BPH)". Mayo Clinic.
^ "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.
^ . doi:10.1136/bmj.f6320. Missing or empty |title= (help)
^ "Tamsulosin Aids Stone Expulsion". Renal and Urology News.
^ "Study Shows Use of Tamsulosin or Nifedipine Helps Patients to Clear Ureteral Stone Fragments Faster and Reduces Rate of Recurrence".
^ 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.
^ Approval letter
^ Australian Medicines Handbook^{[full citation needed]}
^ 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) - Official Site

UpToDate Contents

全文を閲覧するには購読必要です。 To read the full text you will need to subscribe.

1. 男性性機能不全の治療 treatment of male sexual dysfunction
2. 男性の性交時痛 male dyspareunia
3. 前立腺肥大症の内科的治療 medical treatment of benign prostatic hyperplasia
4. 尿管ステントの留置およびマネージメント placement and management of indwelling ureteral stents
5. 男性の尿失禁 urinary incontinence in men

English Journal

Reversible visual loss caused by combination therapy of alfuzosin and finasteride in a patient with uveitic glaucoma.

Lee JW, Lee HJ.SourceDepartment of Ophthalmology, Eulji Medical Center, Eulji University School of Medicine , Seoul , Korea.
Cutaneous and ocular toxicology.Cutan Ocul Toxicol.2013 Jun;32(2):182-4. doi: 10.3109/15569527.2012.733788. Epub 2012 Oct 24.
Purpose: To report a case of ischemic optic neuropathy caused by medication for benign prostatic hyperplasia (BPH). Methods: The medical record of a patient who experienced gradual visual loss during the BPH medication was retrospectively reviewed. Observations: A 60-year-old man who had uveitic
PMID 23094797

Efficacy and safety of orally disintegrating tamsulosin tablets in Taiwanese patients with benign prostatic hyperplasia.

Lin KH, Lin YW, Wen YC, Lee LM.SourceDepartment of Urology, Wan Fang Hospital, Taipei Medical University , Taipei , Taiwan.
The aging male : the official journal of the International Society for the Study of the Aging Male.Aging Male.2012 Dec;15(4):246-52. doi: 10.3109/13685538.2012.724741. Epub 2012 Oct 15.
Objectives: Tamsulosin is an alpha-1 adrenoceptor antagonist applied in treating lower urinary tract symptoms (LUTS) suggestive of benign prostatic hyperplasia (BPH). This study aimed to evaluate safety, efficacy and acceptance of newly formulated orally disintegrating tamsulosin tablets in Taiwanes
PMID 23067262

Japanese Journal

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

タムスロシン塩酸塩口腔内崩壊錠0.1mgの製剤品質および服用性の臨床的評価

ジェネリック研究 : 日本ジェネリック医薬品学会機関誌 10(1), 27-34, 2016-06
NAID 40020879887

Formulation Design for Orally Disintegrating Tablets Containing Enteric-Coated Particles

Chemical and Pharmaceutical Bulletin 62(5), 407-414, 2014
NAID 130004053791

「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
License data	US FDA: Tamsulosin;
Pregnancy; category	AU: B2; US: B (No risk in non-human studies); ;
Routes of; administration	oral
Legal status	AU: S4 (Prescription only); UK: POM (Prescription only); US: ℞-only;
Pharmacokinetic data
Bioavailability	100% (oral)
Metabolism	hepatic
Biological half-life	9–13 hours
Excretion	76% renal
Identifiers
CAS 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
Molar 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 ;
(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

「hydrochloride」

　　[★] 塩酸塩、ハイドロクロライド　

[1] "Tamsulosin". Merriam-Webster Dictionary.

[2] "Benign prostatic hyperplasia (BPH)". Mayo Clinic.

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

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

[pharmnemonics-5] Shen, Howard (2008). Illustrated Pharmacology Memory Cards: PharMnemonics. Minireview. p. 13. ISBN 1-59541-101-1.

[6] . doi:10.1136/bmj.f6320. Missing or empty |title= (help)

[7] "Tamsulosin Aids Stone Expulsion". Renal and Urology News.

[8] "Study Shows Use of Tamsulosin or Nifedipine Helps Patients to Clear Ureteral Stone Fragments Faster and Reduces Rate of Recurrence".

[9] 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.

[10] 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.

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

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

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

[14] 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.

[15] 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.

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

[Roehrborn2008-17] 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.

[18] Approval letter

[19] Australian Medicines Handbook^{[full citation needed]}

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

[21] "Drugs.com Database".

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

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案内

tamsulosin hydrochloride