Tamsulosin
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This article may be too technical for most readers to understand. (February 2012) |
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| 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 cat. | B2 (AU) B (US) |
| Legal status | Prescription Only (S4) (AU) POM (UK) ℞-only (US) |
| Routes | oral |
| Pharmacokinetic data | |
| Bioavailability | 100% (oral) |
| Metabolism | hepatic |
| Half-life | 9–13 hours |
| Excretion | 76% renal |
| Identifiers | |
| CAS number | 106133-20-4  |
| ATC code | G04CA02 |
| PubChem | CID 129211 |
| IUPHAR ligand | 488 |
| DrugBank | DB00706 |
| ChemSpider | 114457 |
| UNII | G3P28OML5I |
| KEGG | D08560 |
| ChEBI | CHEBI:9398 |
| ChEMBL | CHEMBL836 |
| Chemical data | |
| Formula | C20H28N2O5S |
| Mol. mass | 408.51 |
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Tamsulosin (rINN) (pron.: /tæmˈsuːlɵsɨn/ or /tæmsʉˈloʊsɨn/) is a treatment for 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]
More specifically, tamsulosin is an α1a-selective alpha blocker 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. In southeast Asian countries like Bangladesh, Tamsulosin is marketed by Delta Pharma Ltd. under the trade name Tamsin.
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]
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Mechanism [edit]
Tamsulosin is a selective α1 receptor antagonist that has preferential selectivity for the α1A receptor in the prostate versus the α1B 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.
Clinical uses [edit]
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.[5][6]
Adverse effects [edit]
Two adverse drug reactions have been reported:
- Immunologic: It contains a sulfa moiety, thus causing typical reactions to sulfa drugs.[citation needed]
- 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.[7]
Tamsulosin has also affected sexual function in men. It can cause males to experience retrograde ejaculation.[8] 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.
Tamsulosin can occasionally cause a drop in blood pressure, rarely resulting in dizziness or fainting.[citation needed] Other reported side effects include vertigo, headache, nasal congestion and palpitations.[citation needed]
Clinical comparison [edit]
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 [edit]
The results of the CombAT (Combination of Avodart and Tamsulosin) 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. [9] The CombAT trial became the medication Jayln. It was approved by the FDA on June 14, 2010.[10] 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.[11]
Brand names [edit]
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 Flomax, Flomaxtra, Contiflo XL, Urimax and Pradif,[12] 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.[13] In Egypt,[14] Italy and Iceland, it is marketed under the trade name Omnic by Astellas Pharma Europe
References [edit]
- ^ 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.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
- ^ Medscape, Good Cataract Surgery Outcomes Possible in Intraoperative Floppy Iris Syndrome Due to Tamsulosin.
- ^ "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 [edit]
- 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
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