Tamsulosin#Use in combination therapy
{{Short description|Medication}}
{{Use dmy dates|date=October 2021}}
{{cs1 config |name-list-style=vanc |display-authors=6}}
{{Infobox drug
| Watchedfields = changed
| verifiedrevid = 461746753
| image = Tamsulosin.svg
| image_class = skin-invert-image
| width = 250
| alt =
| image2 = Tamsulosin-from-xtal-3D-bs-17.png
| image_class2 = bg-transparent
| alt2 =
| pronounce =
{{IPAc-en|t|æ|m|ˈ|s|uː|l|ə|s|ɪ|n}}{{refn|{{MerriamWebsterDictionary|Tamsulosin}}}}
{{respell|tam|SOO|lə|sin}}
| tradename = Flomax, others
| Drugs.com = {{drugs.com|monograph|tamsulosin-hydrochloride}}
| MedlinePlus = a698012
| DailyMedID = Tamsulosin
| pregnancy_AU = B2
| pregnancy_AU_comment =
| routes_of_administration = By mouth
| class = α1 blocker
| ATC_prefix = G04
| ATC_suffix = CA02
| ATC_supplemental =
| legal_AU = S4
| legal_AU_comment =
| legal_BR =
| legal_BR_comment =
| legal_CA = Rx-only
| legal_DE =
| legal_DE_comment =
| legal_NZ =
| legal_NZ_comment =
| legal_UK = POM
| legal_UK_comment = {{cite web | title=Flomaxtra XL, 400 micrograms, film-coated prolonged-release tablet – Summary of Product Characteristics (SmPC) | website=(emc) | date=12 November 2019 | url=https://www.medicines.org.uk/emc/product/97/smpc | access-date=2 December 2021}}{{cite web | title=Faramsil 400 microgram Prolonged-release Tablets – Summary of Product Characteristics (SmPC) | website=(emc) | date=4 November 2020 | url=https://www.medicines.org.uk/emc/product/4948/smpc | access-date=2 December 2021}}
| legal_US = Rx-only
| legal_EU =
| legal_EU_comment =
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| bioavailability = 100% (by mouth)
| protein_bound =
| metabolism = Liver
| metabolites =
| onset =
| elimination_half-life = 9–13 hours
| duration_of_action =
| excretion = 76% Kidney
| index2_label = as HCl
| CAS_number_Ref = {{cascite|correct|??}}
| CAS_number = 106133-20-4
| PubChem = 129211
| IUPHAR_ligand = 488
| DrugBank_Ref = {{drugbankcite|correct|drugbank}}
| DrugBank = DB00706
| ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}}
| ChemSpiderID = 114457
| UNII_Ref = {{fdacite|correct|FDA}}
| UNII = G3P28OML5I
| KEGG_Ref = {{keggcite|correct|kegg}}
| KEGG = D08560
| KEGG2_Ref = {{keggcite|correct|kegg}}
| KEGG2 = D01024
| ChEBI_Ref = {{ebicite|correct|EBI}}
| ChEBI = 9398
| ChEMBL_Ref = {{ebicite|correct|EBI}}
| ChEMBL = 836
| NIAID_ChemDB =
| PDB_ligand =
| synonyms =
| IUPAC_name = (R)-5-(2-
| C = 20
| H = 28
| N = 2
| O = 5
| S = 1
| SMILES = CCOc1ccccc1OCCN[C@@H](C)Cc1ccc(OC)c(c1)S(=O)(=O)N
| StdInChI_Ref = {{stdinchicite|correct|chemspider}}
| StdInChI = 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
| StdInChIKey_Ref = {{stdinchicite|correct|chemspider}}
| StdInChIKey = DRHKJLXJIQTDTD-OAHLLOKOSA-N
| density =
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File:Tamsulosin - ARISTO Pharma - 0,4 mg Retardtabletten - Urologikum.jpg
Tamsulosin, sold under the brand name Flomax among others, is a medication used to treat symptomatic benign prostatic hyperplasia and chronic prostatitis in men.{{cite web |title=Tamsulosin Hydrochloride Monograph for Professionals |url=https://www.drugs.com/monograph/tamsulosin-hydrochloride.html |website=Drugs.com |publisher=AHFS |access-date=24 December 2018 }}{{cite web |title=Prostatitis |url=https://www.nhs.uk/conditions/prostatitis |website=NHS |access-date=24 December 2018 |date=19 October 2017}} It is also used to help with the passage of kidney stones.{{cite journal | vauthors = Wang RC, Smith-Bindman R, Whitaker E, Neilson J, Allen IE, Stoller ML, Fahimi J | title = Effect of Tamsulosin on Stone Passage for Ureteral Stones: A Systematic Review and Meta-analysis | journal = Annals of Emergency Medicine | volume = 69 | issue = 3 | pages = 353–361.e3 | date = March 2017 | pmid = 27616037 | doi = 10.1016/j.annemergmed.2016.06.044 | doi-access = free | title-link = doi }} The evidence for benefit with a kidney stone is better when the stone is larger. Tamsulosin is taken by mouth.
Common side effects include dizziness, headache, insomnia, nausea, blurry vision, and sexual problems. Other side effects may include feeling lightheaded with standing due to changes in blood pressure, and angioedema. Tamsulosin is an alpha blocker and works by relaxing muscles in the prostate.{{cite book | vauthors = Hutchison LC, Sleeper RB |title=Fundamentals of Geriatric Pharmacotherapy: An Evidence-Based Approach |date=2010 |publisher=ASHP |isbn=9781585283057 |page=209 |url=https://books.google.com/books?id=fUtOugU_KeIC&pg=PA209 }} Specifically it is an α1-adrenergic receptor blocker.
Tamsulosin was approved for medical use in the United States in 1997. It is available as a generic medication.{{cite book|title=British national formulary: BNF 76|date=2018|publisher=Pharmaceutical Press|isbn=9780857113382|pages=767|edition=76}} In 2022, it was the twentieth most commonly prescribed medication in the United States, with more than 25{{nbsp}}million prescriptions.{{cite web | title=The Top 300 of 2022 | url=https://clincalc.com/DrugStats/Top300Drugs.aspx | website=ClinCalc | access-date=30 August 2024 | archive-date=30 August 2024 | archive-url=https://web.archive.org/web/20240830202410/https://clincalc.com/DrugStats/Top300Drugs.aspx | url-status=live }}{{cite web | title = Tamsulosin Drug Usage Statistics, United States, 2013 - 2022 | website = ClinCalc | url = https://clincalc.com/DrugStats/Drugs/Tamsulosin | access-date = 30 August 2024 }}
Medical uses
File:000636lg Flomax 0.4 mg.jpg
Tamsulosin is used for benign prostatic hyperplasia and to help with the passage of kidney stones.{{cite press release | url = 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 | title = Study Shows Use of Tamsulosin or Nifedipine Helps Patients to Clear Ureteral Stone Fragments Faster and Reduces Rate of Recurrence }} Tamsulosin, however, appears to be effective only for stones over 4 mm and less than 10 mm in size.
Tamsulosin is also used as an add-on treatment for acute urinary retention. Men may void more successfully after catheter removal if they are taking tamsulosin, and are less likely to need repeat catheterization.{{cite journal | vauthors = Lucas MG, Stephenson TP, Nargund V | title = Tamsulosin in the management of patients in acute urinary retention from benign prostatic hyperplasia | journal = BJU International | volume = 95 | issue = 3 | pages = 354–357 | date = February 2005 | pmid = 15679793 | doi = 10.1111/j.1464-410X.2005.05299.x | s2cid = 30254915 | doi-access = }}
Tamsulosin does not decrease the overall size of the prostate in men with benign prostatic hyperplasia and is not recommended for the prevention of prostate cancer.{{Cite book|title=Medical-surgical nursing: assessment and management of clinical problems| vauthors = Lewis SM, Dirksen SR, Heitkemper MM, Bucher LH |year= 2013|isbn=978-0-323-10089-2|edition=9th|publisher=Mosby|location=St. Louis, Missouri|oclc=228373703}}
= Combination therapy =
The results of the CombAT (combination of dutasteride (Avodart) and tamsulosin (Duodart)) trial in 2008, demonstrated that treatment with the combination of dutasteride and tamsulosin provides greater symptom benefits compared to monotherapy with either agent alone for treatment of benign prostatic hyperplasia.{{cite journal | vauthors = Roehrborn CG, Siami P, Barkin J, Damião R, Major-Walker K, Morrill B, Montorsi F | title = 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 | journal = The Journal of Urology | volume = 179 | issue = 2 | pages = 616–621; discussion 621 | date = February 2008 | pmid = 18082216 | doi = 10.1016/j.juro.2007.09.084 }} The combination medication dutasteride/tamsulosin (Jalyn) was approved by the US Food and Drug Administration (FDA) in June 2010.{{cite web | title=Drug Approval Package: Jalyn (dutasteride and tamsulosin) NDA #022460 | website=U.S. Food and Drug Administration (FDA) | date=3 February 2011 | url=https://www.accessdata.fda.gov/drugsatfda_docs/nda/2010/022460s000_jalyn_toc.cfm | access-date=30 March 2025}}
Adverse effects
- Eyes: People 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 person's history with this drug, and thus having the option of alternative techniques.{{cite web | last=Taylor | first=Jill | title=Good Cataract Surgery Outcomes Possible in IFIS Due to Tamsulosin | website=Medscape | date=16 November 2006 | url=https://www.medscape.com/viewarticle/547937 | access-date=30 March 2025}}
- Severe hypotension.{{cite journal | vauthors = Bird ST, Delaney JA, Brophy JM, Etminan M, Skeldon SC, Hartzema AG | title = 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 | journal = BMJ | volume = 347 | pages = f6320 | date = November 2013 | pmid = 24192967 | pmc = 3817852 | doi = 10.1136/bmj.f6320 }}{{cite journal | vauthors = Ramirez J | title = Severe hypotension associated with α blocker tamsulosin | journal = BMJ | volume = 347 | pages = f6492 | date = November 2013 | pmid = 24192968 | doi = 10.1136/bmj.f6492 | hdl-access = free | s2cid = 24324483 | hdl = 10906/78488 }}
- Alpha-blockers, including prazosin, terazosin, doxazosin, or tamsulosin, do not appear to affect all-cause mortality in heart failure rehospitalization in those also receiving β-blockers.{{cite journal | vauthors = Page RL, O'Bryant CL, Cheng D, Dow TJ, Ky B, Stein CM, Spencer AP, Trupp RJ, Lindenfeld J | title = Drugs That May Cause or Exacerbate Heart Failure: A Scientific Statement From the American Heart Association | journal = Circulation | volume = 134 | issue = 6 | pages = e32–e69 | date = August 2016 | pmid = 27400984 | doi = 10.1161/CIR.0000000000000426 | doi-access = free | title-link = doi }}
- Tamsulosin can also cause retrograde ejaculation, which occurs when semen is redirected to the urinary bladder instead of being ejaculated normally. This is because tamsulosin relaxes the muscles of the urethral sphincters, which are normally closed during ejaculation.{{Cite web|url=https://www.drugs.com/sfx/tamsulosin-side-effects.html|title=Tamsulosin Side Effects|website=Drugs.com|access-date=27 April 2011}}
Mechanism
{{Main|Alpha blocker}}
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.{{Cite book | vauthors = Shen H | title=Illustrated Pharmacology Memory Cards: PharMnemonics | year=2008 | publisher=Minireview | isbn=978-1-59541-101-3 | page=13}}
When alpha 1 receptors in the bladder neck, prostate, ureter, and urethra are blocked, a relaxation in smooth muscle tissue results. This mechanism decreases resistance to urinary flow, reduces discomfort associated with benign prostatic hyperplasia, and facilitates passage of kidney stones.
Brand names
Tamsulosin was first sold in 1997 under the brand name Flomax. The US patent expired in October 2009.{{cite web|title=Flomax – Big Patent Expirations of 2010|url=http://www.fiercepharma.com/special-reports/flomax-big-patent-expirations-2010|date=10 February 2010|access-date=14 January 2012|archive-date=22 April 2012|archive-url=https://web.archive.org/web/20120422163615/http://www.fiercepharma.com/special-reports/flomax-big-patent-expirations-2010|url-status=dead}} The US Food and Drug Administration (FDA) approved generic versions in March 2010.{{cite web | title=FDA Approves First Generic Tamsulosin to Treat Enlarged Prostate Gland | publisher=U.S. Food and Drug Administration (FDA) | via=PR Newswire | date=2 March 2010 | url=https://www.prnewswire.com/news-releases/fda-approves-first-generic-tamsulosin-to-treat-enlarged-prostate-gland-85995072.html | access-date=30 March 2025}}
It is sold by various companies, including Boehringer Ingelheim and CSL.{{cn|date=March 2025}} Tamsulosin hydrochloride extended-release capsules are sold under the brand names Urimax 0.4 (India),Tamlocept 0.4 (India), Flomax, Flomaxtra, Contiflo XL, bestflo, Mecir LP (France), Urimax, Pamsvax, and Pradif, although generic, unmodified-release capsules are still approved and sold in many countries (such as Canada). Generic extended-release tablets are sold in most countries of the European Economic Area (EEA). In Mexico, it is sold as Secotex, as Harnal D in Japan and Indonesia, and as Harnal OCAS (oral controlled absorption system) in Thailand.{{cite web | title = Drugs.com Database | url= https://www.drugs.com/international/harnal-d.html}} In Egypt,{{cite news |title= Novartis hits Astellas with transplant drug generic|url=https://www.reuters.com/article/americasRegulatoryNews/idUST34424920090811 |publisher= Reuters|date= 11 August 2009|access-date=11 August 2009}} Italy, Russia and Iceland, it is sold under the brand name Omnic by Astellas Pharma Europe. Tamsulosin hydrochloride is sold in Bangladesh under the brand names Uromax, Prostanil MR, Tamisol MR, and Tamsin.{{citation needed|date=August 2017}} It is available to patients in the UK on National Health Service prescription (prescribed without brand name, at nominal or no cost to patients),{{cite web |title=About tamsulosin |publisher=NHS|date=2 February 2023|url=https://www.nhs.uk/medicines/tamsulosin/about-tamsulosin/ |access-date=16 May 2025}} and in 2010 became available for over-the-counter purchase without prescription.{{cite journal | vauthors = | title = OTC tamsulosin for benign prostatic hyperplasia | journal = Drug and Therapeutics Bulletin | volume = 48 | issue = 10 | pages = 113–116 | date = October 2010 | pmid = 20926447 | doi = 10.1136/dtb.2010.10.0052 | s2cid = 32141889 }}
References
{{Reflist}}
{{Drugs used in benign prostatic hypertrophy}}
{{Adrenergic receptor modulators}}
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