Jump to content
 







Main menu
   


Navigation  



Main page
Contents
Current events
Random article
About Wikipedia
Contact us
Donate
 




Contribute  



Help
Learn to edit
Community portal
Recent changes
Upload file
 








Search  

































Create account

Log in
 









Create account
 Log in
 




Pages for logged out editors learn more  



Contributions
Talk
 



















Contents

   



(Top)
 


1 Medical uses  



1.1  By mouth  





1.2  Eye drops  





1.3  On the skin  







2 Contraindications  





3 Side effects  





4 Formulations  





5 Brand names  





6 References  





7 External links  














Timolol






العربية
تۆرکجه
Bosanski
Cymraeg
Deutsch
Ελληνικά
Español
فارسی
Français

Հայերեն
Bahasa Indonesia
Italiano
Magyar
Македонски
Bahasa Melayu
Nederlands

ି
Polski
Português
Română
Русский
Српски / srpski
Srpskohrvatski / српскохрватски
Suomi
Türkçe
Українська
Tiếng Vit
 

Edit links
 









Article
Talk
 

















Read
Edit
View history
 








Tools
   


Actions  



Read
Edit
View history
 




General  



What links here
Related changes
Upload file
Special pages
Permanent link
Page information
Cite this page
Get shortened URL
Download QR code
Wikidata item
 




Print/export  



Download as PDF
Printable version
 




In other projects  



Wikimedia Commons
 
















Appearance
   

 






From Wikipedia, the free encyclopedia
 


Timolol
Clinical data
Trade namesBetimol, Blocadren, Istalol, Timoptic, others[1]
AHFS/Drugs.comMaleate Monograph
eent Monograph
MedlinePlusa684029
License data
Pregnancy
category
  • AU:C
  • Routes of
    administration
    By mouth, topical (eye drop)
    Drug classBeta blocker
    ATC code
    Legal status
    Legal status
  • UK: POM (Prescription only)
  • US: ℞-only
  • Pharmacokinetic data
    Bioavailability60%
    MetabolismLiver (80%, mainly CYP2D6[4])
    Onset of action15–30 min[3]
    Elimination half-life2.5–5 hours
    Duration of action24 hours[3]
    ExcretionKidney
    Identifiers
    • (S)-1-(tert-Butylamino)-3-[(4-morpholin-4-yl-1,2,5-thiadiazol-3-yl)oxy]propan-2-ol

    CAS Number
    PubChem CID
    IUPHAR/BPS
    DrugBank
    ChemSpider
    UNII
    KEGG
  • as salt: D00603 checkY
  • ChEBI
    ChEMBL
    CompTox Dashboard (EPA)
    ECHA InfoCard100.043.651 Edit this at Wikidata
    Chemical and physical data
    FormulaC13H24N4O3S
    Molar mass316.42 g·mol−1
    3D model (JSmol)
    • CC(C)(C)NCC(O)COc1nsnc1N1CCOCC1

    • InChI=1S/C13H24N4O3S/c1-13(2,3)14-8-10(18)9-20-12-11(15-21-16-12)17-4-6-19-7-5-17/h10,14,18H,4-9H2,1-3H3/t10-/m0/s1 checkY

    • Key:BLJRIMJGRPQVNF-JTQLQIEISA-N checkY

      (verify)

    Timolol is a beta blocker medication used either by mouth or as eye drops.[3][5] As eye drops it is used to treat increased pressure inside the eye such as in ocular hypertension and glaucoma.[3] By mouth it is used for high blood pressure, chest pain due to insufficient blood flow to the heart, to prevent further complications after a heart attack, and to prevent migraines.[5]

    Common side effects with the drops is irritation of the eye.[3] Common side effects by mouth include tiredness, slow heart beat, itchiness, and shortness of breath.[5] Other side effects include masking the symptoms of low blood sugar in those with diabetes.[3] Use is not recommended in those with asthma, uncompensated heart failure, or COPD.[3] It is unclear if use during pregnancy is safe for the fetus.[6] Timolol is a non-selective beta blocker.[3]

    Timolol was patented in 1968, and came into medical use in 1978.[7] It is on the World Health Organization's List of Essential Medicines.[8] Timolol is available as a generic medication.[3][9] In 2021, it was the 163rd most commonly prescribed medication in the United States, with more than 3 million prescriptions.[10][11]

    Medical uses[edit]

    By mouth[edit]

    In its by mouth or oral form, it is used:

    The combination of timolol and the alpha-1 blocker prazosin has sedative effects.[13]

    Eye drops[edit]

    In its eye drop form it is used to treat open-angle and, occasionally, secondary glaucoma.[3][14] The mechanism of action of timolol is probably the reduction of the formation of aqueous humor[3] in the ciliary body in the eye. It was the first beta blocker approved for topical use in treatment of glaucoma in the United States (1978).[15] When used by itself, it depresses intraocular pressure (IOP) 18–34% below baseline within first few treatments. However, there are short-term escape and long-term drift effects in some people. That is, tolerance develops. It may reduce the extent of the daytime IOP curve up to 50%. The IOP is higher during sleep. Efficacy of timolol in lowering IOP during the sleep period may be limited.[16][17][18] It is a 5–10× more potent beta blocker than propranolol. Timolol is light-sensitive; it is usually preserved with 0.01% benzalkonium chloride (BAC), but also comes BAC-free. It can also be used in combination with pilocarpine, carbonic anhydrase inhibitors[19]orprostaglandin analogs.[20]

    ACochrane review compared the effect of timolol versus brimonidine in slowing the progression of open angle glaucoma in adults but found insufficient evidence to come to conclusions.[21]

    On the skin[edit]

    In its gel form it is used on the skin to treat infantile hemangiomas.[22]

    Contraindications[edit]

    The medication should not be taken by individuals with:[23]

    Side effects[edit]

    The most serious possible side effects include cardiac arrhythmias and severe bronchospasms.[23] Timolol can also lead to fainting, congestive heart failure, depression, confusion, worsening of Raynaud's syndrome and impotence.[23]

    Side effects when given in the eye include: burning sensation, eye redness, superficial punctate keratopathy, corneal numbness.[25][14]

    Formulations[edit]

    It is available in tablet and liquid formulations.[23][25]

    For ophthalmic use, timolol is also available combined:

    Brand names[edit]

    Timolol is marketed under many trade names worldwide.[1] Timolol eye drops are marketed under the brand name Istalol among others.[26][27]

    References[edit]

    1. ^ a b "Timolol". Drugs.com. Archived from the original on 7 March 2016. Retrieved 28 December 2016.
  • ^ "Product monograph brand safety updates". Health Canada. February 2024. Retrieved 24 March 2024.
  • ^ a b c d e f g h i j k "Timolol eent". The American Society of Health-System Pharmacists. Archived from the original on 28 December 2016. Retrieved 8 December 2016.
  • ^ Volotinen M, Turpeinen M, Tolonen A, Uusitalo J, Mäenpää J, Pelkonen O (July 2007). "Timolol metabolism in human liver microsomes is mediated principally by CYP2D6". Drug Metabolism and Disposition. 35 (7): 1135–1141. doi:10.1124/dmd.106.012906. PMID 17431033. S2CID 794764.
  • ^ a b c "Timolol Maleate". The American Society of Health-System Pharmacists. Archived from the original on 28 December 2016. Retrieved 8 December 2016.
  • ^ "Timolol ophthalmic Use During Pregnancy". The American Society of Health-System Pharmacists. Archived from the original on 28 December 2016. Retrieved 28 December 2016.
  • ^ Fischer J, Ganellin CR (2006). Analogue-based Drug Discovery. John Wiley & Sons. p. 460. ISBN 9783527607495. Archived from the original on 28 December 2016.
  • ^ World Health Organization (2019). World Health Organization model list of essential medicines: 21st list 2019. Geneva: World Health Organization. hdl:10665/325771. WHO/MVP/EMP/IAU/2019.06. License: CC BY-NC-SA 3.0 IGO.
  • ^ "Competitive Generic Therapy Approvals". U.S. Food and Drug Administration (FDA). 29 June 2023. Archived from the original on 29 June 2023. Retrieved 29 June 2023.
  • ^ "The Top 300 of 2021". ClinCalc. Archived from the original on 15 January 2024. Retrieved 14 January 2024.
  • ^ "Timolol - Drug Usage Statistics". ClinCalc. Retrieved 14 January 2024.
  • ^ Marcus DA, Bain PA (27 February 2009). Effective Migraine Treatment in Pregnant and Lactating Women: A Practical Guide. シュプリンガー・ジャパン株式会社. pp. 141–. ISBN 978-1-60327-438-8. Archived from the original on 5 November 2017. Retrieved 14 November 2010.
  • ^ Atkin T, Comai S, Gobbi G (April 2018). "Drugs for Insomnia beyond Benzodiazepines: Pharmacology, Clinical Applications, and Discovery". Pharmacol Rev. 70 (2): 197–245. doi:10.1124/pr.117.014381. PMID 29487083. S2CID 3578916.
  • ^ a b "Timolol Ophthalmic". MedlinePlus. 15 April 2017. Retrieved 31 December 2019.
  • ^ Sambhara D, Aref AA (January 2014). "Glaucoma management: relative value and place in therapy of available drug treatments". Therapeutic Advances in Chronic Disease. 5 (1): 30–43. doi:10.1177/2040622313511286. PMC 3871276. PMID 24381726.
  • ^ Liu JH, Kripke DF, Weinreb RN (September 2004). "Comparison of the nighttime effects of once-daily timolol and latanoprost on intraocular pressure". American Journal of Ophthalmology. 138 (3): 389–95. doi:10.1016/j.ajo.2004.04.022. PMID 15364220.
  • ^ Liu JH, Medeiros FA, Slight JR, Weinreb RN (March 2009). "Comparing diurnal and nocturnal effects of brinzolamide and timolol on intraocular pressure in patients receiving latanoprost monotherapy". Ophthalmology. 116 (3): 449–54. doi:10.1016/j.ophtha.2008.09.054. PMID 19157559.
  • ^ Liu JH, Slight JR, Vittitow JL, Scassellati Sforzolini B, Weinreb RN (September 2016). "Efficacy of Latanoprostene Bunod 0.024% Compared With Timolol 0.5% in Lowering Intraocular Pressure Over 24 Hours". American Journal of Ophthalmology. 169: 249–257. doi:10.1016/j.ajo.2016.04.019. PMID 27457257.
  • ^ Strohmaier K, Snyder E, Adamsons I (July 1998). "A multicenter study comparing dorzolamide and pilocarpine as adjunctive therapy to timolol: patient preference and impact on daily life". Journal of the American Optometric Association. 69 (7): 441–51. PMID 9697378.
  • ^ "Ganfort 0.3 mg/ml + 5 mg/ml eye drops, solution - Summary of Product Characteristics (SmPC)". (emc). 20 February 2020. Retrieved 1 March 2020.
  • ^ Sena DF, Lindsley K (January 2017). "Neuroprotection for treatment of glaucoma in adults". The Cochrane Database of Systematic Reviews. 1 (1): CD006539. doi:10.1002/14651858.CD006539.pub4. PMC 5370094. PMID 28122126.
  • ^ Novoa M, Baselga E, Beltran S, Giraldo L, Shahbaz A, Pardo-Hernandez H, et al. (April 2018). "Interventions for infantile haemangiomas of the skin". The Cochrane Database of Systematic Reviews. 2018 (4): CD006545. doi:10.1002/14651858.CD006545.pub3. PMC 6513200. PMID 29667726.
  • ^ a b c d "Timolol Maleate tablet". DailyMed. 17 August 2006. Retrieved 1 December 2019.
  • ^ "Package leaflet: Information for the user Timolol" (PDF). hpra.ie.
  • ^ a b "Betimol- timolol solution". DailyMed. 18 March 2010. Retrieved 1 December 2019.
  • ^ "Generic Istalol Availability". Drugs.com. Retrieved 20 June 2019.
  • ^ "Istalol". Drugs.com. 1 August 2018. Retrieved 19 July 2019.
  • External links[edit]


    Retrieved from "https://en.wikipedia.org/w/index.php?title=Timolol&oldid=1215292505"

    Categories: 
    Beta blockers
    Ethers
    4-Morpholinyl compounds
    Ophthalmology drugs
    Secondary alcohols
    Thiadiazoles
    World Health Organization essential medicines
    Hidden categories: 
    Articles with short description
    Short description matches Wikidata
    Use dmy dates from October 2022
    ECHA InfoCard ID from Wikidata
    Multiple chemicals in Infobox drug
    Chemicals using indexlabels
    Drugboxes which contain changes to watched fields
    Wikipedia medicine articles ready to translate
     



    This page was last edited on 24 March 2024, at 07:00 (UTC).

    Text is available under the Creative Commons Attribution-ShareAlike License 4.0; additional terms may apply. By using this site, you agree to the Terms of Use and Privacy Policy. Wikipedia® is a registered trademark of the Wikimedia Foundation, Inc., a non-profit organization.



    Privacy policy

    About Wikipedia

    Disclaimers

    Contact Wikipedia

    Code of Conduct

    Developers

    Statistics

    Cookie statement

    Mobile view



    Wikimedia Foundation
    Powered by MediaWiki