Movatterモバイル変換


[0]ホーム

URL:


Jump to content
WikipediaThe Free Encyclopedia
Search

Brimonidine

From Wikipedia, the free encyclopedia
Chemical compound

Pharmaceutical compound
Brimonidine
Clinical data
Pronunciation/brɪˈmnɪdn/bri-MOH-nid-een
Trade namesAlphagan, Mirvaso, Lumify, others
AHFS/Drugs.comMonograph
MedlinePlusa601232
License data
Pregnancy
category
Routes of
administration
Topical
ATC code
Legal status
Legal status
Pharmacokinetic data
MetabolismPrimarilyliver
Eliminationhalf-life3 hours (ocular), 12 hours (topical)
Identifiers
  • 5-Bromo-N-(4,5-dihydro-1H-imidazol-2-yl) quinoxalin-6-amine
CAS Number
PubChemCID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard(EPA)
ECHA InfoCard100.149.042Edit this at Wikidata
Chemical and physical data
FormulaC11H10BrN5
Molar mass292.140 g·mol−1
3D model (JSmol)
Melting point252 °C (486 °F)
  • Brc2c1nccnc1ccc2N/C3=N/CCN3
  • InChI=1S/C11H10BrN5/c12-9-7(17-11-15-5-6-16-11)1-2-8-10(9)14-4-3-13-8/h1-4H,5-6H2,(H2,15,16,17) checkY
  • Key:XYLJNLCSTIOKRM-UHFFFAOYSA-N checkY
  (verify)

Brimonidine is anα2 agonistmedication used to treatopen-angle glaucoma,ocular hypertension, androsacea.[5][6] In rosacea it improves the redness.[6] It is used aseye drops or applied to the skin.[5][6] It is also available in thefixed-dose combination medicationbrimonidine/timolol along withtimolol maleate.[7]

Common side effects when used in the eyes include itchiness, redness, and a dry mouth.[5] Common side effects when used on the skin include redness, burning, and headaches.[6] More significant side effects may includeallergic reactions andlow blood pressure.[6][5] Use inpregnancy appears to be safe.[6][5] When applied to the eye it works by decreasing the amount ofaqueous humor made while increasing the amount that drains from the eye.[5] When applied to the skin it works by causing blood vessels to contract.[6]

Brimonidine was patented in 1972 and came into medical use in 1996.[8] It is available as ageneric medication.[9][10] In 2023, it was the 213th most commonly prescribed medication in the United States, with more than 2 million prescriptions.[11][12]

Medical uses

[edit]

Brimonidine isindicated for the lowering ofintraocular pressure in people with open-angle glaucoma or ocular hypertension.[2] It is also used to reduce redness of the eye.[4] The gel is indicated for the topical treatment of persistent (nontransient) facial erythema of rosacea in adults 18 years of age or older.[3]

A 2017Cochrane review found insufficient evidence to determine if brimonidine slows optic nerve damage.[13]

Mechanism of action

[edit]

Brimonidine is anα2adrenergic agonist.[5]

Peripheral α2 agonist activity results in vasoconstriction of blood vessels (as opposed to central α2 agonist activity that decreases sympathetic tone, as can be seen by the medicationclonidine). This vasoconstriction may explain the acute reduction in aqueous humor flow. The increased uveoscleral outflow from prolonged use may be explained by increased prostaglandin release due to α adrenergic stimulation. This may lead to relaxed ciliary muscle and increased uveoscleral outflow.[14]

Society and culture

[edit]

Names

[edit]

It is sold under the brand names Alphagan, Alphagan-P, Mirvaso, Lumify, Brymont, and others.

References

[edit]
  1. ^"Therapeutic Goods (Poisons Standard— June 2025) Instrument 2025"(pdf).Therapeutic Goods Administration (TGA). May 2025. Retrieved31 August 2025.
  2. ^ab"Alphagan P- brimonidine tartrate solution/ drops".DailyMed. 27 June 2024. Retrieved11 November 2024.
  3. ^ab"Mirvaso- brimonidine tartrate gel".DailyMed. 24 October 2024. Retrieved11 November 2024.
  4. ^ab"Lumify Redness Reliever Eye Drops- brimonidine tartrate solution/ drops".DailyMed. 6 November 2023. Retrieved11 November 2024.
  5. ^abcdefg"Brimonidine Tartrate eent Monograph for Professionals".Drugs.com. American Society of Health-System Pharmacists. Retrieved17 March 2019.
  6. ^abcdefg"Brimonidine Tartrate topical Monograph for Professionals".Drugs.com. American Society of Health-System Pharmacists. Retrieved17 March 2019.
  7. ^"COMBIGAN- brimonidine tartrate, timolol maleate solution/ drops".DailyMed. 26 July 2024. Retrieved11 November 2024.
  8. ^Fischer J, Ganellin CR (2006).Analogue-based Drug Discovery. John Wiley & Sons. p. 550.ISBN 978-3-527-60749-5.
  9. ^"Competitive Generic Therapy Approvals".U.S.Food and Drug Administration (FDA). 29 June 2023. Archived fromthe original on 29 June 2023. Retrieved29 June 2023.
  10. ^British national formulary: BNF 76 (76 ed.). Pharmaceutical Press. 2018. p. 1153.ISBN 978-0-85711-338-2.
  11. ^"The Top 300 of 2023".ClinCalc.Archived from the original on 12 August 2025. Retrieved12 August 2025.
  12. ^"Brimonidine Drug Usage Statistics, United States, 2013 - 2023".ClinCalc. Retrieved20 August 2025.
  13. ^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.
  14. ^Toris CB, Camras CB, Yablonski ME (July 1999). "Acute versus chronic effects of brimonidine on aqueous humor dynamics in ocular hypertensive patients".American Journal of Ophthalmology.128 (1):8–14.doi:10.1016/s0002-9394(99)00076-8.PMID 10482088.

Further reading

[edit]
Drugs used forglaucoma preparations andmiosis (S01E)
Sympathomimetics
Parasympathomimetics
muscarinic
muscarinic/nicotinic
acetylcholinesterase inhibitors
Carbonic anhydrase inhibitors/
(sulfonamides)
Beta blocking agents
Prostaglandin analogues (F)
Other agents
Otherdermatological preparations (D11)
Anti-seborrheics
Skin lightening
Skin darkening
Anti-inflammatories
Alopecia treatments
Hair growth inhibitors
Others
α1
Agonists
Antagonists
α2
Agonists
Antagonists
β
Agonists
Antagonists
Portal:
Retrieved from "https://en.wikipedia.org/w/index.php?title=Brimonidine&oldid=1314171536"
Categories:
Hidden categories:

[8]ページ先頭

©2009-2025 Movatter.jp