World Library  
Flag as Inappropriate
Email this Article

Brimonidine

Article Id: WHEBN0004857534
Reproduction Date:

Title: Brimonidine  
Author: World Heritage Encyclopedia
Language: English
Subject: Apraclonidine, Carteolol, Lofepramine, Alpha-2 adrenergic receptor, Glaucoma
Collection: Alpha-Adrenergic Agonists, Imidazolines, Organobromides, Quinoxalines
Publisher: World Heritage Encyclopedia
Publication
Date:
 

Brimonidine

Brimonidine
Systematic (IUPAC) name
5-Bromo-N-(4,5-dihydro-1H-imidazol-2-yl) quinoxalin-6-amine
Clinical data
Trade names Alphagan, Mirvaso
AHFS/Drugs.com
MedlinePlus
Pregnancy
category
  • US: B (No risk in non-human studies)
Legal status
Routes of
administration
Ocular (eye drops), topical (gel)
Pharmacokinetic data
Metabolism Primarily liver
Biological half-life 3 hours ocular 12 hours topical
Identifiers
CAS Registry Number  Y
ATC code D11 S01
PubChem CID:
IUPHAR/BPS
DrugBank  Y
ChemSpider  Y
UNII  Y
KEGG  Y
ChEBI  Y
ChEMBL  Y
Chemical data
Formula C11H10BrN5
Molecular mass 292.135 g/mol
 Y   

Brimonidine (bri-MOE-ni-deen) is a drug used as eye drops under the brand names Alphagan and Alphagan-P to treat open-angle glaucoma or ocular hypertension, and as a gel, Mirvaso, for rosacea (facial erythema).

It acts via decreasing synthesis of aqueous humor, and increasing the amount that drains from the eye through uveoscleral outflow. In treating erythema, it acts by vasoconstriction (narrowing of blood vessels).

Contents

  • Clinical uses 1
  • Mechanism of action 2
  • References 3
  • External links 4

Clinical uses

Brimonidine is indicated for the lowering of intraocular pressure in patients with open-angle glaucoma or ocular hypertension. It is also the active ingredient of Combigan along with timolol maleate.

A Cochrane Systematic Review compared the effect of brimonidine and timolol in slowing the progression of open angle glaucoma in adult participants.[1]

In 2013, the FDA approved topical application of brimonidine 0.33% (Mirvaso) for facial erythema or rosacea.

Mechanism of action

Brimonidine is an α2 adrenergic agonist.

Alpha 2 agonists, through the activation of a G protein-coupled receptor, inhibit the activity of adenylate cyclase. This reduces cAMP and hence aqueous humour production by the ciliary body.

Peripheral alpha 2 agonist activity results in vasoconstriction of blood vessels (as opposed to central alpha 2 agonist activity that decreases sympathetic tone, as can be seen by the medication clonidine). 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 alpha adrenergic stimulation. This may lead to relaxed ciliary muscle and increased uveoscleral outflow.[2]

References

  1. ^ Sena DF, Lindsley K (2013). "Neuroprotection for treatment of glaucoma in adults". Cochrane Database Syst Rev 2: CD006539.  
  2. ^ Toris, C.; Camras, C.; Yablonski, M. (1999). "Acute versus chronic effects of brimonidine on aqueous humor dynamics in ocular hypertensive patients". American journal of ophthalmology 128 (1): 8–14.  
  • Mosby's Drug Guide for Nurses (7th edition; Skidmore) 2007.

External links

  • Alphagan P product website
  • Alphagan P prescribing information
This article was sourced from Creative Commons Attribution-ShareAlike License; additional terms may apply. World Heritage Encyclopedia content is assembled from numerous content providers, Open Access Publishing, and in compliance with The Fair Access to Science and Technology Research Act (FASTR), Wikimedia Foundation, Inc., Public Library of Science, The Encyclopedia of Life, Open Book Publishers (OBP), PubMed, U.S. National Library of Medicine, National Center for Biotechnology Information, U.S. National Library of Medicine, National Institutes of Health (NIH), U.S. Department of Health & Human Services, and USA.gov, which sources content from all federal, state, local, tribal, and territorial government publication portals (.gov, .mil, .edu). Funding for USA.gov and content contributors is made possible from the U.S. Congress, E-Government Act of 2002.
 
Crowd sourced content that is contributed to World Heritage Encyclopedia is peer reviewed and edited by our editorial staff to ensure quality scholarly research articles.
 
By using this site, you agree to the Terms of Use and Privacy Policy. World Heritage Encyclopedia™ is a registered trademark of the World Public Library Association, a non-profit organization.
 



Copyright © World Library Foundation. All rights reserved. eBooks from World eBook Library are sponsored by the World Library Foundation,
a 501c(4) Member's Support Non-Profit Organization, and is NOT affiliated with any governmental agency or department.