Brimonidine

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