Brimonidine

From Wikipedia, the free encyclopedia
Jump to: navigation, search
Brimonidine
Brimonidine structure.png
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 Consumer Drug Information
MedlinePlus a601232
Pregnancy cat.
Legal status
Routes Ocular (eye drops), topical (gel)
Pharmacokinetic data
Metabolism Primarily liver
Half-life 3 hours ocular 12 hours topical
Identifiers
CAS number 59803-98-4 YesY
ATC code D11AX21 S01EA05
PubChem CID 2435
IUPHAR ligand 520
DrugBank DB00484
ChemSpider 2341 YesY
UNII E6GNX3HHTE YesY
KEGG D07540 YesY
ChEBI CHEBI:3175 YesY
ChEMBL CHEMBL844 YesY
Chemical data
Formula C11H10BrN5 
Mol. mass 292.135 g/mol
 YesY (what is this?)  (verify)

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).

Clinical uses[edit]

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[edit]

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[edit]

  1. ^ Sena DF, Lindsley K (2013). "Neuroprotection for treatment of glaucoma in adults". Cochrane Database Syst Rev 2: CD006539. doi:10.1002/14651858.CD006539.pub3. PMID 20166085. 
  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. doi:10.1016/s0002-9394(99)00076-8. PMID 10482088.  edit
  • Mosby's Drug Guide for Nurses (7th edition; Skidmore) 2007.

External links[edit]