WordNet

a salt or ester of tartaric acid

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2012/06/26 13:06:41」(JST)

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Brimonidine (bri-MOE-ni-deen, brand names Alphagan and Alphagan-P) is a drug used to treat open-angle glaucoma or ocular hypertension.

It acts via decreasing synthesis of aqueous humor, and increasing the amount that drains from the eye through uveoscleral outflow. As a treatment for glaucoma, it is usually given in eyedrop form.

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 adreneric stimulation. This may lead to relaxed ciliary muscle and increased uveoscleral outflow.^[1]

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.

Topical application of brimonidine 0.05% gel is being investigated in phase III trials for facial erythema or rosacea.

References

^ 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. PMID 10482088. edit

Mosby's Drug Guide for Nurses (7th edition; Skidmore) 2007.

External links

Alphagan P product website
Alphagan P prescribing information

UpToDate Contents

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English Journal

The activity of lowering intraocular pressure of cassiae seed extract in a DBA/2J mouse glaucoma model.

Horng CT, Tsai ML, Chien ST, Kao WT, Tsai MK, Chang TH, Chen FA.Source1 Department of Ophthalmology, Kaohsiung Armed Force General Hospital , Kaohsiung, Taiwan .
Journal of ocular pharmacology and therapeutics : the official journal of the Association for Ocular Pharmacology and Therapeutics.J Ocul Pharmacol Ther.2013 Feb;29(1):48-54. doi: 10.1089/jop.2011.0214. Epub 2012 Oct 5.
Abstract Purpose: To evaluate the activity of lowering intraocular pressure (IOP) by Cassiae seed in the DBA/2J mouse glaucoma model. Methods: Young male (mean age: 3 months) inherited glaucoma mice (BDA/2J) were enrolled in this study. To evaluate the potential of Cassiae seed in the treatment
PMID 23039184

[Combination Therapy in the Medical Treatment of Glaucoma.]

Hommer A.SourceAugenheilkunde, Ordination, Vienna, Austria.
Klinische Monatsblatter fur Augenheilkunde.Klin Monbl Augenheilkd.2013 Jan 20. [Epub ahead of print]
A combination of antiglaucoma medications is indicated if monotherapy is not sufficient to achieve the predefined target pressure and/or in case of a progression of glaucomatous damage or conversion from ocular hypertension to glaucomatous optic neuropathy. Most recently many fixed combinations with
PMID 23335083

Alpha2-adrenergic receptors in spiral ganglion neurons may mediate protective effects of brimonidine and yohimbine against glutamate and hydrogen peroxide toxicity.

Cai J, Li J, Liu W, Han Y, Wang H.SourceOtolaryngology-Head and Neck Surgery, Provincial Hospital Affiliated to Shandong University, Jinan, PR China; Shandong Provincial Key Laboratory of Otology, Jinan, PR China.
Neuroscience.Neuroscience.2013 Jan 3;228:23-35. doi: 10.1016/j.neuroscience.2012.10.004. Epub 2012 Oct 13.
Brimonidine, an alpha2-adrenergic receptor (α(2)-AR) agonist, is thought to be neuroprotective in some types of neurons via the activation of α(2)-AR. However, it is still unknown whether the α(2)-ARs exist in cochlear spiral ganglion neurons (SGNs). The authors aimed to demonstrate the presence
PMID 23069749

Japanese Journal

Effect of brimonidine tartrate 0.2% ophthalmic solution on pupil size

KESLER A
J Cataract Refract Surg 30, 1707-1710, 2004
NAID 30006778416

Does topical brimonidine tartrate help NAION?

FAZZONE HE
Br J Ophthalmol 87, 1193-1194, 2003
NAID 30021644730

「ブリモニジン」

Brimonidine
Systematic (IUPAC) name
	5-Bromo-N-(4,5-dihydro-1H-imidazol-2-yl) quinoxalin-6-amine
Clinical data
Trade names	Alphagan
AHFS/Drugs.com	Consumer Drug Information
MedlinePlus	a601232
Pregnancy cat.	B
Legal status	℞ Prescription only
Routes	Ocular, 1 drop
Pharmacokinetic data
Metabolism	Primarily liver
Half-life	3 hours
Identifiers
CAS number	59803-98-4
ATC code	S01EA05
PubChem	CID 2435
IUPHAR ligand	520
DrugBank	DB00484
ChemSpider	2341
UNII	E6GNX3HHTE
KEGG	D07540
ChEBI	CHEBI:3175
ChEMBL	CHEMBL844
Chemical data
Formula	C11H10BrN5
Mol. mass	292.135 g/mol
	SMILES Brc2c1nccnc1ccc2N/C3=N/CCN3;
	InChI 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) ; Key:XYLJNLCSTIOKRM-UHFFFAOYSA-N ;
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