brimonidine

ブリモニジン

Wikipedia preview

出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2015/11/28 00:55:37」(JST)

wiki en

[Wiki en表示]

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	Consumer Drug Information
MedlinePlus	a601232
Pregnancy category	US: B (No risk in non-human studies)
Legal status	US: ℞-only
Routes of administration	Ocular (eye drops), topical (gel)
Pharmacokinetic data
Metabolism	Primarily liver
Biological half-life	3 hours ocular 12 hours topical
Identifiers
CAS Number	59803-98-4 Y
ATC code	D11AX21 S01EA05
PubChem	CID: 2435
IUPHAR/BPS	520
DrugBank	DB00484 Y
ChemSpider	2341 Y
UNII	E6GNX3HHTE Y
KEGG	D07540 Y
ChEBI	CHEBI:3175 Y
ChEMBL	CHEMBL844 Y
Chemical data
Formula	C11H10BrN5
Molecular 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) Y Key:XYLJNLCSTIOKRM-UHFFFAOYSA-N Y
Y (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

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.

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.

References

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

External links

• Alphagan P product website
• Alphagan P prescribing information

UpToDate Contents

全文を閲覧するには購読必要です。 To read the full text you will need to subscribe.

• 1. 酒さのマネージメント management of rosacea
• 2. 非動脈炎性虚血性視神経症：予後および治療 nonarteritic ischemic optic neuropathy prognosis and treatment
• 3. 開放隅角緑内障：治療 open angle glaucoma treatment
• 4. クロニジンおよびイミダゾリンによる中毒 clonidine and related imidazoline poisoning
• 5. 中毒性結膜炎 toxic conjunctivitis

English Journal

• Polyamidoamine dendrimer hydrogel for enhanced delivery of antiglaucoma drugs.

• Holden CA, Tyagi P, Thakur A, Kadam R, Jadhav G, Kompella UB, Yang H.SourceDepartment of Biomedical Engineering, School of Engineering, Virginia Commonwealth University, Richmond, VA 23284.
• Nanomedicine : nanotechnology, biology, and medicine.Nanomedicine.2011 Sep 16. [Epub ahead of print]
• Dendrimer hydrogel (DH), made from UV-cured polyamidoamine dendrimer G3.0 tethered with three polyethylene glycol (PEG, 12000 Da)-acrylate chains (8.1% w/v) in pH7.4 phosphate buffered saline (PBS), was studied for the delivery of brimonidine (0.1 % w/v) and timolol maleate (0.5% w/v), two antiglauc
• PMID 21930109

• Diurnal intraocular pressure efficacy of the timolol-brimonidine fixed combination and the timolol-dorzolamide fixed combination as a first choice therapy in patients with pseudoexfoliation glaucoma.

• Yuksel N, Gok M, Alt?nta? O, Ca?lar Y.SourceOphthalmology Department, Medical School, Kocaeli University , Kocaeli , Turkey.
• Current eye research.Curr Eye Res.2011 Sep;36(9):804-8.
• Purpose: To evaluate the 6- month daytime efficacy of a fixed combination of timolol and brimonidine (BTFC) versus a timolol and dorzolamide fixed combination (DTFC) as a first choice therapy in patients with pseudoexfoliation glaucoma (PXG). Methods: This study was a randomized, prospective, invest
• PMID 21851166

Japanese Journal

• Effects of brimonidine timolol fixed combination therapy on anterior ocular segment configuration

• KIM Joon Mo,PARK Ki Ho,KIM Chan Yun,KIM Hwang Ki,KIM Tae-Woo,KIM Mo Sae
• Japanese journal of ophthalmology 55(4), 356-361, 2011-07-01
• NAID 10029528087

• Effects of Brimonidine 0.2%-Timolol 0.5% Fixed-Combination Therapy for Glaucoma

• CHO Sung Woo,KIM Joon Mo,PARK Ki Ho,CHOI Chul Young
• Japanese journal of ophthalmology 54(5), 407-413, 2010-09-01
• NAID 10027665692

Related Links

• Brimonidine - Wikipedia, the free encyclopedia

Brimonidine (bri-MOE-ni-deen, brand names Alphagan and Alphagan-P) is a drug used to treat open-angle ... Brimonidine is indicated for the lowering of intraocular pressure in patients with open-angle glaucoma or ocular hypertension.

Related Pictures

---

★リンクテーブル★

リンク元	「ブリモニジン」
拡張検索	「brimonidine tartrate」

「ブリモニジン」

　　[★]

英

brimonidine

化

酒石酸ブリモニジン、brimonidine tartrate

商

アイファガン

関

眼科用剤

• α2刺激薬;眼圧低下薬

「brimonidine tartrate」

　　[★] ブリモニジン。酒石酸ブリモニジン