Brimonidine Tartrate Chemical Properties

Melting point:

207-208°C (dec.)

storage temp. 

Inert atmosphere,Store in freezer, under -20°C

solubility 

DMSO: 1 mg/ml; PBS (pH 7.2): 3 mg/ml

form 

Solid

color 

White to off-white

InChIKey

QZHBYNSSDLTCRG-WUUYCOTASA-N

CAS DataBase Reference

70359-46-5(CAS DataBase Reference)

Safety Information

RIDADR 

UN 2811 6.1 / PGIII

HS Code 

29332900

Brimonidine Tartrate Usage And Synthesis

Ocular hypotensive drug

Brimonidine is a highly selective α2-receptor blocker, successfully developed by the US Company Allergan, which is an eye medication. It can reduce intraocular pressure (IOP). Brimonidine tartrate ophthalmic solution saling in the market is brimonidine tartrate form, which is a good IOP-lowering medication for chronic open-angle glaucoma and ocular hypertension treatment of patients, but also for argon laser IOP levels.
Brimonidine tartrate ophthalmic solution has a dual mechanism of action by reducing aqueous humor production and increasing the pigment layer of liquid scleral outflow therapeutic purposes. After dropping into the eye, the effect is rapid, and it can reach the peak when using up to 2h, and the effective time can maintain 12h. Blood can only detect traces of drugs. This product has first-pass metabolism in the liver, and metabolites excreted in the urine by the kidneys. Systemic absorption and distribution are not affected, and the elderly do not need dose adjustment.
 Brimonidine tartrate ophthalmic solution compared with other α-blockers, the fat-soluble is small, while it does not easy to pass through blood-brain barrier and does not produce sedation, hypotension and other similar clonidine central adverse reactions.
Brimonidine tartrate ophthalmic solution is highly selective for α2-adrenergic receptors, and α2/α1 ratio of receptor affinity is more than 1000 times. The effect of alpha 2 receptors can lead to lower intraocular pressure. And the role of the alpha 1 receptors can lead to vascular contraction, eyelid retraction or reduction and dilation of the pupil. Long term application of this product will not cause rapid desensitization.
In addition, compared with β-blockers, brimonidine tartrate eye drops for minor cardiovascular effects, it has no effect on lung function, so it is suitable for disabled patients β-blockers. Furthermore, when used alone β-blocker, it can not achieve therapeutic purposes, and you can simultaneously increase the FDA.
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Clinical Study

This product can reduce intraocular pressure in glaucoma patients, only mild cardiovascular impact. Clinical trials showed that the drug with a 0.5% timolol considerable effect. Two drugs used alone, 2 times a day, one drop every time, the mean decrease in intraocular pressure and reach a peak, respectively: 0.79~1.01 kPa, 0.5% timolol is 0.8~0.88kPa. After the treatment of 12h, the mean decrease in intraocular pressure were: 0.49~0.67kPa and 0.79~0.88kPa.
Brimonidine tartrate ophthalmic solution is recommended for using three times a day program, and some clinical trials showed that 2 times a day, 3 times a day with no difference in efficacy.

Adverse reactions

10% to 30% of people may feel dry mouth, fatigue, ocular hyperemia, burning and tingling, headache, blurred vision, foreign body sensation in the eye, conjunctival follicles, ocular allergic reactions and eye pruritus .
There are 3%~9% of the patients had corneal staining (or ulcer, photophobia, eyelid erythema, eye soreness or pain, dry tears, eyelid edema, conjunctival edema, dizziness, blepharitis, eye irritation, conjunctiva, vision abnormalities, symptoms of upper respiratory tract, gastrointestinal symptoms, weakness, and muscle pain.
Less than 3% of the patients with excision of the eyelid, conjunctival hemorrhage, abnormal taste, conjunctival secretions increase, bazoo, depression, insomnia, anxiety, high blood pressure, heart palpitations and syncope.

Precautions

Patients with highly allergic to tartaric acid bromine brimonidine or clonidine class and are taking monoamine oxidase inhibitors in patients with the drug contraindicated. Patients with severe cardiovascular disease and impaired liver and kidney function should be used with caution. Depression, lack of cerebral or coronary insufficiency, Raynaud's phenomenon, orthostatic hypotension, thrombosis obliterans should use it very carefully. Brimonidine tartrate can cause fatigue in some patients and (or) fatigue, patients should be reminded that the FDA engaged in dangerous operations the possibility of mental concentration decline appears. Three times a day, 1 drop of two eyes. Sleep and reactive power decreased in children aged 7 to 2 years. Not recommended for children under 2 years of age.

Description

Brimonidine is an agonist of α₂-adrenergic receptors (α₂-ARs; K_is = 2.7, 52, and 44 nM for α_2A, α_2B, and α_2C-ARs, respectively, in CHO cells). It is selective for α₂-ARs over α₁-ARs (K_i = 1,800 nM in human brain). Brimonidine lowers intraocular pressure in DBA/2J mice, a model of glaucoma, to control levels when applied topically to the eye as a 0.1% solution. It also inhibits glutamate release, prevents upregulation of NMDA receptors containing NR1 and NR2A subunits, and protects rat retinal ganglion cells against glutamate excitotoxicity in a rat model of retinal ischemia when administered at a dose of 1 mg/kg per day. Formulations containing brimonidine have been used in the treatment of open-angle glaucoma and ocular hypertension.

Chemical Properties

Off-White Crystalline Solid

Uses

It is an a 2 receptor agonist. It is a drug used to treat glaucoma. It acts via decreasing aqueous humor synthesis

Uses

Antitussive

Uses

Used to treat open-angle glaucoma or ocular hypertension

Uses

It is an α2 receptor agonist. It is a drug used to treat glaucoma.

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