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Brimonidine tartrate

Brimonidine tartrate structure

CAS No:
70359-46-5
Formula:
C11H10BrN5.C4H6O6
Chemical Name:
Brimonidine tartrate
Synonyms:
6-Quinoxalinamine,5-bromo-N-(4,5-dihydro-1H-imidazol-2-yl)-,(2R,3R)-2,3-dihydroxybutanedioate (1:1);6-Quinoxalinamine,5-bromo-N-(4,5-dihydro-1H-imidazol-2-yl)-,[R-(R*,R*)]-2,3-dihydroxybutanedioate (1:1);Brimonidine tartrate;AGN 190342LF;Brominide tartrate;Alphagan;Alphagan P;Brimonidine Purite;Mirvaso;(5-Bromo-quinoxalin-6-yl)-(4,5-dihydro-1H-imidazol-2-yl)-amine L-tartrate;109826-56-4;79570-19-7
Categories:
Biochemical Engineering > Inhibitors

Description

UK 14,304 is a full α2-adrenergic receptor (α2-AR) agonist.Target: α2-adrenergic Receptor[3H]UK 14,034 is a full agonist at alpha 2-adrenergic receptors. [3H]UK 14,304 labels at least 2 specific binding sites in human brain that both have the characteristics of an alpha 2-adrenergic binding site. GTP decreases agonist binding at both of these sites, but with different potencies at each site [1-3].

Brimonidine Tartrate is the tartrate salt form of brimonidine, an imidazole derivative and a selective alpha-2 adrenergic receptor agonist. Upon ocular administration, brimonidine tartrate acts on the blood vessels causing them to constrict which leads to a decrease in the production of aqueous humor. Brimonidine tartrate also enhances the outflow of aqueous humor. This drug is used in the treatment of glaucoma to reduce intraocular pressure.|A quinoxaline derivative and ADRENERGIC ALHPA-2 RECEPTOR AGONIST that is used to manage INTRAOCULAR PRESSURE associated with OPEN-ANGLE GLAUCOMA and OCULAR HYPERTENSION.

Brimonidine tartrate Basic Attributes

Molecular Weight：

442.22

Exact Mass：

441.028381

EC Number：

1308068-626-2

UNII：

4S9CL2DY2H

NCI Thesaurus Code：

C47419

ATC Code：

S01EC54|D11AX21

HScode：

2933990090

Characteristics

PSA：

177

XLogP3：

-0.52180

Appearance：

Off-white crystalline solid

Melting Point：

207.5 °C

Boiling Point：

432.6°C at 760 mmHg

Flash Point：

215.4ºC

Storage Conditions：

-20°C Freezer

Safety Information

Transport codes：

UN 2811 6.1 / PGIII

safety instructions：

S36/37

Precautionary statement(s)：

Missing Phrase - N15.00950417-P305 + P351 + P338

Hazard Statements：

H301-H315-H319-H335

GHS Classification：

|Danger|H301 (76.92%): Toxic if swallowed [Danger Acute toxicity, oral]|P260, P261, P264, P270, P271, P272, P280, P285, P301+P310, P301+P312, P302+P352, P304+P340, P304+P341, P305+P351+P338, P309+P311, P311, P312, P314, P321, P330, P332+P313, P333+P313, P337+P313, P342+P311, P362, P363, P403+P233, P405, and P501|Aggregated GHS information provided by 13 companies from 7 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.

Drug Information

Drug Indication：

Decrease of elevated intraocular pressure (IOP) in adult patients with open-angle glaucoma or ocular hypertension for whom monotherapy provides insufficient IOP reduction.|Mirvaso is indicated for the symptomatic treatment of facial erythema of rosacea in adult patients.,|Treatment of rosacea|Treatment of glaucoma

MeSH：

Compounds that bind to and activate ADRENERGIC ALPHA-2 RECEPTORS. (See all compounds classified as Adrenergic alpha-2 Receptor Agonists.)|Drugs used in the treatment of acute or chronic vascular HYPERTENSION regardless of pharmacological mechanism. Among the antihypertensive agents are DIURETICS; (especially DIURETICS, THIAZIDE); ADRENERGIC BETA-ANTAGONISTS; ADRENERGIC ALPHA-ANTAGONISTS; ANGIOTENSIN-CONVERTING ENZYME INHIBITORS; CALCIUM CHANNEL BLOCKERS; GANGLIONIC BLOCKERS; and VASODILATOR AGENTS. (See all compounds classified as Antihypertensive Agents.)

MeSH Entry Terms：

5-Bromo-6-(2-imidazolin-2-ylamino)quinoxaline D-tartrate

Brimonidine tartrate Use and Manufacturing

Uses

Used to treat open-angle glaucoma or ocular hypertension

Use Classification：

Human drugs -> Simbrinza -> EMA Drug Category|Ophthalmologicals -> Human pharmacotherapeutic group|Human drugs -> Mirvaso -> EMA Drug Category|Other dermatological preparations -> Human pharmacotherapeutic group|Human Drugs -> EU pediatric investigation plans|Human Drugs -> FDA Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book) -> Active Ingredients

Computed Properties

Molecular Weight:442.22
Hydrogen Bond Donor Count:6
Hydrogen Bond Acceptor Count:9
Rotatable Bond Count:5
Exact Mass:441.02840
Monoisotopic Mass:441.02840
Topological Polar Surface Area:177
Heavy Atom Count:27
Complexity:442
Defined Atom Stereocenter Count:2
Covalently-Bonded Unit Count:2
Compound Is Canonicalized:Yes

Drug Function and Efficacy

Brimonidine tartrate is an α-adrenergic receptor agonist with a dual mechanism of action: it reduces aqueous humor production and increases uveoscleral outflow, lowering intraocular pressure with minimal effects on cardiovascular and pulmonary function.

This ingredient has been used in drugs with the following functions (note: it does not mean that the ingredient itself has the following health functions)

Related Drugs

Brimonidine tartrate eye drops
Ingredients	The main ingredient of this product is brimonidine tartrate. Each milliliter contains: 2 mg of brimonidine tartrate, 0.05 mg of benzalkonium chloride, 14 mg of polyvinyl alcohol, 7.0 mg of sodium chloride, 4.5 mg of sodium citrate, 0.5 mg of citric acid and pure water.
Indication	Although no specific studies have been conducted on drug interactions with this product, the possibility of additive or enhanced effects with central nervous system depressants (alcohol, barbiturates, opiates, sedatives or anesthetics) should be considered. Clinical studies have not found that this product has a significant effect on pulse or blood pressure, but α-receptor agonists may also slow the pulse or lower blood pressure. Therefore, caution should also be exercised when using β-blockers (topical or systemic), antihypertensive drugs and/or cardiac glycosides at the same time. The literature reports that tricyclic antidepressants can weaken the antihypertensive effect of systemic clonidine. It is not clear whether the simultaneous use of such drugs will interfere with the intraocular pressure-lowering effect of this product. Does the instillation of this product affect the circulating catecholamines?
Specifications	0.15%

Brimonidine tartrate
Specifications	————
Manufacturer	Lunan BETTER Pharmaceutical Co., Ltd.

Brimonidine tartrate
Manufacturer	Changzhou Yabang Pharmaceutical Co., Ltd.

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Registered Holders

MAITHRI DRUGS PRIVATE LTD

United States
Active
MICRO LABS LTD

United States
Active
CENTAUR PHARMACEUTICALS PVT LTD

United States
Active

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