药品详细

Brimonidine(溴莫尼定)

基本信息
剂型规格
适应症
药理
临床
理化性质
相互作用
文档
专利
Pathway
文献
序列

化学结构式图

中文名

溴莫尼定

英文名

Brimonidine

分子式

C₁₁H₁₀BrN₅

化学名

5-bromo-N-(4,5-dihydro-1H-imidazol-2-yl)quinoxalin-6-amine

分子量

Average: 292.135
Monoisotopic: 291.011957992

CAS号

59803-98-4

ATC分类

S01E 抗青光眼制剂及缩瞳药

药物类型

small molecule

阶段

approved

商品名

同义名

基本介绍

Brimonidine is a drug used to treat glaucoma. It acts via decreasing aqueous humor synthesis. [Wikipedia]

生产厂家

Akorn inc
Alcon inc
Alcon research ltd
Allergan
Allergan inc
Allergan, Inc
Bausch and lomb pharmaceuticals inc
Sandoz canada inc
Teva parenteral medicines inc

封装厂家

参考

Synthesis Reference	Not Available
General Reference	Not Available

剂型

规格

化合物类型

Type	small molecule

Classes

Quinoxalines

Substructures

Imidazolines
Benzene and Derivatives
Aryl Halides
Pyrazines
Imidazoles
Heterocyclic compounds
Guanidines
Aromatic compounds
Carboxamidines
Anilines
Quinoxalines
Halobenzenes

适应症

药理

Indication

For the lowering of intraocular pressure in patients with open-angle glaucoma or ocular hypertension.

Pharmacodynamics

Brimonidine significantly lowers intraocular pressure with minimal effects on cardiovascular and pulmonary parameters. It lowers intraocular pressure by reducing aqueous humor production and increasing uveoscleral outflow.

Mechanism of action

Brimonidine is an alpha adrenergic receptor agonist (primarily alpha-2). It has a peak ocular hypotensive effect occurring at two hours post-dosing. Fluorophotometric studies in animals and humans suggest that Brimonidine has a dual mechanism of action by reducing aqueous humor production and increasing uveoscleral outflow.

Absorption

Minimal systemic absorption occurs after ocular insertion.

Volume of distribution

Not Available

Protein binding

Not Available

Metabolism

Metabolized primarily by the liver.

Important The metabolism module of DrugBank is currently in beta. Questions or suggestions? Please contact us.

Substrate	Enzymes	Product
Brimonidine	Aldehyde oxidase	2-oxobrimonidine	Details
Brimonidine	Aldehyde oxidase	3-oxobrimonidine	Details

Route of elimination

It is metabolized primarily by the liver. Urinary excretion is the major route of elimination of the drug and its metabolites.

Half life

2 hours

Clearance

Not Available

Toxicity

Oral LD₅₀ is 50 mg/kg in mice and 100 mg/kg in rats.

Affected organisms

Humans and other mammals

Pathways

Not Available

理化性质

Properties

State

solid

Experimental Properties

Property	Value	Source
melting point	207.5 °C	Not Available
water solubility	Soluble (1.5 mg/mL)	Not Available
logP	1.7	Not Available

Predicted Properties

Property	Value	Source
water solubility	1.54e-01 g/l	ALOGPS
logP	1.27	ALOGPS
logP	1.37	ChemAxon
logS	-3.3	ALOGPS
pKa (strongest basic)	8.32	ChemAxon
physiological charge	1	ChemAxon
hydrogen acceptor count	5	ChemAxon
hydrogen donor count	2	ChemAxon
polar surface area	62.2	ChemAxon
rotatable bond count	1	ChemAxon
refractivity	68.49	ChemAxon
polarizability	25.74	ChemAxon

药物相互作用

Drug	Interaction
Droperidol	Droperidol may enhance the CNS depressant effect of brimonidine. Consider therapy modification.
Isocarboxazid	MAO Inhibitors like isocarboxazid may enhance the hypertensive effect of Alpha2-Agonists (Ophthalmic). The concomitant use of monoamine oxidase inhibitors and ophthalmic alpha2 agonists is contraindicated.
Linezolid	MAO Inhibitors like linezolid may enhance the hypertensive effect of Alpha2-Agonists (Ophthalmic). The concomitant use of monoamine oxidase inhibitors and ophthalmic alpha2 agonists is contraindicated.
Methotrimeprazine	Brimonidine may enhance the CNS depressant effect of Methotrimeprazine. Methotrimeprazine may enhance the CNS depressant effect of brimonidine. Consider therapy modification.
Moclobemide	MAO Inhibitors like moclobemide may enhance the hypertensive effect of Alpha2-Agonists (Ophthalmic). The concomitant use of monoamine oxidase inhibitors and ophthalmic alpha2 agonists is contraindicated.
Phenelzine	MAO Inhibitors like phenelzine may enhance the hypertensive effect of Alpha2-Agonists (Ophthalmic). The concomitant use of monoamine oxidase inhibitors and ophthalmic alpha2 agonists is contraindicated.
Procarbazine	MAO Inhibitors like procarbazine may enhance the hypertensive effect of Alpha2-Agonists (Ophthalmic). The concomitant use of monoamine oxidase inhibitors and ophthalmic alpha2 agonists is contraindicated.
Rasagiline	MAO Inhibitors like rasagiline may enhance the hypertensive effect of Alpha2-Agonists (Ophthalmic). The concomitant use of monoamine oxidase inhibitors and ophthalmic alpha2 agonists is contraindicated.
Selegiline	MAO Inhibitors like selegiline may enhance the hypertensive effect of Alpha2-Agonists (Ophthalmic). The concomitant use of monoamine oxidase inhibitors and ophthalmic alpha2 agonists is contraindicated.
Tranylcypromine	The MAO inhibitor, Tranylcypromine, may increase the vasopressor effect of the alpha2-agonist, Brimonidine. Concomitant therapy is contraindicated.
Treprostinil	Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.

食物相互作用

Not Available

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