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QuickView for Brimonidine (compound)

Summary
General Info

PubChem

PubChem Compound 11236066

PubChem Compound 11236066

Name:	brimonidine
PubChem Compound ID:	11236066
Molecular formula:	C₁₅H₁₆BrN₅O₆
Molecular weight:	442.222 g/mol

DrugBank

Identification

Name:	brimonidine
Name (isomeric):	DB00484
Drug Type:	small molecule
Synonyms:	Brimonidine tartrate; Bromoxidine
Brand:	Alphagan, Alphagan P
Category:	Adrenergic alpha-Agonists, Antihypertensive Agents, EENT Drugs
CAS number:	59803-98-4

Pharmacology

Indication:	For the lowering of intraocular pressure in patients with open-angle glaucoma or ocular hypertension.
Pharmacology:	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.
Biotransformation:	Metabolized primarily by the liver.
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
Toxicity:	Oral LD₅₀ is 50 mg/kg in mice and 100 mg/kg in rats.
Affected organisms:	Humans and other mammals

Interactions

Drug interaction:

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.
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.
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.
Droperidol	Droperidol may enhance the CNS depressant effect of brimonidine. Consider therapy modification.
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.

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.
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.
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.
Droperidol	Droperidol may enhance the CNS depressant effect of brimonidine. Consider therapy modification.
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.
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.
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.
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.
Treprostinil	Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Methotrimeprazine	Brimonidine may enhance the CNS depressant effect of Methotrimeprazine. Methotrimeprazine may enhance the CNS depressant effect of brimonidine. Consider therapy modification.
Tranylcypromine	The MAO inhibitor, Tranylcypromine, may increase the vasopressor effect of the alpha2-agonist, Brimonidine. Concomitant therapy is contraindicated.

Targets

Alpha-2A adrenergic receptor

Alpha-2B adrenergic receptor

Alpha-2C adrenergic receptor

Enzymes

Aldehyde oxidase