Brimonidine
- Atc Codes:S01EA05
- CAS Codes:79570-19-7#59803-98-4
- PHARMGKB ID:79570-19-7#59803-98-4
Table of contents
- Brand Names
- Drug Combinations
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Drug Interactions
- Genes that may be involved
- Nutrition/Nutraceutical Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Austria: Alphagan; Belgium: Alphagan, Brimonidine; Czech Republic: Alphagan, Brimonidin, Luxfen; Denmark: Alphagan, Brimonidintartrat, Brimoratio, Glaudin; Finland: Alphagan, Brimonidin, Glaudin; France: Alphagan, Brimonidine; Germany: Alphagan, Brimonidin; Greece: Alphagan, Benil Eye Drops, Brimodine, Brimonidine, Brimontal, Brinal, Brinidin, Corneax, Glaucoval, Pharmexin; Hungary: Alphagan, Luxfen; Ireland: Alphagan, Brimon; Italy: Alphagan, Brimonidina, Brimostill; Lithuania: Luxfen; Netherlands: Alphagan, Brimonidinetartraat; Poland: Alphagan; Portugal: Alphagan, Bglau, Brimonidina; Romania: Brimonal, Brimonidine, Luxfen; Slovakia: Brimonal, Brimonidin, Luxfen; Spain: Alphagan; Sweden: Alphagan; UK: Alphagan.
North America
Canada: Alphagan, Brimonidine; USA: Alphagan.
Latin America
Argentina: Alphagan, Brimo-Klonal, Brimopress, Oftalmotonil; Brazil: Alphagan, Brimonidina; Mexico: Agglad Ofteno, Alphagan, Briop, Nor-Tenz.
Drug combinations
Brimonidine and Timolol
Chemistry
Brimonidine Tartrate: C~11~H~10~BrN~5~ C~4~H~6~O~6~. Mw: 442.22. (1) 6-Quinoxalinamine, 5-bromo-N-(4,5-dihydro-1H-imidazol-2-yl)-, [S-(R*,R*)]-2,3-dihydroxybutanedioate (1:1); (2) 5-Bromo-6-(2-imidazolin-2-ylamino)quinoxaline D-tartrate (1:1). CAS-79570-19-7; CAS-59803-98-4 (brimonidine)(1991).
Pharmacologic Category
Antiglaucoma Agents; α-Adrenergic Agonists. (ATC-Code: S01EA05).
Mechanism of action
Relatively selective α~2~-adrenergic agonist, structurally and pharmacologically related to apraclonidine and clonidine. Selectivity of brimonidine for the α~2~-receptor may result in a reduced incidence of adverse pulmonary and cardiovascular effects. Following ocular application, brimonidine reduces both elevated and normal intraocular pressure (IOP) in patients with or without glaucoma by decreasing aqueous humor production and increasing uveoscleral outflow.
Therapeutic use
Lowering of IOP in open-angle glaucoma or ocular hypertension.
Pregnancy and lactiation implications
Teratogenic effects not observed in animal studies. There are no adequate studies in pregnant women. Not recommended during lactation.
Unlabeled use
Contraindications
Hypersensitivity to brimonidine tartrate or any component of the formulation. Do not use during or within 14 days of MAO inhibitor therapy.
Warnings and precautions
May cause CNS depression, particularly in young children. Brimonidine is not approved for use in children <2 years. Contraindicated with MAO inhibitors (concurrent use with psychotropics may produce additive sedation). Use with caution in severe cardiovascular disease, hepatic or renal impairment, depression, cerebral or coronary insufficiency, Raynaud’s phenomenon, orthostatic hypotension, or thromboangiitis. Ocular hypersensitivity reactions reported. Possible partial cross-sensitivity between brimonidine and apraclonidine (caution in history of hypersensitivity to apraclonidine). Contains benzalkonium chloride which may be adsorbed by contact lenses.