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Brimonidine/timolol, sold under the brand name Combigan among others, is a fixed-dose combination medication eye drop used for the treatment of glaucoma. [1] It is a combination of brimonidine (an α 2 adrenergic agonist) and timolol (a β adrenergic blocker).
Brimonidine is an α 2 agonist medication used to treat open-angle glaucoma, ocular hypertension, and rosacea. [4] [5] In rosacea it improves the redness. [5] It is used as eye drops or applied to the skin. [4] [5] It is also available in the fixed-dose combination medication brimonidine/timolol along with timolol maleate. [6]
Timolol is a non-selective beta blocker. [3] Timolol was patented in 1968, and came into medical use in 1978. [7] It is on the World Health Organization's List of Essential Medicines. [8] Timolol is available as a generic medication.
Brinzolamide works by blocking an enzyme called carbonic anhydrase, which produces bicarbonate needed for the production of the aqueous humour, while brimonidine tartrate blocks another enzyme known as adenylate cyclase, which is also involved in the production of the aqueous humour. [4]
While definitive sites of metabolism have not been firmly established, there are several metabolites worthy of note. N-Desethylbrinzolamide is an active metabolite of the parent compound, and thus exhibits carbonic anhydrase inhibitory activity (largely carbonic anhydrase-I, when in the presence of Brinzolamide) and also accumulates in the erythrocytes.
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