Drug intelligence / Profile preview

dorzolamide + timolol

Development stage
Approved
Lead developer
Merck
Modality
Small Molecules
Administration
Ophthalmic
01

Overview

Dorzolamide + timolol is a fixed-dose combination of two active pharmaceutical ingredients, dorzolamide hydrochloride (a carbonic anhydrase inhibitor) and timolol maleate (a non-selective beta-adrenergic receptor blocker), formulated as an ophthalmic solution. It is used to reduce elevated intraocular pressure in patients with open-angle glaucoma or ocular hypertension who are insufficiently responsive to beta-blockers alone. Dorzolamide decreases aqueous humor secretion by inhibiting carbonic anhydrase II in the ciliary processes, reducing bicarbonate ion formation and subsequent fluid transport. Timolol reduces aqueous humor production by blocking beta-adrenergic receptors in the eye. The combination provides additive effects for lowering intraocular pressure, thereby reducing the risk of optic nerve damage and glaucomatous visual field loss[1][2][3][4][5][8].

Brand names
CosoptCosopt PFCosopt OcumeterCosopt Ocumeter Plus
Other names
dorzolamide/timolol ophthalmic solutiondorzolamide hydrochloride and timolol maleate ophthalmic solution
02

Targets

CA1 (Carbonic anhydrase 1)ADRB2 (β2)ADRB1 (β1)CA2 (Carbonic Anhydrase 2)

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