Description
Dorzolamide hydrochloride was introduced in the U.S.A. as eye drops
for the treatment of open-angle glaucoma and ocular hypertension. Dorzolamide is a
potent carbonic anhydrase inhibitor that, on topical administration, lowers intraocular
pressure (IOP). In a clinical study in patients with bilateral primary open-angle
glaucoma or ocular hypertension, dorzolamide (0.7-2%) was found to significantly lower
IOP throughout the day. Dorzolamide has been shown to be effective as a single
therapy or in combination with β-blockers.
Chemical Properties
White Powder
Originator
Merck (U.S.A.)
Uses
An inhibitor of carbonic anhydrase.
Uses
Antiglaucoma drug;Carbonic anhydrase inhibitor
Uses
Carbonic anhydrase inhibitor. Antiglaucoma agent.
Uses
Dorzolamide HCl Ophthalmic Solution is indicated in the treatment of elevated intraocular pressure in patients with ocular hypertension or open-angle glaucoma.
Definition
ChEBI: The hydrochloride salt of dorzolamide. It is used in ophthalmic solutions to lower increased intraocular pressure in the treatment of open-angle glaucoma and ocular hypertension.
Manufacturing Process
Manufacturing process for Dorzolamide hydrochloride includes these steps as follows: Step A: Sulfuric Acid Ritter Procedure;Step B: Sulfonylation Procedure Step C: Chlorosulfonylation Procedure;Step D: Amidation Procedure;Step E: Reduction via Borane Generated in situ Procedure;Step F: Maleate Salt Formation Procedure;Step G: Crude Hydrochloride Salt Formation;Step H: Recrystallization Procedure.
Brand name
Trusopt (Merck).
Therapeutic Function
Antiglaucoma
Veterinary Drugs and Treatments
Dorzolamide is often used in the contralateral eye of a dog with
primary glaucoma to prevent development of bilateral disease. It
is also an excellent agent to consider for most secondary glaucomas
in dogs and cats because it has no effect on pupil size. Like the
related oral carbonic anhydrase inhibitors (dichlorphenamide or
Daranide?, methazolamide or Neptazane?), dorzolamide decreases
aqueous humor production by the ciliary body epithelium by altering
pH and affecting the H+/Na+ active transport exchange mechanism.
Oral carbonic anhydrase inhibitors cause numerous systemic
side effects such as metabolic acidosis and panting, diarrhea, vomiting,
anorexia and others, all of which can be avoided with topical
carbonic anhydrase inhibitors.
References
[1] Patent: US2003/220509, 2003, A1. Location in patent: Page/Page column 12
[2] Patent: US2004/198805, 2004, A1. Location in patent: Page/Page column 1; 2
