dorzolamide

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| tradename = Trusopt, others

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| routes_of_administration = eye drops

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| IUPAC_name = (4S,6S)-4-(ethylamino)-6-methyl-7,7-dioxo-5,6-dihydro-4H-thieno[2,3-b]thiopyran-2-sulfonamide

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Dorzolamide, sold under the brand name Trusopt among others, is a medication used to treat high pressure inside the eye, including in cases of glaucoma. It is used as an eye drop. Effects begin within three hours and last for at least eight hours. It is also available as the combination dorzolamide/timolol.{{Cite web |title=Dorzolamide (Ophthalmic Route) Description and Brand Names |url=https://www.mayoclinic.org/drugs-supplements/dorzolamide-ophthalmic-route/description/drg-20063524 |access-date=3 November 2023 |website=Mayo Clinic }}

Common side effects include eye discomfort, eye redness, taste changes, and blurry vision. Serious side effects include Steven Johnson syndrome. Those allergic to sulfonamides may be allergic to dorzolamide.{{cite book|title=British national formulary : BNF 76|date=2018|publisher=Pharmaceutical Press|isbn=9780857113382|pages=1148|edition=76}} Use is not recommended in pregnancy or breastfeeding. It is a carbonic anhydrase inhibitor and works by decreasing the production of aqueous humor.

Dorzolamide was approved for medical use in the United States in 1994.{{cite web |title=Dorzolamide Hydrochloride Monograph for Professionals |url=https://www.drugs.com/monograph/dorzolamide-hydrochloride.html |website=Drugs.com |publisher=American Society of Health-System Pharmacists |access-date=26 March 2019 }} It is available as a generic medication. In 2022, it was the 201st most commonly prescribed medication in the United States, with more than 2{{nbsp}}million prescriptions.{{cite web | title=The Top 300 of 2022 | url=https://clincalc.com/DrugStats/Top300Drugs.aspx | website=ClinCalc | access-date=30 August 2024 | archive-date=30 August 2024 | archive-url=https://web.archive.org/web/20240830202410/https://clincalc.com/DrugStats/Top300Drugs.aspx | url-status=live }}{{cite web | title = Dorzolamide Drug Usage Statistics, United States, 2013 - 2022 | website = ClinCalc | url = https://clincalc.com/DrugStats/Drugs/Dorzolamide | access-date = 30 August 2024 }}

Medical uses

Dorzolamide is used to lower excessive intraocular pressure in open-angle glaucoma and ocular hypertension. This drug is able to cross the cornea, reach the ciliary body of the eye, and produce systemic effects on the carbonic anhydrase enzyme within the eye.

Side effects

Ocular stinging, burning, itching and bitter taste. It causes shallowing of the anterior chamber and leads to transient myopia. As a second generation carbonic anhydrase inhibitor, dorzolamide avoids systemic effects associated with first generation carbonic anhydrase inhibitors such as acetazolamide, methazolamide, and dichlorphenamide.

Pharmacodynamics

Dorzolamide lowers intraocular pressure by about 20%. Normally, carbonic anhydrase converts carbonic acid ({{chem2|H2CO3}}) into bicarbonate ({{chem2|HCO3}}), releasing a proton (H⁺) into solution. The H⁺ is then exchanged for sodium (Na⁺) ions, which facilitates the production of aqueous humor {{Citation needed|date=June 2022}}. By blocking the function of carbonic anhydrase, the Na⁺/H⁺ exchange is unable to occur, which leads to a decrease in Na⁺ in the cell and prevents aqueous humor production {{Citation needed|date=June 2022}}.

History

Dorzolamide, developed by Merck, was the first medication in human therapy (market introduction 1995) that resulted from structure-based drug design. It was developed to circumvent the systemic side effects of acetazolamide which has to be taken orally.{{cite book|title=Essentials of Medical Pharmacology|publisher=Jaypee Brothers Medical Publishers(P) Ltd.|isbn=81-8061-187-6|page=88|author=KD Tripari MD|year=2004|edition=5th}}

dorzolamide

Medical uses

Side effects

Pharmacodynamics

History

References

Further reading