Dorzolamide

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Dorzolamide
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Clinical data
Trade namesTrusopt, others
AHFS/Drugs.comMonograph
MedlinePlusa602022
Routes of
administration		eye drops
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Legal status
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Pharmacokinetic data
Protein binding~33%
Elimination half-life4 months
Identifiers
  • (4S,6S)-4-(ethylamino)-6-methyl-5,6-dihydro-4H-7λ6-thieno[2,3-b]thiopyran-2-sulfonamide-7,7-dioxide
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Chemical and physical data
FormulaC10H16N2O4S3
Molar mass324.43 g·mol−1
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  • CCNC1CC(C)S(=O)(=O)c2sc(cc12)S(=O)(=O)N
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Data page
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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.[3] It is used as an eye drop.[3] Effects begin within three hours and last for at least eight hours.[3] It is also available as the combination dorzolamide/timolol.[3][4]

Common side effects include eye discomfort, eye redness, taste changes, and blurry vision.[3] Serious side effects include Steven Johnson syndrome.[3] Those allergic to sulfonamides may be allergic to dorzolamide.[3][5] Use is not recommended in pregnancy or breastfeeding.[5] It is a carbonic anhydrase inhibitor and works by decreasing the production of aqueous humor.[3]

Dorzolamide was approved for medical use in the United States in 1994.[3] It is available as a generic medication.[5] In 2023, it was the 190th most commonly prescribed medication in the United States, with more than 2 million prescriptions.[6][7]

Medical uses

Dorzolamide is used to lower excessive intraocular pressure in open-angle glaucoma and ocular hypertension.[3] 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.[8] 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.

Pharmacology

Pharmacodynamics

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Dorzolamide lowers intraocular pressure by about 20%.[8] Normally, carbonic anhydrase converts carbonic acid (Page Module:Chem2/styles.css has no content.H2CO3) into bicarbonate (Page Module:Chem2/styles.css has no content.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]. 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].

Dorzolamide is a highly specific inhibitor of carbonic anhydrase II, which is an isoenzyme of carbonic anhydrase. Dorzolamide displays a 4000-fold higher affinity for carbonic anhydrase II than carbonic anhydrase I.[9]

Pharmacokinetics

When applied topically, dorzolamide enters systemic circulation. As a result, dorzolamide can inhibit carbonic anhydrase found in various parts of the body. During chronic dosing, the drug accumulates in red blood cells. Dorzolamide also binds moderately (approximately 33%) to plasma proteins. However, plasma concentrations are low, generally below 15 nM. The drug and its metabolite are primarily excreted in urine. After dosing is complete, the drug concentration in the blood decreases nonlinearly.[10]

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.[8]

References

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  1. ^ Page Module:Citation/CS1/styles.css has no content."Prescription medicines: registration of new generic medicines and biosimilar medicines, 2017". Therapeutic Goods Administration (TGA). 21 June 2022. Retrieved 30 March 2024.
  2. ^ Page Module:Citation/CS1/styles.css has no content."Product monograph brand safety updates". Health Canada. February 2024. Retrieved 24 March 2024.
  3. ^ a b c d e f g h i j Page Module:Citation/CS1/styles.css has no content."Dorzolamide Hydrochloride Monograph for Professionals". Drugs.com. American Society of Health-System Pharmacists. Retrieved 26 March 2019.
  4. ^ Page Module:Citation/CS1/styles.css has no content."Dorzolamide (Ophthalmic Route) Description and Brand Names". Mayo Clinic. Retrieved 3 November 2023.
  5. ^ a b c Page Module:Citation/CS1/styles.css has no content.British national formulary : BNF 76 (76 ed.). Pharmaceutical Press. 2018. p. 1148. ISBN 9780857113382.
  6. ^ Page Module:Citation/CS1/styles.css has no content."Top 300 of 2023". ClinCalc. Archived from the original on 12 August 2025. Retrieved 12 August 2025.
  7. ^ Page Module:Citation/CS1/styles.css has no content."Dorzolamide Drug Usage Statistics, United States, 2014 - 2023". ClinCalc. Retrieved 20 August 2025.
  8. ^ a b c Page Module:Citation/CS1/styles.css has no content.KD Tripari MD (2004). Essentials of Medical Pharmacology (5th ed.). Jaypee Brothers Medical Publishers(P) Ltd. p. 88. ISBN 81-8061-187-6.
  9. ^ Page Module:Citation/CS1/styles.css has no content."Dorzolamide". PubChem. Retrieved 28 December 2025.
  10. ^ Page Module:Citation/CS1/styles.css has no content."TRUSOPT (dorzolamide hydrochloride)" (PDF). U.S. FDA. Retrieved 28 December 2025.

Further reading

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