Dorzolamide
Dorzolamide.svg
Dorzolamide-3D-balls.png
Names
Trade namesTrusopt, others
  • (4S,6S)-4-(ethylamino)-6-methyl-7,7-dioxo-5,6-dihydro-4H-thieno[2,3-b]thiopyran-2-sulfonamide
Clinical data
Pregnancy
category
  • US: C (Risk not ruled out)
Routes of
use		Topical (eye drops)
Defined daily dose0.3 ml[1]
External links
AHFS/Drugs.comMonograph
MedlinePlusa602022
Legal
Legal status
Pharmacokinetics
Protein binding~33%
Elimination half-life4 months
Chemical and physical data
FormulaC10H16N2O4S3
Molar mass324.43 g·mol−1
3D model (JSmol)
  • CCNC1CC(C)S(=O)(=O)c2sc(cc12)S(=O)(=O)N
  • InChI=1S/C10H16N2O4S3/c1-3-12-8-4-6(2)18(13,14)10-7(8)5-9(17-10)19(11,15)16/h5-6,8,12H,3-4H2,1-2H3,(H2,11,15,16)/t6-,8-/m0/s1 checkY
  • Key:IAVUPMFITXYVAF-XPUUQOCRSA-N checkY

Dorzolamide, sold under the brand name Trusopt among others, is medications used to treat high pressure inside the eye including glaucoma.[2] It is used as an eye drop.[2] Effects begin within three hours and lasts for at least eight hours.[2] It is also available as the combination dorzolamide/timolol.[2]

Common side effects include eye discomfort, eye redness, taste changes, and blurry vision.[2] Serious side effects include Steven Johnson syndrome.[2] Those allergic to sulfonamides may be allergic to dorzolamide.[2][3] Use is not recommended in pregnancy or breastfeeding.[3] It is a carbonic anhydrase inhibitor and works by decreasing the production of aqueous humour.[2]

Dorzolamide was approved for medical use in the United States in 1994.[2] It is available as a generic medication.[3] A 5 milliliter bottle in the United Kingdom costs the NHS less than £2 as of 2019.[3] In the United States the wholesale cost of this amount is about US$7.10.[4] In 2017, it was the 281st most commonly prescribed medication in the United States, with more than one million prescriptions.[5][6]

Medical uses[edit | edit source]

Dorzolamide hydrochloride is used to lower excessive intraocular pressure in open-angle glaucoma and ocular hypertension.

Dosage[edit | edit source]

The defined daily dose is 0.3 ml.[1]

Side effects[edit | edit source]

(A) Bilateral eczematous swelling around the eyes after use of dorzolamide eyedrops. (B) Improved periorbital swelling after stopping.

Ocular stinging, burning, itching and bitter taste.[7] It causes shallowing of the anterior chamber and leads to transient myopia.

Pharmacodynamics[edit | edit source]

It lowers IOP by about 20%.[7] Carbonic Anhydrase can convert H2CO3 into HCO3 (bicarbonate) and H+. The H+ is then exchanged for sodium (Na) which allows you to make aqueous humor. By blocking carbonic anhydrase, the Na/H exchanger can't work, which will decrease Na in the cell and prevent aqueous humor production.

History[edit | edit source]

This drug, developed by Merck, was the first drug 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.[7]

Society and culture[edit | edit source]

Cost[edit | edit source]

A 5 milliliter bottle in the United Kingdom costs the NHS less than £2 as of 2019.[3] In the United States the wholesale cost of this amount is about US$7.10.[4] In 2017, it was the 281st most commonly prescribed medication in the United States, with more than one million prescriptions.[5][6]

References[edit | edit source]

  1. ↑ 1.0 1.1 "WHOCC - ATC/DDD Index". www.whocc.no. Archived from the original on 24 August 2019. Retrieved 9 September 2020.
  2. ↑ 2.0 2.1 2.2 2.3 2.4 2.5 2.6 2.7 2.8 "Dorzolamide Hydrochloride Monograph for Professionals". Drugs.com. American Society of Health-System Pharmacists. Archived from the original on 27 March 2019. Retrieved 26 March 2019.
  3. ↑ 3.0 3.1 3.2 3.3 3.4 British national formulary : BNF 76 (76 ed.). Pharmaceutical Press. 2018. p. 1148. ISBN 9780857113382.
  4. ↑ 4.0 4.1 "NADAC as of 2019-02-27". Centers for Medicare and Medicaid Services. Archived from the original on 2019-03-06. Retrieved 3 March 2019.
  5. ↑ 5.0 5.1 "The Top 300 of 2020". ClinCalc. Archived from the original on 12 February 2021. Retrieved 11 April 2020.
  6. ↑ 6.0 6.1 "Dorzolamide Hydrochloride - Drug Usage Statistics". ClinCalc. Archived from the original on 23 May 2020. Retrieved 11 April 2020.
  7. ↑ 7.0 7.1 7.2 KD Tripari MD. Essentials of Medical Pharmacology (5th ed.). Jaypee Brothers Medical Publishers(P) Ltd. p. 88. ISBN 81-8061-187-6.

Further reading[edit | edit source]

== External links ==

Identifiers: