Dorzolamide

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Dorzolamide
Dorzolamide.svg
Dorzolamide-3D-balls.png
Clinical data
Trade namesTrusopt
AHFS/Drugs.comMonograph
MedlinePlusa602022
Pregnancy
category
  • US: C (Risk not ruled out)
Routes of
administration
Topical (eye drops)
ATC code
Legal status
Legal status
Pharmacokinetic data
Protein binding~33%
Elimination half-life4 months
Identifiers
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
Chemical and physical data
FormulaC10H16N2O4S3
Molar mass324.443 g/mol g·mol−1
3D model (JSmol)
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Dorzolamide (trade name Trusopt) is a carbonic anhydrase inhibitor. It is an anti-glaucoma agent, and acts by decreasing the production of aqueous humour.[1] It is administered as a topical ophthalmic in the form of a 2% solution.[2]

In 2016 it was the 271st most prescribed medication in the United States with more than a million prescriptions.[3]

History[edit]

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.[2]

Uses[edit]

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

Pharmacodynamics[edit]

It lowers IOP by about 20%.[2]

Side effects[edit]

Ocular stinging, burning, itching and bitter taste.[2] It causes shallowing of the anterior chamber and leads to transient myopia.

References[edit]

  1. ^ Dorzolamide at Drugs.com. Revised: 12/2011
  2. ^ a b c d KD Tripari MD. Essentials of Medical Pharmacology (5th ed.). Jaypee Brothers Medical Publishers(P) Ltd. p. 88. ISBN 81-8061-187-6.
  3. ^ "The Top 300 of 2019". clincalc.com. Retrieved 22 December 2018.

Further reading[edit]