Dorzolamide, sold under the brand name Trusopt among others, is medications used to treat high pressure inside the eye including glaucoma.[1] It is used as an eye drop.[1] Effects begin within three hours and lasts for at least eight hours.[1] It is also available as the combination dorzolamide/timolol.[1]

Dorzolamide
Dorzolamide.svg
Dorzolamide-3D-balls.png
Clinical data
Trade namesTrusopt, others
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
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC10H16N2O4S3
Molar mass324.443 g/mol g·mol−1
3D model (JSmol)
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Common side effects include eye discomfort, eye redness, taste changes, and blurry vision.[1] Serious side effects include Steven Johnson syndrome.[1] Those allergic to sulfonamides may be allergic to dorzolamide.[1][2] Use is not recommended in pregnancy or breastfeeding.[2] It is a carbonic anhydrase inhibitor and works by decreasing the production of aqueous humour.[1]

Dorzolamide was approved for medical use in the United States in 1994.[1] It is available as a generic medication.[2] A 5 milliliter bottle in the United Kingdom costs the NHS less than 2 £ as of 2019.[2] In the United States the wholesale cost of this amount is about US$7.10.[3] In 2016 it was the 271st most prescribed medication in the United States with more than a million prescriptions.[4]

Medical usesEdit

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

Side effectsEdit

Ocular stinging, burning, itching and bitter taste.[5] It causes shallowing of the anterior chamber and leads to transient myopia.

PharmacodynamicsEdit

It lowers IOP by about 20%.[5]

HistoryEdit

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.[5]

ReferencesEdit

  1. ^ a b c d e f g h i "Dorzolamide Hydrochloride Monograph for Professionals". Drugs.com. American Society of Health-System Pharmacists. Retrieved 26 March 2019.
  2. ^ a b c d British national formulary : BNF 76 (76 ed.). Pharmaceutical Press. 2018. p. 1148. ISBN 9780857113382.
  3. ^ "NADAC as of 2019-02-27". Centers for Medicare and Medicaid Services. Retrieved 3 March 2019.
  4. ^ "The Top 300 of 2019". clincalc.com. Retrieved 22 December 2018.
  5. ^ a b c KD Tripari MD. Essentials of Medical Pharmacology (5th ed.). Jaypee Brothers Medical Publishers(P) Ltd. p. 88. ISBN 81-8061-187-6.

Further readingEdit