Dorzolamide

From Wikipedia, the free encyclopedia
Jump to: navigation, search
Dorzolamide
Dorzolamide.svg
Dorzolamide-3D-balls.png
Systematic (IUPAC) name
(4S,6S)-4-(ethylamino)-6-methyl-7,7-dioxo-5,6-dihydro-4H-thieno[2,3-b]thiopyran-2-sulfonamide
Clinical data
Trade names Trusopt
AHFS/Drugs.com Monograph
MedlinePlus a602022
Pregnancy
category
  • US: C (Risk not ruled out)
Routes of
administration
Topical (eye drops)
Legal status
Legal status
Pharmacokinetic data
Protein binding ~33%
Biological half-life 4 months
Identifiers
CAS Number 130693-82-2 N 120279-96-1
ATC code S01EC03 (WHO)
PubChem CID 5284549
IUPHAR/BPS 6810
DrugBank DB00869 YesY
ChemSpider 4447604 YesY
UNII 9JDX055TW1 YesY
KEGG D07871 N
ChEBI CHEBI:4702 YesY
ChEMBL CHEMBL218490 YesY
Chemical data
Formula C10H16N2O4S3
Molar mass 324.443 g/mol
 NYesY (what is this?)  (verify)

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]

History[edit]

This drug, developed by Merck, was the first drug in human therapy (market introduction 1995) which 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 increased 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. 

Further reading[edit]