Dorzolamide

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Dorzolamide
Systematic (IUPAC) name
(4S,6S)-2-ethylamino-4-methyl-5,5-dioxo-
6,7-dithiabicyclo[4.3.0]nona-8,10-diene-8-sulfonamide
Clinical data
Trade namesTrusopt
AHFS/Drugs.commonograph
MedlinePlusa602022
Pregnancy cat.C (US)
Legal status-only (US)
RoutesTopical (eye drops)
Pharmacokinetic data
Protein binding~33%
Half-life4 months
Identifiers
CAS number130693-82-2 N 120279-96-1
ATC codeS01EC03
PubChemCID 5284549
DrugBankDB00869
ChemSpider4447604 YesY
UNII9JDX055TW1 YesY
KEGGD07871 N
ChEBICHEBI:4702 YesY
ChEMBLCHEMBL218490 YesY
Chemical data
FormulaC10H16N2O4S3 
Mol. mass324.443 g/mol
 N (what is this?)  (verify)
 
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Dorzolamide
Systematic (IUPAC) name
(4S,6S)-2-ethylamino-4-methyl-5,5-dioxo-
6,7-dithiabicyclo[4.3.0]nona-8,10-diene-8-sulfonamide
Clinical data
Trade namesTrusopt
AHFS/Drugs.commonograph
MedlinePlusa602022
Pregnancy cat.C (US)
Legal status-only (US)
RoutesTopical (eye drops)
Pharmacokinetic data
Protein binding~33%
Half-life4 months
Identifiers
CAS number130693-82-2 N 120279-96-1
ATC codeS01EC03
PubChemCID 5284549
DrugBankDB00869
ChemSpider4447604 YesY
UNII9JDX055TW1 YesY
KEGGD07871 N
ChEBICHEBI:4702 YesY
ChEMBLCHEMBL218490 YesY
Chemical data
FormulaC10H16N2O4S3 
Mol. mass324.443 g/mol
 N (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 optically applied in the form of a 2% eye drops.[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, The combination of dorzolamide with timolol is marketed under the trade name Cosopt.

References[edit]

  1. ^ Dorzolamide at Drugs.com. Revised: 12/2011
  2. ^ a b c d KD Tripari MD. Essentials of Medical Pharmacology (5 ed.). Jaypee Brothers Medical Publishers(P) Ltd. p. 88. ISBN 81-8061-187-6. 

Further reading[edit]