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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 names Trusopt
AHFS/Drugs.com monograph
MedlinePlus a602022
Pregnancy cat. C (US)
Legal status -only (US)
Routes Topical (eye drops)
Pharmacokinetic data
Protein binding ~33%
Half-life 4 months
Identifiers
CAS number 130693-82-2 N 120279-96-1
ATC code S01EC03
PubChem CID 5284549
DrugBank DB00869
ChemSpider 4447604 YesY
UNII 9JDX055TW1 YesY
KEGG D07871 N
ChEBI CHEBI:4702 YesY
ChEMBL CHEMBL218490 YesY
Chemical data
Formula C10H16N2O4S3 
Mol. mass 324.443 g/mol
SMILES eMolecules & PubChem
 N (what is this?)  (verify)

Dorzolamide (trade name Trusopt) is a carbonic anhydrase inhibitor. It is an anti-glaucoma agent by decreasing the production of aqueous humour.[1] It is optically applied in the form of eye drops. This drug, developed by Merck, was the first drug in human therapy (market introduction 1995) which resulted from structure-based drug design. Dorzolamide hydrochloride is used to lower increased intraocular pressure in open-angle glaucoma and ocular hypertension.

The combination of dorzolamide with timolol is marketed under the trade name Cosopt.

[edit] External links

[edit] References

  1. ^ Dorzolamide at Drugs.com. Revised: 12/2011

[edit] Further reading

  • Kubinyi H (1999). "Chance favors the prepared mind--from serendipity to rational drug design". J Recept Signal Transduct Res 19 (1–4): 15–39. doi:10.3109/10799899909036635. PMID 10071748. 
  • Plummer C, MacKay E, Gelatt K (2006). "Comparison of the effects of topical administration of a fixed combination of dorzolamide-timolol to monotherapy with timolol or dorzolamide on IOP, pupil size, and heart rate in glaucomatous dogs". Vet Ophthalmol 9 (4): 245–9. doi:10.1111/j.1463-5224.2006.00469.x. PMID 16771760. 
  • Grover S, Apushkin M, Fishman G (2006). "Topical dorzolamide for the treatment of cystoid macular edema in patients with retinitis pigmentosa". Am J Ophthalmol 141 (5): 850–8. doi:10.1016/j.ajo.2005.12.030. PMID 16546110. 
  • Almeida G, Faria e Souza S (2006). "Effect of topical dorzolamide on rabbit central corneal thickness". Braz J Med Biol Res 39 (2): 277–81. doi:10.1590/S0100-879X2006000200015. PMID 16470316. 


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