Dorzolamide

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Image:Dorzolamide-2D-skeletal.png
Image:Dorzolamide-3D-balls.png
Dorzolamide
Systematic (IUPAC) name
2-ethylamino-4-methyl-5, 5-dioxo-5$l^{6}, 7-dithiabicyclo[4.3.0] nona-8,10- diene-8-sulfonamide
Identifiers
CAS number 130693-82-2
120279-96-1
ATC code S01EC03
PubChem 3154
DrugBank APRD00577
Chemical data
Formula C10H16N2O4S3 
Mol. mass 324.443 g/mol
Pharmacokinetic data
Bioavailability  ?
Protein binding ~33%
Metabolism  ?
Half life 4 months
Excretion  ?
Therapeutic considerations
Pregnancy cat.

?

Legal status
Routes  ?

Dorzolamide is a carbonic anhydrase inhibitor. It is an anti-glaucoma agent and topically applied in the form of eye drops. This drug was the first drug in human therapy (market introduction 1995) which resulted from structure-based drug design.

Trusopt (dorzolamide hydrochloride ophthalmic solution) is a carbonic anhydrase inhibitor formulated for topical ophthalmic use. Trusopt is used to lower increased intraocular pressure in open-angle glaucoma and ocular hypertension.

References

  • Kubinyi H (1999). "Chance favors the prepared mind--from serendipity to rational drug design". J Recept Signal Transduct Res 19 (1-4): 15-39. PMID 10071748.
  • Plummer C, MacKay E, Gelatt K. "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. 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. 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. PMID 16470316.

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