Dorzolamide

From DrugPedia: A Wikipedia for Drug discovery

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	Template:OrganicBox atom Template:OrganicBox atom Template:OrganicBox Template:OrganicBox Template:OrganicBox Template:OrganicBox Template:OrganicBox Template:OrganicBox Template:OrganicBox Template:OrganicBox Template:OrganicBox Template:OrganicBox Template:OrganicBox Template:OrganicBox atom Template:OrganicBox Template:OrganicBox atom Template:OrganicBox Template:OrganicBox Template:OrganicBox atom Template:OrganicBox Template:OrganicBox Template:OrganicBox Template:OrganicBox
Mol. mass	324.443 g/mol
SMILES	eMolecules & PubChem
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. This drug was developed by University of Florida researchers.<ref>University of Florida facts</ref> The primary creator most credited with pioneering this drug was Dr. Thomas H. Maren.<ref>University of Florida News - Dr. Thomas Maren, A Founding Father Of UF’s Medical College And Renowned Basic Scientist, Dies At Summer Home In Maine</ref>

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[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. 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. 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.