Anti Glaucoma And Anti Ocular Hypertension

970 WordsDec 7, 20164 Pages
Travatan (travoprost) Anti-glaucoma and Anti-ocular hypertension MW1 = 500.56 g mol-1 Molecular Formula1 = C26H35F3O6 IUPAC name: [1R-[[1α (Z), 2β (1E, 3R*), 3α, 5α]]-7-[3,5- Dihydroxy-2-[3-hydroxy-4-[3-(trifluoromethyl)phenoxy]-1- butenyl]cyclopentyl]-5-heptenoic acid, 1-methylethyl ester1 Description Travatan (travoprost) ophthalmic solution contains a highly lipophilic prostaglandin F2a (PGF2a) analog that is approved and indicated as a first-line therapy for managing open-angle glaucoma and lowering intraocular pressure (IOP); the drug is available in 0.004% and 0.0015% formulations.1,2 The isopropyl ester moiety of the prodrug parent compound is hydrolyzed in the cornea by ester hydrolase activity; the travoprost free acid is the biologically active structure that functions as a selective agonist with high potency (EC50 = 4 nM) for the prostaglandin F (FP) receptor.1,2 Topical ocular administration is the approved mechanism of administration with recommended doses of 25µL per affected eye(s) daily.1,2 Mechanism of Action After ester hydrolase catalyzed hydrolysis of travoprost in the cornea, travoprost free acid has been found in the aqueous humor of the anterior cavity of the eye.1,2 The free acid compound binds with high selectivity and affinity (Km = 52 nM) to PGF2a G-protein coupled receptors that are predominantly localized in the longitudinal ciliary muscle as well as the iris sphincter of the eye.1,3 Although the exact mechanism of intraocular pressure
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