title: Two topical carbonic anhydrase inhibitors sezolamide and dorzolamide in Gelrite vehicle: a multiple-dose efficacy study.
abstract: The ocular hypotensive activities of the two potent topical carbonic anhydrase inhibitors sezolamide (previously known as MK-417) and dorzolamide (previously known as MK-507 and L-671,152) were compared formulated in Gelrite vehicle, a novel ophthalmic drug delivery system. This was a four-center, double-blind, randomized, placebo-controlled, parallel study in 73 patients with a diagnosis of bilateral primary open-angle glaucoma or ocular hypertension and a morning intraocular pressure (IOP) of greater than 23 mmHg in both eyes following washout of ocular hypotensive medications. Parallel 12-h modified diurnal curves were performed prestudy and on day 6, with a 4-h IOP curve on day 1. On day 6 the peak mean percentage decrease in IOP from baseline occurred 4 h after the dose of dorzolamide (22.1%) and 6 h after the dose of sezolamide (21.3%). There were no significant differences between 2% dorzolamide and 1.8% sezolamide at any time point, although the decrease in IOP for sezolamide tended to be slightly greater than that for dorzolamide. Duration of action of both compounds was, at most, slightly prolonged by the use of Gelrite vehicle when compared with former studies on sezolamide and dorzolamide.
authors.affiliation: Glaucoma Center, Academic Medical Center, Amsterdam, The Netherlands.
authors.forename: F P
authors.initials: FP
authors.lastname: Gunning
authors.forename: E L
authors.initials: EL
authors.lastname: Greve
authors.forename: A M
authors.initials: AM
authors.lastname: Bron
authors.forename: J M
authors.initials: JM
authors.lastname: Bosc
authors.forename: J G
authors.initials: JG
authors.lastname: Royer
authors.forename: J L
authors.initials: JL
authors.lastname: George
authors.forename: P
authors.initials: P
authors.lastname: Lesure
authors.forename: D
authors.initials: D
authors.lastname: Sirbat
mesh_terms: D000328:Adult; D000368:Aged; D000369:Aged, 80 and over; D002257:Carbonic Anhydrase Inhibitors / Q000627:therapeutic use*; D004311:Double-Blind Method; D016503:Drug Delivery Systems; D005260:Female; D005902:Glaucoma, Open-Angle / Q000188:drug therapy*; D006801:Humans; D008297:Male; D008875:Middle Aged; D009798:Ocular Hypertension / Q000188:drug therapy*; D009883:Ophthalmic Solutions; D011135:Polysaccharides, Bacterial; D013449:Sulfonamides / Q000627:therapeutic use*; D013876:Thiophenes / Q000627:therapeutic use*
chemical_list: D002257:Carbonic Anhydrase Inhibitors; D009883:Ophthalmic Solutions; D011135:Polysaccharides, Bacterial; D013449:Sulfonamides; D013876:Thiophenes; C048288:gellan gum; C062765:dorzolamide; C057921:sezolamide