title: [MK-507 (L-671 152): local tolerance and effectiveness of a new local carbonic anhydrase inhibitor in healthy probands].
abstract: A three-dose, randomized, double-blind parallel, placebo-controlled ocular tolerancy study was undertaken in 24 healthy, normal volunteers with two formulations of 2% MK-507 (L-671 152), a novel water-soluble, topical carbonic anhydrase inhibitor. In this study MK-507 was administered to humans for the first time. Subjects received 3 sequential drops of the test drug in one randomly selected eye (at 13:00, 14:00, and 14:10 o'clock): ten received 2% MK-507 formulated with 0.5% hydroxyethylcellulose (HEC); ten, 2% MK-507 with no HEC; two, vehicle with HEC; and two, vehicle without HEC. Local tolerance of 2% MK-507 was good with predominantly mild and transient local symptoms, somewhat fewer for the formulation without HEC. Significant lowering of intraocular pressure (IOP) by up to 7 mmHg was noted when comparing IOP 4 h and 5 h after the first dose with IOP 20 h and 19 h before the first dose in the treated eyes of subjects receiving MK-507. Slightly greater activity was noted when MK-507 was formulated with HEC.
authors.affiliation: Augenklinik und Poliklinik, Klinikum rechts der Isar, Technischen Universität, München, Bundesrepublik Deutschland.
authors.forename: H M
authors.initials: HM
authors.lastname: Hofmann
authors.forename: B
authors.initials: B
authors.lastname: Feicht
authors.forename: E
authors.initials: E
authors.lastname: Brunner-Ferber
authors.forename: E
authors.initials: E
authors.lastname: Lippa
authors.forename: H
authors.initials: H
authors.lastname: von Denffer
mesh_terms: D000328:Adult; D000959:Antihypertensive Agents / Q000633:toxicity*; D002257:Carbonic Anhydrase Inhibitors / Q000633:toxicity*; D002482:Cellulose / Q000031:analogs & derivatives / Q000633:toxicity; D004311:Double-Blind Method; D006801:Humans; D008297:Male; D009883:Ophthalmic Solutions; D013449:Sulfonamides / Q000633:toxicity*; D013876:Thiophenes / Q000633:toxicity*
chemical_list: D000959:Antihypertensive Agents; D002257:Carbonic Anhydrase Inhibitors; D009883:Ophthalmic Solutions; D013449:Sulfonamides; D013876:Thiophenes; D002482:Cellulose; C002283:hydroxyethylcellulose; C062765:dorzolamide
vernacular_title: MK-507 (L-671 152): lokale Verträglichkeit und Wirksamkeit eines neuen lokalen Karboanhydrasehemmers bei gesunden Probanden.