title: The Ocular Hypotensive Efficacy of Topical Fasudil, a Rho-Associated Protein Kinase Inhibitor, in Patients With End-Stage Glaucoma.
abstract: To investigate the effects of topical administration of a selective Rho-associated kinase (ROCK) inhibitor, fasudil 0.5% and 1.2% in glaucomatous patients. In this interventional case series study, 4 eyes of 4 patients with unilateral end-stage primary open-angle glaucoma and no light perception vision were assigned to receive topical fasudil 0.5% (in 3 eyes) or 1.2% (in 1 eye) ophthalmic solution twice daily for 8 weeks. At weeks 1, 2, 3, 4, and 8, intraocular pressure (IOP) and adverse events were evaluated. Baseline mean IOP was 53.5 ± 3.4 mm Hg and mean IOP reductions of the last visit were -8.25 ± 1.2 mm Hg at 2 hours and -8.75 ± 2.2 mm Hg at 4 hours. Mean IOP reductions were clinically and statistically significant with 0.5% and 1.2% fasudil and peak effects occurred 2-4 hours after application (P = 0.0002). The largest IOP reductions were produced by 1.2% fasudil (up to -12 mm Hg). Conjunctival hyperemia was found in 1 patient with 1.2% fasudil. Topical administration of fasudil in end-stage primary open-angle glaucoma patients, caused reduction in IOP and was well tolerated. ROCK inhibitors could be considered as a candidate for glaucoma therapy in future.
authors.affiliation: 1Ophthalmic Epidemiology Research Center, Labbafinejad Medical Center, Shahid Beheshti University of Medical Sciences, Tehran, Iran; 2Ophthalmic Research Center, Shahid Beheshti University of Medical Sciences, Tehran, Iran; 3Nanotechnology Research Center, Faculty of Pharmacy, Tehran University of Medical Science, Tehran, Iran; and 4Ocular Tissue Engineering Research Center, Shahid Beheshti University of Medical Sciences, Tehran, Iran.
authors.forename: Mohammad
authors.initials: M
authors.lastname: Pakravan
authors.forename: Afsaneh Naderi
authors.initials: AN
authors.lastname: Beni
authors.forename: Elham
authors.initials: E
authors.lastname: Ghahari
authors.forename: Reyhaneh
authors.initials: R
authors.lastname: Varshochian
authors.forename: Shahin
authors.initials: S
authors.lastname: Yazdani
authors.forename: Hamed
authors.initials: H
authors.lastname: Esfandiari
authors.forename: Hamid
authors.initials: H
authors.lastname: Ahmadieh
mesh_terms: D019307:1-(5-Isoquinolinesulfonyl)-2-Methylpiperazine / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000627:therapeutic use; D060433:Administration, Ophthalmic; D000368:Aged; D003228:Conjunctiva / Q000098:blood supply / Q000187:drug effects; D004311:Double-Blind Method; D005260:Female; D005902:Glaucoma, Open-Angle / Q000188:drug therapy*; D006801:Humans; D006940:Hyperemia / Q000139:chemically induced; D007429:Intraocular Pressure / Q000187:drug effects*; D008297:Male; D008875:Middle Aged; D009883:Ophthalmic Solutions / Q000627:therapeutic use*; D047428:Protein Kinase Inhibitors / Q000627:therapeutic use*; D014065:Tonometry, Ocular; D054460:rho-Associated Kinases / Q000037:antagonists & inhibitors*
chemical_list: D009883:Ophthalmic Solutions; D047428:Protein Kinase Inhibitors; D019307:1-(5-Isoquinolinesulfonyl)-2-Methylpiperazine; D054460:rho-Associated Kinases; C049347:fasudil