The Ocular Hypotensive Efficacy of Topical Fasudil, a Rho-Associated Protein Kinase Inhibitor, in Patients With End-Stage Glaucoma

Am J Ther. 2017 Nov/Dec;24(6):e676-e680. doi: 10.1097/MJT.0000000000000362.

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.

MeSH terms

  • 1-(5-Isoquinolinesulfonyl)-2-Methylpiperazine / administration & dosage
  • 1-(5-Isoquinolinesulfonyl)-2-Methylpiperazine / analogs & derivatives*
  • 1-(5-Isoquinolinesulfonyl)-2-Methylpiperazine / therapeutic use
  • Administration, Ophthalmic
  • Aged
  • Conjunctiva / blood supply
  • Conjunctiva / drug effects
  • Double-Blind Method
  • Female
  • Glaucoma, Open-Angle / drug therapy*
  • Humans
  • Hyperemia / chemically induced
  • Intraocular Pressure / drug effects*
  • Male
  • Middle Aged
  • Ophthalmic Solutions / therapeutic use*
  • Protein Kinase Inhibitors / therapeutic use*
  • Tonometry, Ocular
  • rho-Associated Kinases / antagonists & inhibitors*

Substances

  • Ophthalmic Solutions
  • Protein Kinase Inhibitors
  • 1-(5-Isoquinolinesulfonyl)-2-Methylpiperazine
  • rho-Associated Kinases
  • fasudil