Phase III Long-term Study and Comparative Clinical Study of Nipradilol Ophthalmic Solution in Patients with Primary Open-angle Glaucoma and Ocular Hypertension

Route of Penetration of Topically Instilled Nipradilol into the Ipsilateral Posterior Retina

“…Nipradilol has nonselective ␤-, and selective ␣ 1 -receptor, blocking properties [21][22][23][24][25][26] with nitric oxide (NO) donative action 11 and a molecular weight (326. 35) and octanol/buffer ratio (0.79 at pH 7.3) close to those of timolol, 27 a representative antiglaucoma ophthalmic solution.…”

Propranolol Transport Across the Inner Blood–Retinal Barrier: Potential Involvement of a Novel Organic Cation Transporter

“…In the treatment of retinal diseases, several cationic β‐adrenergic antagonists, α 2 ‐adrenergic agonists and tricyclic antidepressants, are thought to be good drug candidates because of their neuroprotective effects 24–26. Propranolol is a β‐adrenergic antagonist used for the treatment of hypertension, and its protective effect has been reported against BRB dysfunction, showing its possible usefulness in the treatment of the retinal diseases such as retinopathy of prematurity 23.…”

“…Propranolol is a cationic, nonselective β‐adrenergic antagonist used for the treatment of essential hypertension, angina, and tachyarrhythmia and it has recently been reported that propranolol is protective against retinal angiogenesis to ameliorate BRB dysfunction in an animal model of human retinopathy of prematurity 23. Regarding other β‐adrenergic antagonists, timolol and nipradilol are used for the treatment of glaucoma,24,25 and it has also been reported that nipradilol exhibits a neuroprotective effect,26 suggesting that the clarification of the mechanism for the BRB permeability of β‐adrenergic antagonists will provide helpful information to improve the treatment of retinal dysfunction.…”

Visual field loss in patients with normal-tension glaucoma under topical nipradilol or timolol: Subgroup and subfield analyses of the nipradilol-timolol study

“…[6][7][8]10,11 The ocular hypotensive effect is identical to that of 0.5% timolol (nonselective beta-receptor blocker) in glaucoma patients. 12,13 Nipradilol also has a neuroprotective effect in experimental animal models. For example, it suppresses N-methyl-D-aspartate-induced retinal damage in rats, 14 and improves the survival rate of cultured postnatal rat retinal ganglion cells (RGCs).…”