Effects of topically applied falintolol: a new beta-adrenergic antagonist for treatment of glaucoma

• Published in: Journal of ocular pharmacology Vol. 3; no. 2; p. 111
• Main Authors: Himber, J, Sallee, V L, Andermann, G, Bouzoubaa, M, Leclerc, G, De Santis, L
• Format: Journal Article
• Language: English
• Published: United States 1987
• Subjects: Administration, Topical; Adrenergic beta-Antagonists - pharmacokinetics; Adrenergic beta-Antagonists - pharmacology; Adrenergic beta-Antagonists - therapeutic use; Anesthetics, Local - pharmacology; Animals; Cattle; Cornea - drug effects; Cornea - metabolism; Cornea - physiology; Electrophysiology; Glaucoma - drug therapy; Heart Rate - drug effects; Intraocular Pressure - drug effects; Macaca fascicularis; Propanolamines - pharmacokinetics; Propanolamines - pharmacology; Propanolamines - therapeutic use; Pupil - drug effects; Rabbits; Timolol - pharmacology
• ISSN: 8756-3320
• DOI: 10.1089/jop.1987.3.111

Changes in intraocular pressure (IOP) following topical administration of falintolol (0.5%-0.25%), a new beta-blocking agent, were studied in conscious albino rabbits with alpha-chymotrypsin-induced ocular hypertension. The drug produced a reduction in IOP equal to that of timolol. A longer duration of activity was noted with falintolol. The rate of transport of topically applied falintolol through the isolated bovine cornea under conditions simulating normal physiology was linear up to three hours and twice as fast as timolol from 3 to 6 hours. Since topical ocular application of beta-adrenergic antagonists useful in glaucoma therapy can also cause a number of troublesome systemic side effects, several conclusive preclinical investigations were carried out with falintolol. Of major concern was the effect falintolol might have on the pupil, cornea, and heart rate when administered topically. The results show that falintolol does not produce any noteworthy side effects and is capable of being an effective beta-blocking agent in open-angle glaucoma therapy.