Sezolamide: Additivity to timolol twice daily

• Published in: Eye (London) Vol. 6; no. 5; pp. 525 - 529
• Main Authors: Gunning, Frans, Béchetoille, Alain, Lippa, Erik A, Pfeiffer, Norbert, Gerling, Jurgen, Holder, Daniel, Clineschmidt, Coleen, Buntinx, Agnes, Brunner-Ferber, Françoise L, Grehn, Franz, Greve, Erik
• Format: Journal Article
• Language: English
• Published: London Nature Publishing Group UK 01.01.1992; Nature Publishing Group
• Subjects: Aged; Aged, 80 and over; Biological and medical sciences; Carbonic Anhydrase Inhibitors - therapeutic use; Drug Administration Schedule; Drug Therapy, Combination; Eye; Female; Glaucoma, Open-Angle - drug therapy; Humans; Laboratory Medicine; Male; Medical sciences; Medicine; Medicine & Public Health; Middle Aged; Ocular Hypertension - drug therapy; Ophthalmology; Pharmaceutical Sciences/Technology; Pharmacology. Drug treatments; Sulfonamides - therapeutic use; Surgery; Surgical Oncology; Thiophenes - therapeutic use; Timolol - therapeutic use; Glaucoma; Carbonic anhydrase inhibitors; Sezolamide; Timolol; Eye drop; Human; Chemotherapy; Eye disease; Randomization; Treatment; Open angle glaucoma; Ocular hypertension; Double blind study; Enzyme inhibitor; Comparative study
• ISSN: 0950-222X; 1476-5454
• DOI: 10.1038/eye.1992.111

Sezolamide, a potent topical carbonic anhydrase inhibitor previously known as MK-417, was studied to determine its ocular hypotensive activity in patients with elevated intraocular pressure while on continuing therapy with topical timolol. This was a three-centre, double-masked, randomised, placebo-controlled, parallel study in 36 patients with bilateral primary open angle glaucoma or ocular hypertension on therapy receiving 0.5% timolol twice daily, with a morning intraocular pressure greater than or equal to 22 mmHg in both eyes 2–4 hours following an 8 a.m. dose of timolol. Sezolamide 1.8% or placebo twice daily was added to treatment with timolol on the evening of day 1 and continued for 2 weeks. Twelve-hour diurnal curves were performed before the study on day 1 (timolol alone) and on day 15. Intraocular pressure measurements were also taken on days 2 and 8 at 8 a.m. and 9 a.m. Patients who received timolol and sezolamide showed additional intraocular pressure reductions from day 1 (timolol alone) of 8.0 to 15.5%, which were significant at all times. At hours 1, 2, 4 and 8 the reductions in intraocular pressure observed in the group receiving sezolamide and timolol were significantly greater than those in the group receiving timolol and placebo.