Phase III long-term study and comparative clinical study of nipradilol ophthalmic solution in patients with primary open-angle glaucoma and ocular hypertension.
Nipradilol (CAS 81486-22-8) is a non-selective beta-blocker with alpha-1 blocking and nitroglycerin-like vasodilating activities. In the present communication, the long-term efficacy and safety of nipradilol were investigated and the efficacy, safety and utility of topical nipradilol and timolol (CAS 91524-16-2) were compared in patients with primary open-angle glaucoma or ocular hypertension. In the long-term study, nipradilol for 1 year (52 weeks) was performed by registration method. 67 out of 68 patients were subjected to analysis and 57 patients (83.8 %) completed 52-week instillation. 0.25 % nipradilol was applied twice daily to patients. As a result, intraocular pressure (IOP) decreased significantly by 4.0 mmHg to 4.8 mmHg compared with the baseline without tachyphylaxis. The incidence of adverse events was 12.5 % at 52 weeks by analysis with Kaplan-Meier life-table method. It showed no significant trend of increase after 3 months. In the multi-centered double-masked comparative randomized study, 0.25 % nipradilol was assigned to 96 patients and 0.5 % timolol to 100 patients. Each patient was instilled nipradilol or timolol twice daily for 8 weeks. IOP significantly decreased by 4.2 mmHg and by 4.7 mmHg at 8 weeks and the incidence of adverse events was 10.5 % and 12.1 % in the nipradilol and timolol group, respectively. No significant between-group difference in IOP reduction or incidence of adverse events was seen. Topical nipradilol showed long-term ocular hypotensive effects and clinical safety in a 52-week study, and its efficacy and safety equivalent to timolol was confirmed in a 8-week comparative study.
Kanno
Mikiko
M
Department of Ophthalmology, School of Medicine, University of Tokyo, Japan.
Araie
Makoto
M
Masuda
Kanjiro
K
Takase
Masahiro
M
Kitazawa
Yoshiaki
Y
Shiose
Yoshihiko
Y
Azuma
Ikuo
I
Ogawa
Nobuya
N
Ohdo
Shigehiro
S
D000287:Administration, Topical; D000319:Adrenergic beta-Antagonists / Q000008:administration & dosage / Q000009:adverse effects / Q000627:therapeutic use*; D000328:Adult; D000368:Aged; D004311:Double-Blind Method; D005260:Female; D005902:Glaucoma, Open-Angle / Q000188:drug therapy*; D006801:Humans; D008297:Male; D008875:Middle Aged; D009798:Ocular Hypertension / Q000188:drug therapy*; D009883:Ophthalmic Solutions; D011412:Propanolamines / Q000008:administration & dosage / Q000009:adverse effects / Q000627:therapeutic use*; D013999:Timolol / Q000627:therapeutic use; D014665:Vasodilator Agents / Q000008:administration & dosage / Q000009:adverse effects / Q000627:therapeutic use*
D000319:Adrenergic beta-Antagonists; D009883:Ophthalmic Solutions; D011412:Propanolamines; D014665:Vasodilator Agents; D013999:Timolol; C036089:nipradilol