Diacetyl derivative of nadolol. I. Ocular pharmacology and short-term ocular hypotensive effect in glaucomatous eyes

E. Duzman, C. C. Chen, J. Anderson, M. Blumenthal and H. Twizer

On topical application to rabbit eyes, the diacetate ester of nadolol was more easily absorbed into ocular tissue than nadolol and was enzymatically hydrolyzed to nadolol within the eye. In a 24-hour clinical study, the ocular hypotensive activities of 0.5% diacetyl nadolol, 2% diacetyl nadolol, 2% nadolol, and 0.5% timolol maleate in subjects with open-angle glaucoma or ocular hypertension were compared. Both concentrations of diacetyl nadolol significantly reduced intraocular pressure during the first six hours. Two percent diacetyl nadolol was as effective as 0.5% timolol maleate during the first eight hours. During the remainder of the testing period, timolol showed greater IOP control. Two percent diacetyl nadolol and 2% nadolol showed similar ocular hypotensive effects both in magnitude and duration in this short-term study.