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Diacetyl Derivative of Nadolol: I. Ocular Pharmacology and Short-term Ocular Hypotensive Effect in Glaucomatous Eyes

Diacetyl Derivative of Nadolol: I. Ocular Pharmacology and Short-term Ocular Hypotensive Effect... Abstract • 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 openangle 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. References 1. Lee RJ, Evans DB, Sherrin HB, et al: Pharmacology of nadolol (SQ 11725), a β-adrenergic antagonist lacking direct myocardial depression . Eur J Pharmacol 1975;33:371-382.Crossref 2. Volicer L, Liang CS, Gavras H, et al: Effect of nadolol in treatment of hypertension . J Clin Pharmacol 1979;19:137-147.Crossref 3. Hitzenberger G: Initial experience with a new long-acting beta-blocker, nadolol, in hypertensive patients . J Int Med Res 1979;7:33-38. 4. Prager G: Angina pectoris: Effective therapy once daily . J Int Med Res 1979;7:39-44. 5. Ling ASC, Groel JT: Improved physical performance as a therapeutic objective in patients with angina . Br J Clin Pharmacol 1979;7( (suppl 2) ):161S-166S.Crossref 6. Wei C, Anderson J, Leopold I: Ocular absorption and metabolism of topically applied epinephrine and a dipivalyl ester of epinephrine . Invest Ophthalmol Vis Sci 1978;17:315-321. 7. Neufeld AH, Page ED: In vitro determination of the ability of drugs to bind to adrenergic receptors . Invest Ophthalmol Vis Sci 1977; 16:1118-1124. 8. Lazare R, Horlington M: Pilocarpine levels in the eyes of rabbits following topical application . Exp Eye Res 1975;21:281-287.Crossref http://www.deepdyve.com/assets/images/DeepDyve-Logo-lg.png Archives of Ophthalmology American Medical Association

Diacetyl Derivative of Nadolol: I. Ocular Pharmacology and Short-term Ocular Hypotensive Effect in Glaucomatous Eyes

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Publisher
American Medical Association
Copyright
Copyright © 1982 American Medical Association. All Rights Reserved.
ISSN
0003-9950
eISSN
1538-3687
DOI
10.1001/archopht.1982.01030040896005
Publisher site
See Article on Publisher Site

Abstract

Abstract • 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 openangle 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. References 1. Lee RJ, Evans DB, Sherrin HB, et al: Pharmacology of nadolol (SQ 11725), a β-adrenergic antagonist lacking direct myocardial depression . Eur J Pharmacol 1975;33:371-382.Crossref 2. Volicer L, Liang CS, Gavras H, et al: Effect of nadolol in treatment of hypertension . J Clin Pharmacol 1979;19:137-147.Crossref 3. Hitzenberger G: Initial experience with a new long-acting beta-blocker, nadolol, in hypertensive patients . J Int Med Res 1979;7:33-38. 4. Prager G: Angina pectoris: Effective therapy once daily . J Int Med Res 1979;7:39-44. 5. Ling ASC, Groel JT: Improved physical performance as a therapeutic objective in patients with angina . Br J Clin Pharmacol 1979;7( (suppl 2) ):161S-166S.Crossref 6. Wei C, Anderson J, Leopold I: Ocular absorption and metabolism of topically applied epinephrine and a dipivalyl ester of epinephrine . Invest Ophthalmol Vis Sci 1978;17:315-321. 7. Neufeld AH, Page ED: In vitro determination of the ability of drugs to bind to adrenergic receptors . Invest Ophthalmol Vis Sci 1977; 16:1118-1124. 8. Lazare R, Horlington M: Pilocarpine levels in the eyes of rabbits following topical application . Exp Eye Res 1975;21:281-287.Crossref

Journal

Archives of OphthalmologyAmerican Medical Association

Published: Dec 1, 1982

References