Ocular Beta-blockers in Glaucoma Management. Clinical Pharmacological Aspects

Overview

Journal Drugs Aging

Specialties Geriatrics
Pharmacology

Date 1992 May 1

PMID 1351412

Citations 27

Authors

A M Brooks

W E GILLIES

Affiliations

Soon will be listed here.

Abstract

Topical beta-blockers reduce the intraocular pressure (IOP) by blockade of sympathetic nerve endings in the ciliary epithelium causing a fall in aqueous humour production. Two types of topical beta-blockers are available for use in glaucoma: nonselective, which block both beta 1- and beta 2-adrenoceptors; and cardioselective, which block only beta 1-receptors. Of the beta-Blockers commercially available, timolol, levobunolol, metipranolol and carteolol are nonselective, and betaxolol is cardioselective. Twice-daily timolol is probably the most effective agent in lowering IOP, although levobunolol is equally effective and can be used once daily with little difference in effect. Carteolol is used twice daily and any theoretical advantage in diminished side effects conferred by its partial beta-agonist activity compared with timolol has not been fully substantiated. Metipranolol is effective twice daily and does not have partial beta-agonist activity. Betaxolol has an effect comparable to timolol in lowering IOP, but is less effective in some patients. beta-Blockers can be used with other antiglaucoma medications, but their combined action with epinephrine (adrenaline) is suspect, particularly in the case of the nonselective beta-blockers, and the effect should be assessed in patients on an individual basis. Local stinging can be a problem in some patients with betaxolol. The most serious side effects of beta-blockers are the exacerbation of chronic obstructive airways disease with nonselective agents and the precipitation of bronchospasm in some patients. Betaxolol seems relatively free of adverse respiratory effects, although this may be dose-related and extreme caution should still be exercised in patients with any history of respiratory illness. Because of the lower risk of precipitating side effects, betaxolol is probably the beta-blocker of first choice for use in glaucoma; timolol or levobunolol are reserved for patients who do not respond satisfactorily to betaxolol and are quite free of respiratory disease.

Citing Articles

Dual targeting carbonic anhydrase inhibitors as promising therapeutic approach: a structural overview.

DAmbrosio K, Di Fiore A, Langella E Front Mol Biosci. 2025; 12:1511281.

PMID: 39963267 PMC: 11830626. DOI: 10.3389/fmolb.2025.1511281.

Change in Systemic Medication and its Influence on Intraocular Pressure - Results From the Gutenberg Health Study.

Laspas P, Hartmann A, Scholz I, Hoffmann E, Khawaja A, Lackner K Invest Ophthalmol Vis Sci. 2024; 65(14):4.

PMID: 39625443 PMC: 11620004. DOI: 10.1167/iovs.65.14.4.

Chemical Insights into Topical Agents in Intraocular Pressure Management: From Glaucoma Etiopathology to Therapeutic Approaches.

Patton G, Lee H Pharmaceutics. 2024; 16(2).

PMID: 38399328 PMC: 10891530. DOI: 10.3390/pharmaceutics16020274.

Next generation therapeutics for retinal neurodegenerative diseases.

Appell M, Pejavar J, Pasupathy A, Rompicharla S, Abbasi S, Malmberg K J Control Release. 2024; 367:708-736.

PMID: 38295996 PMC: 10960710. DOI: 10.1016/j.jconrel.2024.01.063.

Glaucoma and Systemic Disease.

Hsu E, Desai M Life (Basel). 2023; 13(4).

PMID: 37109547 PMC: 10143901. DOI: 10.3390/life13041018.

References

Collignon-Brach J . Early visual field changes with beta-blocking agents. Surv Ophthalmol. 1989; 33 Suppl:429-30; discussion 435-6. DOI: 10.1016/0039-6257(89)90073-8. View

Weinreb R, Van Buskirk E, Cherniack R, Drake M . Long-term betaxolol therapy in glaucoma patients with pulmonary disease. Am J Ophthalmol. 1988; 106(2):162-7. DOI: 10.1016/0002-9394(88)90828-8. View

Duff G, Graham P . A double-crossover trial comparing the effects of topical carteolol and placebo on intraocular pressure. Br J Ophthalmol. 1988; 72(1):27-8. PMC: 1041361. DOI: 10.1136/bjo.72.1.27. View

Martin F . Timolol maleate. A report from the Glaucoma Clinic, Sydney Eye Hospital. Aust J Ophthalmol. 1980; 8(2):177-8. DOI: 10.1111/j.1442-9071.1980.tb01679.x. View

Brooks A, Burden J, GILLIES W . The significance of reactions to betaxolol reported by patients. Aust N Z J Ophthalmol. 1989; 17(4):353-5. View

Ohrstrom A, Pandolfi M . Regulation of intraocular pressure and pupil size by beta-blockers and epinephrine. Arch Ophthalmol. 1980; 98(12):2182-4. DOI: 10.1001/archopht.1980.01020041034005. View

CINOTTI A, CINOTTI D, Grant W, Jacobs I, GALIN M, Silverstone D . Levobunolol vs timolol for open-angle glaucoma and ocular hypertension. Am J Ophthalmol. 1985; 99(1):11-7. DOI: 10.1016/s0002-9394(14)75859-3. View

HOVDING G, AASVED H . Timolol/pilocarpine combination eye drops in open angle glaucoma and in ocular hypertension. A controlled randomized study. Acta Ophthalmol (Copenh). 1987; 65(5):594-601. DOI: 10.1111/j.1755-3768.1987.tb07048.x. View

Chrisp P, Sorkin E . Ocular carteolol. A review of its pharmacological properties, and therapeutic use in glaucoma and ocular hypertension. Drugs Aging. 1992; 2(1):58-77. DOI: 10.2165/00002512-199202010-00007. View

10.

Gerber S, Cantor L, Brater D . Systemic drug interactions with topical glaucoma medications. Surv Ophthalmol. 1990; 35(3):205-18. DOI: 10.1016/0039-6257(90)90090-i. View

11.

Duff G, Newcombe R . The 12-hour control of intraocular pressure on carteolol 2% twice daily. Br J Ophthalmol. 1988; 72(12):890-1. PMC: 1041615. DOI: 10.1136/bjo.72.12.890. View

12.

Frumar K, McGuinness R . A study of the intraocular pressure lowering effect of timolol and dipivalyl epinephrine. Trans Ophthalmol Soc N Z. 1981; 33:27-9. View

13.

CHER I . Transfer to timolol: selective use of a new mode of therapy. Aust J Ophthalmol. 1980; 8(2):165-72. DOI: 10.1111/j.1442-9071.1980.tb01677.x. View

14.

Neufeld A . Epinephrine and timolol: how do these drugs lower intraocular pressure?. Ann Ophthalmol. 1981; 13(10):1109-11. View

15.

Brooks A, GILLIES W, West R . Betaxolol eye drops as a safe medication to lower intraocular pressure. Aust N Z J Ophthalmol. 1987; 15(2):125-9. DOI: 10.1111/j.1442-9071.1987.tb00057.x. View

16.

Serle J, Lustgarten J, Podos S . A clinical trial of metipranolol, a noncardioselective beta-adrenergic antagonist, in ocular hypertension. Am J Ophthalmol. 1991; 112(3):302-7. DOI: 10.1016/s0002-9394(14)76731-5. View

17.

Coakes R, Brubaker R . The mechanism of timolol in lowering intraocular pressure. In the normal eye. Arch Ophthalmol. 1978; 96(11):2045-8. DOI: 10.1001/archopht.1978.03910060433007. View

18.

Stewart R, Kimbrough R, Ward R . Betaxolol vs timolol. A six-month double-blind comparison. Arch Ophthalmol. 1986; 104(1):46-8. DOI: 10.1001/archopht.1986.01050130056019. View

19.

Van Buskirk E . Adverse reactions from timolol administration. Ophthalmology. 1980; 87(5):447-50. DOI: 10.1016/s0161-6420(80)35215-9. View

20.

Keates E, Stone R . Safety and effectiveness of concomitant administration of dipivefrin and timolol maleate. Am J Ophthalmol. 1981; 91(2):243-8. DOI: 10.1016/0002-9394(81)90182-3. View