Clinical experience with brimonidine 0.2% and timolol 0.5% in glaucoma and ocular hypertension

doi:10.1016/S0039-6257(96)82029-7

Survey of Ophthalmology

Volume 41, Supplement 1, November 1996, Pages S27-S37

https://doi.org/10.1016/S0039-6257(96)82029-7 Get rights and content

Abstract

The ocular hypotensive efficacy and safety of brimonidine tartrate 0.2%, a highly selective alpha₂-adrenergic agonist, was compared with that of timolol 0.5%, a nonselective beta-blocker in two multicenter, randomized, double-masked studies. Combined data from a 12-month completed study and 6-month interim data from an ongoing study are reported. Efficacy and safety were evaluated at baseline, weeks 1 and 2, and months 1, 2, 3, 6, 9, and 12. Intraocular pressure (IOP) was measured at peak (2 hours after the morning dose) and trough (12 hours after the evening dose). Patients (n = 926) instilled either brimonidine tartrate 0.2% or timolol maleate 0.5% twice daily. At peak, the mean decreases from baseline IOP ranged from 5.9 ± 3.2 mm Hg to 7.6 ± 3.6 mm Hg for brimonidine and 6.0 ± 3.4 mm Hg to 6.6 ± 3.6 mm Hg for timolol (p < 0.001 within groups compared with baseline). No significant between-group differences were seen at peak except for weeks 1 and 2 and month 3 (p ≤ 0.04), when brimonidine had lower mean IOP. At trough the mean decreases from baseline ranged from 3.7 ± 4.0 mm Hg to 5.0 ± 3.0 mm Hg for brimonidine and 5.9 ± 3.4 to 6.6 ± 3.0 for timolol. A significant between-group difference was seen at trough at all visits (< 0.001), when timolol had a lower mean IOP. Brimonidine and timolol showed sustained efficacy. Both drugs were well-tolerated. The brimonidine group had more ocular allergy, oral dryness and conjunctival follicles. The timolol group had more burning and stinging. In the brimonidine group, 38/513 (7.4%) discontinued treatment due to ocular allergy. The timolol group had significantly lower mean heart rate compared to baseline. The effect on blood pressure was minimal for both drugs. Briinonidine showed efficacy similar to timolol and a relatively low rate of ocular allergy. Brimonidine 0.2% administered twice daily is an effective and safe ocular hypotensive agent that maintains IOP-lowering in chronic use.

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Brimonidine is a commonly used intra-ocular pressure-lowering agent for glaucoma patients. Allergic follicular or papillary conjunctivitis is a well-known side effect of brimonidine. Brimonidine is associated with ocular allergic symptoms such as conjunctival hyperemia, stinging sensation, photophobia and, in severe cases, corneal erosions. Here, we report a case of atypical conjunctival lesion following long-term administration of brimonidine.
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Patients followed at the Federal University of São Paulo were enrolled from August to November 2013 and were initially submitted to an ophthalmologic examination where the IOP was measured at 8 am, 10 am, and 12 pm. Afterward, patients underwent a 15-day washout of the carbonic anhydrase inhibitor and had their IOP measured again.
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: The author wishes to thank Kuankuan S. Chen, M.S., principal biostatistician, Allergan, Inc., for statistical analyses of the data.

: Presented in part at the American Glaucoma Society, Vancouver, British Columbia, July 30–August 2, 1996

^a: Dr. Schuman has no proprietary interest in Allergan, Inc., or brimonidine.

View full text

Clinical experience with brimonidine 0.2% and timolol 0.5% in glaucoma and ocular hypertension

Abstract

Eur J Pharmacol

Bioorg Med Chem Lett

Bioorg Med Chem Lett

Bioorg Med Chem Lett

Ophthalmology

Surv Ophthalmol

Long term effect of apraclonidine

Br J Ophthalmol

Long-term efficacy of brimonidine on IOP lowering (abstract)

Invest Ophthalmol Vis Sci

Preclinical evaluation of brimonidine

Surv Ophthalmol

Therapeutic use of α2-adrenoceptor agonists in glaucoma

Clinical experience with long-term use of 1% apraclonidine

Arch Ophthalmol

Incidence of characteristics of allergic reaction to apraclonidine 0.5%

Invest Ophthalmol Vis Sci

The potential of α2-adrenergic agonists in the medical treatment of glaucoma

Curr Opinion Ophthalmol

Brimonidine tartrate: a one month dose response study (abstract)

Invest Ophthalmol Vis Sci

Therapeutic use of α₂-adrenoceptor agonists in glaucoma

The potential of α₂-adrenergic agonists in the medical treatment of glaucoma