The early information on the clinical efficacy, safety, and tolerability of brimonidine 0.2% were obtained from studies that compared brimonidine monotherapy with timolol and betaxolol. These studies showed its intra-ocular pressure lowering efficacy to be comparable with timolol and superior to betaxolol. The data from the timolol studies showed consistent results after four years. These findings have been confirmed by additional studies in the clinical setting.
More recently, several clinical trials have been completed investigating the role of brimonidine as adjunctive medication to beta-blockers and as replacement therapy to other intraocular pressure lowering compounds. When added to beta-blockers, brimonidine is superior to dorzolamide, similar in efficacy but better tolerated than pilocarpine, and more predictable than latanoprost.
Data from replacement studies have indicated that there may be advantages in replacing rather than adding medications in the treatment of glaucoma.
SchumanJ.S., HorwitzB., ChoplinN.T., DavidR., AlbrachtD., ChenK., and the Chronic Bromonidine Study Group. A 1-year study of brimonidine twice daily in glaucoma and ocular hypertension. A controlled, randomized, multicenter clinical trial.Arch Ophthalmol1997; 115: 847–52.
2.
SchumanJ.S.. Clinical experience with brimonidine 0.2% and timolol 0.5% in glaucoma and ocular hypertension.Surv Ophthalmol1996; 41(suppl): S27–S37.
3.
LeBlancR.P., for the Brimonidine Study Group II: Twelve-month results of an ongoing randomized trial comparing brimonidine tartrate 0.2% and timolol 0.5% given twice daily in patients with glaucoma or ocular hypertension.Ophthalmology1998; 105: 1960–7.
4.
KatzL.J., for the Brimonidine Study Groups. Brimonidine tartrate 0.2% twice daily vs timolol 0.5%: 1-year results in glaucoma patients.Am J Ophthalmol1999; 127: 20–6.
5.
SerleJ.B.. A comparison of the safety and efficacy of twice daily brimonidine 0.2% versus betaxolol 0.25% in subjects with elevated intraocular pressure.Surv Ophthalmol1996; 41(suppl): S39–S47.
6.
MelamedS., DavidR., and the Brimonidine Study Group II. Ongoing assessment of the safety profile and efficacy of brimonidine compared with timolol: year-three results.Clin Ther2000; 22: 103–11.
7.
CantorL.B.. The evolving pharmacotherapeutic profile of brimonidine, an alpha-2-adrenergic agonist, after four years of continuous use.Exp Opin Pharmacother2000; 1: 815–34.
8.
ShumanJ., and Brimonidone Study Groups 1 and 2. Effects of systemic beta-blocker therapy on the efficacy and safety of topical brimonidine and timolol.Ophthalmology2000; 107: 1171–7.
9.
GordonR.N., LiebmannJ.M., GreenfieldD.S., LamaP., RitchR.. Lack of cross-reactive allergic response to brimonidine in patients with known apraclonidine allergy.Eye1998; 12: 697–700.
10.
JavittJ.C., SchiffmanR.C., and the Brimonidine Outcomes Study Group I. Clinical success and quality of life with brimonidine 0.2% or timolol 0.5% used twice daily in glaucoma or ocular hypertension: a randomized clinical trial.J Glaucoma2000; 9: 224–34.
11.
JavittJ., GoldbergI., and the Brimonidine Outcomes Study Group II. Comparison of the clinical success rates and quality of life effects of brimonidine tartrate 0.2% and betaxolol 0.25% suspension in patients with open-angle glaucoma and ocular hypertension.J Glaucoma2000; 9: 398–408.
12.
TraversoC.E., for the Brimonidine Additivity Study Group I: additivity of brimonidine 0.2% b.i.d. or pilocarpine 2% t.i.d. to beta-blocker monotherapy.Invest Ophthalmol Vis Sci1998; 39(suppl): S480.
13.
SimmonsS.T.. Comparison of the efficacy and tolerability of Alphagan and Trusopt as adjunct therapy with beta-blockers in patients with chronic open-angle glaucoma or ocular hypertension.Clin Ther2001; 23: 604–14.
14.
SamuelsonT., SimmonsS.T.. Efficacy and tolerability of Alphagan versus Xalatan as adjunct therapy in chronic open-angle glaucoma or ocular hypertension patients uncontrolled on beta-blockers alone.Invest Ophthalmol Vis Sci2000; 41(suppl): S573.
15.
SimmonsS.T., SamuelsonT.W., and the Alphagan/Xalatan Study Group. Comparison of brimonidine with latanoprost in the adjunctive treatment of glaucoma.Clin Ther2000; 22: 388–99.
16.
LeeD.A.. Efficacy of brimonidine as replacement therapy in patients with open-angle glaucoma or ocular hypertension.Clin Ther2000; 22: 53–65.
17.
WangF., JavittJ.C., RoweM., MengK.. Measuring the impact of glaucoma and its treatment on quality of life: the Glaucoma Disability Index.Invest Ophthalmol Vis Sci1996; 37(suppl): S643.
18.
NetlandP., AbelsonM.B., WelchD.L., ChapinM.J., LatinaM.. A two month evaluation of Alphagan alone compared to patient's previous two line therapy.J Glaucoma1999; 8 (Suppl.): S14.
19.
KorschE., GroteA., SeyboldM., SodittV.. Systemic adverse effects of topical treatment with brimonidine in an infant with secondary glaucoma.Eur J Pediatr1999; 158: 685.
20.
CarlsenJ.O., ZabriskieN.A., KwonY.H., BarbeM.E., ScottW.E.. Apparent central nervous system depression in infants after the use of topical brimonidine.Am J Ophthalmol1999; 128: 255–6.
21.
RodierP.M.. Developing brain as a target of toxicity.Environ Health Perspect1995; 103(Suppl.): S73–6.
22.
TanakaE.. In vivo age-related changes in hepatic drug-oxidizing capacity in humans.J Clin Pharm Ther1998; 23: 247–55.
