[Skip to Content]
Access to paid content on this site is currently suspended due to excessive activity being detected from your IP address 54.211.41.181. Please contact the publisher to request reinstatement.
[Skip to Content Landing]
Article
January 1995

The Cardiovascular, Pulmonary, and Ocular Hypotensive Effects of 0.2% Brimonidine

Author Affiliations

From The Wilmer Ophthalmological Institute (Drs Nordlund, Pasquale, and Robin), The School of Hygiene and Public Health (Dr Robin), and the Department of Medicine (Drs Rudikoff and Ordman), The Johns Hopkins University School of Medicine, Baltimore, Md, and Allergan Inc, Irvine, Calif (Ms Chen and Mr Walt).; Dr Nordlund is currently with the Department of Ophthalmology, University of Virginia, Charlottesville, and Dr Pasquale, the Division of Ophthalmology, Brigham and Women's Hospital, Boston, Mass. Drs Nordlund, Pasquale, Robin, Rudikoff, and Ordman do not have any proprietary interest in Allergan Inc, or any of the study medications.

Arch Ophthalmol. 1995;113(1):77-83. doi:10.1001/archopht.1995.01100010079024
Abstract

Objective:  To compare the cardiovascular, pulmonary, and ocular hypotensive effects of 0.2% brimonidine tartrate with those of 0.5% timolol maleate, 0.25% betaxolol suspension, and brimonidine vehicle.

Design and Patients:  A single-center, double-masked, randomized, crossover study of 24 young, healthy men.

Interventions:  Baseline heart rate, blood pressure, respiratory rate, and intraocular pressure were recorded at hour 0. At hour 2, heart rate, blood pressure, respiratory rate, and forced expiratory volume in 1 second were measured and a 15-minute treadmill test performed. Hour 0 measurements were repeated at hour 4. On four subsequent visits, we instilled one drop of a study medication into each eye after the baseline measurements at hour 0.

Results:  Timolol reduced resting (−5.3 to −6.5 beats/min; P≤.004) and exercise-induced heart rate (−4.3 to −13.6 beats/min; P≤.022) compared with brimonidine, betaxolol suspension, and brimonidine vehicle. At hour 4, brimonidine reduced resting systolic blood pressure compared with all other study medications (−5.2 to −7.3 mm Hg; P≤.024). Timolol reduced systolic blood pressure during exercise and brimonidine reduced systolic blood pressure during recovery more than betaxolol suspension and brimonidine vehicle (−5.1 to −7.7 mm Hg; P≤.033; and −5.4 to −6.0 mm Hg; P≤.002, respectively). Mean respiratory rate and forced expiratory volume in 1 second were not significantly altered by any study medication. At hour 4, brimonidine lowered intraocular pressure as well as timolol and better than betaxolol suspension (−1.9 mm Hg; P<.001) or brimonidine vehicle (−1.8 mm Hg; P<.001).

Conclusions:  The cardiopulmonary effects of 0.2% brimonidine were limited to a slight reduction in systolic blood pressure during recovery from exercise and at 4 hours after instillation. The ocular hypotensive effect of brimonidine was comparable to that of timolol and greater than that of betaxolol suspension in this patient population.

References
1.
Burke JA, Potter DE.  Ocular effects of a relatively selective α-2 agonist (UK-14, 304-18) in cats, rabbits and monkeys . Curr Eye Res . 1986;5:665-676.Article
2.
Serle JB, Steidl S, Wang R-F, Mittag TN, Podos SM.  Selective α-2 adrenergic agonists B-HT920 and UK14304-18: effects on aqueous humor dynamics in monkeys . Arch Ophthalmol . 1991;109:1158-1162.Article
3.
Barnebey HS, Robin AL, Zimmerman TJ, et al.  Efficacy of brimonidine in decreasing elevations in intraocular pressure after laser trabeculoplasty . Ophthalmology . 1993;100:1083-1088.Article
4.
David R, Spaeth GL, Clevenger CE, et al.  Brimonidine in the prevention of intraocular pressure elevation following argon laser trabeculoplasty . Arch Ophthalmol . 1993;111:1387-1390.Article
5.
Derick RJ, Walters TR, Robin AL, et al.  Brimonidine tartrate: a one month dose response study . Invest Ophthalmol Vis Sci . 1993;34( (suppl) ):929.
6.
Starke K.  Regulation of norepinephrine release by presynaptic receptor system . Rev Physiol Biochem Pharmacol . 1977;77:1-124.
7.
Hodapp E, Kolker AE, Kass MA, Goldberg I, Becker B, Gordon M.  Effect of topical clonidine on intraocular pressure . Arch Ophthalmol . 1981;99:1208-1211.Article
8.
Coleman AL, Robin AL, Pollack IP, Rudikoff MT, Enger C, Mayer PR.  Cardiovascular and intraocular pressure effects and plasma concentrations of apraclonidine . Arch Ophthalmol . 1990;108:1264-1267.Article
9.
Hurvitz LM, Kaufman PL, Robin AL, Weinreb RN, Crawford K, Shaw B.  New developments in the drug treatment of glaucoma . Drugs . 1991;41:514-532.Article
10.
Hernandez y Hernandez H, Cervantes R, Frati A, Hurtado R, McDonald TO, DeSoura B.  Cardiovascular effects of topical glaucoma therapies in normal subjects . J Toxicol Cutan Ocul Toxicol . 1983;2:99-106.Article
11.
Doyle WJ, Weber PA, Meeks RH.  The effect of topical timolol maleate on exercise performance . Arch Ophthalmol . 1984;102:1517.Article
12.
Atkins JM, Pugh BR, Timewell RM.  Cardiovascular effects of topical β-blockers during exercise . Am J Ophthalmol . 1985;99:173-175.
13.
Nakaskima M, Uematsu T, Takiguchi Y, et al.  Effect of ophthalmic administration of S-596 (arotinolol) on intraocular pressure and haemodynamics in healthy volunteers: comparison with timolol . Eur J Clin Pharmacol . 1985;28:391-395.Article
14.
Leier CV, Baker D, Weber PA.  Cardiovascular effects of ophthalmic timolol . Ann Intern Med . 1986;104:197-199.Article
15.
Brazier DJ, Smith SE.  Ocular and cardiovascular response to topical carteolol 2% and timolol 0.5% in healthy volunteers . Br J Ophthalmol . 1988;72:101-103.Article
16.
Dickstein K, Hapnes R, Aarsland T, et al.  Comparison of topical timolol vs betaxolol on cardiopulmonary exercise performance in healthy volunteers . Acta Ophthalmol . 1988;66:463-466.Article
17.
Cochran WG, Cox GM. Experimental Designs . 2nd ed. New York, NY: John Wiley & Sons Inc; 1957:133-139.
18.
Fleiss JL. The Designs and Analysis of Clinical Experiments . New York, NY: John Wiley & Sons Inc; 1986:281-286.
19.
SAS/STAT User's Guide, Version 6 . 4th ed. Cary, NC: SAS Institute Inc; 1989; 1-2.
20.
Schoene RB, Abuan T, Ward RL, Beasley CH.  Effects of topical betaxolol, timolol, and placebo on pulmonary function in asthmatic bronchitis . Am J Ophthalmol . 1984;97:86-92.
21.
Bruce RA, Blackmon IR, Jones JW, Strait G.  Exercising testing in normal subjects and cardiac patients . Pediatrics . 1963;32:742-756.
22.
Van Buskirk EM, Weinreb RN, Berry DP, et al.  Betaxolol in patients with glaucoma and asthma . Am J Ophthalmol . 1986;101:531-534.
23.
Dunn TL, Gerber MJ, Shen AS, et al.  The effect of topical ophthalmic instillation of timolol and betaxolol on lung function in asthmatic subjects . Am Rev Respir Dis . 1986;133:264-268.
24.
Harris LS, Greenstein SH, Bloom AF.  Respiratory difficulties with betaxolol . Am J Ophthalmol . 1986;102:274-275.Article
25.
Marcus DF, Krupin T, Podos SM, Becker B.  The effects of exercise on intraocular pressure . Invest Ophthalmol Vis Sci . 1970;9:749-752.
26.
Passo MS, Goldberg L, Elliot DL, Van Buskirk EM.  Exercise conditioning and intraocular pressure . Am J Ophthalmol . 1987;103:754-757.
27.
Sargent RG, Blair SN, Magun JC, et al.  Physical fitness and intraocular pressure . Am J Optom Physiol Optics . 1981;58:460-466.Article
×