Drugs & Aging

, Volume 26, Issue 5, pp 437–446 | Cite as


In Open-Angle Glaucoma and Ocular Hypertension
  • Jamie D. CroxtallEmail author
  • Lesley J. Scott
Adis Drug Profile


▲ Brinzolamide 1%/timolol 0.5% fixed combination (brinzolamide/timolol) is a twice-daily eyedrops suspension comprising the carbonic anhydrase-II inhibitor brinzolamide and the β-adrenergic receptor antagonist timolol.

▲ Brinzolamide/timolol produced clinically relevant reductions in mean intraocular pressure (IOP) from baseline and was more effective than brinzolamide or timolol monotherapy in lowering IOP in a 6-month, randomized, phase III trial in patients with open-angle glaucoma or ocular hypertension (n = 523). The proportion of patients achieving a mean IOP of <18 mmHg was significantly greater in recipients of brinzolamide/timolol than in recipients of brinzolamide or timolol monotherapy.

▲ The IOP-lowering efficacy of brinzolamide/timolol was maintained for up to 12 months, and was no less effective than dorzolamide 2%/timolol 0.5% solution (dorzolamide/timolol) in a randomized, phase III, noninferiority trial (n = 437).

▲ Brinzolamide/timolol was generally well tolerated and was associated with significantly lower ocular discomfort scores than dorzolamide/timolol. Moreover, a significantly greater number of patients expressed a preference for brinzolamide/timolol over dorzolamide/timolol. The main ocular adverse event was blurred vision, and was not considered to be a safety issue.


Glaucoma Retinal Nerve Fibre Layer Aqueous Humour Timolol Ocular Hypertension 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.


Acknowledgements and Disclosures

This manuscript was reviewed by: G. Manni, Ophthalmology Department, University of Roma, Roma, Italy; F. Ziemssen, University Eye Hospital, Centre of Ophthalmology, Eberhard Karl University, Tuebingen, Germany

The preparation of this review was not supported by any external funding. During the peer review process, the manufacturer of the agent under review was offered an opportunity to comment on this article. Changes resulting from comments received were made on the basis of scientific and editorial merit.


  1. 1.
    Resnikoff S, Pascolini D, Etya’ale D, et al. Global data on visual impairment in the year 2002. Bull World Health Organ 2004; 82(11): 844–51PubMedGoogle Scholar
  2. 2.
    Glaucoma Research Foundation. African-Americans and glaucoma [online]. Available from URL: [Accessed 2009 Feb 12]
  3. 3.
    Muñoz B, West S, Rubin G, et al. Causes of blindness and visual impairment in a population of older Americans. Arch Ophthalmol 2000; 118(6): 819–25PubMedGoogle Scholar
  4. 4.
    Goldberg L. Clinical guidelines for the treatment of glaucoma. Manag Care 2002; 11(11): 16–24PubMedGoogle Scholar
  5. 5.
    Fechtner RD, Khouri AS. Evolving global risk assessment of ocular hypertension to glaucoma. Curr Opin Ophthalmol 2007; 18(2): 104–9PubMedCrossRefGoogle Scholar
  6. 6.
    Glaucoma Research Foundation. Are you at risk for glaucoma? [online]. Available from URL: [Accessed 2009 Feb 12]
  7. 7.
    The Eye Digest: University of Illinois Eye & Ear Infirmary. Glaucoma causes optic nerve cupping (atrophy) and vision loss [online]. Available from URL: [Accessed 2009 Feb 13]
  8. 8.
    Foster A, Johnson G. Magnitude and causes of blindness in the developing world. Int Ophthalmol 1990; 14(3): 135–40PubMedCrossRefGoogle Scholar
  9. 9.
    Klaver C, Wolfs R, Vingerling J, et al. Age-specific prevalence and causes of blindness in an older population. Arch Ophthalmol 1998; 116(5): 653–8PubMedGoogle Scholar
  10. 10.
    Forsman E, Kivela T, Vesti E. Lifetime visual disability in open-angle glaucoma and ocular hypertension. J Glaucoma 2007; 16(3): 313–9PubMedCrossRefGoogle Scholar
  11. 11.
    The Royal College of Ophthalmologists. A national research strategy for ophthalmology (March 2002) [online]. Available from URL: [Accessed 2009 Feb 5]
  12. 12.
    European Glaucoma Society. Terminology and guidelines for glaucoma. 3rd ed. Savona, Italy: Dogma, 2008Google Scholar
  13. 13.
    Japan Glaucoma Society. Guidelines for glaucoma [online]. Available from URL: [Accessed 2009 Feb 13]
  14. 14.
    Kass M, Heuer D, Higginbotham E, et al. The ocular hypertension treatment study: a randomized trial determines that topical ocular hypotensive medication delays prevents the onset of open-angle glaucoma. Arch Ophthalmol 2002; 120(6): 701–13PubMedCrossRefGoogle Scholar
  15. 15.
    Geringer C, Imami N. Medical management of glaucoma. Int Ophthamol Clin 2008; 48(4): 115–41CrossRefGoogle Scholar
  16. 16.
    International Council of Ophthalmology. Primary open-angle glaucoma (initial evaluation) [online]. Available from URL: [Accessed 2009 Feb 13]
  17. 17.
    Fechtner R, Realini T. Fixed combinations of topical glaucoma medications. Curr Opin Ophtahalmol 2004; 15(2): 132–5CrossRefGoogle Scholar
  18. 18.
    Cvetkovic RS, Perry CM. Brinzolamide: a review of its use in the management of primary open-angle glaucoma and ocular hypertension. Drugs Aging 2003; 20(12): 919–47PubMedCrossRefGoogle Scholar
  19. 19.
    Iester M. Brinzolamide. Expert Opin. Pharmacother 2008; 9(4): 653–62Google Scholar
  20. 20.
    DeSantis L. Preclinical overview of brinzolamide. Surv Opthalmol 2000; 44(Suppl. 2): S119–29CrossRefGoogle Scholar
  21. 21.
    Heel R, Brogden R, Speight T, et al. Timolol: a review of its therapeutic efficacy in the topical treatment of glaucoma. Drugs 1979; 17(1): 38–55PubMedCrossRefGoogle Scholar
  22. 22.
    Han JA, Frishman WH, Wu Sun S, et al. Cardiovascular and respiratory considerations with pharmacotherapy of glaucoma and ocular hypertension. Cardiol Rev 2008; 16(2): 95–108PubMedCrossRefGoogle Scholar
  23. 23.
    March W, Ochsner K. The long-term safety and efficacy of brinzolamide 1.0% (Azopt) in patients with primary open-angle glaucoma or ocular hypertension. Brinzolamide Long-Term Therapy Study Group. Am J Ophthalmol 2000; 129(2): 136–43PubMedCrossRefGoogle Scholar
  24. 24.
    European Agency for the Evaluation of Medicinal Products. Brinzolamide/timolol: summary of product characteristics [online]. Available from URL: [Accessed 2009 Feb 2]
  25. 25.
    Kaup M, Plange N, Niegel M, et al. Effects of brinzolamide on ocular haemodynamics in healthy volunteers. Br J Ophthalmol 2004; 88(2): 257–62PubMedCrossRefGoogle Scholar
  26. 26.
    Izzotti A, Saccà S, Di Marco B, et al. Antioxidant activity of timolol on endothelial cells and its relevance for glaucoma course. Eye 2008; 22(3): 445–53PubMedCrossRefGoogle Scholar
  27. 27.
    Kiland J, Gabelt B, Kaufman P. Studies on the mechanism of action of timolol and the effects and redirection of aqueous flow on outflow facility. Exp Eye Res 2004; 78(3): 639–51PubMedCrossRefGoogle Scholar
  28. 28.
    Korte J, Kaila T, Saari K, et al. Systemic bioavailability and cardiopulmonary effects of 0.5% timolol eyedrops. Graefes Arch Clin Exp Ophthalmol 2002; 240(6): 430–5PubMedCrossRefGoogle Scholar
  29. 29.
    Manni G, Denis P, Chew P, et al. The safety and efficacy of brinzolamide 1%/timolol 0.5% fixed combination versus dorzolamide 2%/timolol 0.5% in patients with open-angle glaucoma or ocular hypertension. J Glaucoma 2009; 18(4): 293–300PubMedCrossRefGoogle Scholar
  30. 30.
    Kaback M, Scoper SV, Arzeno G, et al. Intraocular pressure-lowering efficacy of brinzolamide 1%/timolol 0.5% fixed combination compared with brinzolamide 1 % and timolol 0.5%. Ophthalmology 2008; 115(10): 1728–34PubMedCrossRefGoogle Scholar
  31. 31.
    Vold SD, Evans RM, Stewart RH, et al. A one-week comfort study of BID-dosed brinzolamide 1%/timolol 0.5% ophthalmic suspension fixed combination compared to BID-dosed dorzolamide 2%/timolol 0.5% ophthalmic in patients with open-angle glaucoma or ocular hypertension. J Ocul Pharmacol Ther 2008; 24(6): 601–5PubMedCrossRefGoogle Scholar
  32. 32.
    Mundorf TK, Rauchman SH, Williams RD, et al. A patient preference comparison of Azarga™ (brinzolamide/timolol fixed combination) vs Cosopt® (dorzolamide/timolol fixed combination) in patients with open-angle glaucoma or ocular hypertension. Clin Ophthalmol 2008; 2(3): 623–8PubMedGoogle Scholar

Copyright information

© Adis Data Information BV 2009

Authors and Affiliations

  1. 1.Wolters Kluwer Health | AdisMairangi Bay, North Shore 0754, AucklandNew Zealand
  2. 2.Wolters Kluwer HealthPhiladelphiaUSA

Personalised recommendations