Topical brimonidine 0.2%/timolol 0.5% ophthalmic solution: in glaucoma and ocular hypertension

Drugs Aging. 2006;23(9):753-61. doi: 10.2165/00002512-200623090-00005.

Abstract

A fixed combination of brimonidine (a highly selective alpha(2)-adrenergic agonist) and timolol (a non-selective beta-blocker) [brimonidine 0.2%/timolol 0.5% ophthalmic solution; brimonidine/timolol] is available for the topical treatment of glaucoma and ocular hypertension (OH). Brimonidine and timolol decrease elevated intraocular pressure (IOP) by complementary mechanisms of action and have an additive effect when coadministered to healthy volunteers and patients with glaucoma or OH. When assessed over a 3- or 12-month period in large, well designed clinical studies, brimonidine/timolol instilled twice daily (one drop in each eye) was superior to monotherapy with the individual components instilled two (brimonidine) or three (timolol) times daily, and noninferior to concomitant therapy with the individual components instilled twice daily, in lowering raised IOP in patients with glaucoma or OH. In small, randomised, comparative studies of 1 or 3 months' duration, the IOP-lowering effect of brimonidine/timolol twice daily was similar or superior to that of fixed combination dorzolamide 2%/timolol 0.5% ophthalmic solution (dorzolamide/timolol) twice daily (preliminary data). Brimonidine/timolol is generally well tolerated with a predictable local and systemic adverse event profile based on that of the individual components used alone and concomitantly. No unexpected or serious adverse events associated with the fixed combination were reported in key clinical trials. Brimonidine/timolol may be advantageous over dorzolamide/timolol with respect to ocular tolerability and comfort (preliminary data).

Publication types

  • Review

MeSH terms

  • Antihypertensive Agents* / administration & dosage
  • Antihypertensive Agents* / adverse effects
  • Antihypertensive Agents* / pharmacokinetics
  • Antihypertensive Agents* / therapeutic use
  • Brimonidine Tartrate
  • Clinical Trials as Topic
  • Drug Therapy, Combination
  • Glaucoma, Open-Angle / drug therapy*
  • Humans
  • Ocular Hypertension / drug therapy*
  • Ophthalmic Solutions* / administration & dosage
  • Ophthalmic Solutions* / adverse effects
  • Ophthalmic Solutions* / pharmacokinetics
  • Ophthalmic Solutions* / therapeutic use
  • Quinoxalines* / administration & dosage
  • Quinoxalines* / adverse effects
  • Quinoxalines* / pharmacokinetics
  • Quinoxalines* / therapeutic use
  • Timolol* / administration & dosage
  • Timolol* / adverse effects
  • Timolol* / pharmacokinetics
  • Timolol* / therapeutic use
  • Treatment Outcome

Substances

  • Antihypertensive Agents
  • Ophthalmic Solutions
  • Quinoxalines
  • Brimonidine Tartrate
  • Timolol