About: Brinzolamide     Goto   Sponge   NotDistinct   Permalink

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http://linked.open...gbank/description
  • Brinzolamide is a highly specific, non-competitive, reversible carbonic anhydrase inhibitor. Carbonic anhydrase (CA) is an enzyme found in many tissues of the body including the eye. It catalyzes the reversible reaction involving the hydration of carbon dioxide and the dehydration of carbonic acid. In humans, carbonic anhydrase exists as a number of isoenzymes, the most active being carbonic anhydrase II (CA-II). Inhibition of carbonic anhydrase in the ciliary processes of the eye decreases aqueous humor secretion, presumably by slowing the formation of bicarbonate ions with subsequent reduction in sodium and fluid transport. The result is a reduction in intraocular pressure. Brinzolamide is indicated in the treatment of elevated intraocular pressure in patients with ocular hypertension or open-angle glaucoma. (en)
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http://linked.open...generalReferences
  • # Ermis SS, Ozturk F, Inan UU: Comparing the effects of travoprost and brinzolamide on intraocular pressure after phacoemulsification. Eye. 2005 Mar;19(3):303-7. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/15258611 # Iester M, Altieri M, Michelson G, Vittone P, Traverso CE, Calabria G: Retinal peripapillary blood flow before and after topical brinzolamide. Ophthalmologica. 2004 Nov-Dec;218(6):390-6. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/15564757 # Kaup M, Plange N, Niegel M, Remky A, Arend O: Effects of brinzolamide on ocular haemodynamics in healthy volunteers. Br J Ophthalmol. 2004 Feb;88(2):257-62. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/14736787 # Iester M: Brinzolamide ophthalmic suspension: a review of its pharmacology and use in the treatment of open angle glaucoma and ocular hypertension. Clin Ophthalmol. 2008 Sep;2(3):517-23. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/19668749 # DeSantis L: Preclinical overview of brinzolamide. Surv Ophthalmol. 2000 Jan;44 Suppl 2:S119-29. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/10665514 (en)
http://linked.open...gy/drugbank/group
  • approved (en)
http://linked.open...drugbank/halfLife
  • 111 days (en)
http://linked.open...ugbank/indication
  • For the treatment of elevated intraocular pressure in patients with ocular hypertension or open-angle glaucoma. (en)
sameAs
Title
  • Brinzolamide (en)
adms:identifier
http://linked.open...mechanismOfAction
  • Brinzolamide is a highly specific inhibitor of CA-II, which is the main CA isoenzyme involved in the secretion of aqueous humor. Inhibition of CA in the ciliary process of the eye slows the formation of bicarbonate, and reduces sodium and fluid transport. This results in a reduction in the rate of aqueous humor secretion and the intraocular pressure. Brinzolamide is absorbed systemically following topical ocular administration. Since it has a high affinity for CA-II, brinzolamide binds extensively to red blood cells, where CA-II is primarily found. As sufficient CA-II activity remains, adverse effects resulting from the systemic inhibition of CA by brinzolamide are not observed. The metabolite N-desethyl brinzolamide is also formed. This metabolite binds to CA and accumulates in red blood cells as well. In the presence of brinzolamide, the metabolite binds mainly to carbonic anhydrase I (CA-I). (en)
http://linked.open...drugbank/packager
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  • Brinzolamide (en)
  • Azopt (en)
http://linked.open.../drug/hasAHFSCode
http://linked.open...nk/proteinBinding
  • Approximately 60%. (en)
http://linked.open...ynthesisReference
  • Alessandro Falchi, Ottorino De Lucchi, Andrea Castellin, "PROCESS FOR THE PREPARATION OF BRINZOLAMIDE." U.S. Patent US20110118461, issued May 19, 2011. (en)
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  • Absorbed into systemic circulation following topical ocular application (en)
http://linked.open.../affectedOrganism
  • Humans and other mammals (en)
http://linked.open...casRegistryNumber
  • 138890-62-7 (en)
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  • (en)
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