Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C12H21N3O5S3.ClH |
| Molecular Weight | 419.968 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 1 / 1 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
Cl.CCN[C@H]1CN(CCCOC)S(=O)(=O)C2=C1C=C(S2)S(N)(=O)=O
InChI
InChIKey=UGAMYTZPFRXCOG-PPHPATTJSA-N
InChI=1S/C12H21N3O5S3.ClH/c1-3-14-10-8-15(5-4-6-20-2)23(18,19)12-9(10)7-11(21-12)22(13,16)17;/h7,10,14H,3-6,8H2,1-2H3,(H2,13,16,17);1H/t10-;/m0./s1
DescriptionCurator's Comment: description was created based on several sources, including:
https://www.drugs.com/mtm/brinzolamide-ophthalmic.html
http://www.rxlist.com/azopt-drug.htm
http://www.wikidoc.org/index.php/Brinzolamide
Curator's Comment: description was created based on several sources, including:
https://www.drugs.com/mtm/brinzolamide-ophthalmic.html
http://www.rxlist.com/azopt-drug.htm
http://www.wikidoc.org/index.php/Brinzolamide
Brinzolamide reduces the amount of fluid in the eye, which decreases pressure inside the eye. Brinzolamide is a carbonic anhydrase inhibitor that is FDA approved for the treatment of elevated intraocular pressure in patients with ocular hypertension or open-angle glaucoma. Common adverse reactions include abnormal taste in mouth and blurred vision. The concomitant administration of brinzolamide and oral carbonic anhydrase inhibitors is not recommended. Plus, in patients treated with oral carbonic anhydrase inhibitors, rare instances of acid-base alterations have occurred with high-dose salicylate therapy.
Originator
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: CHEMBL205 |
3.19 nM [IC50] |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Primary | AZOPT Approved UseINDICATIONS & USAGE SECTION SIMBRINZA† (brinzolamide/brimonidine tartrate ophthalmic suspension) 1%/0.2% is a fixed combination of a carbonic anhydrase inhibitor and an alpha 2 adrenergic receptor agonist indicated for the reduction of elevated intraocular pressure (IOP) in patients with open-angle glaucoma or ocular hypertension. SIMBRINZA is a fixed combination of a carbonic anhydrase inhibitor and an alpha 2 adrenergic receptor agonist indicated for the reduction of elevated intraocular pressure in patients with open-angle glaucoma or ocular hypertension. (1) Launch Date1998 |
|||
| Primary | AZOPT Approved UseINDICATIONS & USAGE SECTION SIMBRINZA† (brinzolamide/brimonidine tartrate ophthalmic suspension) 1%/0.2% is a fixed combination of a carbonic anhydrase inhibitor and an alpha 2 adrenergic receptor agonist indicated for the reduction of elevated intraocular pressure (IOP) in patients with open-angle glaucoma or ocular hypertension. SIMBRINZA is a fixed combination of a carbonic anhydrase inhibitor and an alpha 2 adrenergic receptor agonist indicated for the reduction of elevated intraocular pressure in patients with open-angle glaucoma or ocular hypertension. (1) Launch Date1998 |
Cmax
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
2.17 μg/mL |
3 % 3 times / day multiple, ocular dose: 3 % route of administration: Ocular experiment type: MULTIPLE co-administered: |
BRINZOLAMIDE blood | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
T1/2
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
111 day |
3 % 3 times / day multiple, ocular dose: 3 % route of administration: Ocular experiment type: MULTIPLE co-administered: |
BRINZOLAMIDE blood | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
Funbound
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
40% |
unknown, unknown |
BRINZOLAMIDE plasma | Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
PubMed
| Title | Date | PubMed |
|---|---|---|
| Brinzolamide : a review of its use in the management of primary open-angle glaucoma and ocular hypertension. | 2003 |
|
| Medical therapy cost considerations for glaucoma. | 2003 Jul |
|
| Effects of commercial antiglaucoma drugs to glutamate-induced [Ca2+)]i increase in cultured neuroblastoma cells. | 2003 Jun |
|
| Carbonic anhydrase inhibitors. Inhibition of tumor-associated isozyme IX by halogenosulfanilamide and halogenophenylaminobenzolamide derivatives. | 2003 May 22 |
|
| Effects of brinzolamide on aqueous humor dynamics in monkeys and rabbits. | 2003 Oct |
|
| Effect of topical brinzolamide 1% and brimonidine 0.2% on intraocular pressure after phacoemulsification. | 2004 Aug |
|
| Ocular hypotensive effect and safety of brinzolamide ophthalmic solution in open angle glaucoma patients. | 2004 May |
|
| Retinal peripapillary blood flow before and after topical brinzolamide. | 2004 Nov-Dec |
|
| Short-term ocular tolerability of dorzolamide 2% and brinzolamide 1% vs placebo in primary open-angle glaucoma and ocular hypertension subjects. | 2004 Sep |
|
| Intraocular pressure lowering effect of brinzolamide 1.0% as adjunctive therapy to latanoprost 0.005% in patients with open angle glaucoma or ocular hypertension: an uncontrolled, open-label study. | 2005 Apr |
|
| The efficacy and safety of topical brinzolamide and dorzolamide when added to the combination therapy of latanoprost and a beta-blocker in patients with glaucoma. | 2005 Apr |
|
| Effects of glaucoma drugs on ocular hemodynamics in normal tension glaucoma: a randomized trial comparing bimatoprost and latanoprost with dorzolamide [ISRCTN18873428]. | 2005 Apr 5 |
|
| [Clinical investigation: the intraocular pressure-lowering efficacy and safety of brinzolamide combined with betaxolol]. | 2005 Dec |
|
| Intraocular pressure-lowering effects of all commonly used glaucoma drugs: a meta-analysis of randomized clinical trials. | 2005 Jul |
|
| Corneal edema in glaucoma patients after the addition of brinzolamide 1% ophthalmic suspension. | 2005 Jul-Aug |
|
| Water-drinking test in patients with primary open-angle glaucoma while treated with different topical medications. | 2005 Jun |
|
| Prediction of genotoxicity of chemical compounds by statistical learning methods. | 2005 Jun |
|
| Medical control of intraocular pressure after phacoemulsification. | 2005 Mar |
|
| Brinzolamide induced reversible corneal decompensation. | 2005 Mar |
|
| Comparing the effects of travoprost and brinzolamide on intraocular pressure after phacoemulsification. | 2005 Mar |
|
| The efficacy and ocular discomfort of substituting brinzolamide for dorzolamide in combination therapy with latanoprost, timolol, and dorzolamide. | 2005 Oct |
|
| Carbonic anhydrase inhibitors: inhibition of the transmembrane isozyme XIV with sulfonamides. | 2005 Sep 1 |
|
| [Therapeutic difficulties in neovascular glaucoma]. | 2006 |
|
| [Combined therapy in glaucoma treatment: travoprost 0.004% and brinzolamid]. | 2006 |
|
| A randomized, investigator-masked, 4-week study comparing timolol maleate 0.5%, brinzolamide 1%, and brimonidine tartrate 0.2% as adjunctive therapies to travoprost 0.004% in adults with primary open-angle glaucoma or ocular hypertension. | 2006 Apr |
|
| Carbonic anhydrase inhibitors: cloning and sulfonamide inhibition studies of a carboxyterminal truncated alpha-carbonic anhydrase from Helicobacter pylori. | 2006 Apr 15 |
|
| A comparative study on the cost of new antibiotics and drugs of other therapeutic categories. | 2006 Dec 20 |
|
| Effects of antiglaucoma drugs on calcium mobility in cultured corneal endothelial cells. | 2006 Feb |
|
| Topical brinzolamide and metabolic acidosis. | 2006 Feb |
|
| Switching from dorzolamide to brinzolamide: effect on intraocular pressure and patient comfort. | 2006 Jan-Feb |
|
| Carbonic anhydrase inhibitors: DNA cloning and inhibition studies of the alpha-carbonic anhydrase from Helicobacter pylori, a new target for developing sulfonamide and sulfamate gastric drugs. | 2006 Mar 23 |
|
| Screening for drug-induced spoliation of the hydrogel optic of the AlphaCor artificial cornea. | 2006 May |
|
| The in vitro effects of some pesticides on carbonic anhydrase activity of Oncorhynchus mykiss and Cyprinus carpio carpio fish. | 2006 May 20 |
|
| The efficacy and safety of timolol maleate versus brinzolamide each given twice daily added to travoprost in patients with ocular hypertension or primary open-angle glaucoma. | 2006 Nov-Dec |
|
| [Blurred vision after instillation of topical carbonic anhydrase inhibitor]. | 2006 Sep |
|
| Ocular hypotensive efficacy and safety of brinzolamide ophthalmic suspension 1% added to travoprost ophthalmic solution 0.004% therapy in patients with open-angle glaucoma or ocular hypertension. | 2006 Sep |
|
| Brinzolamide 1% versus apraclonidine 0.5% to prevent intraocular pressure elevation after neodymium:YAG laser posterior capsulotomy. | 2006 Sep |
|
| The development of topically acting carbonic anhydrase inhibitors as anti-glaucoma agents. | 2007 |
|
| Influence of ocular hypotensive eyedrops on intraocular pressure fluctuation with postural change in eyes with normal-tension glaucoma. | 2007 Apr |
|
| Carbonic anhydrase inhibitors. DNA cloning, characterization, and inhibition studies of the human secretory isoform VI, a new target for sulfonamide and sulfamate inhibitors. | 2007 Jan 25 |
|
| Comparison of the ocular hypotensive efficacy of adjunctive brimonidine 0.15% or brinzolamide 1% in combination with travoprost 0.004%. | 2007 Jul |
|
| Effect of concomitant use of latanoprost and brinzolamide on 24-hour variation of IOP in normal-tension glaucoma. | 2007 Jun-Jul |
|
| Cellular cytotoxicity of antiglaucoma drugs in cultured corneal endothelial cells. | 2007 Mar |
|
| Comparison of ocular hypotensive effect and safety of brinzolamide and timolol added to latanoprost. | 2008 Apr-May |
|
| Tear film and ocular surface alterations in chronic users of antiglaucoma medications. | 2008 Jan-Feb |
|
| Intraocular pressure reduction with travoprost/timolol fixed combination, with and without adjunctive brinzolamide, in glaucoma. | 2008 Jun |
|
| Efficacy of brinzolamide and levobetaxolol in pediatric glaucomas: a randomized clinical trial. | 2008 Jun |
|
| Advanced juvenile open-angle glaucoma in an 8-year-old Haitian girl. | 2008 Mar |
|
| Brimonidine purite 0.1% versus brinzolamide 1% as adjunctive therapy to latanoprost in patients with glaucoma or ocular hypertension. | 2008 May |
|
| Short-term effect of topical brinzolamide on human central corneal thickness. | 2008 May-Jun |
Sample Use Guides
One drop of 1% brinzolamide ophthalmic suspension in the affected eye(s) three times daily.
Route of Administration:
Topical
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N36YTS80H4
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11711447
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m2652
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DTXSID40164655
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150937-43-2
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300000033932
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SUBSTANCE RECORD
