BRINZOLAMIDE

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C12H21N3O5S3
Molecular Weight	383.507
Optical Activity	UNSPECIFIED
Defined Stereocenters	1 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

SMILES

CCN[C@H]1CN(CCCOC)S(=O)(=O)C2=C1C=C(S2)S(N)(=O)=O

InChI

InChIKey=HCRKCZRJWPKOAR-JTQLQIEISA-N

InChI=1S/C12H21N3O5S3/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)/t10-/m0/s1

HIDE SMILES / InChI

Molecular Formula	C12H21N3O5S3
Molecular Weight	383.507
Charge	0
Count	MOL RATIO 1 MOL RATIO (average)

Stereochemistry	ABSOLUTE
Additional Stereochemistry	No
Defined Stereocenters	1 / 1
E/Z Centers	0
Optical Activity	UNSPECIFIED

Description

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.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Carbonic anhydrase II 88	Inhibitor 8,297		3.19 nM [IC50]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Open-angle glaucoma 51	Primary		Approved 8,429	AZOPT
Ocular hypertension 50	Primary		Approved 8,429	AZOPT

C_max

Value	Dose	Co-administered	Analyte	Population
2.17 μg/mL	3 % 3 times / day multiple, ocular		BRINZOLAMIDE blood	Homo sapiens

T_1/2

Value	Dose	Co-administered	Analyte	Population
111 day	3 % 3 times / day multiple, ocular		BRINZOLAMIDE blood	Homo sapiens

F_unbound

Value	Dose	Co-administered	Analyte	Population
40%	unknown, unknown		BRINZOLAMIDE plasma	Homo sapiens

Sourcing

Sourcing

Show entries

Vendor/Aggregator	ID	URL
ChEBI	CHEBI:3176	https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:3176
ChemicalBook	CB3458912	https://www.chemicalbook.com/ChemicalProductProperty_EN_CB3458912
MolPort	MolPort-005-940-291	https://www.molport.com/shop/molecule-link/MolPort-005-940-291
Selleck Chemicals	brinzolamide	http://www.selleckchem.com/products/brinzolamide.html
ZINC	ZINC000003953037	http://zinc15.docking.org/substances/ZINC000003953037

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PubMed

Show entries

Title	Date	PubMed
Does glaucoma medication influence the diameter of the retinal arteriole in the human eye? (A pilot study using the retinal vessel analyser).	2001	12162586
[Innovative glaucoma therapy. Glaucoma therapy with topical carbonic anhydrase inhibitors].	2001 Oct	11699313
[The role of Brinzolamide 1% ophtalmic suspension in corneal edema].	2002	12723185
Effects of topical administration of 1% brinzolamide on normal cat eyes.	2003 Dec	14641824
Carbonic anhydrase inhibitors: inhibition of the tumor-associated isozyme IX with aromatic and heterocyclic sulfonamides.	2003 Mar 24	12643899

Showing 1 to 5 of 40 entries

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Patents

Sample Use Guides

In Vivo Use Guide

One drop of 1% brinzolamide ophthalmic suspension in the affected eye(s) three times daily.

Route of Administration: Topical

In Vitro Use Guide

Protein-binding study in human plasma showed binding in the range of 58.5% to 62.7%,which was independent of brinzolamide concentration over the range of 0.01 to 10 mg/g.