Brinzolamide

Brinzolamide
Black Box Warning
Adult Indications & Dosage
Pediatric Indications & Dosage
Contraindications
Warnings & Precautions
Adverse Reactions
Drug Interactions
Use in Specific Populations
Administration & Monitoring
Overdosage
Pharmacology
Clinical Studies
How Supplied
Images
Patient Counseling Information
Precautions with Alcohol
Brand Names
Look-Alike Names

Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]; Associate Editor(s)-in-Chief: Gerald Chi

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Black Box Warning

Title See full prescribing information for complete Boxed Warning. ConditionName: Content

Overview

Brinzolamide is a that is FDA approved for the {{{indicationType}}} of . There is a Black Box Warning for this drug as shown here. Common adverse reactions include .

Adult Indications and Dosage

FDA-Labeled Indications and Dosage (Adult)

Condition1

• Dosing Information

• Dosage

Condition2

• Dosing Information

• Dosage

Condition3

• Dosing Information

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Condition4

• Dosing Information

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Off-Label Use and Dosage (Adult)

Guideline-Supported Use

Condition1

• Developed by:

• Class of Recommendation:

• Strength of Evidence:

• Dosing Information

• Dosage

Condition2

There is limited information regarding Off-Label Guideline-Supported Use of Brinzolamide in adult patients.

Non–Guideline-Supported Use

Condition1

• Dosing Information

• Dosage

Condition2

There is limited information regarding Off-Label Non–Guideline-Supported Use of Brinzolamide in adult patients.

Pediatric Indications and Dosage

FDA-Labeled Indications and Dosage (Pediatric)

Condition1

• Dosing Information

• Dosage

Condition2

There is limited information regarding FDA-Labeled Use of Brinzolamide in pediatric patients.

Off-Label Use and Dosage (Pediatric)

Guideline-Supported Use

Condition1

• Developed by:

• Class of Recommendation:

• Strength of Evidence:

• Dosing Information

• Dosage

Condition2

There is limited information regarding Off-Label Guideline-Supported Use of Brinzolamide in pediatric patients.

Non–Guideline-Supported Use

Condition1

• Dosing Information

• Dosage

Condition2

There is limited information regarding Off-Label Non–Guideline-Supported Use of Brinzolamide in pediatric patients.

Contraindications

• Condition1

Warnings

Title See full prescribing information for complete Boxed Warning. ConditionName: Content

Description

Adverse Reactions

Clinical Trials Experience

There is limited information regarding Clinical Trial Experience of Brinzolamide in the drug label.

Central Nervous System

Cardiovascular

Respiratory

Gastrointestinal

Hypersensitivity

Miscellaneous

Postmarketing Experience

There is limited information regarding Postmarketing Experience of Brinzolamide in the drug label.

Central Nervous System

Cardiovascular

Respiratory

Gastrointestinal

Hypersensitivity

Miscellaneous

Drug Interactions

• Drug

• Description

Use in Specific Populations

Pregnancy

Pregnancy Category (FDA):

• Pregnancy Category B

Pregnancy Category (AUS):

• Australian Drug Evaluation Committee (ADEC) Pregnancy Category

There is no Australian Drug Evaluation Committee (ADEC) guidance on usage of Brinzolamide in women who are pregnant.

Labor and Delivery

There is no FDA guidance on use of Brinzolamide during labor and delivery.

Nursing Mothers

There is no FDA guidance on the use of Brinzolamide with respect to nursing mothers.

Pediatric Use

There is no FDA guidance on the use of Brinzolamide with respect to pediatric patients.

Geriatic Use

There is no FDA guidance on the use of Brinzolamide with respect to geriatric patients.

Gender

There is no FDA guidance on the use of Brinzolamide with respect to specific gender populations.

Race

There is no FDA guidance on the use of Brinzolamide with respect to specific racial populations.

Renal Impairment

There is no FDA guidance on the use of Brinzolamide in patients with renal impairment.

Hepatic Impairment

There is no FDA guidance on the use of Brinzolamide in patients with hepatic impairment.

Females of Reproductive Potential and Males

There is no FDA guidance on the use of Brinzolamide in women of reproductive potentials and males.

Immunocompromised Patients

There is no FDA guidance one the use of Brinzolamide in patients who are immunocompromised.

Administration and Monitoring

Administration

Oral

Intravenous

Monitoring

There is limited information regarding Monitoring of Brinzolamide in the drug label.

Condition1

Description

IV Compatibility

There is limited information regarding IV Compatibility of Brinzolamide in the drug label.

Overdosage

Acute Overdose

Signs and Symptoms

Description

Management

Description

Chronic Overdose

There is limited information regarding Chronic Overdose of Brinzolamide in the drug label.

Pharmacology

Template:Px
Brinzolamide
Systematic (IUPAC) name
(5R)-5-ethylamino-3-(3-methoxypropyl)- 2,2-dioxo-2λ6,9-dithia- 3-azabicyclo[4.3.0]nona-7,10-diene- 8-sulfonamide
Identifiers
CAS number	138890-62-7
ATC code	S01EC04
PubChem	68844
DrugBank	DB01194
Chemical data
Formula	Template:OrganicBox atomTemplate:OrganicBox atomTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBox atomTemplate:OrganicBoxTemplate:OrganicBox atomTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBox atomTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBox
Mol. mass	383.51 g/mol
SMILES	eMolecules & PubChem
Pharmacokinetic data
Bioavailability	Absorbed systemically, but below detectable levels (less than 10 ng/mL)
Protein binding	~60%
Metabolism	?
Half life	111 days
Excretion	Renal (60%)
Therapeutic considerations
Licence data	EU, US
Pregnancy cat.	C(US)
Legal status	[[Prescription drug|Template:Unicode-only]](US)
Routes	Ophthalmic

Mechanism of Action

• 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), found primarily in red blood cells (RBCs), but also in other tissues. 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 (IOP).

• AZOPT® (brinzolamide ophthalmic suspension) 1% contains brinzolamide, an inhibitor of carbonic anhydrase II (CA-II). Following topical ocular administration, brinzolamide inhibits aqueous humor formation and reduces elevated intraocular pressure. Elevated intraocular pressure is a major risk factor in the pathogenesis of optic nerve damage and glaucomatous visual field loss.

Structure

• AZOPT® (brinzolamide ophthalmic suspension) 1% contains a carbonic anhydrase inhibitor formulated for multidose topical ophthalmic use. Brinzolamide is described chemically as: (R)-(+)-4-Ethylamino-2-(3-methoxypropyl)-3,4-dihydro-2H-thieno [3,2-e]-1,2-thiazine-6-sulfonamide-1,1- dioxide. Its empirical formula is C12H21N3O5S3, and its structural formula is:

This image is provided by the National Library of Medicine.

• Brinzolamide has a molecular weight of 383.5 and a melting point of about 131°C. It is a white powder, which is insoluble in water, very soluble in methanol and soluble in ethanol.

• AZOPT® (brinzolamide ophthalmic suspension) 1% is supplied as a sterile, aqueous suspension of brinzolamide which has been formulated to be readily suspended and slow settling, following shaking. It has a pH of approximately 7.5 and an osmolality of 300 mOsm/kg.

• Each mL of AZOPT® (brinzolamide ophthalmic suspension) 1% contains: Active ingredient: brinzolamide 10 mg. Preservative: Benzalkonium chloride 0.1 mg. Inactives: mannitol, carbomer 974P, tyloxapol, edetate disodium, sodium chloride, purified water, with hydrochloric acid and/or sodium hydroxide to adjust pH.

Pharmacodynamics

There is limited information regarding Pharmacodynamics of Brinzolamide in the drug label.

Pharmacokinetics

• Following topical ocular administration, brinzolamide is absorbed into the systemic circulation. Due to its affinity for CA-II, brinzolamide distributes extensively into the RBCs and exhibits a long half-life in whole blood (approximately 111 days). In humans, the metabolite N-desethyl brinzolamide is formed, which also binds to CA and accumulates in RBCs. This metabolite binds mainly to CA-I in the presence of brinzolamide. In plasma, both parent brinzolamide and N-desethyl brinzolamide concentrations are low and generally below assay quantitation limits (<10 ng/mL). Binding to plasma proteins is approximately 60%. Brinzolamide is eliminated predominantly in the urine as unchanged drug. N-Desethyl brinzolamide is also found in the urine along with lower concentrations of the N-desmethoxypropyl and O-desmethyl metabolites.

• An oral pharmacokinetic study was conducted in which healthy volunteers received 1 mg capsules of brinzolamide twice per day for up to 32 weeks. This regimen approximates the amount of drug delivered by topical ocular administration of AZOPT® (brinzolamide ophthalmic suspension) 1% dosed to both eyes three times per day and simulates systemic drug and metabolite concentrations similar to those achieved with long-term topical dosing. RBC CA activity was measured to assess the degree of systemic CA inhibition. Brinzolamide saturation of RBC CA-II was achieved within 4 weeks (RBC concentrations of approximately 20 μM). N-Desethyl brinzolamide accumulated in RBCs to steady-state within 20-28 weeks reaching concentrations ranging from 6-30 μM. The inhibition of CA-II activity at steady-state was approximately 70-75%, which is below the degree of inhibition expected to have a pharmacological effect on renal function or respiration in healthy subjects.

Nonclinical Toxicology

There is limited information regarding Nonclinical Toxicology of Brinzolamide in the drug label.

Clinical Studies

There is limited information regarding Clinical Studies of Brinzolamide in the drug label.

Condition1

Description

How Supplied

There is limited information regarding Brinzolamide How Supplied in the drug label.

Storage

There is limited information regarding Brinzolamide Storage in the drug label.

Images

Drug Images

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Package and Label Display Panel

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Patient Counseling Information

There is limited information regarding Patient Counseling Information of Brinzolamide in the drug label.

Precautions with Alcohol

Alcohol-Brinzolamide interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication.

Brand Names

There is limited information regarding Brinzolamide Brand Names in the drug label.

Look-Alike Drug Names

• A® — B®

Drug Shortage Status

Price

References

The contents of this FDA label are provided by the National Library of Medicine.

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