Bromfenac sodium hydrate
[CAS# 120638-55-3]

Identification

• Classification: API >> Nervous system medication
• Name: Bromfenac sodium hydrate
• Synonyms: Sodium (2-amino-3-(4-bromobenzoyl)phenyl)acetate hydrate
• Molecular Formula: 2(C₁₅H₁₁BrNNaO₃).3(H₂O)
• Molecular Weight: 766.34
• CAS Registry Number: 120638-55-3
• EC Number: 695-342-6
• SMILES: C1=CC(=C(C(=C1)C(=O)C2=CC=C(C=C2)Br)N)CC(=O)[O-].C1=CC(=C(C(=C1)C(=O)C2=CC=C(C=C2)Br)N)CC(=O)[O-].O.O.O.[Na+].[Na+]

Safety Data

• Hazard Symbols: GHS06;GHS08;GHS09 Danger
• Risk Statements: H300-H360-H371-H372-H400
• Safety Statements: P203-P260-P264-P270-P273-P280-P301+P316-P308+P316-P318-P319-P321-P330-P391-P405-P501

Hazard Classification

Hazard	Class	Category Code	Hazard Statement
Acute toxicity	Acute Tox.	2	H300
Specific target organ toxicity - repeated exposure	STOT RE	1	H372
Reproductive toxicity	Repr.	1B	H360
Specific target organ toxicity - single exposure	STOT SE	2	H371
Acute hazardous to the aquatic environment	Aquatic Acute	1	H400

Discovery and Applications

Bromfenac sodium hydrate is the sodium salt hydrate form of bromfenac, a nonsteroidal anti-inflammatory drug (NSAID) belonging to the class of brominated phenylacetic acids. The discovery of bromfenac traces back to efforts in the late 20th century aimed at improving the therapeutic profile of earlier NSAIDs by enhancing potency and reducing gastrointestinal side effects. Researchers introduced a bromine atom onto the phenylacetic acid scaffold, which enhanced both the lipophilicity and anti-inflammatory efficacy of the molecule.

Bromfenac sodium hydrate exhibits its primary pharmacological activity by inhibiting cyclooxygenase (COX) enzymes, specifically COX-2, leading to a reduction in prostaglandin synthesis. This mechanism of action underlies its effectiveness in reducing inflammation and pain. The bromine substitution plays a significant role by increasing the drug's affinity for the COX-2 enzyme, thus improving its therapeutic selectivity and reducing adverse effects typically associated with nonselective NSAID use.

The most prominent application of bromfenac sodium hydrate is in ophthalmology. It is commonly formulated as an ophthalmic solution for the treatment of postoperative inflammation and reduction of ocular pain following cataract surgery. Its enhanced lipophilicity facilitates greater penetration into ocular tissues, providing effective anti-inflammatory action at the site of administration. In clinical settings, bromfenac sodium hydrate is valued for its once-daily dosing regimen, offering greater convenience and improved patient compliance compared to other ophthalmic NSAIDs that require more frequent administration.

Beyond its primary use in ophthalmic inflammation, bromfenac sodium hydrate has also been investigated for potential application in other inflammatory ocular conditions, such as age-related macular degeneration and diabetic macular edema. However, its use remains largely centered around postoperative inflammation management. It is generally well tolerated, with reported side effects being mild and primarily localized to the eye, such as transient irritation or a burning sensation upon administration.

The development of bromfenac sodium hydrate reflects the broader pharmaceutical trend of refining chemical structures to achieve improved clinical performance. Its introduction into clinical practice provided ophthalmologists with an effective and convenient tool for managing inflammation and pain, contributing to better surgical outcomes and enhanced patient recovery experiences. Bromfenac sodium hydrate continues to be widely prescribed globally under various brand names, affirming its established role in modern ophthalmic care.

References

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