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| Clinical data | |
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| Trade names | Bromday, Prolensa (US), Yellox (EU) |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a611018 |
| License data | |
| Routes of administration | Eye drops |
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| Pharmacokinetic data | |
| Protein binding | 99.8% |
| Metabolism | CYP2C9 |
| Metabolites | Lactam, others |
| Eliminationhalf-life | 1.4 hours inaqueous humour |
| Excretion | 82% urine, 13%faeces |
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| Chemical and physical data | |
| Formula | C15H12BrNO3 |
| Molar mass | 334.169 g·mol−1 |
| 3D model (JSmol) | |
| Melting point | 284 to 286 °C (543 to 547 °F) (bromfenac sodium·1.5H2O) |
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Bromfenac is anonsteroidal anti-inflammatory drug (NSAID)[2] marketed in the US as anophthalmic solution (brand namesProlensa andBromday,[3] prior formulation brand nameXibrom, which has since been discontinued) byISTA Pharmaceuticals for short-term, local use. Prolensa and Bromday are the once-daily formulation of bromfenac, while Xibrom was approved for twice-daily administration. In the European Union, the brand name isYellox. Bromfenac is indicated for the treatment of ocular inflammation and pain aftercataract surgery.[4]
Bromfenac isindicated for the treatment of postoperative ocular inflammation following cataract extraction.[5][6]
The drug has been shown to reducemacular edema and thickness of theretina (an indicator for inflammation) and improve visual acuity after surgery.[7]
Bromfenac is contraindicated for people with adverse reactions to NSAIDs, such as asthma or rashes.[4][8]
Bromfenac eye drops are generally well tolerated. Comparatively common side effects in clinical studies included abnormal sensations in eye (0.5% of people treated with bromfenac), mild to moderate erosion of thecornea (0.4%), eyepruritus (0.4%), eye pain (0.3%) and redness (0.3%). Serious side effects such ascorneal perforation were not reported in studies but only during post-marketing in less than one patient in 1000.[4][8]
No systematic interaction studies have been performed. There are no known cases of interactions with antibiotic eye drops.[4][8]Blood plasma levels remain very low during bromfenac therapy, so interactions with drugs taken by mouth are unlikely.
As an NSAID, bromfenac works by inhibitingprostaglandin synthesis by blocking thecyclooxygenase (COX) enzymes. It preferably acts onCOX-2 and only has a low affinity forCOX-1.[8]
Bromfenac is well absorbed through the cornea and reaches highest concentrations in theaqueous humour after 150 to 180 minutes, with abiological half-life of 1.4 hours and high drug levels being maintained for at least 12 hours. It is mainly concentrated in the aqueous humour andconjunctiva, and much less in thelens andvitreous body.[4][8]
Concentrations in the blood plasma are too low to be measured quantitatively. 99.8% of the substance are bound to plasma proteins. The enzyme mainly responsible formetabolization of bromfenac isCYP2C9, and metabolites include thelactam and severalconjugated compounds. 82% are excreted via the urine, and 13% via thefaeces.[4][8]
Compared toamfenac, the halogenation of bromfenac's chemical structure (thebromine atom at C4) increases its penetration into ocular tissues, and increases its potency for COX enzyme inhibition.[7][9]
Along withindomethacin,diclofenac and others, bromfenac belongs to the acetic acid group of NSAIDs. It is used in form of bromfenac sodium · 1.5H2O (CAS number:120638-55-3 ), which is soluble in water,methanol and aqueous bases, insoluble inchloroform and aqueous acids, and melts at 284 to 286 °C (543 to 547 °F) under decomposition.[10]
For ophthalmic use, bromfenac has been prescribed more than 20,000,000 times across the world.[8] As an eye drop, it has been available since 2000, starting in Japan where it was sold asBronuck.[11] It was first FDA approved for use in the United States in 2005, and it was marketed asXibrom, twice-daily.[12] In October 2010Bromday received US FDA approval as a new, once-daily formulation.[13] In 2013,Prolensa has also been approved by the FDA.[12] Bromfenac eye drops have been marketed in the European Union since 2011,[8] and are available on worldwide markets with agreements fromBausch & Lomb,[8]Croma-Pharma, and other companies.[14]
Bromfenac was formerly marketed in the United States byWyeth-Ayerst in an oral formulation calledDuract for short-term relief of pain (less than 10 days at a time). It was brought to market in July 1997, and was withdrawn 22 June 1998, following numerous reports ofhepatotoxicity in patients who had taken the medication for longer than the recommended 10-day period.[15][16]
