PROLENSA
Clinical safety rating: caution
Comprehensive clinical and safety monograph for PROLENSA (PROLENSA).
Bromfenac is a nonsteroidal anti-inflammatory drug (NSAID) that inhibits cyclooxygenase (COX-1 and COX-2) enzymes, reducing prostaglandin synthesis and thereby decreasing inflammation, pain, and angiogenesis in the eye.
| Metabolism | Primarily metabolized by CYP2C9 and glucuronidation; minor metabolism by CYP2C8 and CYP3A4. |
| Excretion | Primarily renal elimination (approximately 70% of the dose as unchanged drug and metabolites), with the remainder excreted in feces via biliary secretion (approximately 30%). |
| Half-life | Terminal elimination half-life is approximately 1.5 hours for the ocular route; after systemic absorption, half-life is about 4.5 hours. The short half-life limits systemic exposure but requires multiple daily dosing for sustained ocular effect. |
| Protein binding | Bromfenac is extensively bound to plasma proteins (>99%), primarily to albumin. |
| Volume of Distribution | Volume of distribution is approximately 0.7 L/kg, indicating distribution into total body water. Following ocular administration, high concentration is achieved in aqueous humor and cornea. |
| Bioavailability | Ophthalmic: Systemic bioavailability is low (approximately 0.1%) due to minimal absorption from the eye; plasma concentrations are negligible after topical administration. Oral bioavailability (not relevant for ophthalmic use) is about 100% but formulation is not available; ophthalmic route only. |
| Onset of Action | Ophthalmic: Therapeutic effect (analgesia, reduction of corneal edema) typically begins within 1-2 hours after instillation. |
| Duration of Action | Ophthalmic: Duration of analgesia and anti-inflammatory effect is approximately 4-6 hours, requiring dosing 4 times daily. Clinical effect may persist longer with repeated dosing. |
Adults: 1 drop in affected eye(s) twice daily (morning and evening) for 2 weeks.
| Dosage form | SOLUTION/DROPS |
| Renal impairment | No dosage adjustment required for renal impairment; drug is primarily metabolized and minimally excreted renally. |
| Liver impairment | No dosage adjustment recommended for mild to moderate hepatic impairment (Child-Pugh A or B); not studied in severe impairment (Child-Pugh C). |
| Pediatric use | Safety and efficacy not established in pediatric patients; no approved dosing guidelines. |
| Geriatric use | No specific dosage adjustment required; no significant differences in safety or efficacy observed in elderly patients compared to younger adults. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for PROLENSA (PROLENSA).
| Breastfeeding | No data on bromfenac in human milk. It is unlikely to be excreted in significant amounts due to minimal systemic absorption. The M/P ratio is unknown. Use caution and consider the benefits of breastfeeding versus the potential for infant exposure. |
| Teratogenic Risk | PROLENSA (bromfenac ophthalmic solution) is a topical NSAID. Systemic absorption is minimal, so no known teratogenic effects from topical use. However, NSAIDs as a class may cause premature closure of the ductus arteriosus and oligohydramnios in the third trimester. The risk is theoretical but cannot be excluded. |
■ FDA Black Box Warning
No FDA boxed warning.
| Serious Effects |
["Hypersensitivity to bromfenac or any component of the formulation.","History of asthma, urticaria, or allergic-type reactions after taking aspirin or other NSAIDs.","Concurrent use with other topical ophthalmic NSAIDs."]
| Precautions | ["Risk of increased bleeding time; use with caution in patients with known bleeding tendencies or receiving anticoagulants.","Potential for corneal complications including keratitis, ulceration, and perforation, especially in patients with compromised corneal integrity or use beyond 14 days.","Cross-sensitivity with aspirin and other NSAIDs; use caution in patients with history of asthma or allergic reactions to NSAIDs.","May delay wound healing.","Concomitant use with topical corticosteroids may increase risk of corneal adverse events."] |
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| Fetal Monitoring |
| No specific fetal monitoring required due to topical administration. However, if used chronically or at high frequency, monitor for oligohydramnios or fetal ductus arteriosus constriction in the third trimester. |
| Fertility Effects | Topical bromfenac is not expected to affect fertility. Systemic NSAIDs may impair female fertility; however, the minimal systemic absorption from ophthalmic use makes this unlikely. |