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. |
| Molecular Weight | 334.15 |
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 | NSAIDs are generally avoided in the first trimester due to potential increased risk of miscarriage and congenital malformations; there are no adequate and well-controlled studies for bromfenac; use only if potential benefit justifies risk. |
| 2nd trimester | Use with caution; avoid if possible as NSAIDs may cause oligohydramnios and fetal renal impairment; use only if clearly needed and at lowest effective dose. |
| 3rd trimester | Contraindicated from 30 weeks gestation onward due to risk of premature closure of the ductus arteriosus and oligohydramnios. |
Clinical note
Comprehensive clinical and safety monograph for PROLENSA (PROLENSA).
| Placental transfer | NSAIDs including bromfenac are known to cross the placenta; ophthalmic administration results in low systemic levels but transfer can occur. |
| Breastfeeding | No data on bromfenac excretion in human milk; systemic absorption after ophthalmic administration is low. Caution should be exercised because of potential adverse effects in nursing infants, particularly gastrointestinal or renal effects. |
■ FDA Black Box Warning
No FDA boxed warning.
| Serious Effects |
Hypersensitivity to bromfenac or any component of the formulationHistory of asthma, urticaria, or other allergic-type reactions to aspirin or other NSAIDsThird trimester of pregnancy (≥30 weeks gestation)
| 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. |
| Food/Dietary | No specific food interactions. Avoid alcohol as it may increase risk of gastrointestinal bleeding with systemic NSAIDs, but relevance to ophthalmic use is minimal. |
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| Lactation Rating | L3 (Moderately Safe) |
| 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. |
| 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. |
| Clinical Pearls | PROLENSA (bromfenac ophthalmic solution) is a NSAID for postoperative ocular inflammation and pain. Use the lowest effective dose for the shortest duration. Contraindicated in patients with aspirin or NSAID hypersensitivity. Monitor for corneal epithelial breakdown, especially in patients with corneal denervation, epithelial defects, diabetes, ocular surface disease, or concomitant topical steroids. Avoid use during ocular surgery due to risk of corneal melting. |
| Patient Advice | Do not touch the dropper tip to any surface to avoid contamination. · Remove contact lenses before instillation and wait 15 minutes before reinserting. · May cause transient stinging or blurred vision; avoid driving until vision clears. · Report any eye pain, redness, or vision changes immediately. · Use exactly as prescribed; do not exceed recommended duration. · Inform your doctor if you have a history of asthma, ulcers, or bleeding disorders. |