FLURBIPROFEN
Clinical safety rating: avoid
Positive evidence of fetus risks but benefits may outweigh risks in some cases
Cyclooxygenase (COX) inhibitor, reducing prostaglandin synthesis; nonsteroidal anti-inflammatory drug (NSAID) with anti-inflammatory, analgesic, and antipyretic effects.
| Metabolism | Hepatic metabolism via CYP2C9; forms hydroxylated metabolites (e.g., 4'-hydroxyflurbiprofen) and conjugates. Less than 5% excreted unchanged in urine. |
| Excretion | Renal: 70% as conjugated metabolites (e.g., glucuronides) and <5% unchanged; biliary/fecal: 30%, with enterohepatic circulation. |
| Half-life | Terminal elimination half-life: 3-4 hours (healthy adults) in short-term use; prolonged to 6-12 hours in elderly or renal impairment. |
| Protein binding | 99% bound to albumin primarily. |
| Volume of Distribution | 0.12-0.15 L/kg; small Vd indicates limited tissue distribution, likely due to high protein binding. |
| Bioavailability | Oral: 92-96% (extensive absorption); ophthalmic: systemic absorption negligible (<0.05% of dose). |
| Onset of Action | Oral: analgesic effect within 30-60 minutes; ophthalmic: within 30 minutes for intraoperative miosis prevention; topical: local effect within 1 hour. |
| Duration of Action | Oral: 4-6 hours for analgesia; ophthalmic: effect persists up to 4 hours following a single dose. |
| Molecular Weight | 244.26 |
Oral: 50-100 mg every 6-8 hours; maximum 300 mg/day. Ophthalmic: 1 drop every 30 minutes starting 2 hours before surgery, then 1 drop every 4-6 hours for 24-48 hours post-surgery.
| Dosage form | TABLET |
| Renal impairment | GFR >50 mL/min: no adjustment. GFR 10-50 mL/min: avoid use if possible; if necessary, reduce dose to 50% and monitor. GFR <10 mL/min: contraindicated. |
| Liver impairment | Child-Pugh A: no adjustment. Child-Pugh B: reduce dose by 50%. Child-Pugh C: contraindicated. |
| Pediatric use | Oral: Not recommended for children <12 years; safety and efficacy not established. Ophthalmic: Not approved in pediatric patients. |
| Geriatric use | Initiate at lowest effective dose; monitor renal function and GI bleeding risk; maximum 200 mg/day oral. |
| 1st trimester | Avoid use during first trimester due to potential risk of miscarriage and congenital malformations (e.g., cardiac defects) associated with NSAIDs. |
| 2nd trimester | Use only if clearly needed; may cause oligohydramnios premature closure of ductus arteriosus. |
| 3rd trimester | Contraindicated due to risk of premature closure of ductus arteriosus, oligohydramnios, and neonatal renal impairment. |
Clinical note
ACE inhibitors and ARBs may have diminished antihypertensive effect Increases risk of serious cardiovascular thrombotic events and GI bleeding.
| Placental transfer | Crosses placenta; detected in fetal plasma at concentrations ~50% of maternal levels. |
| Breastfeeding | Excreted into breast milk in low amounts; considered compatible with breastfeeding but avoid if possibility of adverse effects on infant (e.g., platelet dysfunction). Use lowest effective dose for shortest duration. |
■ FDA Black Box Warning
Nonsteroidal anti-inflammatory drugs (NSAIDs) cause an increased risk of serious cardiovascular thrombotic events, including myocardial infarction and stroke, which can be fatal. This risk may occur early in treatment and may increase with duration of use. Flurbiprofen is contraindicated in the setting of coronary artery bypass graft (CABG) surgery.
| Common Effects | inflammation |
| Serious Effects |
Hypersensitivity to flurbiprofen or other NSAIDsHistory of asthma, urticaria, or allergic-type reactions after taking aspirin or other NSAIDsActive peptic ulcer or gastrointestinal bleedingSevere heart failure (NYHA class III-IV)Coronary artery bypass graft (CABG) surgeryThird trimester of pregnancy
| Precautions | Cardiovascular risk: increased risk of thrombosis, MI, stroke, and hypertension, Gastrointestinal risk: increased risk of serious GI adverse events including bleeding, ulceration, and perforation of stomach or intestines, Renal toxicity: impaired renal function, papillary necrosis in long-term use, Hepatic effects: elevation of liver enzymes, rare severe hepatic reactions, Anaphylactoid reactions: may occur in patients without prior exposure, Fluid retention and edema, Use in late pregnancy: avoid due to risk of premature closure of ductus arteriosus, Ophthalmic use: do not use while wearing contact lenses (for ophthalmic solution) |
Loading safety data…
| Lactation Rating | L2 (Safer) |
| Teratogenic Risk | First trimester: Risk of cardiac defects and gastroschisis with NSAID use; second trimester: Potential renal dysfunction and oligohydramnios; third trimester: Premature closure of ductus arteriosus, pulmonary hypertension, oligohydramnios, and necrotizing enterocolitis. |
| Fetal Monitoring | Monitor amniotic fluid index, fetal echocardiography for ductus arteriosus patency, and renal function in prolonged use. |
| Fertility Effects | Reversible inhibition of ovulation and implantation due to prostaglandin inhibition; may delay or prevent conception. |
| Food/Dietary | Avoid alcohol. No significant food interactions; however, food can delay absorption but does not affect overall bioavailability. Taking with food or milk can minimize GI irritation. |
| Clinical Pearls | Flurbiprofen is a propionic acid derivative NSAID with potent anti-inflammatory, analgesic, and antipyretic properties. It has a short half-life (approx. 3-4 hours) and is highly protein-bound. Use with caution in elderly due to increased risk of GI bleeding and renal impairment. For ophthalmic use (e.g., flurbiprofen 0.03% drops), it is indicated for inhibition of intraoperative miosis during cataract surgery. Systemic absorption from ophthalmic drops is minimal but possible. Contraindicated in patients with aspirin triad (aspirin sensitivity, nasal polyps, asthma) due to risk of bronchospasm. Avoid concurrent use with other NSAIDs or anticoagulants. |
| Patient Advice | Take with food or milk to reduce GI upset. · Avoid alcohol while taking this medication as it increases the risk of stomach bleeding. · Do not take with other NSAIDs (e.g., ibuprofen, naproxen) or aspirin unless directed by your doctor. · Report signs of GI bleeding (black/tarry stools, coffee-ground vomit) or allergic reaction (rash, swelling, difficulty breathing) immediately. · For ophthalmic use: do not touch the dropper tip to any surface; remove contact lenses before instillation; may cause transient stinging; wait at least 5 minutes before using other eye drops. |