RUFEN
Clinical safety rating: caution
Comprehensive clinical and safety monograph for RUFEN (RUFEN).
Non-selective cyclooxygenase (COX-1 and COX-2) inhibitor, decreasing prostaglandin synthesis.
| Metabolism | Hepatic metabolism primarily via CYP2C9; also undergoes glucuronidation. |
| Excretion | Primarily renal (approximately 90% as glucuronide conjugates and unchanged drug), with minor biliary/fecal elimination (<10%). |
| Half-life | Terminal elimination half-life is 2-4 hours; clinical context: short half-life requires frequent dosing for sustained analgesia. |
| Protein binding | >99% bound, primarily to albumin. |
| Volume of Distribution | 0.1-0.2 L/kg; low Vd indicates limited extravascular distribution, consistent with high protein binding. |
| Bioavailability | Oral: ~80% (fasting); rectal: ~70%; topical: ~5-10% (systemic absorption minimal). |
| Onset of Action | Oral: 30 minutes; rectal: 60 minutes; topical: 2-4 hours. |
| Duration of Action | Oral/rectal: 4-6 hours; topical: 4-8 hours; note: analgesic effect often outlasts plasma levels. |
| Molecular Weight | 206.28 |
400-800 mg orally three to four times daily; maximum 3200 mg/day.
| Dosage form | TABLET |
| Renal impairment | GFR 30-60 mL/min: reduce dose by 50%; GFR <30 mL/min: avoid use. |
| Liver impairment | Child-Pugh A: no adjustment; Child-Pugh B: reduce dose by 50%; Child-Pugh C: avoid use. |
| Pediatric use | 5-10 mg/kg/dose every 6-8 hours; maximum 40 mg/kg/day. |
| Geriatric use | Initiate at lowest effective dose (e.g., 400 mg daily), increase cautiously; monitor renal function. |
| 1st trimester | Avoid use during first trimester; associated with increased risk of cardiac defects and gastroschisis. |
| 2nd trimester | Use only if clearly needed; may cause oligohydramnios and premature closure of ductus arteriosus. |
| 3rd trimester | Contraindicated after 30 weeks gestation due to risk of premature closure of ductus arteriosus and persistent pulmonary hypertension. |
Clinical note
Comprehensive clinical and safety monograph for RUFEN (RUFEN).
| Placental transfer | Crosses placenta; fetal concentrations reach about 1% of maternal plasma levels. |
| Breastfeeding | Ibuprofen (RUFEN) is excreted in breast milk in low amounts. The American Academy of Pediatrics considers it compatible with breastfeeding. Use lowest effective dose for shortest duration. |
■ FDA Black Box Warning
Non-steroidal 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 increase with duration of use. Patients with cardiovascular disease or risk factors for cardiovascular disease may be at greater risk. RUFEN is contraindicated for the treatment of peri-operative pain in the setting of coronary artery bypass graft (CABG) surgery.
| Serious Effects |
Hypersensitivity to ibuprofen or any NSAIDHistory of asthma, urticaria, or allergic-type reactions after taking aspirin or other NSAIDsActive or history of recurrent peptic ulcer disease or gastrointestinal bleedingSevere heart failure (NYHA class III-IV)Severe renal impairment (CrCl <30 mL/min)Perioperative pain in the setting of coronary artery bypass graft (CABG) surgeryThird trimester of pregnancy (after 30 weeks gestation)
| Precautions | Cardiovascular thrombotic events, Gastrointestinal bleeding, ulceration, and perforation, Hypertension, Heart failure, Renal toxicity, Anaphylactoid reactions, Serious skin reactions (e.g., Stevens-Johnson syndrome) |
| Food/Dietary |
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| Lactation Rating |
| L2 (Safer) |
| Teratogenic Risk | First trimester: NSAIDs (including RUFEN) are associated with an increased risk of miscarriage and cardiac defects. Second trimester: Generally considered safer, but avoid prolonged use. Third trimester: Contraindicated due to risk of premature closure of ductus arteriosus, oligohydramnios, and neonatal renal impairment. |
| Fetal Monitoring | Monitor maternal blood pressure, renal function, and signs of gastrointestinal bleeding. Fetal ultrasound to assess ductus arteriosus and amniotic fluid volume if used in third trimester. |
| Fertility Effects | NSAIDs, including RUFEN, may impair female fertility by inhibiting prostaglandin synthesis and affecting ovulation. Reversible upon discontinuation. Effect on male fertility is minimal. |
| Alcohol increases GI bleeding risk. Taking with food may decrease GI irritation but does not eliminate risk. Avoid high-potassium foods if renal impairment is present. |
| Clinical Pearls | RUFEN (ibuprofen) is an NSAID; use lowest effective dose for shortest duration to minimize GI and cardiovascular risks. Avoid in patients with CrCl <30 mL/min or with significant aspirin allergy. Monitor renal function in elderly and volume-depleted patients. |
| Patient Advice | Take with food or milk to reduce stomach upset. · Do not exceed recommended dose or combine with other NSAIDs. · Report signs of GI bleeding (black stools, coffee-ground vomit) or cardiovascular symptoms (chest pain, shortness of breath). · Avoid alcohol while taking this medication. · If you are taking low-dose aspirin for heart protection, take ibuprofen at least 30 minutes after or 8 hours before aspirin. |