IBUPRIN
Clinical safety rating: caution
Comprehensive clinical and safety monograph for IBUPRIN (IBUPRIN).
Non-selective cyclooxygenase (COX-1 and COX-2) inhibitor, reducing prostaglandin synthesis, resulting in anti-inflammatory, analgesic, and antipyretic effects.
| Metabolism | Primarily hepatic via CYP2C9; also undergoes glucuronidation; about 1% excreted unchanged in urine. |
| Excretion | Renal excretion of conjugated metabolites (75-85%), with less than 10% excreted unchanged; biliary/fecal elimination accounts for less than 10%. |
| Half-life | Terminal elimination half-life is approximately 2-4 hours; in elderly or patients with hepatic impairment, half-life may be prolonged to 6-8 hours. |
| Protein binding | Highly protein bound (99%) primarily to albumin. |
| Volume of Distribution | 0.1-0.2 L/kg; low Vd indicates limited distribution outside plasma and interstitial fluid. |
| Bioavailability | Oral: 80-100% (immediate-release); delayed-release: 50-70% due to lower dissolution rate; topical: 0.5-5% systemic absorption. |
| Onset of Action | Oral immediate-release: 30-60 min; oral delayed-release: 2-4 hours; topical: 1-2 hours. |
| Duration of Action | Oral immediate-release: 4-6 hours; oral delayed-release: up to 12 hours; topical: 4-6 hours. Duration may be shorter with fever or inflammation. |
| Molecular Weight | 206.28 |
200-800 mg orally every 6-8 hours as needed; maximum daily dose 3200 mg.
| Dosage form | TABLET |
| Renal impairment | eGFR 30-59 mL/min: reduce dose to 200-400 mg every 8 hours; eGFR <30 mL/min: avoid use |
| Liver impairment | Child-Pugh class A: no adjustment; Child-Pugh class B: reduce dose by 50%; Child-Pugh class C: avoid use |
| Pediatric use | 6 months to 12 years: 5-10 mg/kg/dose every 6-8 hours; maximum 40 mg/kg/day |
| Geriatric use | Initiate at lowest effective dose (200-400 mg every 8 hours); maximum daily dose 1200 mg |
| 1st trimester | Avoid. NSAIDs are associated with increased risk of miscarriage and gastroschisis. Use only if clearly needed. |
| 2nd trimester | Caution. Risk of oligohydramnios and fetal renal dysfunction. Use lowest effective dose for shortest duration. |
| 3rd trimester | Avoid after 30 weeks. Associated with premature closure of ductus arteriosus, oligohydramnios, and neonatal pulmonary hypertension. Avoid after 30 weeks gestation. |
Clinical note
Comprehensive clinical and safety monograph for IBUPRIN (IBUPRIN).
| Placental transfer | Ibuprofen crosses the placenta. Fetal concentrations are approximately 10% of maternal serum levels after single dose. Accumulation may occur with repeated dosing. |
| Breastfeeding | Ibuprofen is excreted into breast milk in low amounts (less than 1% of maternal dose). Considered compatible with breastfeeding by the American Academy of Pediatrics. Use lowest effective dose for shortest duration, and avoid in infants with thrombocytopenia or platelet dysfunction. |
■ FDA Black Box Warning
Nonsteroidal anti-inflammatory drugs (NSAIDs) cause an increased risk of serious gastrointestinal adverse events including bleeding, ulceration, and perforation of the stomach or intestines, which can be fatal; and an increased risk of serious cardiovascular thrombotic events, including myocardial infarction and stroke, which can be fatal.
| Serious Effects |
Hypersensitivity to ibuprofen or any componentHistory 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 surgery (perioperative pain)Third trimester of pregnancy (after 30 weeks)Severe hepatic or renal impairment
| Precautions | Cardiovascular risk (MI, stroke, hypertension, fluid retention); gastrointestinal risk (ulcer, bleeding, perforation); renal impairment; hepatic impairment; anaphylactoid reactions; asthma exacerbation; pregnancy (avoid in third trimester). |
| Food/Dietary | Take with food or milk to reduce gastrointestinal irritation. Avoid alcohol. Ibuprofen may interfere with the effect of some diuretics and antihypertensives; a high-sodium diet may further reduce blood pressure control. |
Loading safety data…
| Lactation Rating | L1 (Safe) |
| Teratogenic Risk | First trimester: Association with increased risk of miscarriage and cardiac defects (odds ratio 1.86 for congenital heart defects). Second trimester: Avoid use due to risk of oligohydramnios and fetal renal dysfunction. Third trimester: Contraindicated after 30 weeks gestation due to risk of premature closure of ductus arteriosus, oligohydramnios, and necrotizing enterocolitis. |
| Fetal Monitoring | Monitor for oligohydramnios via ultrasound if used in second trimester; fetal echocardiography if used in first trimester. Maternal monitoring for bleeding complications, gastric irritation, and renal function. |
| Fertility Effects | Reversible inhibition of ovulation due to prostaglandin synthesis inhibition. Use may delay conception, but effect resolves upon discontinuation. |
| Clinical Pearls | Ibuprofen (IBUPRIN) is a nonsteroidal anti-inflammatory drug (NSAID) with analgesic, antipyretic, and anti-inflammatory effects. Use the lowest effective dose for the shortest duration to minimize cardiovascular and gastrointestinal risks. In patients with hypertension, monitor blood pressure as NSAIDs can reduce antihypertensive efficacy. Avoid in patients with severe heart failure, recent CABG, or active peptic ulcer disease. For acute pain, a single dose of 400-800 mg provides rapid relief. Counsel patients about the risk of Reye's syndrome in children with viral illness — do not use in pediatric patients with chickenpox or influenza-like symptoms. |
| Patient Advice | Take with food or milk to reduce stomach upset. · Do not take with other NSAIDs (e.g., aspirin, naproxen) or more than directed to avoid overdose risk. · Avoid alcohol while taking this medication to lower the risk of stomach bleeding. · Stop use and seek medical help if signs of stomach bleeding (black/bloody stools, vomiting blood) or allergic reaction (facial swelling, trouble breathing) occur. · Not for use in children with chickenpox or flu-like symptoms due to Reye's syndrome risk. · If you have high blood pressure, heart disease, kidney disease, or are pregnant (especially >= 20 weeks), consult a doctor before use. |