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. |
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 | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for IBUPRIN (IBUPRIN).
| Breastfeeding | Ibuprofen is excreted into breast milk in very low concentrations (M/P ratio approximately 0.01). Considered compatible with breastfeeding, but use lowest effective dose for shortest duration. |
| 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. |
■ 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 NSAID; history of asthma, urticaria, or allergic-type reactions after taking aspirin or other NSAIDs; in setting of coronary artery bypass graft (CABG) surgery; active gastrointestinal bleeding; advanced renal disease.
| 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). |
Loading safety data…
| 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. |