IBU
Clinical safety rating: caution
Comprehensive clinical and safety monograph for IBU (IBU).
Non-selective inhibitor of cyclooxygenase (COX-1 and COX-2), decreasing prostaglandin synthesis, thereby reducing inflammation, pain, and fever.
| Metabolism | Hepatic metabolism primarily via CYP2C9 to inactive metabolites; minor pathways include CYP2C8. |
| Excretion | Renal (90% as conjugated metabolites, 10% unchanged), biliary/fecal (minor, <5%) |
| Half-life | Terminal elimination half-life: 2-4 hours in adults; prolonged in neonates (30 hours) and elderly (up to 6 hours). No accumulation with recommended dosing due to short t½. |
| Protein binding | 99% bound primarily to albumin |
| Volume of Distribution | 0.1-0.2 L/kg, indicating low tissue distribution; predominantly confined to plasma and extracellular fluid. |
| Bioavailability | Oral: 80-100% (immediate-release), 70-90% (extended-release); Topical: approximately 5-10% systemic absorption; Intravenous: 100%. |
| Onset of Action | Oral immediate-release: 30-60 minutes; Oral extended-release: 1-2 hours; Topical: 1-2 hours; Intravenous: 5-10 minutes. |
| Duration of Action | Oral immediate-release (analgesic/antipyretic): 4-6 hours; Anti-inflammatory effect: requires multiple doses over days; Topical: approximately 4-6 hours; Intravenous: 4-6 hours. |
| Molecular Weight | 206.28 |
| Action Class | NSAID's- Non-Selective COX 1&2 Inhibitors (propionic acid) |
| Brand Substitutes | Ibupal 400mg Tablet, Bruriff 400mg Tablet, IBUFLAMAR 400MG TABLET, ALFAM 400MG TABLET, NORSWEL 400MG TABLET, Multigon Tablet, Ibuwin 400 mg/500 mg Tablet, Tolfen Tablet, Ibuflam 400 mg/500 mg Tablet, Arden Plus 400 mg/500 mg Tablet |
200-800 mg orally every 6-8 hours as needed; maximum 3200 mg/day. For OTC use: 200-400 mg every 4-6 hours; max 1200 mg/day.
| Dosage form | TABLET |
| Renal impairment | CrCl >30 mL/min: no adjustment. CrCl 10-30 mL/min: 200 mg every 12 hours; avoid if CrCl <10 mL/min. |
| Liver impairment | Child-Pugh A: no adjustment. Child-Pugh B: reduce dose by 50% or avoid. Child-Pugh C: contraindicated due to risk of hepatotoxicity. |
| Pediatric use | 6 months to 12 years: 5-10 mg/kg/dose every 6-8 hours; max 40 mg/kg/day. For juvenile idiopathic arthritis: 30-40 mg/kg/day divided every 6-8 hours; max 50 mg/kg/day. |
| Geriatric use | Initiate at lowest effective dose; consider 200 mg every 8-12 hours; monitor renal function and GI bleeding risk. |
| 1st trimester | Avoid especially during late first trimester due to increased risk of spontaneous abortion and gastroschisis. No specific association with major malformations. |
| 2nd trimester | Use only if clearly needed; may cause oligohydramnios and premature ductus arteriosus constriction with prolonged use. |
| 3rd trimester | Contraindicated due to risk of premature closure of ductus arteriosus and oligohydramnios; labeled category D. |
Clinical note
Comprehensive clinical and safety monograph for IBU (IBU).
| Placental transfer | Crosses the placenta; measured in cord blood and fetal tissues. |
| Breastfeeding | Ibuprofen is excreted in breast milk in very low concentrations (estimated infant dose <0.1% of maternal weight-adjusted dose) and is considered compatible with breastfeeding. Use the lowest effective dose for the shortest duration. |
■ FDA Black Box Warning
NSAIDs cause an increased risk of serious cardiovascular thrombotic events, myocardial infarction, and stroke, which can be fatal. Risk may increase with duration of use. Contraindicated for treatment of peri-operative pain in coronary artery bypass graft (CABG) surgery.
| Serious Effects |
NSAID hypersensitivity (including aspirin)Acute asthma exacerbationActive peptic ulcer disease or gastrointestinal bleedingSevere heart failure (NYHA III-IV)Perioperative pain in coronary artery bypass graft (CABG) surgeryThird trimester of pregnancyHistory of GI perforation or bleeding related to previous NSAID therapy
| Precautions | Cardiovascular thrombotic events, Gastrointestinal bleeding, ulceration, and perforation, Hypertension, Heart failure exacerbation, Renal toxicity, Anaphylactic reactions, Serious skin reactions (e.g., Stevens-Johnson syndrome), Hematologic effects (anemia, bleeding) |
| Food/Dietary | Ibuprofen can increase the risk of stomach bleeding when taken with alcohol. No specific food restrictions, but taking with food or milk can reduce GI irritation. |
Loading safety data…
| Lactation Rating | L1 (Safe) |
| Teratogenic Risk | First and second trimester: Increased risk of miscarriage and congenital malformations (particularly cardiac defects) associated with NSAID use. Third trimester: Known risk of premature closure of ductus arteriosus, oligohydramnios, and neonatal renal impairment; contraindicated after 30 weeks gestation. |
| Fetal Monitoring | Monitor amniotic fluid index (oligohydramnios risk), fetal echocardiography for ductal constriction after 24 weeks, and neonatal renal function if exposed near term. |
| Fertility Effects | Reversible impairment of female fertility via inhibition of prostaglandin synthesis affecting follicular rupture and ovulation; resolves upon discontinuation. |
| Clinical Pearls | Ibuprofen is a nonselective COX inhibitor with anti-inflammatory, analgesic, and antipyretic effects. Avoid in patients with aspirin allergy, active peptic ulcer, or severe renal impairment. Use lowest effective dose for shortest duration to minimize GI and cardiovascular risks. Not recommended in patients with advanced chronic kidney disease (eGFR <30 mL/min/1.73 m²). For acute pain, ibuprofen 200-400 mg every 6 hours PRN. Monitor for signs of GI bleeding, hypertension, and fluid retention. |
| Patient Advice | Take with food or milk to reduce stomach upset. · Do not exceed 1200 mg per day unless directed by your doctor. · Avoid alcohol while taking this medication. · Stop use and seek medical help if you experience chest pain, weakness, slurred speech, or signs of stomach bleeding (black/tarry stools, vomit that looks like coffee grounds). · Do not take with other NSAIDs or aspirin without consulting your healthcare provider. |