IBUPROHM
Clinical safety rating: caution
Comprehensive clinical and safety monograph for IBUPROHM (IBUPROHM).
Non-selective cyclooxygenase (COX-1 and COX-2) inhibitor, reducing prostaglandin synthesis, thereby decreasing pain, inflammation, and fever.
| Metabolism | Hepatic via CYP2C9; metabolites are glucuronidated and excreted renally. |
| Excretion | Renal: 90% as metabolites (mostly glucuronide conjugates) and unchanged drug (1%); biliary/fecal: <5%. |
| Half-life | 2-4 hours in adults; prolonged to 1.5-2.5 hours in neonates? Actually: terminal half-life ~2-4 h in adults, up to 12 h in overdose; context: requires frequent dosing. |
| Protein binding | >99% bound to albumin primarily, also alpha1-acid glycoprotein. |
| Volume of Distribution | 0.1-0.2 L/kg; indicates low tissue distribution, primarily in plasma and extracellular fluid. |
| Bioavailability | Oral: 80-100%; rectal: 80-90% relative to oral; topical: <10% systemically absorbed. |
| Onset of Action | Oral: 30-60 min; topical: 1-2 h for local effect; rectal: similar to oral. |
| Duration of Action | Oral: 4-6 h for analgesia/antipyretic; anti-inflammatory effect requires longer dosing; topical: 4-8 h. |
200-800 mg orally every 6-8 hours as needed; maximum 3200 mg/day.
| Dosage form | TABLET |
| Renal impairment | eGFR 30-59 mL/min: reduce dose by 25-50% and avoid doses >400 mg; eGFR <30 mL/min: avoid use or use with extreme caution at lowest effective dose. |
| Liver impairment | Child-Pugh A: no adjustment; Child-Pugh B: reduce dose by 50%; Child-Pugh C: avoid use. |
| Pediatric use | Children 6 months to 12 years: 5-10 mg/kg/dose every 6-8 hours; maximum 40 mg/kg/day or 2000 mg/day, whichever is less. |
| Geriatric use | Initiate at lowest effective dose (200 mg every 8-12 hours); maximum 1200 mg/day; monitor renal function and gastrointestinal bleeding risk. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for IBUPROHM (IBUPROHM).
| Breastfeeding | Ibuprofen is excreted into breast milk in low concentrations (M/P ratio approximately 0.01-0.05). The American Academy of Pediatrics considers it compatible with breastfeeding. However, caution is advised in infants with known hypersensitivity or thrombocytopenia. |
| Teratogenic Risk | First trimester: Avoid use; NSAIDs are associated with increased risk of miscarriage and cardiac defects. Second trimester: Use with caution; no clear evidence of major malformations but potential for oligohydramnios. Third trimester: Contraindicated; risk of premature closure of ductus arteriosus, fetal renal impairment, and oligohydramnios. |
■ FDA Black Box Warning
Cardiovascular thrombotic events risk; gastrointestinal bleeding risk.
| Serious Effects |
Hypersensitivity, history of asthma/urticaria after aspirin/NSAIDs, perioperative pain in CABG surgery, severe renal/hepatic impairment, active GI bleeding, third trimester pregnancy.
| Precautions | Cardiovascular events, GI bleeding, renal toxicity, hypertension, fluid retention, anaphylactoid reactions, hepatic impairment, asthma exacerbation, pregnancy (third trimester). |
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| Fetal Monitoring | Monitor maternal blood pressure, renal function (serum creatinine, BUN), and signs of fluid retention. Fetal monitoring includes ultrasound for amniotic fluid volume (especially with prolonged use), and fetal echocardiography if used after 28 weeks gestation. |
| Fertility Effects | Ibuprofen may impair female fertility by interfering with prostaglandin synthesis, affecting ovulation and implantation. Reversible upon discontinuation. No significant effect on male fertility has been documented. |