IBUPROFEN LYSINE
Clinical safety rating: avoid
ACE inhibitors and ARBs may have diminished antihypertensive effect Increases risk of serious cardiovascular thrombotic events and GI bleeding.
Ibuprofen lysine is a nonsteroidal anti-inflammatory drug (NSAID) that inhibits cyclooxygenase (COX-1 and COX-2) enzymes, thereby reducing prostaglandin synthesis. This results in anti-inflammatory, analgesic, and antipyretic effects.
| Metabolism | Ibuprofen is primarily metabolized in the liver via oxidation by cytochrome P450 enzymes, mainly CYP2C9 and CYP2C8, to inactive metabolites. Conjugation with glucuronic acid also occurs. A small portion is metabolized via CYP2C19. |
| Excretion | Renal excretion of metabolites and conjugates accounts for >90% of elimination; less than 1% is excreted unchanged in urine. Fecal excretion is minimal (<5%). |
| Half-life | 2–4 hours in adults; extended to 4–6 hours in neonates. In severe hepatic or renal impairment, half-life may increase up to 8–10 hours. |
| Protein binding | >99% bound to plasma albumin at therapeutic concentrations. |
| Volume of Distribution | 0.1–0.3 L/kg in adults. Higher in neonates (0.3–0.5 L/kg) due to increased extracellular fluid. |
| Bioavailability | Oral: 80–90% (immediate-release); intravenous: 100%. |
| Onset of Action | Oral: 30–60 minutes; intravenous: 5–10 minutes. |
| Duration of Action | Oral immediate-release: 4–6 hours; intravenous: 4–6 hours. Extended-release oral formulations last up to 12 hours. Analgesic effect may persist slightly longer than antipyretic effect. |
200-800 mg orally every 6-8 hours as needed; maximum 2400 mg/day. Intravenous: 400-800 mg every 6 hours; maximum 3.2 g/day.
| Dosage form | INJECTABLE |
| Renal impairment | CrCl 30-89 mL/min: no adjustment. CrCl <30 mL/min: avoid use or reduce dose by 50% and monitor renal function. Hemodialysis: not dialyzable; avoid use. |
| Liver impairment | Child-Pugh Class A: no adjustment. Child-Pugh Class B: reduce dose by 50% or avoid. Child-Pugh Class C: contraindicated due to risk of GI bleeding and renal impairment. |
| Pediatric use | Oral: 5-10 mg/kg/dose every 6-8 hours; maximum 40 mg/kg/day. Intravenous: 10 mg/kg/dose every 6 hours; maximum 40 mg/kg/day or 2.4 g/day. |
| Geriatric use | Start at lowest effective dose (e.g., 200-400 mg every 8 hours); maximum 1200 mg/day due to increased risk of GI bleeding, renal impairment, and cardiovascular events. Monitor renal function and electrolytes. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
ACE inhibitors and ARBs may have diminished antihypertensive effect Increases risk of serious cardiovascular thrombotic events and GI bleeding.
| FDA category | Positive |
| Breastfeeding | Ibuprofen excreted into breast milk in low concentrations (M/P ratio 0.01-0.1). American Academy of Pediatrics considers ibuprofen compatible with breastfeeding; no adverse effects reported in infants. Ibuprofen lysine: likely same profile; caution with preterm infants or those with thrombocytopenia. |
| Teratogenic Risk |
■ FDA Black Box Warning
NSAIDs, including ibuprofen lysine, increase the risk of serious cardiovascular thrombotic events, 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. NSAIDs are also contraindicated for the treatment of perioperative pain in the setting of coronary artery bypass graft (CABG) surgery.
| Common Effects | fever |
| Serious Effects |
["Hypersensitivity to ibuprofen or any component of the formulation","History of asthma, urticaria, or allergic-type reactions after taking aspirin or other NSAIDs","Perioperative pain in the setting of coronary artery bypass graft (CABG) surgery","Active gastrointestinal bleeding or peptic ulcer disease","Severe renal impairment","Premature neonates with certain conditions (e.g., active bleeding, thrombocytopenia, coagulation defects, necrotizing enterocolitis, congenital heart disease where PDA patency is necessary)"]
| Precautions | ["Cardiovascular thrombotic events","Gastrointestinal (GI) adverse events including bleeding, ulceration, and perforation","Renal toxicity including fluid retention and acute renal failure","Anaphylactoid reactions","Serious skin reactions (e.g., Stevens-Johnson syndrome)","Risk in premature neonates: potential for necrotizing enterocolitis, renal impairment, and bleeding","Hepatic impairment","Asthma exacerbation in aspirin-sensitive patients","Pregnancy: avoid in third trimester due to risk of premature closure of ductus arteriosus"] |
Loading safety data…
| First trimester: NSAIDs are associated with increased risk of spontaneous abortion and cardiac malformations (odds ratio 1.86 for cardiovascular defects). Second trimester: avoid; no specific fetal risks but limited safety data. Third trimester: contraindicated; may cause premature closure of ductus arteriosus, oligohydramnios, and necrotizing enterocolitis. Ibuprofen lysine is a prodrug; fetal risks similar to ibuprofen. |
| Fetal Monitoring | Monitor for signs of premature ductal closure (fetal echocardiography) if used beyond 30 weeks. Assess amniotic fluid volume (ultrasound) for oligohydramnios. Monitor maternal platelet function and bleeding time if used near delivery. Evaluate renal function in fetus if prolonged use. |
| Fertility Effects | May impair fertility by inhibiting prostaglandin synthesis, affecting ovulation. Reversible upon discontinuation. Ibuprofen lysine: same mechanism. Consider alternative analgesia in women attempting conception. |