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. |
| Molecular Weight | 452.54 Da (ibuprofen lysine) |
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 | Avoid use during first trimester unless clearly needed; associated with increased risk of miscarriage and congenital malformations (e.g., cardiac defects). |
| 2nd trimester | Use with caution; may cause oligohydramnios and premature ductus arteriosus constriction; avoid prolonged use or high doses. |
| 3rd trimester | Contraindicated after 30 weeks gestation due to risk of premature closure of ductus arteriosus and oligohydramnios. |
Clinical note
ACE inhibitors and ARBs may have diminished antihypertensive effect Increases risk of serious cardiovascular thrombotic events and GI bleeding.
| FDA category | Positive |
| Placental transfer | Crosses placenta; fetal serum levels approximately 50% of maternal levels after oral administration. |
■ 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 |
History of allergic reaction to ibuprofen or NSAIDsActive peptic ulcer or gastrointestinal bleedingSevere renal impairment (CrCl <30 mL/min)Advanced hepatic diseaseThird trimester pregnancy (after 30 weeks)
| 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 |
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| Breastfeeding |
| Ibuprofen and its lysine salt are excreted in breast milk in low concentrations. Considered compatible with breastfeeding; use lowest effective dose for shortest duration. |
| Lactation Rating | L1 (Safe) |
| Teratogenic Risk | 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. |
| Food/Dietary | No food interactions; administered intravenously in neonates. For oral forms, take with food to reduce GI upset. |
| Clinical Pearls | Ibuprofen lysine is a water-soluble salt that allows for intravenous administration, providing faster onset than oral ibuprofen. It is primarily used for patent ductus arteriosus (PDA) closure in preterm neonates. Monitor renal function and platelet counts closely. Contraindicated in patients with active bleeding, thrombocytopenia, or coagulation defects. Not for use in neonates with proven or suspected necrotizing enterocolitis (NEC). |
| Patient Advice | This medication is given intravenously to close a blood vessel in premature infants. · The infant will be closely monitored for kidney function, bleeding, and intestinal issues. · Report any signs of bleeding, such as bruising or blood in stool. · This drug should not be used if the infant has active bleeding or a bleeding disorder. |