MOTRIN
Clinical safety rating: caution
Comprehensive clinical and safety monograph for MOTRIN (MOTRIN).
Non-selective COX-1 and COX-2 inhibitor, reducing prostaglandin synthesis.
| Metabolism | Hepatic via CYP2C9 and glucuronidation; minor via CYP2C8. |
| Excretion | Renal excretion of conjugated metabolites (approximately 70-80% as glucuronide and sulfate conjugates); less than 10% excreted unchanged. Biliary/fecal elimination accounts for about 10-20%. |
| Half-life | Terminal elimination half-life approximately 2-4 hours in adults with normal renal function; prolonged in elderly and patients with renal impairment (up to 6-8 hours). No significant accumulation occurs with regular dosing. |
| Protein binding | Highly protein-bound (approximately 99%) primarily to albumin. |
| Volume of Distribution | Approximately 0.1-0.2 L/kg (range 0.1-0.2 L/kg); indicative of limited tissue distribution due to high protein binding. Larger Vd in neonates (0.3-0.4 L/kg). |
| Bioavailability | Oral immediate-release: 80-100%; oral extended-release: approximately 85-90% relative to immediate-release; intravenous: 100%; topical (e.g., gel): 3-8% systemic absorption. |
| Onset of Action | Oral immediate-release: 30-60 minutes; intravenous: within 15-30 minutes; topical: 1-2 hours. |
| Duration of Action | Oral immediate-release: analgesic effect 4-6 hours; antipyretic effect 6-8 hours. Extended-release forms: up to 12 hours. Duration may be shorter with higher pain intensity. |
| Molecular Weight | 206.28 |
Ibuprofen (Motrin) 200-800 mg orally every 6-8 hours as needed; maximum 3200 mg/day for acute pain, and 2400 mg/day for chronic use.
| Dosage form | SUSPENSION/DROPS |
| Renal impairment | GFR 30-59 mL/min: use minimum effective dose, monitor renal function; GFR <30 mL/min: avoid use; dialysis: not removed by hemodialysis, avoid use. |
| Liver impairment | Child-Pugh Class A: no adjustment; Class B: use with caution, reduce dose by 50%; Class 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, not to exceed adult maximum; for fever >39°C, 10 mg/kg/dose; available as oral suspension (100 mg/5 mL). |
| Geriatric use | Initiate at the lowest effective dose (e.g., 200-400 mg every 6-8 hours), maximum 3200 mg/day; monitor for GI bleeding and renal impairment; avoid prolonged use due to increased cardiovascular and GI risks. |
| 1st trimester | Avoid use due to potential increased risk of miscarriage and malformations (e.g., gastroschisis). Use only if clearly needed and after consideration of alternatives. |
| 2nd trimester | Use with caution; associated with risk of oligohydramnios and fetal renal dysfunction. Short-term use at lowest effective dose is preferred. |
| 3rd trimester | Contraindicated due to risk of premature closure of the ductus arteriosus, pulmonary hypertension, and oligohydramnios. |
Clinical note
Comprehensive clinical and safety monograph for MOTRIN (MOTRIN).
| Placental transfer | Ibuprofen readily crosses the placenta with a cord-to-maternal ratio of approximately 0.5-0.9. |
| Breastfeeding | Ibuprofen (Motrin) is excreted into breast milk in very low amounts (<1% of maternal dose). Considered compatible with breastfeeding; use lowest effective dose for shortest duration. Monitor infant for potential adverse effects (e.g., gastrointestinal upset). |
■ FDA Black Box Warning
Nonsteroidal anti-inflammatory drugs (NSAIDs) cause an increased risk of serious cardiovascular thrombotic events, including myocardial infarction and stroke, which can be fatal. This risk may occur early in treatment and may increase with duration of use. Contraindicated for treatment of perioperative pain in the setting of coronary artery bypass graft (CABG) surgery.
| Serious Effects |
Known hypersensitivity to ibuprofen or any NSAIDHistory of asthma, urticaria, or allergic-type reactions after taking aspirin or other NSAIDsActive peptic ulcer disease or gastrointestinal bleedingSevere heart failure (NYHA Class III/IV)History of coronary artery bypass graft (CABG) surgery in the perioperative settingThird trimester of pregnancySevere renal impairment (CrCl <30 mL/min)Severe hepatic impairment (Child-Pugh Class C)
| Precautions | Increased risk of cardiovascular thrombotic events; risk of serious GI adverse events including bleeding, ulceration, and perforation; renal toxicity; hypertension; anaphylactoid reactions; serious skin reactions; hematologic toxicity; avoid in advanced renal disease. |
| Food/Dietary |
Loading safety data…
| Lactation Rating | L1 (Safe) |
| Teratogenic Risk | Motrin (ibuprofen) is an NSAID. First trimester: Risk of miscarriage and congenital malformations, particularly cardiac defects, with use. Second trimester: Generally considered safer but avoid prolonged use due to potential for oligohydramnios. Third trimester: Contraindicated after 20 weeks due to risk of premature ductus arteriosus closure, oligohydramnios, and neonatal complications including pulmonary hypertension and renal impairment. |
| Fetal Monitoring | In pregnancy, monitor for signs of oligohydramnios (ultrasound, amniotic fluid index) and evaluate fetal echocardiography if used in third trimester. Monitor maternal renal function, blood pressure, and signs of gastrointestinal bleeding. Fetal monitoring may include Doppler studies for ductus arteriosus patency if used near term. |
| Fertility Effects | Ibuprofen may impair fertility by interfering with ovulation through inhibition of prostaglandin synthesis, which is reversible upon discontinuation. Chronic use can affect luteinized unruptured follicle syndrome and may delay conception. |
| Concurrent alcohol consumption increases risk of GI bleeding and ulceration. Avoid high-sodium foods to minimize fluid retention and potential exacerbation of hypertension. Grapefruit juice may slightly reduce rate of absorption but is not clinically significant. |
| Clinical Pearls | For acute pain, use lowest effective dose for shortest duration to minimize GI and renal risks. Administer with food or milk to reduce GI irritation. Avoid in patients with severe renal impairment (CrCl <30 mL/min) or active peptic ulcer disease. Ibuprofen can mask fever, making infection detection difficult. Caution in asthma patients as it may precipitate bronchospasm. Monitor blood pressure in hypertensive patients due to potential for fluid retention. |
| Patient Advice | Take with food or milk to prevent stomach upset. · Do not exceed 1200 mg per day for OTC use (adults) or as directed by your doctor. · Avoid alcohol while taking this medication to reduce risk of stomach bleeding. · Stop use and consult doctor if symptoms persist for more than 10 days (pain) or 3 days (fever). · Do not take with other NSAIDs or pain relievers without consulting your healthcare provider. · Notify your doctor if you have a history of heart disease, high blood pressure, or stomach ulcers. |