Introduction
Motrin (ibuprofen) is a widely used nonsteroidal anti-inflammatory drug (NSAID) available both by prescription and over-the-counter. First approved by the FDA in 1974, it belongs to the propionic acid derivative class of NSAIDs and is commonly used for its analgesic, antipyretic, and anti-inflammatory properties.
Mechanism of Action
Ibuprofen exerts its therapeutic effects through nonselective inhibition of cyclooxygenase (COX) enzymes, primarily COX-1 and COX-2. These enzymes catalyze the conversion of arachidonic acid to prostaglandins, thromboxanes, and prostacyclins. By inhibiting prostaglandin synthesis, ibuprofen reduces inflammation, pain, and fever. The antipyretic effect is mediated through action on the hypothalamic heat-regulating center.
Indications
FDA-approved indications:- Mild to moderate pain
- Primary dysmenorrhea
- Inflammatory diseases including rheumatoid arthritis and osteoarthritis
- Fever reduction
- Migraine headaches
- Gout attacks
- Patent ductus arteriosus closure in premature infants (IV formulation)
Dosage and Administration
Adults:- Analgesia/antipyresis: 200-400 mg every 4-6 hours (max 1200 mg/day OTC, 3200 mg/day prescription)
- Rheumatoid arthritis/osteoarthritis: 400-800 mg three to four times daily (max 3200 mg/day)
- Fever/pain: 5-10 mg/kg every 6-8 hours (max 40 mg/kg/day)
- Renal impairment: Use lowest effective dose; avoid if severe impairment
- Hepatic impairment: Use with caution; consider dose reduction
- Elderly: Start with lower doses due to increased NSAID sensitivity
- Take with food or milk to minimize GI upset
- Swallow tablets whole with adequate fluid
Pharmacokinetics
Absorption: Rapid and complete oral absorption with peak plasma concentrations within 1-2 hours Distribution: Volume of distribution ~0.1 L/kg; 99% protein-bound; crosses placenta and enters breast milk Metabolism: Primarily hepatic via CYP2C9 with minor metabolism via CYP2C8 Elimination: Half-life 2-4 hours; excreted primarily in urine (90%) as metabolites and unchanged drugContraindications
- Hypersensitivity to ibuprofen or other NSAIDs
- History of asthma, urticaria, or allergic reactions after taking aspirin or NSAIDs
- Perioperative pain in coronary artery bypass graft (CABG) surgery
- Third trimester of pregnancy
Warnings and Precautions
Boxed Warning:- Increased risk of serious cardiovascular thrombotic events, including MI and stroke
- Increased risk of serious GI adverse events including bleeding, ulceration, and perforation
- Hypertension exacerbation or new onset
- Heart failure exacerbation
- Renal toxicity, including papillary necrosis
- Hepatotoxicity
- Anaphylactoid reactions
- Serious skin reactions
- Hematologic toxicity (anemia, bleeding)
Drug Interactions
Major interactions:- Anticoagulants (warfarin): Increased bleeding risk
- Aspirin: Decreased antiplatelet effect
- Other NSAIDs: Increased toxicity
- ACE inhibitors/ARBs: Reduced antihypertensive effect
- Diuretics: Reduced diuretic effectiveness
- Lithium: Increased lithium levels
- Methotrexate: Increased methotrexate toxicity
Adverse Effects
Common (≥1%):- Nausea, epigastric pain
- Dyspepsia, heartburn
- Diarrhea or constipation
- Dizziness, headache
- Rash
- GI bleeding/ulceration
- Cardiovascular events
- Acute renal failure
- Hepatotoxicity
- Anaphylaxis
- Stevens-Johnson syndrome
- Aseptic meningitis
Monitoring Parameters
- Blood pressure at initiation and periodically
- Renal function (BUN, creatinine) in at-risk patients
- Liver enzymes with long-term use
- Hemoglobin/hematocrit with chronic use
- GI symptoms assessment
- Signs of fluid retention
- Therapeutic response and pain control
Patient Education
- Take with food to reduce stomach upset
- Do not exceed recommended dosage
- Avoid concurrent use with other NSAIDs
- Report signs of GI bleeding (black stools, abdominal pain)
- Seek immediate care for chest pain, shortness of breath, weakness
- Discuss all medication use with healthcare provider
- Avoid alcohol during therapy
- Notify provider if pregnancy is suspected
- Store at room temperature away from moisture
References
1. FDA Prescribing Information: Motrin (ibuprofen) 2. Brunton LL, Hilal-Dandan R, Knollmann BC. Goodman & Gilman's: The Pharmacological Basis of Therapeutics. 13th ed. 3. McEvoy GK, ed. AHFS Drug Information. American Society of Health-System Pharmacists. 4. Cryer B, Feldman M. Effects of nonsteroidal anti-inflammatory drugs on endogenous gastrointestinal prostaglandins and therapeutic strategies for prevention and treatment of nonsteroidal anti-inflammatory drug-induced damage. Arch Intern Med. 1992;152(6):1145-1155. 5. McGettigan P, Henry D. Cardiovascular risk with non-steroidal anti-inflammatory drugs: systematic review of population-based controlled observational studies. PLoS Med. 2011;8(9):e1001098. 6. American Geriatrics Society Beers Criteria Update Expert Panel. American Geriatrics Society 2023 Updated AGS Beers Criteria for Potentially Inappropriate Medication Use in Older Adults. J Am Geriatr Soc. 2023;71(7):2052-2081.