Introduction
Advil (ibuprofen) is a widely used nonsteroidal anti-inflammatory drug (NSAID) available both by prescription and over-the-counter. It belongs to the propionic acid derivative class of NSAIDs and is marketed by Pfizer. First approved by the FDA in 1974, ibuprofen has become one of the most commonly used medications worldwide for its analgesic, anti-inflammatory, and antipyretic properties.
Mechanism of Action
Ibuprofen exerts its therapeutic effects through nonselective inhibition of cyclooxygenase (COX) enzymes, specifically COX-1 and COX-2. These enzymes are responsible for the conversion of arachidonic acid to prostaglandins, thromboxanes, and prostacyclins. By inhibiting prostaglandin synthesis, ibuprofen reduces inflammation, pain, and fever. The analgesic effect is primarily peripheral, though some central nervous system activity may contribute to its pain-relieving properties.
Indications
FDA-Approved Indications:- Mild to moderate pain
- Inflammatory diseases including rheumatoid arthritis and osteoarthritis
- Primary dysmenorrhea
- Fever reduction
- Migraine headaches
- Gout
- Ankylosing spondylitis
- Juvenile idiopathic arthritis
Dosage and Administration
Adults:- Analgesia/Antipyretic: 200-400 mg every 4-6 hours (max 1200 mg/day OTC; 3200 mg/day prescription)
- Inflammatory conditions: 400-800 mg three to four times daily
- Fever: 5-10 mg/kg every 6-8 hours (max 40 mg/kg/day)
- Juvenile arthritis: 30-40 mg/kg/day in 3-4 divided doses
- Renal impairment: Use lowest effective dose; avoid in advanced renal disease
- Hepatic impairment: Use with caution; consider dose reduction
- Elderly: Start with lowest effective dose due to increased risk of adverse effects
Pharmacokinetics
Absorption: Rapid and complete oral absorption with peak concentrations occurring within 1-2 hours Distribution: Volume of distribution approximately 0.1-0.2 L/kg; 99% protein-bound Metabolism: Primarily hepatic via CYP2C9 with minor metabolism via CYP2C8 and CYP3A4 Elimination: Half-life of 2-4 hours; excreted primarily in urine (90%) with less than 1% excreted unchanged Food Effect: Rate of absorption decreased with food, but total bioavailability unaffectedContraindications
- Hypersensitivity to ibuprofen or other NSAIDs
- History of asthma, urticaria, or allergic-type reactions after taking aspirin or other NSAIDs
- Peri-operative pain in setting of coronary artery bypass graft (CABG) surgery
- Third trimester of pregnancy
Warnings and Precautions
Boxed Warning:- Increased risk of serious cardiovascular thrombotic events, myocardial infarction, and stroke
- Increased risk of serious gastrointestinal bleeding, ulceration, and perforation
- Hypertension exacerbation or new-onset hypertension
- Renal toxicity, including acute renal failure
- Hepatotoxicity with elevated liver enzymes
- Anaphylactoid reactions
- Hematologic effects including anemia and bleeding
- Fluid retention and edema
- Exacerbation of asthma in aspirin-sensitive patients
Drug Interactions
Major Interactions:- Aspirin: Decreased cardioprotective effect of aspirin
- Anticoagulants (warfarin): Increased bleeding risk
- Other NSAIDs: Increased risk of gastrointestinal toxicity
- ACE inhibitors/ARBs: Reduced antihypertensive effect
- Diuretics: Reduced diuretic effectiveness
- Lithium: Increased lithium levels
- Methotrexate: Increased methotrexate toxicity
- CYP2C9 inhibitors (fluconazole, amiodarone): Increased ibuprofen levels
- CYP2C9 inducers (rifampin): Decreased ibuprofen levels
Adverse Effects
Common (≥1%):- Dyspepsia (10-15%)
- Nausea (3-9%)
- Headache (1-5%)
- Dizziness (3-9%)
- Rash (3-9%)
- Gastrointestinal bleeding and ulceration
- Cardiovascular thrombotic events
- Acute renal failure
- Hepatotoxicity
- Severe skin reactions (Stevens-Johnson syndrome, toxic epidermal necrolysis)
- Anaphylaxis
Monitoring Parameters
- Blood pressure at baseline and periodically during treatment
- Renal function (BUN, creatinine) in patients at risk
- Liver function tests with long-term use
- Complete blood count with chronic therapy
- Gastrointestinal symptoms assessment
- Signs of fluid retention
- Therapeutic response and pain control
Patient Education
- Take with food or milk to minimize gastrointestinal upset
- Use lowest effective dose for shortest duration possible
- Do not exceed recommended dosage
- Avoid concurrent use with other NSAIDs or aspirin
- Report signs of gastrointestinal bleeding (black stools, abdominal pain)
- Report signs of allergic reaction (rash, swelling, difficulty breathing)
- Monitor for cardiovascular symptoms (chest pain, shortness of breath)
- Avoid alcohol consumption during therapy
- Notify healthcare provider if pregnant, planning pregnancy, or breastfeeding
- Store at room temperature away from moisture
References
1. FDA Prescribing Information: Advil (ibuprofen). 2023 2. Brunton LL, Hilal-Dandan R, Knollmann BC. Goodman & Gilman's: The Pharmacological Basis of Therapeutics. 13th ed. 2017 3. McEvoy GK, ed. AHFS Drug Information. American Society of Health-System Pharmacists. 2023 4. Rainsford KD. Ibuprofen: pharmacology, efficacy and safety. Inflammopharmacology. 2009;17(6):275-342 5. Coxib and traditional NSAID Trialists' (CNT) Collaboration. Vascular and upper gastrointestinal effects of non-steroidal anti-inflammatory drugs: meta-analyses of individual participant data from randomised trials. Lancet. 2013;382(9894):769-779 6. American Geriatrics Society. Updated AGS Beers Criteria® for Potentially Inappropriate Medication Use in Older Adults. J Am Geriatr Soc. 2023;71(7):2052-2081