Ibuprofen (Brufen, Ibufen)

Clinical pharmacology of ibuprofen
Abdelwahab Ward, BS Pharm, PharmD
Analgesic, NSAID (nonopioid), anti-inflammatory, antipyretic and antirheumatic. For further information, see topic on Recommendations for safety use of NSAIDs.
Mechanism of Action ã…¡ Ibuprofen competitively inhibits both cyclooxygenase (COX) isoenzymes, COX-1 and COX-2, by blocking arachidonate binding resulting in analgesic, antipyretic, and anti-inflammatory pharmacologic effects.

  • Fever and headache
  • Treatment of dysmenorrhea.
  • Treatment of rheumatoid arthritis (RA) and juvenile rheumatoid arthritis
  • Severe pain in hospitalized patients.
  • For self-treatment of minor aches and pains due to the common cold, toothache, muscular aches or backache (musculoskeletal pain), and the minor pains of arthritis.
  • Osteoarthritis and acute gouty arthritis
  • Patients with cystic fibrosis to slow the rate of decline in lung function.
  • Analgesia (Adult): 200-400 mg, Every 4-6 hrs.
  • Anti-inflammatory: (Adult) 300 mg, Every 6-8 hrs or 400-800 mg 3-4 times daily, (Children) 20-40 mg/kg/day in 3-4 divided dose.
  • Anti pyretic (Children): 5-10 mg/kg. Every 6 hrs (max. 40 mg/kg per day).
  • Contraindicated with allergy to ibuprofen, salicylates, or other NSAIDs (more common in patients with rhinitis, asthma, chronic urticaria, nasal polyps). Black box warning, Contraindicated for treatment of perioperative pain after coronary artery bypass graft.
  • Use cautiously with CV dysfunction, hypertension, peptic ulceration, GI bleeding, pregnancy, lactation, impaired hepatic or renal function.
  • Route: Oral and rectal
  • Peak: 1–2 hours
  • Duration: 4–6 hours
  • Metabolism: Hepatic; T1/2: 1.8–2.5 hr
  • Distribution: Crosses placenta; may enter breast milk (best analgesic choice for breastfeeding)
  • Excretion: Urine
  • Gastrointestinal effects include gastrointestinal intolerance, gastrointestinal bleeding and peptic ulcer disease (Erosive Gastritis). For further information, see topic on Peptic ulcer, assessment and management.
  • Central nervous system effects include headache, dizziness, somnolence, insomnia, fatigue, tiredness, dizziness, tinnitus.
  • Ophthalmologic effects.
  • Cardiovascular: Hypertension, palpitations, arrhythmia, heart failure.
  • Respiratory: Dyspnea, hemoptysis, pharyngitis, bronchospasm, rhinitis.
  • Hematologic: Bleeding, platelet inhibition with higher doses, neutropenia, eosinophilia, leukopenia, pancytopenia, thrombocytopenia, agranulocytosis, granulocytopenia, aplastic anemia, decreased Hgb or Hct, bone marrow depression.
  • Increased toxic effects of lithium with ibuprofen.
  • Decreased diuretic effect with loop diuretics—bumetanide, furosemide, ethacrynic acid.
  • Potential decrease in antihypertensive effect of beta-adrenergic blocking drugs and ACE inhibitors.
  • Increased risk of gastric ulceration with bisphosphonates.
  • Increased risk of bleeding with anticoagulants.
  • Increased risk of bleeding with concurrent use of ginkgo biloba.
Abdelwahab Ward, BS Pharm, PharmD