Ibuprofen

Ibuprofen (INN) is a non-steroidal anti-inflammatory drug (NSAID) widely marketed under various trademarks including Herron Blue, Act-3, Advil, Brufen, Motrin, Nuprin, and Nurofen. It is used for relief of symptoms of arthritis, primary dysmenorrhoea, fever, and as an analgesic, especially where there is an inflammatory component. Ibuprofen was developed by the research arm of Boots Group.

Clinical use

Low doses of ibuprofen (200 mg., and sometimes 400 mg.) are available over the counter (OTC) in most countries. Ibuprofen has a dose-dependent duration of action of approximately 4–8 hours, which is longer than suggested by its short half-life. The recommended dose varies with body mass and indication. Generally, the oral dose is 200–400 mg (5–10 mg/kg in children) every 4–6 hours, up to a usual maximum daily dose of 800–1200 mg. Under medical direction, a maximum daily dose of 3200 mg may sometimes be used.

Off-Label and investigational use

  • As with other NSAIDs, ibuprofen may be useful in the treatment of severe orthostatic hypotension.
  • In some studies, ibuprofen showed superior results compared to placebo in the prophylaxis of Alzheimer's disease, when given in low doses over a long time. Further studies are needed to confirm the results before ibuprofen can be recommended for this indication.
  • Ibuprofen has been associated with a lower risk of Parkinson's disease, and may delay or prevent Parkinson's disease. Aspirin, other NSAIDs, and paracetamol had no effect on the risk for Parkinson's. Further research is warranted before recommending ibuprofen for this use.

    • Ibuprofen lysine

    In Europe, Australia, and New Zealand, ibuprofen lysine (ibuprofenlysinat, the lysine salt of ibuprofen) is licensed for treatment of the same conditions as ibuprofen. Ibuprofen lysine has been shown to have a more rapid onset of action compared to base ibuprofen.

    Mechanism of action

    Ibuprofen is an NSAID which is believed to work through inhibition of cyclooxygenase (COX), thus inhibiting prostaglandin synthesis. There are at least 2 variations of cyclooxygenase (COX-1 and COX-2), ibuprofen inhibits both COX-1 and COX-2. It appears that its analgesic, antipyretic, and anti-inflammatory activity are achieved principally through COX-2 inhibition; whereas COX-1 inhibition is responsible for its unwanted effects on platelet aggregation and the GI mucosa.

    Adverse effects

    Ibuprofen appears to have the lowest incidence of gastrointestinal adverse drug reactions (ADRs) of all the non-selective NSAIDs. However, this only holds true at lower doses of ibuprofen, so over-the-counter preparations of ibuprofen are generally labelled to advise a maximum daily dose of 1,200 mg.

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