|
Ibuprofen (INN) (IPA: ) 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 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. Main article: Non-steroidal anti-inflammatory drug 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. Main article: Non-steroidal anti-inflammatory drug Reported adverse drug reactions In low single doses (200 to 400 mg) and daily doses of up to 1,200 mg the incidence of side effects is low. However, in patients treated on a long-term basis with more than 1,200 mg daily discontinuation rates are as high as 10 to 15%. Common adverse effects include: nausea, dyspepsia, gastrointestinal ulceration/bleeding, raised liver enzymes, diarrhoea, headache, dizziness, salt and fluid retention, hypertension.• Photosensitivity As with other NSAIDs, ibuprofen has been reported to be a photosensitising agent. However, this only rarely occurs with ibuprofen and it is considered to be a very weak photosensitising agent when compared with other members of the 2-arylpropionic acids. This is because the ibuprofen molecule contains only a single phenyl moiety and no bond conjugation, resulting in a very weak chromophore system and a very weak absorption spectrum which does not reach into the solar spectrum. Cardiovascular risk Along with several other NSAIDs, ibuprofen has been implicated in elevating the risk of myocardial infarction, particularly among those chronically using high doses.• Stereochemistry
Human toxicology Ibuprofen overdose has become common since it was licensed for over-the-counter use. There are many overdose experiences reported in the medical literature.• Since ibuprofen has acidic properties and is also excreted in the urine, forced alkaline diuresis is theoretically beneficial. However, due to the fact ibuprofen is highly protein bound in the blood, there is minimal renal excretion of unchanged drug. Forced alkaline diuresis is therefore of limited benefit.• Symptomatic therapy for hypotension, GI bleeding, acidosis, and renal toxicity may be indicated. Occasionally, close monitoring in an intensive care unit for several days is necessary. If a patient survives the acute intoxication, he/she will usually experience no late sequelae. Availability Ibuprofen was made available under prescription in the United Kingdom in 1969. In the years since, the good tolerability profile along with extensive experience in the community (otherwise known as Phase IV trials), has resulted in the rescheduling of small packs of ibuprofen to allow availability over-the-counter in pharmacies worldwide. Indeed there has been an increasing trend towards descheduling ibuprofen such that it is now available in supermarkets and other general retailers. The wider availability has meant that ibuprofen is now almost as commonly used as aspirin and paracetamol. See also | |||||||||
|
| ||||||||||
 |
|
| |