 |
|
| ||||||||||||||||||||||||||
|
|
| ||||||||||||||||||||||||||
|
|
|
|
|
| ||||||||
|
| |
|
2-(para-isobutylphenyl)propionic acid | |
| Empirical formula | C13H18O2 |
| Molecular weight | 206.3 |
| Bioavailability (Oral) | unknown |
| Metabolism | hepatic |
| Half life | 1.9-2.2 hours |
| Excretion | renal |
| Pregnancy category | C (Australia) |
Ibuprofen is a nonsteroidal anti-inflammatory drug used to relieve the symptoms of arthritis, primary dysmenorrhoea, pyrexia; and as an analgesic, especially where there is an inflammatory component . Ibuprofen was developed by the research arm of Boots. It is widely marketed under the trade names including Advil®, Nurofen®, Motrin®, Nuprin®, Brufen® and Act-3®.
Approved clinical indications for ibuprofen include:
Ibuprofen is used widely in the community for the relief of headache including migraine. It is also widely marketed as an analgetic agent (rather than as an antiinflammatory) and is often used for general pain conditions including those that arise from various injuries (such as sporting injuries), illnesses (such as influenza, shingles, gout), and post-operative pain.
Ibuprofen is an NSAID and, as such, is believed to work through inhibition of cyclooxygenase (COX); thus inhibiting prostaglandin synthesis.
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 1.2 grams.
Common adverse effects include: nausea, dyspepsia, gastrointestinal ulceration/bleeding, raised liver enzymes, diarrhoea, headache, dizziness, salt and fluid retention, hypertension (AMH, 2004)
Infrequent adverse effects include: oesophageal ulceration, heart failure, hyperkalaemia, renal impairment, confusion, bronchospasm, rash (AMH, 2004)
Ibuprofen, like other 2-arylpropionate derivatives (including ketoprofen, flurbiprofen, naproxen, etc) contains a chiral carbon in the β-position of the propionate moiety. As such there are two possible enantiomers of ibuprofen with the potential for different biological effects and metabolism for each enantiomer.
Indeed it was found that S-ibuprofen was the active form both in vitro and in vivo.
Logically then, there was the potential for improving the selectivity and potency of ibuprofen formulations by marketing ibuprofen as a single-enantiomer product (as occurs with naproxen, another NSAID).
Further in vivo testing, however, revealed the existence of an isomerase which converted R-ibuprofen to the active S-enantiomer. Thus, due to the expense and futility that might be involved in marketing the single-enantiomer, all ibuprofen formulations currently marketed are a racemic mixture of both enantiomers.
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 is now an increasing trend towards descheduling ibuprofen such that it will be available in supermarkets and other general retailers.
| Analgesics | |||||||
|---|---|---|---|---|---|---|---|
|
| ||||||
| [ ] | |||||||
This article is part of the Wikiproject on Drugs, which is an attempt to facilitate the categorization and creation of accurate and formal drug-related articles on BambooWeb. If you are interested in editing this article, please see its talk page and ensure your edits are consistent with the goals of the project.
|
||||
| View Live Article | This article is from Wikipedia. All text is available under the terms of the GNU Free Documentation License | |
||
