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ibuprofen

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ibuprofen
IUPAC name(RS)-2-(4-(2-methylpropyl)phenyl)propanoic acid
Width200
TradenameAdvil, Motrin, Nurofen, others
Drugs.commonograph, ibuprofen
Legal AUS2
Legal UKGSL
Legal USOTC
Routes of administrationBy mouth, topical, intravenous

ibuprofen is a widely used nonsteroidal anti-inflammatory drug (NSAID) employed for treating pain, fever, and inflammation. It is available over-the-counter in most countries under various brand names like Advil and Motrin. The medication works by inhibiting cyclooxygenase enzymes, thereby reducing the production of prostaglandins.

Medical uses

ibuprofen is indicated for the relief of mild to moderate pain, including conditions like dysmenorrhea, migraine, and dental pain. It is also effective in reducing fever and managing inflammatory diseases such as rheumatoid arthritis and osteoarthritis. Clinical guidelines from organizations like the American College of Rheumatology often recommend it as a first-line therapy. It is commonly used for post-surgical pain, such as following tonsillectomy, and is a component of some cold and flu preparations marketed by companies like Reckitt Benckiser.

Adverse effects

Common adverse effects involve the gastrointestinal tract, including dyspepsia and, with long-term use, an increased risk of peptic ulcer disease and gastrointestinal bleeding. The drug carries warnings from the U.S. Food and Drug Administration (FDA) regarding cardiovascular risks, such as myocardial infarction and stroke, particularly with high doses. Other potential effects include impaired renal function, hepatotoxicity, and rare but severe Stevens–Johnson syndrome. Concurrent use with other NSAIDs like naproxen or anticoagulants such as warfarin can increase these risks.

Pharmacology

ibuprofen functions as a non-selective inhibitor of cyclooxygenase-1 and cyclooxygenase-2 (COX-1 and COX-2), enzymes crucial for the synthesis of prostaglandins and thromboxane. It is administered as a racemic mixture; the S-enantiomer is primarily responsible for its anti-inflammatory activity through interference with the arachidonic acid pathway. The drug is well-absorbed orally, highly bound to plasma proteins, and metabolized in the liver by enzymes including CYP2C9. Its metabolites are excreted primarily by the kidneys.

History

ibuprofen was discovered in 1961 by Stewart Adams and his team at the Boots UK research laboratory in Nottingham. It was developed as a safer alternative to aspirin and was first launched in the United Kingdom in 1969 under the brand name Brufen. It received approval from the U.S. Food and Drug Administration for prescription use in 1974 and became available over-the-counter in the United States in 1984. The patent for ibuprofen is held by Boots Pure Drug Company.

Society and culture

ibuprofen is one of the most commonly used medications globally, listed on the World Health Organization's List of Essential Medicines. It is marketed under numerous brand names worldwide, including Nurofen in Australia and Advil by Pfizer. Its availability has been impacted by regulatory actions, such as those by the European Medicines Agency. The drug's profile has been featured in media, including discussions on programs like BBC News, and it is a subject of ongoing research at institutions like the University of Oxford.

Category:Drugs