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Ibuprofen was born in a Boots lab in Nottingham in 1961

One of the world's most familiar painkillers came out of a Boots research lab in Nottingham, where Stewart Adams and John Nicholson discovered it in 1961. First sold as Brufen, ibuprofen now sits on the WHO's essential medicines list, and the enzyme trick that eases pain may also account for its best-known side effects.

Britain got the drug in 1969 and the United States in 1974, and it now travels under names such as Advil, Motrin and Nurofen as well as in generic form. In 2023 it ranked 32nd among American prescriptions, with more than 17 million written. It is taken by mouth or into a vein, usually starts acting within an hour, and is used for fever, mild to moderate pain, period pain, migraine and rheumatoid arthritis. Roughly 60% of people respond to any given anti-inflammatory of this class, and someone who gets little from one may do better on another. A salt form, ibuprofen lysine, won FDA approval in 2006 to help close a persistent fetal blood vessel in premature babies weighing 500 to 1,500 g.

Its target is cyclooxygenase, the COX enzyme that turns arachidonic acid into a molecule called PGH2. That compound is the raw material for prostaglandins, which drive pain, inflammation and fever, and for thromboxane A2, which helps platelets clump. Like aspirin, ibuprofen blocks both COX-1 and COX-2; relief is thought to come mainly from the second, while the first is blamed for stomach trouble, though the split is not settled. Tablets contain two mirror-image forms, and the body converts the weaker R form into the more active S form. Levels peak after 1–2 hours, and most of a dose leaves in the urine within 24 hours. Unusually, it also inhibits Rho kinase and the sweet taste receptor.

Common problems include heartburn, nausea and indigestion, with gastrointestinal bleeding a known risk and kidney failure linked to long-term use. It can aggravate asthma and heart failure, and at higher doses may raise heart attack risk; on 9 July 2015 the FDA strengthened its warnings on heart attack and stroke for this drug family, excluding aspirin, and European regulators followed. The FDA also notes ibuprofen can blunt low-dose aspirin's protective effect on platelets, and alcohol may add to the chance of stomach bleeding.

Pregnancy evidence is mixed. A 2012 Canadian study linked these drugs to a 2.4-fold higher miscarriage rate, while a 2014 Israeli study found no increase and argued the earlier work missed key confounders; use late in pregnancy appears harmful. Overdoses have become common since over-the-counter sale, though serious complications are rare, and toxicity is unlikely below 100 mg/kg.

Source: Ibuprofen

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