Ibuprofen

[10] Ibuprofen was discovered in 1961 by Stewart Adams and John Nicholson[12] while working at Boots UK Limited and initially marketed as Brufen.[24] In 2006, ibuprofen lysine was approved in the United States by the Food and Drug Administration (FDA) for closure of patent ductus arteriosus in premature infants weighing between 500 and 1,500 g (1 and 3 lb), who are no more than 32 weeks gestational age when usual medical management (such as fluid restriction, diuretics, and respiratory support) is not effective.[25] Adverse effects include nausea, heartburn, indigestion, diarrhea, constipation, gastrointestinal ulceration, headache, dizziness, rash, salt and fluid retention, and high blood pressure.[8][21][26] Infrequent adverse effects include esophageal ulceration, heart failure, high blood levels of potassium, kidney impairment, confusion, and bronchospasm.[28] Ibuprofen may be quantified in blood, plasma, or serum to demonstrate the presence of the drug in a person having experienced an anaphylactic reaction, confirm a diagnosis of poisoning in people who are hospitalized, or assist in a medicolegal death investigation.A monograph relating ibuprofen plasma concentration, time since ingestion, and risk of developing renal toxicity in people who have overdosed has been published.[29] In October 2020, the U.S. FDA required the drug label to be updated for all NSAID medications to describe the risk of kidney problems in unborn babies that result in low amniotic fluid.If ibuprofen is taken only occasionally without the recommended timing, though, the reduction of the cardioprotection and stroke prevention of a daily aspirin regimen is minimal.Most symptoms are an excess of the pharmacological action of ibuprofen and include abdominal pain, nausea, vomiting, drowsiness, dizziness, headache, ear ringing, and nystagmus.Rarely, more severe symptoms such as gastrointestinal bleeding, seizures, metabolic acidosis, hyperkalemia, low blood pressure, slow heart rate, fast heart rate, atrial fibrillation, coma, liver dysfunction, acute kidney failure, cyanosis, respiratory depression, and cardiac arrest have been reported.PGH2, in turn, is converted by other enzymes into various prostaglandins (which mediate pain, inflammation, and fever) and thromboxane A2 (which stimulates platelet aggregation and promotes blood clot formation).The analgesic, antipyretic, and anti-inflammatory activity of NSAIDs appears to operate mainly through inhibition of COX-2, which decreases the synthesis of prostaglandins involved in mediating inflammation, pain, fever, and swelling.Antipyretic effects may be due to action on the hypothalamus, resulting in an increased peripheral blood flow, vasodilation, and subsequent heat dissipation.[55] Ibuprofen is practically insoluble in water, but very soluble in most organic solvents like ethanol (66.18 g/100 mL at 40 °C for 90% EtOH), methanol, acetone and dichloromethane.A modern, greener technique with fewer waste byproducts for the synthesis involves only three steps and was developed in the 1980s by the Celanese Chemical Company.[78] In November 2013, work on ibuprofen was recognized by the erection of a Royal Society of Chemistry blue plaque at Boots' Beeston Factory site in Nottingham,[79] which reads: In recognition of the work during the 1980s by The Boots Company PLC on the development of ibuprofen which resulted in its move from prescription-only status to over-the-counter sale, therefore expanding its use to millions of people worldwideand another at BioCity Nottingham, the site of the original laboratory,[79] which reads: In recognition of the pioneering research work, here on Pennyfoot Street, by Dr Stewart Adams and Dr John Nicholson in the Research Department of Boots which led to the discovery of ibuprofen used by millions worldwide for the relief of pain.Ibuprofen was made available by prescription in the United Kingdom in 1969 and in the United States in 1974.[91] In March 2011, researchers at Harvard Medical School announced in Neurology that ibuprofen had a neuroprotective effect against the risk of developing Parkinson's disease.[92][93][94] People regularly consuming ibuprofen were reported to have a 38% lower risk of developing Parkinson's disease, but no such effect was found for other pain relievers, such as aspirin and paracetamol.Use of ibuprofen to lower the risk of Parkinson's disease in the general population would not be problem-free, given the possibility of adverse effects on the urinary and digestive systems.