Rita Fabela 5th Hour 1/17/2010

Ibuprofen
Ibuprofen is an NSAID (non-steroidal anti-inflammatory drug). Nonsteroidal means they are not steroids, which often have similar effects. They are generally non-narcotic. Along with ibuprofen, aspirin, and narpoxen mainly because most of them are over the counter medications.The chemical formula is C13H18O2. It's name comes from the nomenclature iso-butylpropanic-phenolic acid. It is also known as Nurofen, Advil, and Motrin. It is a white powder that belongs to the propionic acid derivatives, with a melting point of 74 to 77 degrees. It is slightly soluble in water and readily soluble in organic solvents such as ethanol. Racemic Ibuprofen is usually used, still only one form is active medicinally. Ibuprofen was derived from propionic acid by the research arm of Boots Group during the 1960s, discovered by Stewart Adams, with colleagues Andrew RM Dunlop, John Nicholson, Jeffery Bruce Wilson & Colin Burrows and was patented in 1961. The drug was launched as a treatment for rheumatoid arthritis in the United Kingdom in 1969, and in the United States in 1974. Famously, it is recorded that Dr. Adams initially tested his drug on a hangover. He was subsequently awarded an OBE in 1987. Boots was awarded the Queen's Award For Technical Achievement for the development of the drug in the same year. There have been many commercial and laboratory publications for the synthesis of Ibuprofen. Two of the most popular ways to obtain Ibuprofen are the Boot process and the Hoechst process. The Boot process is an older commercial process developed by the Boot Pure Drug Company and the Hoechst process is a newer process developed by the Hoechst Company. Most of these routes to Ibuprofen begin with isobutylbenzene and use Friedel-Crafts acylation. The Boot process requires six steps, while the Hoechst process, with the assistance of catalysts, is completed in only three steps.Cheminor Drugs have developed a process for an improved version of ibuprofen based on chiral synthesis. The move is significant given that pure S-Ibuprofen (the active form of ibuprofen) could near halve the regular ibuprofen dosage, besides improving the side-effect profile.However the human body can convert the inactive (R) form into the (S) form, so eventually 100% of the ibuprofen taken becomes active. The process discovered by Cheminor is therefore unlikely to have commercial significance. It is generally used for relieving muscular and skeletal pain. It also can be used as relieve postoperative pain and morning stiffness and has been shown to slow down pulmonary decline in cystic fibrosis sufferers. Ibuprofen blocks the production of prostaglandins. It can

cause pain and swelling. The prostaglandins are released to our brain and can cause fever. Ibuprofen's painkilling effects immediately take effect after dose is taken, but for the anti-inflammatory effects it can take a bit longer, sometimes even a few weeks Ibuprofen can also have its side effects. The most common are diarrhea, nausea, vomiting, dyspepsia, and any pain in the stomach or intestines. But it can also cause dizziness, edema, hypertension, and stomach inflammation, ulcers, rash, and worsening of asthma symptoms. You also have to be careful if you are taking other medications because you can cause a drug interaction. Causing one medication interferes with the effects of another medication. Like acetylsalicylic acid (aspirin), another NSAID, and acetaminophen, ibuprofen works by inhibiting the activity of a class of enzymes called cyclooxygenases (COX). These enzymes are significant because they catalyze the synthesis of prostaglandins, molecules that have both positive and negative effects in the body. Prostaglandins are, for example, protective against the development of stomach ulcers, but they can also mediate inflammation (as well as the pain response). One of the most interesting things about human COX enzymes is that there is more than one of them—definitely two, and probably at least three. This is important to our understanding of the therapeutic effects of ibuprofen, aspirin, and acetaminophen. It had long been suspected that there was more than one COX enzyme, but it was not until 1991 that evidence for the existence of two forms, COX-1 and COX-2, materialized. It was then recognized that COX-1 is present at near constant levels in the body under all conditions (that is, it is a constitutive enzyme), whereas the levels of COX2 could increase in response to inflammatory conditions (i.e., it is an inducible enzyme). This led to the idea that the side effects of ibuprofen and aspirin (including stomach ulcers) probably arose from inhibition of the constitutive COX-1 enzyme, whereas the therapeutic benefits arose from inhibition of the inducible COX-2 enzyme. Ibuprofen and aspirin both inhibit COX-1 and COX-2, but they do it in different ways. Ibuprofen binds noncovalently to a COX enzyme and thus competes with the enzyme's natural substrate. (This is referred to as reversible inhibition.) On the other hand, aspirin forms a covalent bond to a serine residue in the enzyme, and this bond cannot be broken. (This is called irreversible inhibition.) Acetaminophen does not interact with either COX-1 or COX-2, but it is now understood that it may interact with a newly identified cyclooxygenase, COX-3. Selective targeting of the COX enzymes is an exciting area of pharmacology, in which the challenge continues to be the development of drugs that interact with specific COX enzymes. To sum it all up Ibuprofen has changed history in numerous ways. The one's that stand out most are: in certain studies it has shown better results than a placebo in the prevention of Alzheimer's disease when given in small amounts over a long stretch of time. It has also shown to lower the risk or

sometimes even prevent Parkinson's disease, while other drugs like Aspirin did not. A recent study has also shown that it works best compared to common painkillers for kids with broken bones, bruises, and sprains. Most commonly, it has allowed us to lessen or altogether eliminate any pains mentioned such as headaches, toothaches, arthritis, and temporarily remove fever.

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