Ibuprofen is a drug in the class of nonsteroidal anti-inflammatory drugs (NSAIDs) used to treat pain, fever, and inflammation. These include painful menstrual periods, migraines, and rheumatoid arthritis. It may also be used to close patent ductus arteriosus in premature infants. Can be used by mouth or intravenously. Usually start working in one hour.
Common side effects include heartburn and rash. Compared with other NSAIDs, there may be fewer side effects such as gastrointestinal bleeding. This increases the risk of heart failure, kidney failure, and liver failure. At low doses, it does not seem to increase the risk of heart attack; However, at higher doses may be. Ibuprofen can also aggravate asthma. Although it is unclear whether it is safe in early pregnancy, it appears to be dangerous in later pregnancies and is therefore not recommended. Like other NSAIDs, it works by inhibiting prostaglandin production by reducing the activity of cyclooxygenase enzymes. Ibuprofen may be more anti-inflammatory than any other NSAID.
Ibuprofen was discovered in 1961 by Stewart Adams and originally marketed as Brufen . These are available under a number of trade names, including Advil and Motrin . It was first marketed in 1969 in the United Kingdom and in the United States in 1974. It is a List of Essential Medicines of the World Health Organization, the most effective and safe medicines needed in the health system. It is available as a generic drug. Wholesale costs in developing countries are between 0.01 and 0.04 USD per dose. In the United States it costs around 0.05 USD per dose.
Video Ibuprofen
Medical use
Ibuprofen is used primarily to treat fever (including postimmunisation fever), mild to moderate pain (including pain relief after surgery), painful menstruation, osteoarthritis, dental pain, headache, and pain due to kidney stones. About 60% of people respond to every NSAID; those who do not respond well to a particular person can respond to others.
It is used for inflammatory diseases such as juvenile idiopathic arthritis and rheumatoid arthritis. It is also used for pericarditis and patent ductus arteriosus.
Ibuprofen lysine
In some countries, ibuprofen lysine (ibuprofen lysine salt, sometimes called "ibuprofen lysine") is licensed for the treatment of the same conditions as ibuprofen; lysine salt is used because it is more soluble in water. In 2006, ibuprofen lysine was approved in the US by the Food and Drug Administration (FDA) for the closure of patent ductus arteriosus in preterm infants weighing between 500 and 1,500 grams (1 and 3 Â £), which is no more of 32 weeks of gestational age when regular medical management (such as fluid restriction, diuretics, and respiratory support) is ineffective.
Maps Ibuprofen
Adverse effects
Side effects include nausea, dyspepsia, diarrhea, constipation, gastrointestinal ulceration/bleeding, headache, dizziness, rash, salt and fluid retention, and high blood pressure.
Rare side effects include esophageal ulceration, heart failure, high blood potassium levels, renal impairment, confusion, and bronchospasm. Ibuprofen may aggravate asthma, sometimes fatal.
Ibuprofen can be quantified in blood, plasma, or serum to indicate the presence of drugs in a person experiencing anaphylactic reactions, confirming the diagnosis of toxicity in hospitalized patients, or assisting in the investigation of medicolegal death. A monograph relating to ibuprofen plasma concentration, time since consumption, and risk of developing renal toxicity in overdose patients has been published.
Cardiovascular Risk
Together with some other NSAIDs, the use of chronic ibuprofen has been found to correlate with the risk of hypertension and myocardial infarction (heart attack), especially among those treated chronically using high doses. On July 9, 2015, the US FDA tightened warnings of increased heart attacks and stroke risk associated with ibuprofen and related NSAIDs; aspirin NSAIDs are not included in this warning.
Skin
Together with other NSAIDs, ibuprofen has been associated with the onset of bullous pemphigoid or peliduran such as pemphigoid. Like other NSAIDs, ibuprofen has been reported as a photosensitizing agent, but is considered a weak photosensitizing agent compared to other members of the 2-arylpropionic acid class. Like other NSAIDs, ibuprofen is a very rare cause of autoimmune disease Stevens-Johnson syndrome (SJS). Ibuprofen is also a very rare cause of toxic epidermal necrolysis.
Interactions
Drinking alcohol while taking ibuprofen may increase the risk of stomach bleeding.
According to the US Food and Drug Administration (FDA), "ibuprofen may interfere with the low-dose aspirin antiplatelet effect, potentially making aspirin less effective when used for cardiovascular protection and stroke prevention." Allowing sufficient time between the doses of ibuprofen and fast-release aspirin (IR) can avoid this problem. The recommended length of time between the dose of ibuprofen and the dose of aspirin depends on the first taken. This will be 30 minutes or more for ibuprofen taken after IR aspirin, and eight hours or more for ibuprofen taken before aspirin IR. However, this time can not be recommended for plated enteric aspirin. But, if ibuprofen is only taken occasionally without the recommended time, the reduction of cardiovascular protection and the prevention of a daily daily aspirin regimen stroke is minimal.
Overdose
Overdose Ibuprofen has become common because it is licensed for OTC use. Many overdose experiences are reported in the medical literature, although the frequency of life-threatening complications of low ibuprofen overdose. Human response in overdose cases ranges from absence of symptoms to fatal outcomes despite intensive care treatment. Most symptoms are the advantages of the pharmacological action of ibuprofen, and include abdominal pain, nausea, vomiting, drowsiness, dizziness, headache, ringing ears, and nystagmus. Rarely, more severe symptoms, such as gastrointestinal bleeding, seizures, metabolic acidosis, high blood potassium levels, low blood pressure, slow heart rate, rapid heartbeat, atrial fibrillation, coma, liver dysfunction, acute renal failure, cyanosis, respiratory depression, and cardiac arrest has been reported. The severity of the symptoms varies with the ingested dose and the elapsed time; However, individual sensitivity also plays an important role. Generally, the symptoms observed with ibuprofen overdose are similar to those caused by other NSAID overdoses.
The correlation between symptom severity and ibuprofen plasma levels was measured weakly. Toxic effects are not possible at doses below 100 mg/kg, but may weigh over 400 mg/kg (about 150 tablets from 200 mg units for the average male); however, large doses do not indicate that clinical course is likely to be lethal. The exact deadly dose is difficult to determine, as it may vary with age, weight, and individual concomitant conditions.
Therapy is mostly symptomatic. In earlier cases, stomach decontamination is recommended. This is achieved by using activated charcoal; charcoal absorbs the drug before it can enter the bloodstream. Gastric rinse is now rarely used, but it can be considered if the digested amount is potentially life-threatening, and it can be done within 60 minutes of consumption. Vomiting is not recommended. The majority of ibuprofen consumption only produces mild effects and the management of overdose is very easy. Standard measures to maintain normal urine output should be institutionalized and renal function monitored. Because ibuprofen has acid properties and is also excreted in urine, theoretically enforced alkaline diuresis is advantageous. However, because ibuprofen is heavily bound to proteins in the blood, renal excretion of the unchanged drug is minimal. The forced alkaline diuresis, therefore, is of limited benefit. Symptomatic therapy for hypotension, gastrointestinal bleeding, acidosis, and renal toxicity may be indicated. Sometimes, close monitoring of the intensive care unit for several days is required. A patient who survives acute intoxication usually does not experience late consequences.
Miscarriage
A study of pregnant women showed that those taking all kinds or amounts of NSAIDs (including ibuprofen, diclofenac and naproxen) were 2.4 times more likely to have miscarriages than those who did not take the drug. However, a study in Israel found no increased risk of miscarriage in the group of women using NSAIDs.
Pharmacology
NSAIDs such as ibuprofen work by inhibiting the enzyme cyclooxygenase (COX), which converts arachidonic acid into prostaglandin H 2 (PGH 2 ). PGH 2 , in turn, is converted by another enzyme into some other prostaglandin (which is a mediator of pain, inflammation, and fever) and thromboxane A 2 (which stimulates platelet aggregation, which leads to the formation of blood clots).
Like aspirin and indomethacin, ibuprofen is a non-selective COX inhibitor, in this case inhibiting two cyclooxygenase, COX-1 and COX-2 isoforms. The analgesic, antipyretic, and anti-inflammatory activity of NSAIDs appears to operate primarily through COX-2 inhibition, which decreases the synthesis of prostaglandins involved in mediating inflammation, pain, fever, and swelling. The antipyretic effect may be due to action on the hypothalamus, resulting in increased peripheral blood flow, vasodilation, and subsequent heat dissipation. COX-1 inhibition will in fact be responsible for the adverse effects on the gastrointestinal tract. However, the respective role of COX isoform in the analgesic, anti-inflammatory, and stomach effects of NSAIDs is uncertain and different compounds cause different levels of analgesia and stomach damage.
Ibuprofen is given as a racemic mixture. The R-enantiomer undergoes extensive interconversion to S-enantiomer in vivo . S-enantiomer is believed to be a more pharmacologically active enantiomer. The R-enantiomer is altered through a series of three major enzymes. These enzymes include acyl-CoA-synthetase, which converts R-enantiomer into (-) - R-ibuprofen I-CoA; Epimerase 2-arylpropionyl-CoA, which converts (-) - R-ibuprofen I-CoA into () - S-Ibuprofen I-CoA; and hydrolytes, which convert () - S-ibuprofen I-CoA to S-enantiomer. In addition to the conversion of ibuprofen to S-enantiomer, the body can metabolize ibuprofen into several other compounds, including many hydroxyl, carboxyl and glucoronyl metabolites. Almost all of these have no pharmacological effects.
Chemistry
Ibuprofen is practically insoluble in water, but highly soluble in most organic solvents such as ethanol (66.18 g/100 mL at 40 ° C for 90% EtOH), methanol, acetone and dichloromethane.
The original synthesis of ibuprofen by Boots Group begins with a 2-methylpropylbenzene compound. Synthesis takes six steps. A greener modern technique for synthesis involves only three steps.
Stereochemistry
This is the optical active compound with both the S and R -isomer, where the isomer S (dextrorotatory) is more biologically active; This isomer has also been isolated and used medically (see dexibuprofen for details).
Ibuprofen is produced industrially as a racemate. Compounds, such as other 2-arylpropionate derivatives (including ketoprofen, flurbiprofen, naproxen, etc.), Contain stereocenters within -position of the propionate portion. Thus two enantiomers of ibuprofen occur, with potentially different biological and metabolic effects for each enantiomer.
An isomerase (alpha-methylacyl-CoA racemase) converts ( R ) - ibuprofen to active ( S ) - enantiomer.
History
Ibuprofen derived from propionic acid by the Boots Group research group during the 1960s. The discovery was the result of research during the 1950s and 1960s to find a safer alternative to aspirin. Discovered by a team led by Stewart Adams and a patent application filed in 1961. Adams initially tested the drug as a treatment for his intoxication. The drug was launched as a treatment for rheumatoid arthritis in England in 1969, and in the United States in 1974. Later, in 1983 and 1984, it became the first NSAID (in addition to aspirin) available on the table (OTC). ) in these two countries. Dr. Adams was later awarded the OBE in 1987. Boots was awarded the Queen's Prize for Technical Achievement for drug development in 1987.
Society and culture
Marketing
Ibuprofen was made available under a recipe in England in 1969, and in the United States in 1974. In the years since then, a good tolerability profile, along with extensive experience in the population, as well as in so-called IV- Postapproval studies), have produced the availability of ibuprofen OTC at pharmacies worldwide, as well as in supermarkets and other general retailers. Ibuprofen is the name approved by INN, BAN, AAN and USAN. Advil is produced by Pfizer and has been on the market since 1984.
North America
Ibuprofen is commonly available in the United States up to the FDA limit of 1984 OTC, rarely used higher by prescription. In 2009, the first ibuprofen injection formulation was approved in the United States, under the trade name Caldolor.
Research
Ibuprofen is sometimes used for the treatment of acne because of its anti-inflammatory properties, and has been sold in Japan in topical form for adult acne. Like other NSAIDs, ibuprofen may be useful in the treatment of severe orthostatic hypotension (low blood pressure when standing). In some studies, ibuprofen showed superior results compared with placebo in the prevention of Alzheimer's disease, when administered in low doses for a long time.
Ibuprofen has been associated with lower risk of Parkinson's disease, and may delay or prevent it. Aspirin, other NSAIDs, and paracetamol (acetaminophen) have no effect on risk for Parkinson's. In March 2011, researchers at Harvard Medical School announced in Neurology that ibuprofen had a neuroprotective effect on the risk of developing Parkinson's disease. People who regularly consume ibuprofen are reported to have 38% lower risk of Parkinson's disease, but no such effects are found for other pain relievers, such as aspirin and paracetamol. The use of ibuprofen to reduce the risk of Parkinson's disease in the general population will not be problem-free, given the possible adverse effects on the urinary and digestive system.
Some dietary supplements may be harmful to take along with ibuprofen and other NSAIDs, but by 2016 more research needs to be done to be sure. These supplements include those that can prevent platelet aggregation, including ginkgo, garlic, ginger, bilberry, dong quai, feverfew, ginseng, turmeric, meadowsweet and willow; those containing coumarin, including chamomile, horse chestnut, fenugreek and red clover; and those that increase the risk of bleeding, such as Javanic acid.
References
External links
- US. National Library of Medicine: MedlinePlus Drug Information: Ibuprofen
- The University of Bristol chemistry page on Ibuprofen
- US. National Drug Library: Drug Information Portal - Ibuprofen
Source of the article : Wikipedia
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