Molecular structure of ibuprofen3D model of (R)-ibuprofen
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Ibuprofen

Ibuprofen is a nonsteroidal anti-inflammatory drug (NSAID) widely marketed under various trademarks including Act-3, Advil, Brufen, Motrin, Nuprin, and Nurofen; a standing joke about some athletes' regular use has produced "Vitamin I" as a slang term for it. It is used for relief of symptoms of arthritis, primary dysmenorrhoea, and fever; and as an analgesic, especially where there is an inflammatory component. Ibuprofen was developed by the research arm of Boots Group. more...

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Clinical use

Low doses of ibuprofen (200 mg, and sometimes 400 mg) are available over the counter (OTC) in most countries. Ibuprofen has a dose-dependent duration of action of approximately 4–8 hours, which is longer than suggested by its short half-life. The recommended dose varies with body mass and indication. Generally, the oral dose is 200–400 mg (5–10 mg/kg in children) every 4–6 hours, up to a usual maximum daily dose of 800–1200 mg. Under medical direction, a maximum daily dose of 3200 mg may sometimes be used.

Indications

Approved clinical indications for ibuprofen include:

  • Rheumatoid arthritis (DMARDs should also be considered)
  • Osteoarthritis, ibuprofen can reduce pain and, if present, joint inflammation
  • Juvenile rheumatoid arthritis, alone or with corticosteroids
  • Morbus Bechterew (spondylitis ankylosans) together with corticosteroids
  • Rheumatic fever, together with antibiotic therapy
  • Acute gout attack, ibuprofen is not useful for chronic treatment
  • Primary dysmenorrhoea (ibuprofen proved superior to placebo and propoxyphen, and at least as effective as aspirin)
  • Fever
  • Pericarditis, chiefly after myocardial infarction, to reduce pain, fever and inflammation
  • Minor aches and pains such as toothache, backache, fever and pain associated with common flu, symptomatic relief of influenza, shingles, and postoperative pain
  • Sporting injuries and pain after mild to moderate trauma
  • Headache including mild to moderate migraine attack

Off-Label and investigational use

  • As with other NSAIDs, ibuprofen may be useful in the treatment of severe orthostatic hypotension (PMID 7041104)
  • In some studies, ibuprofen showed superior results compared to placebo in the prophylaxis of Alzheimer's disease, when given in low doses over a long time (PMID 16195368). Further studies are needed to confirm the results, before ibuprofen can be recommended for this indication.
  • Ibuprofen has been associated with a lower risk of Parkinson's disease, and may delay or prevent Parkinson's disease. Aspirin, other NSAIDs, and acetaminophen had no effect on the risk for Parkinson's (PMID 16240369). Further research is warranted before recommending ibuprofen for this use.

Ibuprofen lysine

In Europe and Australia, ibuprofen lysine (ibuprofenlysinat, the lysine salt of ibuprofen) is licensed for treatment of the same conditions as ibuprofen. Ibuprofen lysine is said to have a more rapid onset of action compared to base ibuprofen.

Mechanism of action

Ibuprofen is an NSAID which is believed to work through inhibition of cyclooxygenase (COX); thus inhibiting prostaglandin synthesis. As with other NSAIDs, ibuprofen inhibits platelet aggregation, but is not used therapeutically for this action since it is a minor and reversible effect.

Read more at Wikipedia.org


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Soothing athletic aches: can't decide between aspirin and ibuprofen? Here's the latest on over-the-counter pain meds
From Muscle & Fitness/Hers, 8/1/04 by Dana Sullivan

there's a reason why the athletes who are in Athens this summer are there: They're talented, they're tough, and when it comes to handling pain, they're probably a bit hardier than the rest of us. "I'm amazed by how averse many athletes are to taking pain relievers, even when they really need it," says Alexandra Chrysanthis, MD, team physician for the women's United States Water Polo Team. "Elite athletes seem to get used to dealing with musculoskeletal pain, because they work their bodies so hard day in and day out." For them, pain is just part of the job description.

For the rest of us, though, the sore muscles that result from adding one small hill to a favorite running route or putting a few more pounds on the squat bar have us reaching into the medicine cabinet. And we're usually going after one of the five most common over-the-counter pain relievers: aspirin; acetaminophen; and the nonsteroidal anti-inflammatory drugs (NSAIDs) ibuprofen, naproxen and ketoprofen. But is relying on painkillers, even familiar and widely accepted ones, a good idea? And if you do take a pill, which should you choose?

Pain relievers generally are considered safe, except when people take too much of them--and many people do. "This is America. If the label says one or two, we take three or four," says William O. Roberts, MD, president of the American College of Sports Medicine. These drugs can have serious side effects if taken in larger-than-recommended dosages: acetaminophen can be toxic to the liver, ibuprofen and naproxen can harm the kidneys, aspirin can cause stomach bleeding.

If you take nonprescription painkillers exactly as directed, there's a lot to recommend them beyond the relief of aches and pains. As you've probably heard, aspirin is used to prevent heart attacks, and some research suggests that ibuprofen may help protect against Alzheimer's disease (also see "Pain Relief Update," page 90).

But there's been some disturbing news about these OTC meds as well. One of the most interesting studies, conducted at the University of Arkansas for Medical Sciences in Little Rock, suggests that routinely popping ibuprofen or acetaminophen postexercise may diminish your hard work in the gym--particularly if you're strength training.

"We discovered that both ibuprofen and acetaminophen inhibit the way muscles respond to exercise," says Todd A. Trappe, PhD, an associate professor of geriatrics and physiology at the University of Arkansas and the study's lead researcher. Usually, muscle tissue is broken down after a vigorous workout, only to rebuild itself and come back stronger. But it turns out that along with blocking pain, both ibuprofen and acetaminophen block muscle building, at least when taken after exercise. "If you take either pain reliever regularly, then over the long haul you might not get the benefits you're looking for," says Trappe.

While it's not entirely clear at this time whether certain painkillers' pros outweigh their cons, it is known that individuals respond differently to different drugs. What works for your best friend might not work that well for you, and you may experience side effects that she doesn't.

"You have to experiment with them," says Bill Gurley, PhD, a pharmaceutical scientist at the University of Arkansas' College of Pharmacy. The one thing that all pain relievers do have in common is that they work best if you take them with plenty of water. "Water dissolves the medication so it works faster, and water also helps prevent stomach upset," he adds.

To weigh your options, check out the chart at right for a look at what each nonprescription pain reliever is recommended for, and what its risks are. (If you have any diseases or conditions that require a physician's care, check with her before taking any medication.)

RELATED ARTICLE: PAIN RELIEF UPDATE: Three preliminary studies of interest

IBUPROFEN MAY HELP PREVENT BREAST CANCER.

In the last couple of years, several studies have suggested that regular use of aspirin and nonsteroidal anti-inflammatory drugs (NSAIDs) lowers a person's risk of developing colon, lung and prostate cancers. Now we can add breast cancer to that list. According to researchers involved with the National Cancer Institute's Women's Health Initiative, women who take at least two NSAIDs a week were 21 percent less likely to develop breast cancer than women who didn't. And women who took NSAIDs regularly for more than 10 years reduced their risk by more than 28 percent. The study was published in the 2003 issue of Proceedings, which is put out by the American Association for Cancer Research.

SOME PAIN RELIEVERS ARE LINKED TO HYPERTENSION IN WOMEN.

According to a study published in the November 2002 issue of Hypertension, women who take aspirin or acetaminophen at least one day per month or NSAIDs five or more days per month are at a greater risk for developing hypertension. Another study, published in the October 2002 issue of the Archives of Internal Medicine, also found that acetaminophen and NSAIDs--but not aspirin--were linked to hypertension.

ASPIRIN LOSES ITS ANTI-CLOTTING EFFECTS OVER TIME.

People who take aspirin as part of a cardiotherapy regimen may have to use a different type of drug to keep their blood from clotting. Researchers in Rome discovered that the benefits of using aspirin decline after two years, according to a study published in the Journal of the American College of Cardiology (March 2004).

RELATED ARTICLE: Take as Directed

"Nonprescription" and "over-the-counter" are not synonymous with harmless. Here are five tips to keep in mind when taking pain relievers:

1. Take only the dose that is recommended on the label--unless your doctor has OK'd a higher dose.

2. Abstain from alcohol. Mixing alcohol with acetaminophen can damage your liver; mixing it with aspirin or any NSAID--ibuprofen, naproxen and ketoprofen--can cause stomach bleeding.

3. Take NSAIDs with food and/or milk. This will help minimize stomach upset.

4. Check the labels of other medications you take. One reason for acetaminophen overdoses is that people take a cold/flu preparation that contains it along with plain acetaminophen, unaware that they are doubling or tripling the dose.

5. Know your personal risks. For example, NSAIDs are not recommended for people who have kidney disorders, ulcers or are allergic to aspirin.

6. Never take any medication for pain for more than 10 days without checking with your doctor. (And if you're taking it for fever, check with your doctor after three days.) Finally, don't forget that pain might mask an injury. "Pain is your body's way of telling you that something is wrong," says William O. Roberts, MD, president of the ACSM. "Listen to that."

Photography by Alicia Patel

COPYRIGHT 2004 Weider Publications
COPYRIGHT 2004 Gale Group

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