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Ibuprofen and other non-steroidal anti-inflammatory drugs (NSAIDs)
Content provided by the Alzheimer Research Forum, written by Hakon Heimer

(Latest Update at end of page)

Some years ago, researchers noticed that people with severe arthritis have strikingly low rates of Alzheimer's disease. More recently, Japanese researchers noted a similar unusually low rate of Alzheimer's disease in people being treated for leprosy. Treatment of both leprosy and arthritis involves large doses of medications known as nonsteroidal anti-inflammatory drugs (NSAIDs). These drugs include such common, over-the-counter medications as ibuprofen (Motrin, Advil, Nuprin), naproxen (Aleve), and aspirin, plus many prescription drugs -- but not acetaminophen (Tylenol). Several studies have supported the speculation that NSAIDs might prevent Alzheimer's disease, or even help treat it. In 1993, researchers divided 44 people with mild to moderate Alzheimer's into two groups. One group took a placebo; the other, 100 or 150 mg/day of the NSAID indomethacin (Indocin). After six months, the placebo group showed an 8.4% decline in cognitive test scores. But the indomethacin group registered a 1.3% improvement.(1)

Researchers at the Johns Hopkins Alzheimer's Disease Research Center tested 210 people with the disease over time to see how rapidly they lost cognitive ability. Some showed rapid mental deterioration, while others declined more slowly. Then the researchers reviewed everyone's medical records to see who had been taking NSAIDs. They found that as NSAID use increased, the rate of mental deterioration decreased.(2) Finally, as part of the 38-year Baltimore Longitudinal Study of Aging, researchers from the National Institute on Aging assessed NSAID use in 1,828 elderly people, 110 of whom developed Alzheimer's from 1980 to 1995. Every two years, all subjects filled out extensive food and drug surveys, and were given a battery of cognition and memory tests. People who took NSAIDs more than occasionally for at least two years were 30% to 60% less likely to develop Alzheimer's disease. As duration of NSAID use increased, Alzheimer's risk decreased. All NSAIDs other than aspirin significantly reduced risk. Aspirin did not reach statistical significance, but there was a trend toward lower risk with increased duration of more-than-occasional aspirin use.(3) The main problem with NSAIDs is that they carry a significant risk of stomach distress, and gastrointestinal bleeding. According to these studies, many different NSAIDs have Alzheimer's-protective effects, including: Ibuprofen (Motrin, Advil, Nuprin), Naproxen (Naprosyn, Aleve, Anaprox), Indomethacin (Indocin). Meclofenamate (Meclomen), and Aspirin (possibly).

Anti-inflammatories such as Ibuprofen help protect against nerve cell death that results from the generation of free radicals in the brain. When nerve cells die in the brain, other cells called glial cells mount anti-inflammatory responses and shoot off free radicals. These are usually intended to kill invading agents like bacteria, but if the response is too strong the glial cells can kill the nerve cells with these free radicals. So this can be reduced with non-steroidal anti-inflammatory drugs like ibuprofen. Check with your doctor about the best dose because of the gastrointestinal side effects.

  1. Rogers, J., et al. "Clinical Trial of Indomethacin in Alzheimer's Disease," Neurology (1993) 43:1609
  2. Rich, J.B., et al. "Nonsteroidal Anti-Inflammatory Drugs in Alzheimer's Disease," Neurology (1995) 45:51
  3. Stephenson, J. "More Evidence Links NSAIDs, Estrogen with Reduced Alzheimer's Risk," Journal of the American Medical Association (May 8, 1996) 275:1389

Update: 8 November 2001

Anti-inflammatory Drugs Side-Step COX Cascade To Target Ab . If anti-inflammatory drugs are, in fact, helping some patients counteract the neurodegeneration of Alzheimer's disease, the benefit may not come from the most obvious effects of those drugs.

Eddie Koo and Sascha Weggen report in today's issue of Nature that a subset of nonsteroidal anti-inflammatory drugs (NSAIDs) lower toxic amyloid-b (Ab) levels independent of effects on inflammatory processes. A number of factors have pointed to inflammatory processes in Alzheimer's disease, including elevated levels of inflammatory molecules and the presence of astrocytes and microglia surrounding amyloid plaques. In addition, epidemiological studies have hinted that regular use of NSAIDs reduces the risk of AD. The assumption has been that it was the direct anti-inflammatory action of NSAIDs, principally against cyclooxygenase (COX) activity, that conferred this benefit. Koo and colleagues looked in another direction, at the effects of NSAIDs on the Ab42 peptide, which is widely considered the culprit in AD.

They found that the NSAIDs ibuprofen, indomethacin*, and sulindac sulphide (Advil; Genpril; Haltran; Medipren; Midol 200; Motrin; Nuprin; Indochron E-R, Indocin, PediaProfen; Actron9, Advil7, Aleve14, Anaprox14, Ansaid6, Bayer Select Ibuprofen, Cataflam1, Clinoril18, Cotylbutazone16, Cramp End7, Daypro15, Dolgesic7, Dolobid2, EC-Naprosyn14, Excedrin IB, Feldene17, Genpril7, Haltran7, Ibifon 600, Ibren7, Ibu7, Indocin, Lodine3, Lodine XL3, Meclomen10 , Medipren Caplets7, Midol IB7, Mobic12, Motrin, Nalfon4, Nalfon 2004, Naprelan14, Naprosyn14, Nuprin7, Nuprin Caplets7, Orudis9, Oruvail9, Pamprin-IB7, Ponstel11, Q-Profen7, Relafen13, Rufen7, Tolectin 20021, Tolectin, Trendar7, Voltaren1) decrease, by as much as 80%, the amount of Ab42 secreted from a variety of cultured cells. In contrast, other NSAIDs (e.g., sulindac sulphone, naproxen) did not reduce Ab42 levels. Because naproxen is a COX inhibitor, the results suggested that COX inhibition is not essential to the reduction of Ab42. Evidence supporting this hypothesis came from an experiment in which sulindac sulphide successfully reduced Ab42 in cells deficient in COX enzymes.

Extending their work to the Tg2576 mouse model of AD, which produces mutant human b-amyloid precursor protein, the researchers found that ibuprofen, but not naproxen, significantly reduced levels of Ab42 (but not of the less toxic Ab40). A second focus of this study was to examine how NSAIDs affect the mechanism whereby the AbPP protein is cleaved to produce either the Ab42 peptide or other, less toxic, forms. Recent efforts to inhibit Ab42 production by targeting the g-secretase enzyme have run into the problem that g -secretase inhibition also interferes with normal physiological processes, in particular proteolysis of the notch receptor. Koo et al. discovered that sulindac sulphide did not interfere with notch processing.

They also found that NSAID treatment apparently lowered Ab42 production by raising the levels of the shorter peptide Ab38. For their part, the researchers anticipate the development of "'anti-amyloid' drugs that selectively target production of the highly amyloidogenic Ab42 species without inhibiting either COX activity or the vital physiological functions of g-secretase." -Hakon Heimer.

  1. Weggen S, et al. "A subset of NSAIDs lower amyloidogenic A-b-42 independently of cyclooxygenase activity." Nature. 2001 Nov 8;414:212-6.
  2. De Strooper B, Konig G. "An inflammatory drug prospect." Nature. 2001 Nov 8;414:212-6.

* Indomethacin has been found to protect mild-to-moderately impaired AD patients from some of the decline they would otherwise show.

Rogers, J et al Neurology, 43: 1609-1611, 1993.

Updates:

September, 2002 Journal: Neurology
John Breitner's huge group of researchers found substantial reductions in AD rates among people who used aspirin or other anti-inflammatory drugs for at least 2 years; long term use that preceded AD by at least several years was best.

June, 2006 Journal: New England Journal of Medicine (t' Veld BA, Ruitenberg A, Hofman A, et al) "The relative risk of Alzheimer's disease was 0.95 (95 percent confidence interval) in subjects with short-term use of NSAIDs, 0.83 (95 percent confidence interval) in those with intermediate-term use, and 0.20 (95 percent confidence interval) in those with long-term use.....The long-term use of NSAIDs may protect against Alzheimer's disease but not against vascular dementia."

May, 2008: A longer study of nearly 50,000 US vets who acquired AD diagnoses and nearly 200,000 who never became demented (over 5 years) confirmed substantial reductions in the risk of AD with Ibuprofin and other NSAIDs.


   
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