Nutrition expert Joseph Mercola, MD, explains the neurodegenerative potential of anticholinergic drugs, popular for sleep and night-time pain relief, and suggests some time-tested natural alternatives. First published Aug 3, 2010 & Jan 6, 2009, this information is reproduced with kind permission from Dr. Mercola’s educational website (http://www.Mercola.com). See footnote* for links to more.
Studies Prove That These Drugs May Negatively Affect Your Brain
Drugs commonly taken for a variety of common medical conditions negatively affect your brain, causing long term cognitive impairment. These drugs, called anticholinergics, block acetylcholine, a nervous system neurotransmitter. They include such common over-the-counter brands as Benadryl, Dramamine, Excedrin PM, Nytol, Sominex, Tylenol PM, and Unisom. Other anticholinergic drugs, such as Paxil, Detrol, Demerol and Elavil, are available only by prescription.
"Researchers… conducted a six-year observational study, evaluating 1,652 Indianapolis area African-Americans over the age of 70 who had normal cognitive function when the study began… ‘Taking one anticholinergic significantly increased an individual’s risk of developing mild cognitive impairment and taking two of these drugs doubled this risk.’"
Many view over-the-counter (OTC) drugs as safe because they don’t require a prescription. Well, nothing could be further from the truth.
In fact, many OTC drugs were previously carefully monitored prescription drugs. Many people are not aware that while I was in college in the 1970s, I worked as a full time pharmacy apprentice and helped sell drugs to patients all day long.
Motrin was the first non-salicylate prescription NSAID. Now it is a popular OTC ibuprofen option. Similarly, anti-ulcer drugs like Tagamet, Zantec, and Prilosec used to be carefully controlled. Now they can all be easily purchased in a smaller "OTC strength" that nearly doubles the number of pills required to equal the prescription dose.
Just because a drug is available without a prescription does not make it any less dangerous. It is still a chemical, which in no way, shape, or form treats the cause of the problem and can lead to complications that can seriously injure, if not kill, you or someone you love.
So this is clearly important information that can help you or someone you love reduce your risk of dementia as you get older. Based on the findings of this study, I would strongly recommend that seniors in particular avoid all anticholinergic drugs, like Benadryl (generic is diphenhydramine) which is pervasive and commonly used in virtually all of the OTC sleeping pills.
Researchers will continue studying the matter to see whether anticholinergic-induced cognitive impairment can be reversed, but don’t hold your breath. Avoidance is really the best solution.
What are Anticholinergic Drugs?
Anticholinergic drugs block a nervous system neurotransmitter called acetylcholine. Those suffering from Alzheimer’s disease typically have a marked shortage of acetylcholine.
Anticholinergic drugs are available both over-the-counter and by prescription, as medications used for a variety of symptoms can have this effect. Examples include night-time pain relievers, antihistamines, and other sleep aids, such as: Excedrin PM, Tylenol PM, Nytol, Sominex, Unisom, Benadryl, and Dramamine.
Prescription drugs with anticholinergic effects include certain antidepressants, medications to control incontinence, and certain narcotic pain relievers. Examples of prescription meds in these categories include: Paxil, Detrol, Demerol, and Elavil.
A Special Note for Aspartame ‘Reactors’
Many of the drugs listed here, as well as a long list of additional ones, contain diphenhydramine. As an important side note, you need to beware that chewable tablets and rapidly disintegrating tablets that contain diphenhydramine may be sweetened with aspartame.
If you have the genetic disease phenylketonuria (PKU), you must be particularly careful to avoid these types of drugs and all other types of aspartame-sweetened foods and beverages in order to prevent mental retardation.
But many other people also suffer detrimental health effects from aspartame, so you should know that this is yet another potential source of this toxic sweetener.
Anticholinergic Drugs Increase Dementia in the Elderly
I’ve previously written about the health dangers of many of these individual drugs. Paxil, for example, is an addictive antidepressant that is well known to increase the risk of suicide in children and teens. It is also known to increase violent behavior.
Benadryl and Sominex have previously been found to cause hallucinations in the elderly, and a number of the drugs on the list also promote dental decay.
The results of the [Indianapolis] study indicate that drugs with anticholinergic effects may be yet another piece of the puzzle that might explain the sharp rise in dementia and cognitive decline.
According to the University of Michigan, dementia strikes about 50% of people who reach the age of 85. Of those, about 60% go on to develop Alzheimer’s disease.
In the Indianapolis study, the researchers tracked the intake of anticholinergic drugs and monitored the cognitive abilities of 1,652 African-American seniors, aged 70 and older, for six years. All of the participants had normal cognitive function at the outset of the study.
Fifty-three percent of the participants used a ‘possible anticholinergic,’ and 11% used a ‘definitive anticholinergic’ drug.
• They found that those who took drugs classified as ‘definite anticholinergics’ had a four times higher incidence of cognitive impairment.
• In those who were not carriers of the specific gene, APOE e4 allele, the risk was over seven times higher. (The APOE e4 gene is known to influence many neurological diseases, and is considered a high risk factor for Alzheimer’s.)
• Taking two of these drugs further increased the risk of cognitive impairment.
"Simply put, we have confirmed that anticholinergics, something as seemingly benign as a medication for inability to get a good night’s sleep or for motion sickness, can cause or worsen cognitive impairment, specifically long-term mild cognitive impairment which involves gradual memory loss.
"As a geriatrician I tell my Wishard Healthy Aging Brain Center patients not to take these drugs and I encourage all older adults to talk with their physicians about each and every one of the medications they take," said Malaz Boustani, M.D., IU School of Medicine associate professor of medicine, Regenstrief Institute investigator and IU Center for Aging Research center scientist."
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Even More Reasons to Ditch the Sleep Meds
In 2008, Americans filled more than 56 million prescriptions for sleeping pills and spent more than $600 million on over-the-counter sleep aids. But anticholinergic sleep medications in particular may be causing far more harm than good, especially long term, without providing any benefit at all.
In a recent article, CBC News reported that the U.S. Food and Drug Administration has had data for 15 years which shows that over-the-counter sleep aids like Tylenol PM and Excedrin PM do not offer any significant benefit to patients. (See “Over-the-counter sleep meds not effective: FDA.”)
There’s no explanation for why the FDA took 15 years to evaluate the industry’s research, but upon final analysis CBC News reported:
"The data suggests the combination products are statistically better than a placebo but not by much."
…Another analysis of sleeping pill studies from 2007 (financed by the National Institutes of Health) found that sleeping pills like Ambien, Lunesta, and Sonata reduced the average time to go to sleep by just under 13 minutes compared with fake pills – hardly a major improvement. (See “Sleep Drugs are Wildly Popular Despite Barely Working.”)
Yet, the participants believed they had slept longer, by up to one hour, when taking the pills. This may actually be a sign of a condition called anterograde amnesia, which causes trouble with forming memories. When people wake up after taking sleeping pills, they may, in fact, simply forget that they had been unable to sleep!
You would be far better off putting your money toward authentic solutions to help you sleep than on sleeping pills, as it’s now clear that they do next to nothing to help you sleep – in fact, they may actually make it more difficult for you to get a good night’s rest naturally – and may significantly increase your risk of dementia.
Sleeping Pills are NOT a Safe Solution for Sleepless Nights
Please understand that resorting to sleep medications is risky business, and that these pills do not address the underlying reasons why you’re having trouble sleeping in the first place.
In addition to the long-term problems already discussed, there are other serious, not to mention bizarre, risks involved.
• For starters, these pills are notorious for being addictive, which means that once you want to stop taking them, you’ll likely suffer withdrawal symptoms that could be worse than your initial insomnia.
• Some, such as Ambien, may also become less effective when taken for longer than two weeks, which means you may find yourself needing ever higher dosages.
• Ambien may also make you want to – and I don’t mean sneaking down to grab a piece of fruit. The sleep eating can include bizarre foods such as buttered cigarettes, salt sandwiches, and raw bacon.
• Sleeping pills, and again Ambien in particular, are also known to increase your risk of getting into a traffic accident. Ambien actually ranks among the top 10 drugs found in the bloodstreams of impaired drivers, according to some state toxicology labs.
• Among the elderly, using sleeping pills may increase the risk of nighttime falls and injuries, and anyone who takes them may find they wake up feeling drowsy if the effects of the drug have not worn off yet.
You’re far better off finding safe and natural solutions that will actually address the underlying causes of your sleepless nights instead of just cover up the resulting symptoms.
How to Get a Good Night’s Sleep Without Dangerous Drugs
If you are having trouble sleeping, please do not ignore the problem or simply wait for it to go away. Quality sleep just as important as your need for food, water, and pure air – and there are very simple methods to help you get yours.
Please read my comprehensive sleep guide with 33 Secrets to a Good Night’s Sleep for my full set of recommendations, but to start:
• Make certain you are exercising regularly. [Obviously a strategy to be undertaken only very judiciously for ME/CFS patients prone to post-exertion malaise.] A Stanford University Medical School study found that after 16 weeks in a moderate-intensity exercise program, subjects were able to fall asleep about 15 minutes earlier and sleep about 45 minutes longer at night. However, don’t exercise too close to bedtime or it may keep you awake.
• Stress is another major reason why people have trouble sleeping, which is why I suggest you start to wind down from your day at least an hour before your bedtime (but preferably two or more). Calming activities such as journaling, meditating, sipping herbal tea, washing your face, using the Emotional Freedom Techniques (EFT) or reading a book may soothe your mind and help you unwind. Be sure your phone, email, and television are all off during this time.
• Make sure your sleeping environment is comfortable and conducive to sleep. This includes keeping the temperature cool, adding in some white noise if you need it and making sure your room is pitch-black. If there is even the tiniest bit of light in the room it can disrupt your circadian rhythm and your pineal gland’s production of melatonin and serotonin. For this reason, I highly recommend adding room-darkening drapes to your bedroom, or if this is not possible wearing an eye mask to block out any stray light.
Again, by following my 33 Secrets to a Good Night’s Sleep, the majority of people will be able to fall asleep and stay asleep. However, for times when sleep is especially difficult, these eight natural remedies may also help and are far safer than sleeping pills of any kind.
Eight Natural Remedies That May Help You Sleep
Before you rush to the drugstore to buy an over-the-counter sleep medication, try one of the following natural sleep remedies. They are safer and have fewer side effects. Many of these can not only help you fall asleep and stay asleep, but they can also promote muscle relaxation. (And they are far safer than sleeping pills of any kind.)
Magnesium and calcium – Magnesium and calcium are both sleep boosters, and when taken together they become even more effective. Plus, by taking magnesium you cancel out any potential heart problems that might arise from taking calcium alone. … [Take at night. You can lower the dose of magnesium if it causes diarrhea.]
Wild lettuce – If you’ve suffered anxiety, headaches, or muscle or joint pain, you might already be familiar with wild lettuce. It’s also effective at calming restlessness and reducing anxiety, and may even quell restless legs syndrome. [Take before bed.]
Hops – Beer fans are already familiar with the calming effect of hops, the female flowers used in beer making. For sleep purposes, this extract has been widely used as a mild sedative for anxiety and insomnia. [Take before climbing under the covers.]
Aromatherapy – Lavender is the trick here, as studies have proven that it aids in sleep. It’s also an inexpensive, nontoxic way to slip into a peaceful slumber. Find a spray with real lavender and spritz it on your pillow before bedtime, or buy a lavender-filled pillow.
Melatonin – Melatonin is the hormone that controls sleep, so it’s no wonder that it naturally induces sleep. Studies show that lower doses are more effective – plus, there’s concern that too-high doses could cause toxicity as well as raise the risk of depression or infertility. [Take at bedtime.]
Yoga and meditation – Choose gentle yoga or stretching, not vigorous power or ashtanga yoga, which could energize you instead. Try easy yoga stretches in bed followed by simple meditation. Close your eyes and, for 5 to 10 minutes, pay attention to nothing but your breathing.
L-theanine – This amino acid comes from green tea, and not only helps maintain a calm alertness during the day but also a deeper sleep at night. However, green tea doesn’t contain enough L-theanine to significantly boost your REM cycles, and might make you wake up to go to the bathroom. Instead, buy pure, active L-theanine (some brands have inactive forms of theanine – e.g., d-theanine – that block the effectiveness), and take…at bedtime.
Valerian – Valerian is one of the most common sleep remedies for insomnia. Numerous studies have found that valerian improves deep sleep, speed of falling asleep, and overall quality of sleep. However, it’s most effective when used over a longer period of time. Keep in mind that about 10% of the people who use it actually feel energized, which may keep them awake. If that happens to you, take valerian during the day. Otherwise… take before bed.
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Note: This information (© 1997-2012 Dr. Joseph Mercola. All Rights Reserved) has not been reviewed by the FDA. It is general information, based on the research and opinions of Dr. Mercola unless otherwise noted, and is not meant to prevent, diagnose, treat or cure any condition, illness, or disease. It is not intended to replace a one-on-one relationship with a qualified healthcare professional and is not intended as medical advice. It is always very important that you make no change in your healthcare plan or health support regimen without researching and discussing it in collaboration with your professional healthcare team.