The Encyclopedia of Natural Medicine, 3rd Ed.

Insomnia

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• Difficulty falling asleep (sleep-onset insomnia)

• Frequent or early awakening (sleep-maintenance insomnia)

Insomnia is one of the most common complaints seen by physicians. Within the course of a year, up to 30% of the population suffers from insomnia, and roughly 10% of the adult population has chronic insomnia.1 Many people use over-the-counter medications to combat the problem, and others seek stronger sedatives. Approximately 12.5% of the adult population uses a prescribed anxiolytic or sedative hypnotic in the course of a year; about 2% of the population takes one on any given day. Nearly 100 million prescriptions are written each year for these drugs.2

Causes

Psychological factors such as depression and anxiety account for 50% of all cases of insomnia.1 Psychological counseling with cognitive behavioral therapy can produce improvements in sleep quality.3

Eliminating factors that impair sleep quality is another important consideration. There are many recreational drugs, prescription and nonprescription drugs, and foods and beverages that can interfere with sleep, such as:

• Alcohol

• Beta-blockers

• Caffeine and related compounds:

  images Coffee

  images Tea

  images Chocolate

  images Caffeinated colas and energy drinks

• Marijuana

• Oral contraceptives

• Thyroid preparations

Sleep Apnea

It is important to rule out sleep apnea in anyone suffering from insomnia. First described in 1965, sleep apnea is a breathing disorder characterized by brief interruptions of breathing during sleep. These breathing pauses (as many as several hundred a night) are almost always accompanied by snoring between pauses, although not everyone who snores has this condition. Sleep apnea can also be characterized by a choking sensation. People with sleep apnea experience periods of anoxia (oxygen deprivation of the brain) with each episode; the anoxia arouses the sleeper enough to reinitiate breathing. Seldom does the sufferer awaken enough to be aware of the problem. But the frequent interruptions mean that people get less deep, restorative sleep, and this lack often leads to excessive daytime sleepiness, early morning headache, and other quality-of-life problems.4 Approximately 18 million Americans are thought to suffer from sleep apnea.

Early recognition and treatment of sleep apnea are important because the disorder is also associated with irregular heartbeat, high blood pressure, heart attack, and stroke as well as a loss of memory function and of other intellectual capabilities. The patient usually does not know he or she has a problem. It is important that people see a doctor if they snore heavily or if their sleep partners have noticed periods of interrupted breathing during sleep. Sleep apnea should also be considered in anyone with significant daytime drowsiness or changes in intellectual function. Sleep apnea can be properly diagnosed only through the services of a sleep disorder specialist and usually in a sleep laboratory.

Sleep apnea is most often caused by narrowing of the airway from an accumulation of fatty tissue. This is called obstructive sleep apnea. With a narrowed airway, air cannot easily flow into or out of the nose or mouth. This results in heavy snoring, periods of no breathing, and frequent arousals (abrupt changes from deep sleep to light sleep). Alcohol and sleeping pills increase the frequency and duration of breathing pauses in people with sleep apnea. In some cases sleep apnea occurs even if no airway obstruction or snoring is present. This form, called central sleep apnea, is caused by a loss of brain control over breathing. In both obstructive and central sleep apneas, obesity is the major risk factor, and weight loss is the most important aspect of long-term management.

The most common treatment of sleep apnea is the use of nasal continuous positive airway pressure (CPAP). In this procedure, the patient wears a mask over the nose during sleep, and pressure from an air blower forces air through the nasal passages. The air pressure is adjusted so that it is just enough to prevent the throat from collapsing during sleep. Nasal CPAP prevents airway closure while in use, but apnea episodes return when CPAP is stopped or is used improperly. Surgery to reduce soft tissue in the throat or soft palate should be used only as a last resort because it often does not work or can make the problem worse. Laser-assisted surgery (uvulopalatoplasty) is a highly promoted surgical option. In this procedure lasers are used to surgically remove excessive soft tissue from the back of the throat and from the palate. This procedure works well initially in about 90% of sleep apnea sufferers, but within one year many people are the same as or even worse than before because of the scar tissue that invariably forms.4

Causes of Insomnia

SLEEP-ONSET INSOMNIA*

SLEEP-MAINTENANCE INSOMNIA*

Anxiety or tension

Depression

Environmental change

Environmental change

Emotional arousal

Sleep apnea

Fear of insomnia

Nocturnal myoclonus

Phobia of sleep

Hypoglycemia

Disruptive environment

Parasomnias

Pain or discomfort

Pain or discomfort

Caffeine

Drugs

Alcohol

Alcohol

* The boundary between the categories is not entirely distinct.

Therapeutic Considerations

Adequate sleep is absolutely necessary for long-term health and regeneration. Most people can tolerate a few days without sleep and fully recover. However, chronic sleep deprivation appears to accelerate aging of the brain, cause neuronal damage, and lead to nighttime elevations in cortisol.5

Avoidance of Stimulants, Especially Caffeine

As with all conditions, the best treatment is to first remove the causes. The average American consumes 150 to 225 mg caffeine per day, roughly the amount of caffeine in one to two cups of coffee. Although most people can handle this amount, there is a huge variation in the rate at which different people detoxify stimulants such as caffeine. Owing to the genetic variation in the liver enzyme that breaks down caffeine, some people can eliminate caffeine very quickly (for example, half of a dose of caffeine is eliminated within 30 minutes), while in others the breakdown process is much less effective (it can take as much as 12 hours to eliminate half of a dose of caffeine). Everyone who drinks more than one cup of coffee in the early morning and who has trouble sleeping should simply try caffeine avoidance for 7 to 10 days. All sources of caffeine—not just coffee but tea, chocolate, drugs with caffeine, and energy drinks—must be avoided.

Exercise

Regular physical exercise is known to improve general well-being and promote improvement in sleep quality.3 Exercise should take place in the morning or early evening, not right before bedtime, and should be of moderate intensity. Usually 20 minutes of aerobic exercise at a heart rate between 60 and 75% of maximum (with the maximum rate calculated as 220 minus the patient’s age in years) is sufficient.

Progressive Relaxation

Numerous techniques can promote relaxation and prepare the body and mind for sleep. One of the most popular and easy-to-use techniques is progressive relaxation, in which an individual is taught what it feels like to relax by comparing relaxation with muscle tension. Each muscle is contracted forcefully for a period of one to two seconds, then relaxed. The procedure begins with contraction and then relaxation of the muscles of the face and neck; next the upper arms and chest are contracted and then relaxed, followed by the lower arms and hands. The process is repeated progressively down the body—abdomen, buttocks, thighs, calves, and feet. Because the procedure goes progressively through all the muscles of the body, a deep state of relaxation eventually results. This whole procedure is repeated two or three times.

Nocturnal Glucose Levels

Dips in blood glucose levels during the night may be an important cause of sleep-maintenance insomnia, especially when the drops are rapid. The brain is highly dependent on glucose for energy, and a quick drop in blood glucose level stimulates the release of adrenaline and cortisol, which promote awakening. See the chapter “Hypoglycemia” for strategies to stabilize blood sugar levels.

Serotonin Precursor and Cofactor Therapy

Serotonin is an important initiator of sleep. The synthesis of serotonin in the central nervous system depends on availability of the amino acid tryptophan. Supplemental L-tryptophan has shown modest effects in the treatment of insomnia.68 It is certainly not a panacea; however, excellent results have been reported even in severe cases. Although not every patient has shown response to tryptophan in clinical trials, those who do respond have experienced dramatic relief. The key advantage of tryptophan over prescription and over-the-counter pills is that, unlike these agents, tryptophan does not produce any significant distortions of normal sleep processes. Dosages of tryptophan smaller than 2,000 mg are generally ineffective.

Current knowledge about the sleep-inducing effects of tryptophan suggests that it is generally more effective in sleep-onset insomnia and less effective in sleep-maintenance insomnia.6 The sleep-promoting effect is often thought to be the result of enhanced serotonin synthesis, but there is evidence to suggest that other mechanisms may play a role, including tryptophan-enhanced melatonin synthesis. For example, administration of large dosages of tryptophan causes a massive elevation of plasma melatonin concentration.9 There may be other effects as well that do not involve either serotonin or melatonin.10,11

It appears that the insomnia-relieving and sleep-promoting actions of tryptophan are cumulative, in that it often takes a few nights for l-tryptophan to start working. In one double-blind study, the effects of 3 g tryptophan on sleep performance, arousal threshold, and brain electrical activity during sleep were assessed in 20 men with chronic sleep-onset insomnia.12 After a sleep laboratory screening night, all subjects received a placebo for three consecutive nights; then 10 subjects received tryptophan and 10 received a placebo for six nights. All subjects received a placebo for the last two nights. L-tryptophan had no effect during the first three nights of administration. However, on nights four through six, the time it took to fall asleep was significantly reduced. Consistently with other studies, this study found that unlike sleeping pills (especially benzodiazepines), tryptophan did not alter sleep stages, impair daytime performance, or alter brain electrical activity during sleep. This study suggests that tryptophan should be used for a minimum of one week before its effects can be assessed in chronic insomnia. However, single dosages of tryptophan can have good sleep-promoting effects in other situations, such as in people who regularly experience insomnia the first time they sleep in a new place, such as a hotel.

Administration of high-dose tryptophan (4 g) during the day can cause daytime sleepiness. This suggests that consumption of foods high in tryptophan during the day may contribute to daytime sleepiness. Conversely, an evening meal high in tryptophan relative to competing amino acids may promote sleep.

The important cofactors vitamin B6, niacin, and magnesium should be administered along with the tryptophan to ensure its conversion to serotonin. Also, because other amino acids compete with tryptophan for transport into the central nervous system, avoid consuming protein at the same time as you take the tryptophan. But, because insulin increases tryptophan uptake, do take a carbohydrate source (such as fruit or fruit juice) with the tryptophan.

Niacin has been reported to have a sedative effect, probably owing to its ability to dilate peripheral blood vessels and shunt tryptophan metabolism toward serotonin synthesis.

5-Hydroxytryptophan (5-HTP)

Chemically speaking, 5-HTP is one step closer to serotonin than tryptophan is and does not depend on a transport system for entry into the brain. Several clinical studies have shown 5-HTP to produce dramatically better results than tryptophan in promoting and maintaining sleep, even though it is used at lower dosages.1316

One of the key benefits of 5-HTP is its ability to increase REM sleep (typically by about 25%) while increasing deep sleep (stages 3 and 4) without lengthening total sleep time.10,11 The sleep stages that are reduced to compensate for the increases are non-REM stages 1 and 2, the least important ones.

The dosage recommendation for 5-HTP is 100 to 300 mg taken 30 to 45 minutes before retiring. Start with the lower dose for at least three days before increasing it.

Melatonin

The most popular natural aid for sleep is melatonin. Supplementation with melatonin has been shown in several studies to be very effective in helping induce and maintain sleep in both children and adults and in both people with normal sleep patterns and those with insomnia. However, the sleep-promoting effects of melatonin are apparent only if melatonin levels are low.17 When melatonin is taken just before going to bed by normal subjects or by patients with insomnia who have normal melatonin levels, it produces no sedative effect. This is because people normally have a rise in melatonin secretion before falling asleep. Melatonin supplementation appears to be most effective in treating insomnia in the elderly, in whom low melatonin levels are quite common.18

In one of the most interesting studies, 26 elderly insomniacs with lower than normal melatonin levels were given 1 to 2 mg melatonin two hours before the desired bedtime for one week. Although there was no discernible difference in sleep onset and sleep efficiency (time asleep as a percentage of total time in bed) between the two forms, the slow-release form yielded better effects on sleep maintenance.19

A dose of 3 mg at bedtime is more than enough (in fact, doses as low as 0.1 or 0.3 mg have been shown to produce a sedative effect when melatonin levels are low).20 Although melatonin appears to have no serious side effects at recommended doses, melatonin supplementation could conceivably disrupt the normal circadian rhythm. In one study, a dosage of 8 mg per day for only four days resulted in significant alterations in hormone secretions.21

Restless Legs Syndrome and Nocturnal Myoclonus

Restless legs syndrome and nocturnal leg cramps (myoclonus) are significant causes of insomnia. Restless legs syndrome occurs when the patient is awake and is characterized by an irresistible urge to move the legs. Almost all patients with restless legs syndrome have nocturnal myoclonus.1 Nocturnal myoclonus is a neuromuscular disorder characterized by repeated contractions of one or more muscle groups, typically of the leg, during sleep. Each jerk usually lasts less than 10 seconds. The patient is normally unaware of the myoclonus and complains only of either frequent nocturnal awakenings or excessive daytime sleepiness, but questioning of the sleep partner often reveals the myoclonus.

If there is a family history of restless legs syndrome (such a history is present in about one-third of all cases of the syndrome), high-dose folic acid, 35 to 60 mg per day, can be helpful.22 Doses in this range require a prescription, because the U.S. Food and Drug Administration limits the amount available per capsule to 800 mcg. Restless legs syndrome is also a common finding in patients with malabsorption syndromes.22

If there is no family history, low iron levels may be the problem, so a blood test for serum ferritin should be done. The association between low iron levels and restless legs syndrome was documented in clinical studies more than 30 years ago. A later study reproduced these observations, finding serum ferritin levels to be lower in 18 patients with restless legs syndrome than in 18 control subjects.23 Serum iron, vitamin B12, folic acid, and hemoglobin levels did not differ in the two groups. However, serum ferritin levels were inversely correlated with the severity of symptoms. Fifteen of the patients with the syndrome were treated with iron (ferrous sulfate) at a dosage of 200 mg three times per day for two months. The severity of restless legs syndrome decreased by an average of 4 points in sixteen patients with an initial ferritin level lower than 18 mg/l, by 3 points in four patients with ferritin levels between 18 and 45 mg/l, and by 1 point in five patients with ferritin levels between 45 and 100 mg/l.

In addition to restless legs syndrome, low serum ferritin levels have been found in psychiatric patients experiencing a condition called akathisia, a drug-induced state of agitation (the name comes from the Greek and means “cannot sit down”). The drugs that most commonly produce akathisia are antidepressant drugs, such as fluoxetine (Paxil, Prozac) and sertraline (Zoloft). Level of iron depletion also correlates with the severity of akathisia. Anyone suffering from drug-induced akathisia should ask a physician to perform a serum ferritin assessment. If serum ferritin levels are below 35 mg/l, take 30 mg iron bound to either succinate or fumarate twice per day between meals. If this recommendation causes abdominal discomfort, try 30 mg with meals three times per day.

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QUICK REVIEW

• Psychological factors account for 50% of all insomnias evaluated in sleep laboratories.

• There are many recreational drugs, prescription and nonprescription drugs, and foods and beverages that can interfere with sleep.

• Early recognition and treatment of sleep apnea is important because it is associated with marked daytime fatigue, irregular heartbeat, high blood pressure, heart attack, and stroke as well as a loss of memory function and other intellectual capabilities.

• In both obstructive and central sleep apneas, obesity is the major risk factor, and weight loss is the most important aspect of long-term management.

• Chronic sleep deprivation appears to accelerate aging of the brain, causes neuronal damage, and leads to nighttime elevations in cortisol.

• Regular physical exercise promotes improvements in sleep quality.

• Rapid drops in blood glucose level can promote awakening during sleep.

• Several clinical studies have shown 5-HTP to be effective in promoting and maintaining sleep.

• Supplementation with melatonin has been shown in several studies to be very effective in helping induce and maintain sleep.

• More than 20 double-blind clinical studies have now substantiated valerian’s ability to improve sleep quality and relieve insomnia.

Botanicals with Sedative Properties

Numerous plants have sedative action. Plants commonly prescribed as aids in promoting sleep include:

Valerian (Valeriana officinalis)

Passionflower (Passiflora incarnata)

Hops (Humulus lupulus)

Skullcap (Scutellaria lateriflora)

Chamomile (Matricaria chamomilla)

Of the herbs listed, the one on which the most clinical research has been done is valerian. More than 20 double-blind clinical studies have now substantiated valerian’s ability to improve sleep quality and relieve insomnia.24,25Additional research is warranted, but these studies show that extracts of valerian root improve sleep quality and reduce the time needed to fall asleep. The studies, which were usually performed under strict laboratory conditions, demonstrated quite clearly that valerian is as effective at bringing on sleep as small doses of barbiturates or benzodiazepines. However, although these latter compounds also increase morning sleepiness, valerian usually reduces morning sleepiness.

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THE DARK SIDE OF SLEEPING PILLS

Most sleeping pills are technically “sedative hypnotics.” This class of drugs is also widely used to treat anxiety and stress. Examples include:

Alprazolam (Alprazolam, Xanax)

Chlordiazepoxide (Librium)

Diazepam (Valium)

Eszopiclone (Lunesta)

Flurazepam (Dalmane)

Quazepam (Doral)

Ramelteon (Rozerem)

Temazepam (Restoril)

Triazolam (Halcion)

Zaleplon (Sonata)

Zolpidem (Ambien)

All of these drugs are associated with significant risks. Most of them are highly addictive and very poor candidates for long-term use. Common side effects include dizziness, drowsiness, and impaired coordination; it is important not to drive or engage in any potentially dangerous activities while on these drugs. Alcohol should never be consumed with these drugs, as it could be fatal.

The most serious side effects of the conventional antianxiety drugs relate to their effects on memory and behavior. Because these drugs have a powerful effect on brain chemistry, significant changes in brain function and behavior can occur. Severe memory impairment and amnesia, nervousness, confusion, hallucinations, bizarre behavior, and extreme irritability and aggressiveness may result. They have also been shown to increase feelings of depression, including suicidal thinking.

Daniel F. Kripke, M.D., professor of psychiatry emeritus at the University of California, San Diego, worked for over 30 years assessing the risk of sleeping pills. The most shocking of his findings was that people who take sleeping pills die sooner than people who do not use sleeping pills. Dr. Kripke examined data from a very large study known as the Cancer Prevention Study I. In this study, American Cancer Society volunteers gave questionnaires to more than 1 million Americans and then followed up six years later. Dr. Kripke and his colleagues found that 50% more of those who said that they often took sleeping pills had died, compared with participants of the same age, sex, and reported health status who never took sleeping pills.26

To reexamine these risks, the American Cancer Society agreed to ask new questions about sleeping pills to of 1.1 million new participants in another study, called the Cancer Prevention Study II, or CPSII. In the CPSII, it was again found that people who said that they used sleeping pills had significantly higher mortality. Those who reported taking sleeping pills 30 or more times per month had 25% higher mortality than those who said that they took no sleeping pills. Those that who took sleeping pills just a few times per month showed a 10% to 15% increase in mortality, compared with those who took no sleeping pills. Deaths from common causes such as heart disease, cancer, and stroke were all increased among sleeping pill users. Sleeping pills appeared unsafe in any amount.27

All told, there are now 18 population-based studies that show a clear link between the use of sleeping pills and increased mortality risk. Four of these studies specifically found that use of sleeping pills predicted increased risk of death from cancer.2729

In a more recent study, Dr. Kripke’s team obtained medical records for 10,529 people who were prescribed hypnotic sleeping pills and for 23,676 matched patients who were never prescribed sleeping pills. Over an average of 2.5 years, the death rate for those who did not use sleeping pills was 1.2%. It was 6.1% for people with sleeping pill prescriptions. They also had a 35% higher risk of cancer. Based on these findings, Kripke and colleagues estimate that sleeping pills are linked to 320,000 to 507,000 U.S. deaths each year.29

So what do all of these data really mean? They may mean that the use of sleeping pills is just an indicator of stress, anxiety, insomnia, and depression. In other words, maybe these people were taking sleeping pills because they were really stressed out or depressed, and it was actually the stress or depression that did them in. Or it could be that the drugs produce complications. For example, it is possible that the drugs interfere with normal sleep repair mechanisms as well as promote depression. The bottom line is that it is clear that the risks of taking the drugs far outweigh any benefits.

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TREATMENT SUMMARY

The aim of treatment with natural measures is to improve sleep quality without any of the side effects of over-the-counter and prescription sleeping pills. In addition to psychological support if needed, the foremost component of treatment is the control of any factors known to disrupt normal sleep patterns, such as the following:

• Stimulants (e.g., coffee, tea, chocolate, energy drinks, coffee ice cream)

• Alcohol

• Hypoglycemia

• Stimulant-containing herbs (e.g., ephedra, guarana)

• Marijuana and other recreational drugs

• Numerous OTC medications

• Prescription drugs

If this approach produces no response, try natural sleep aids. Once a normal sleep pattern has been established, the recommended supplements and botanicals should be slowly decreased.

If there is a family history of restless legs syndrome, high-dose folic acid, 35 to 60 mg per day, can be helpful but requires a prescription. It is not known if lower dosages might work just as well. If there is no family history, ask for a serum ferritin test to rule out iron deficiency.

Exercise

Engage in a regular exercise program that elevates heart rate to 60 to 75% of maximum for at least 20 minutes a day (but do not exercise right before going to bed).

Diet

The guidelines given in the chapter “A Health-Promoting Diet” can be helpful. Especially important to preventing sleep maintenance insomnia is eating a lowglycemic-load diet to reduce blood sugar volatility. For additional information on how to stabilize blood sugar levels, see the chapter “Hypoglycemia.”

Nutritional Supplements

The following supplements can be taken 45 minutes before bedtime:

• Niacin: 30 to 50 mg

• Vitamin B6: 25 to 50 mg

• Magnesium: 150 to 200 mg

• 5-HTP: 25 to 50 mg

• Melatonin: 1 to 3 mg

• L-theanine: 200 to 600 mg

Botanical Medicines

• Valerian (Valeriana officinalis), 45 minutes before bedtime:

  images Dried root (or as tea): 2 to 3 g

  images Tincture (1:5): 4 to 6 ml (1 to 11/2 tsp)

  images Fluid extract (1:1): 2 to 4 ml (1/2 to 1 tsp)

  images Dry powdered extract (0.8% valerenic acid): 150 to 300 mg