Herbal Remedies and Sleep Medicine

d05a.jpg (9384 bytes)When I looked through the program of the 15th Associated Professional Sleep Societies Annual Meeting in Chicago on June 5-10, 2001, I did not come across a lecture or postgraduate course on herbal remedies or alternative therapies in sleep disorders. Similarly, the report of an international workshop on Sleep and Health: Research and Clinical Perspectives1 focuses on insomnia in primary care and public health, and its economic impact, but fails to address the abuse of herbal remedies by the general population in their self-treatment of insomnia.

When I did a literature search on this topic, I found numerous articles about the use of herbs in sleep disorders. Advertisements for herbal products abound on the Internet, including natural medicine for insomnia, herbs to support a natural, quality sleep, melatonin herbal combinations, Chinese medicine’s view of insomnia and depression, sleep balance, and testimonials from product users (of course, with disclaimers—“the testimonials are intended for information only, and not to diagnose, treat, prevent, or cure any disease. These statements have not been evaluated by the Food and Drug Administration [FDA]”). There are many articles available regarding Chinese, homeopathic, and Ayurvedic medicines. According to Chinese medicine, insomnia and depression are attributed to yin-yang imbalance due to a weak liver, spleen, heart, or kidneys. “Chinese Bitters” in the morning and “Coptis” or “Curcuma” at night are promoted to improve sleep quality. Depression, according to Chinese medicine, indicates blocked liver energy and is also common in individuals with gallstones or whose gallbladders were removed.

Herbal Remedies
My research on herbal remedies led me to local grocery stores and pharmacies. To my surprise, I found numerous displays of herbal and alternative therapies. These included one product containing citrus extract, Saint-John’s-wort, L-phenylalanine, and guarana seed extract; ginseng; valerian root tablets; and various herbal formulas to provide energy including combinations of vitamin E, magnesium, zinc, chromium, guarana, ma huang extract (ephedrine), bee pollen, Siberian ginseng, ginger, lecithin, Damiana leaf, sarsaparilla, gotu kola, spirulina, and royal jelly.

Interestingly, a recent issue of Arthritis Today2 published an excellent supplement guide. Some of the salient features of this guide in regard to sleep disorders are shown in Table 1.

(Eleutherococcus senticosus)
Asian (Panax ginseng)
decreases fatigue, fibromyalgia stimulant, causes hyper- tension and hyperglycemia
Do not take with monoamine oxidase inhibitors
(Centella asiatica, Centella coriacea)
increases circulation GI symptoms, abortion, increased cholesterol and blood glucose, potentiates sedative effects of other drugs
(Piper methysticum)
treats depression and     anxiety GI symptoms, headache, dizziness, impairs concentration
(N-acetyl-5- methoxytryptamine)
cures sleep problems, fibromyalgia, and depression avoid in autoimmune diseases and depression
(Hypericum perfora    
natural Prozac for depression (increases  brain serotonin) sun sensitivity; blocks   effects of oral contraceptive pills, tricyclic antidepressants, warfarin, cyclosporin; may  cause insomnia, dizziness, headache
(Valeriana officinalis)                         
treats insomnia, promotes deep sleep with-out disturbing natural REM sleep pattern. Mild sedative and tranquilizer avoid with alcohol and tranquilizers; drowsiness
(Ginkgo biloba) 
increases circulation    headache, upset stomach, risk of bleeding
(Passiflora incarnata) 
herb of choice for transient insomnia unknown
(Scutellaria laterifolia)
nervine tonic and sedative unknown
(Matricaria recutita)
sedative, antianxiety   relatively safe
helps fibromyalgia, sleep   disorders, and fatigue eosinophilia myalgia, (severe rashes, acute pain)
“date rape” drug, coma, or death
helps fibromyalgia, sleep problems, depression, and improves sexual health coma, seizures, death
L-TRYPTOPHAN eases sleep disorders and depression illegal in the United  States, eosinophilia myalgia
MAGNESIUM eases sleep disorders    and depression interacts with BP   medications, diarrhea, kidney failure, GI symptoms
Table 1. Herbs, supplements, and sleep disorders.

The “experts” on herbs and supplements are flourishing since consumers are becoming more interested in herbal remedies/dietary supplements, and products continue to flood the marketplace. Some MDs, osteopathic doctors, naturopathic physicians, pharmacists, herbalists, practitioners of Chinese and Ayurvedic medicine, physical therapists, and chiropractors use herbs and supplements in their practices.2

During the past decade, the use of herbal preparations among adults increased from 2.5% to 12.4%.3 The 1994 Dietary Supplements Health and Education Act stimulated the proliferation of herbal medicines.3

The popularity of herbal medicine for treating depression, anxiety, and sleep disorders is at an all-time peak4 (Table 1, page 12). For example, Valeriana officinalis (valerian) is widely used for insomnia, but it has not been shown beyond a reasonable doubt to be effective for this sleep disorder.4 Use of ambient odors as a replacement for drug therapy in insomnia has also been reported.5 Conventional therapy for insomnia includes behavioral and pharmacological approaches, but long-term use of hypnotics can lead to drug tolerance, habituation, and withdrawal symptoms. Hence, herbal and other natural sleep aids are becoming popular and are promoted as safe. Patients perceive dietary supplements as a safer and more natural alternative.6 Besides valerian, agents used in sleep disorders include melatonin, 5-hydroxytryptamine (serotonin), catnip, chamomile, gotu kola, hops, L-tryptophan, lavender, passionflower, and skullcap (Table 1, on page 12). More sophisticated investigations are necessary to corroborate any conclusive evidence for the value of herbal medicine in the psychiatric field.7

Evidence-Based Medicine?
Donath and coworkers8 studied the effects of valerian extract on sleep structure and quality. The short-term (single dose) and long-term (14 days with multiple dosages) effects were studied in a randomized, double-blind, placebo-controlled, cross-over study in 16 patients (four males, 12 females) with diagnoses of psychophysiological insomnia.8 Their median age was 49 (22 to 55). After a single dose of valerian, no effects on sleep structure and subjective sleep parameters were observed. After multiple-dose treatment, there was a significant increase in sleep efficiency for both the placebo and valerian groups. However, in comparison with placebo, slow wave sleep (SWS) latency was reduced after administration of valerian (21.3 vs 13.5 min, respectively; P<0.05). The SWS percentage of time in bed was increased after long-term valerian treatment, in comparison to baseline (9.8% vs 8.1%, respectively; P<0.5). Adverse events during the valerian treatment periods were extremely low (3 vs 18 in the placebo group). The authors concluded that treatment with an herbal extract of radix valerianae demonstrated positive effects on sleep structure and sleep perception (shorter subjective sleep latency) of insomnia patients and recommended this herbal therapy for mild psychophysiological insomnia.8

Valerian Root
The roots of the genus Valeriana (Valerianaceae), as well as related genera such as Nardostachys, are used in many cultures as mild sedatives and tranquilizers.9 V. officinalis is the species most commonly used in northern Europe. The major constituents of its volatile oil include the monoterpene bornyl acetate, sesquiterpene valerenic acid, and other types of sesquiterpenes.9 Valerenic acid has a direct action on the amygdaloid body of the brain (inhibits enzyme-induced breakdown of GABA [gamma-aminobutyric acid]), resulting in sedation. The nonvolatile monoterpenes (valepotriates) have sedative activity on the central nervous system by an unknown mode of action. Recent studies have shown that aqueous extracts of valerian roots contain GABA, which could directly cause sedation, and a lignan, hydroxypinoresinol, which binds to benzodiazepine receptors.9

The problems with valerian are a variation in its composition and content due to differences in genetics and environmental factors, and the instability of some of its constituents poses serious problems with standardization.9

Gyllenhaal and coworkers10 studied the efficiency and safety of herbal stimulants and sedatives in sleep disorders. They addressed the propensity of individuals with sleep disorders to self-treat using herbs. In 1998, 10%-15% of US adults reported using over-the-counter medications or dietary supplements for daytime sleepiness. These researchers studied caffeine and caffeinated herbs, ephedrine-containing herbs, yohimbine, and ginseng (antifatigue activity) and valerian, German chamomile, kava kava, lavender, hops, lemon balm, and passionflower (ability to improve sleep). Caffeine and caffeinated herbs such as guarana, kola nut, and yerba mate are widely used for sleepiness. Ephedra (ma huang) and other ephedrine-containing herbs (Indian sida and orange bitter) are used as stimulants and to promote wakefulness and weight loss. Yohimbine is used as an aphrodisiac stimulant and in body-building preparations. Asian or Panax ginseng/Siberian ginseng is used to treat fatigue and exhaustion. The herbal sedatives valerian and kava kava decrease sleep onset time and promote deeper sleep. However, these experimental studies were small. German chamomile, lavender, hops, lemon balm, and passionflower are claimed to be mild sedatives but need experimental evidence to support their efficiency and safety.

Sleep researchers and medical professional need to address the use of herbs by collecting data about the use of herbal remedies by individuals with sleep disorders; study herb-drug interactions in elderly individuals with sleep disorders; promote basic research to identify the active compounds and their stability in a variety of preparations; conduct large-sample, double-blind, placebo-controlled trials of herbal sedatives; study the prevalence of adulteration and contamination in herbs, particularly imported herbs; explore the activity of herbal sedatives in sleep initiation vs sleep maintenance; obtain patients’ medication histories about their use of herbal preparations to aid sleep and wakefulness; understand that herbal stimulants may interfere with biological sleep need and with circadian biorhythm; use caution that individuals may use herbal stimulants to treat symptoms of a serious underlying sleep disorder (narcolepsy); be aware of side effects and toxicity of herbs like yohimbine that can increase blood pressure and must be avoided in patients with kidney, heart, or liver disease, ulcers, glaucoma, and diabetes mellitus. The Asian herb ephedra (ephedrine) may cause side effects ranging from chest pain and anxiety to heart attacks, syncope, and stroke. Since ephedra, when combined with caffeine, may increase the risk of cardiac side effects, patients should be encouraged to tell their health care provider if they are taking herbs or dietary supplements.

Health care professionals need to educate themselves and their patients about the use and safety of herbal preparations.11 This can help to prevent the double jeopardy of physicians who are uninformed about herbal remedies, and patients who do not tell their primary care provider or sleep specialist if they are taking over-the-counter herbs and supplements.

Taj M. Jiva, MD, is clinical assistant professor of medicine, State University of New York at Buffalo, and a pulmonologist, intensivist, and sleep specialist at Buffalo Medical Group PC, NY.

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