By Ward Dean, M.D.
With the growing unavailability of legal GHB and its precursors, many law-abiding, sleep-deprived Americans are searching for a safe, legal replacement. The South Pacific herb, kava kava (Piper methysticum) induces effects that are remarkably similar to GHB and its dietary supplement precursors, such as the no-longer-available RenewTrient and SomatoPro. I have previously hypothesized that the mechanism of action of kava kava is through its chemical similarity to GHB. The active ingredients in kava kava are a group of substances known as kavalactones (GBL—the active ingredient in RenewTrient—is butyrolactone).
One of the greatest traditional uses of kava kava is as a treatment for anxiety. A study in Germany confirmed its efficacy for this use (Volz, and Kieser, 1997). The authors evaluated 101 patients suffering from anxiety in a 25-week multicenter trial using a special extract of kava kava. The kava was given in a dose of 100 mg of dry extract (= 70 mg kavalactones) per capsule 3 times daily. The authors stated that “the Kava extract is as effective as tricyclic antidepressants and benzodiazepines in treating anxiety disorders, without any of the problems of addiction or tolerance experienced with these drugs.”
Kava kava contains six kava-pyrones: Kavain, dihydrokavain, methysticin, dihydromethysticin, yangonin and desmethoxy-yangonin. The first four of these compounds have a central nervous system muscle-relaxing and anticonvulsive effect, comparable to that of the drug, mephenesin. The electric excitability of the limbic system of cats is diminished after application of kavain or methysticin. This is analogous to what occurs after administration of benzodiazepines. In addition, methysticin and dihydromethysticin act as neuroprotectors in mice and rats. They reduce the infarct (oxygen-deprived) area of the brain after experimental interruption of the cerebral arteries. In the periphery of the body, kavain and methysticin act as local anesthetics (all of these effects are similar to those of GHB). Kava demonstrates significant gamma-aminobutyric acid (GABA) receptor-binding activity (the same binding sites as GHB), and appears to be one of the most potent anxiolytic (anxiety-reducing) agents known. Kava extract has muscle-relaxant, anticonvulsant and analgesic properties. It causes less cognitive impairment than benzodiazepines like Valium (Sherman, 1997).
In her book, Kava—Nature’s Answer to Stress, Anxiety and Insomnia, Dr. Hyla Cass pointed out that “in addition to kava’s ability to fight anxiety and depression, it may be an effective natural treatment for insomnia. At … [an] increased dosage, kava seems to work with the body to bring on deep restful sleep without interfering with sleep’s natural cycles.” Specifically, 1 to 1.5 gm of crude kavalactone residues induce a deep sleep within 30 minutes—an effect comparable to many conventional drugs. The next day, users reported no after-effects such as drowsiness or low energy levels (Lebot, 1988). In a study in Germany in 1991, scientists administered only 100 mg of kava extract three times daily. EEG changes that demonstrated relaxation responses were experienced by 11 of the 12 subjects. Time to fall asleep at night was reduced, and deep and slow-wave sleep increased. These are similar to the sleep pattern induced by GHB. It is conceivable (though untested) that kava may also act as a growth hormone secretagogue, just like GHB. The authors of the study concluded that “kava supports the natural course of sleep cycles, unlike conventional sedative drugs, which often suppress deep and REM sleep” (Emser and Bartylla, 1991). Sleep-deprived people, who are no longer able to legally obtain GHB, or its precursor metabolites GBL or BD, may find relief by supplementing at bedtime with kava kava extract.
Emser, W., and Bartylla, K. Effect of Lava Extract WS 1490 on the sleep pattern in healthy subjects, Neurologie/Psychiatry, 1998, May, 4.
Cass, Hyla, and Mcnally, Terrence. Kava—Nature’s Answer to Stress, Anxiety, and Insomnia. Prima Health, Rocklin, California, 1998.
Lebot, Vincent, Les kavas en Oceanie: Etude Pluridisciplinaire D’une Culture Traditionnelle, 1988.
Sherman, C. Herbal anxiolytics have novel mechanisms, Family Practice News, 1998, July 15, 30.
Volz, H. P. and Kieser, M. Kava-Kava Extract WS 1490 Versus Placebo in Anxiety Disorders—A Randomized Placebo-Controlled 25-Week Outpatient Trial, Pharmacopsychiat, 1997, 30: 1-5.