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Though kava's primary use throughout Oceania is as a social, mood-enhancing beverage*, the plant is also part of the native pharmacopoeia of that region, and is used medicinally for a wide range of conditions. The primary use of kava in folk herbalism is for urogenital inflammation and cystitis. But kava is also drunk to treat headaches, to restore vigor in the face of general weakness, to promote urination, to soothe an unruly stomach, and to treat whooping cough, tuberculosis, and the symptoms of asthma.

Applied topically, kava is used for treating fungal infections and for soothing stings and skin inflammations. Interestingly, kava appears to inhibit gonorrhea*. In those areas where kava is consumed regularly, the rate of gonorrhea is very low and there are many anecdotal tales of kava being drunk to treat gonorrhea*, though no mechanism for this action is known.

The first researcher to engage in a serious investigation of the medicinal applications of kava was Cuzent, who in 1860 made extracts of kava rootstock and roots, and isolated a crystalline substance he dubbed kavahine. Cuzent developed kava-based pills, an oleoresin, an alcohol extract, and a syrup. By the end of the 1800s, kava preparations were available in German herbal shops.

In the early 1900s kava-based remedies made their way into the British pharmaceutical codex. In 1914 kava was listed in the British Pharmacopoeia under the name "kava rhizome."

In 1920 kava appeared in European dispensaries as a sedative and hypotensive. Kava also appeared in the U.S. Dispensatory as a treatment for chronic irritations of the urogenital tract. In 1950 the U.S. Dispensatory listed kava for the treatment of both gonorrhea and nervous disorders, under the drug names "Gonosan" and "Neurocardin" respectively.

Prior to World War II kava from Pohnpei was used by the Japanese for the preparation of a medicine used to treat gonorrhea. According to export records from that time, large shipments of kava were sent to Japan for the manufacture of pills. In 1985, popular Japanese newspapers touted kava as an effective remedy for the common cold. Today Kaviase, a French pharmaceutical product manufactured by drug giant Merrell Dow, is marketed for the treatment of urinary tract infections.

Currently, approximately 100 tons of kava are shipped annually to European laboratories for the manufacture of medicinal kava preparations. U.S. companies are now becoming aware of kava as well, and are beginning to release kava products in liquid extract, pill, and capsule forms. The following kava products are currently available in the European market.

Kava's chemistry has been investigated intensively. The medicinally active constituents of kava are a group of resinous compounds known as kavalactones, or kavapyrones. The kavalactones have been the objects of chemical research since the mid-1800s, and much is known about their mode of activity. While as many as fifteen kavalactones are known, only six appear in kava to any significant extent. These six kavalactones are demethoxy-yangonin, dihydrokavain, yangonin, kavain, dihydromethysticin and methysticin. Their detection, analysis, and study over the past 130 years is a peripatetic detective tale worthy of Sir Arthur Conan Doyle's telling.

While today the analysis of the kavalactones is made easy by advanced analytical laboratory machinery, in the 1800s such research was slow and arduous. Almost simultaneously, Gobley in 1860 and Cuzent in 1861 isolated the first of the kavalactones, known today as methysticin. Prior to agreement on its proper name, methysticin was known variously as kavatin, kanakin, kavakin, and kawakin. The giant scientific step of isolating methysticin opened the door to subsequent chemical progress with the resinous extract of kava. In 1874, Scientists Nolting and Kopp isolated another kavalactone which went nameless until it was dubbed yangon in by Lewin in 1886.

Following the publication of Lewin's seminal 1886 treatise on kava, Uber Piper Methysticum, numerous researchers leapt test-tube first into the kava fray. In 1908, Winzheimer isolated dihydromethysticin, the most active tranquilizer of all the kavalactones. Between 1914 and 1933, Borsche and his various colleagues isolated two additional kavalactones, kawain and dihydrokawain. They also determined the chemical structures of those two kavalactones and the three others that had been previously discovered.

Borsche and his colleagues published a series of fourteen papers on the subject, adding greatly to the body of kava science. A chemical error made by Borsche regarding the actual structure of yangonin was corrected in 1950 by Macierewicz, and yangonin was subsequently synthesized in 1960 by Bu'Lock and Smith. In 1959 Klohs, Keller, and Williams isolated demethoxyyangonin, and in 1962, Mors, Magalhaes, and Gottlieb reported the isolation of 5,6-dihydromethysticin, 11- methoxyyangonin and 11methoxynoryangonin. Further detailed analysis of the structure of kavalactones and their activity has been conducted by Keller and Klohs, Shulgin, and Duve and Duffield.

Parallel to the chemical investigation of the kavalactones, the study of their pharmacology, or chemical activity in humans and other animals, has also been of keen interest to researchers, and continues unabated to this day. Pioneering plant researcher Lewin was the first to evaluate the activity of the kavalactones.

Using kava resin administered by intraperitoneal injection, Lewin found that the compound produced paralysis in frogs, and sedated pigeons and sparrows to such an extent that they were temporarily rendered unable to fly. When resin was injected subcutaneously into cats, the animals fell into a deep sleep. While these experiments may seem crude by today's standards, at the time they were groundbreaking, and they set the pace for further pharmacological investigation.

In Schubel's investigations as reported in 1924, he found that kava resin administered in large enough doses could produce temporary paralysis of sensory nerves and smooth muscle. Interestingly, Schubel also made a discovery that supported the mastication of kava as the most effective means of preparation.

In experiments conducted with frog hearts, he discovered that kava extract was stronger if made from root that had been incubated with saliva. He speculated that the starch-digesting enzyme (ptyalin) in saliva more effectively liberated the resinous compounds from the root, thus yielding a stronger extract.

In Van Veen's 1938 work with pigeons, administration of kava resin put the birds to sleep within fifteen minutes. Upon awakening the birds appeared fully revived and recovered. The same results were achieved with monkeys. In an important discovery, Van Veen found that the effect of kava extract was enhanced when put into a lecithin/ water emulsion. This has been subsequently confirmed. The presence of lipids such as lecithin or vegetable oils appears to enhance the absorption and uptake of the kavalactones, rendering them more effective.

After Van Veen, the soporific effects of large doses of kava's active agents was subsequently demonstrated by Hansel and Beiersdorff in their 1959 work on the kavalactones dihydrokawain and dihydromethysticin. In 1967 Meyer was able to show that the primary activity of the kavalactones was as muscle relaxants. This work opened ?the door for further research on the kavalactones as potent skeletal muscle relaxants that work on the central spinal nerves*.

While work using the various isolated, synthesized kavalactones has yielded interesting results, the activity of each as a separate molecule is less significant than the synergy that is created when all the kavalactones are taken together in their natural form. For example, in humans isolated dihydromethysticin must be taken in doses of 800-1200 milligrams to produce a tranquilizing effect. Yet a single coconut shell of kava, yielding approximately 250 milligrams of resinous kavalactones, can produce a tranquilizing effect*. In 1959 Klohs was able to demonstrate that there is a synergistic activity among the kavalactones that enhances their strength when taken together. This is not an uncommon finding in the investigation of natural substances.

The various antioxidant carotenoids, including alpha and beta carotene, lutein, zeaxanthin, and cryptoxanthin, appear to enhance immunity* better and offer greater protection against certain forms of cancer* when consumed together from natural sources as compared with their isolated, synthesized forms. The kavalactones do the same. Time and again researchers discover that the extraction and isolation of specific molecules produces an inferior medicine as compared with the same compound in its natural complex of ancillary and related compounds.

Let me recap in brief what is known regarding kava's pharmacological activity. The nature of the effects that kava produces depends on the variety of kava plant being used, the age of the plant, and the ratio of kavalactones found in that type. The type of kava preparation, whether it is consumed on a full or empty stomach, and the set and setting of the user will all influence the effects each user will experience.

First and foremost, kava acts as a topical anesthetic*. It numbs the tongue and throat when drunk in its traditional form or when taken orally as a liquid extract. Kava produces a state of calm and tranquility*, and promotes sleep* if taken in sufficient quantity.

Kava is also an effective analgesic*, but its mode of activity as a pain reliever has yet to be determined. Kava is an excellent muscle relaxant and can make the pain of an aching back, a sore neck, or any other cramped, sore, or injured muscle disappear*. As an aid in the relief of both cystitis and gonorrhea, kava appears to be beneficial*, though the exact mechanism for this action is not yet fully understood. Some researchers believe that this action is due to kava's antifungal activity.

The kavalactones have demonstrated significant antifungal activity against some human pathogens*. Unfortunately, kava appears to have no effect on Candida albicans yeast. Kava also possesses recognized anticonvulsant properties*.

While side effects with kava are rare and mild when taken in moderate doses, its abuse can admittedly lead to health problems. A 1988 study of heavy kava use among Aboriginals in Arnhem Land in Australia showed that excessive kava consumption in the range of 310 to 440 grams of kava per week contributed to deteriorating health. Like Native Americans, Australian Aboriginals were overwhelmed by European colonists, who over the course of a couple of centuries succeeded in pushing the natives off their land, disenfranchising them, and irreparably damaging their traditional culture.

Today some tribal Aboriginals are making a concerted effort to restore traditional customs and culture, but for many Aboriginals the future is bleak. Relegated to history, they no longer fit into the new Australian culture, a construct devised by foreign interlopers. Left floating in a social limbo, Australian Aboriginals have followed in the footsteps of virtually all displaced native people before them; they have a ferociously high rate of alcoholism and drug abuse. One of the primary causes of death among young Aboriginal men is petrol sniffing, a practice in which gas tanks are punctured and the fumes inhaled.

Into this downward spiral of cultural entropy came kava, a cheap, regionally-produced plant which is readily available and legal. Kava can stupefy if consumed in very high doses on a regular basis. Some malnourished Aboriginals reputedly combine strong kava and hard alcohol, a combination that is extremely detrimental to the body, particularly the liver. The ravages of advanced malnutrition, coupled with the extreme overuse of kava and other substances, result in a pitiable condition of deteriorated health and stupefaction.

Because those studied also smoked tobacco heavily and consumed large quantities of alcohol, separating out the risk factors of overconsumption of kava is difficult. To put the Aboriginals' daily kava dose into perspective, such amounts require drinking well over a gallon of kava per day, a significant feat.

Heavy abusers studied suffered from shortness of breath, dry, scaly skin, liver damage, and alterations in red and white blood cells and platelets. The malnutrition was due to the fact that kava consumption literally replaced much of the subjects' food intake. Just as one hundred cups of coffee per day can kill you, gallons of kava per day can ruin your health. This is no surprise. Even beneficial plants must be used in appropriate doses.

Excerpted from "Kava: Medicine Hunting in Paradise" by Chris Kilham.

*These statements have not been evaluated by the Food and Drug Administration. This product is not intended to cure, treat, diagnose, or prevent any disease.