Kava

Kava or Piper Methysticum is a pacific island plant in the same genus as the common pepper plant in the family Piperaceae. It is know as Awa, Ava Yaqona and sakau on other islands with many variations depending on whet island it originated from. The root of this plant has been and is still to this day consumed by many pacific islanders from New Guinea all the way to Hawaii and down into french Polynesia. Its primary use is as a sedative and a anxiolytic with many other tradional medicinal remedies. The primary active ingredients are in the root and are a series of kavalactones witch is concentrated in the roots but found also in lower amounts in the leaves and stems. The roots can be used fresh by maceration and cold water infusion or more popularly dried and stored for better shelf life and used in cold or warm water extractions. There is on going debate whether or not kava and its kavalactones have a hepatoxicity mainly to the liver due to unwanted chemicals from the leaves or extracted from the roots due to solvent based extracts.

Morphology

Piper Methysticum is a member of the pepper family, Piperaceae, which belongs to the order Piperales in the class Dicotyledonae. Ten of these in the Piperaceae species are products of human consumption used as spices or medicinal drugs. these include:

• P. nigrum (Pepper), one of the oldest known spices,
• P. betle
• P. cubeba (java pepper or tailed pepper), a plant native to indonesia wich was formerly used as a medicine and now as a spice.

It is a hardy, slow growing Perennial reaching heights of more then 3 meters. It is harvested for its rootstock or stump with Monopedial stems with sympodial branches growing from the stump. The stump is knotty, Think, and sometimes tuberous. From this rootstock extends laterally up to 3 meteres long. Rootstock color varies between white to dark yellowdepending upon the amount of kavalactones that are contained in the lemon yellow resin.

Cultivation

Although kava does produce flowers it is incapable of reproducing sexually; its propagation is vegetatively and is dependent solely on human effort. Farmers take cuttings from existing stems off harvested plants and planted i the ground somewhat sideways. New growth occurs at the stem bud at the axil of a lateral branch scar. An upright shoot develops, and then axillary buds and lateral axes appear. In the same way the root stock develops. Choose a site away from prevailing winds air currents can damage kava stems and rootstock, making them susceptible to disease. Shade must be provided during the first 30 months of growth. Along with adequate shade and protection from the wind, kava requires fairly high average temperatures (20-35c) and high humidity (70-100%). Kave grows best in deep, friable, well-draining soils that are rich in organic matter. The plant is very nutrient demanding. Highest yields are obtained on silica-clay soils with a pH OF 5.5-6.5 good drainage is essential.

Preparation and consumption

Traditional

In the Pacific kava is typically drunk at dusk, usually before the evening meal.Infused kava is never kept for long; Islanders prepare kava for immediate consumption. After drinking, people eat small amounts of food because kava tends to reduce appetite and over eating can cause nausea.

Several traditional methods of kava preparation all serve to extract the active chemical constitutes of fresh or dried rootstock. Processing basically involves chewing, grating, grinding or pounding kava stumps and roots and then infusing the processes mass into cold water. These methods break up and macerate the rootstock so that the kavalactones after more readily released in the cold water. Today mastication of fresh rootstock is only practiced in southern vanauatu and among some tribes in papua new guinea.

In Fiji men serving as village priests prepared kava every morning in men's houseshouses, or houses of ancestor worship, as an offering tho village ancestors. The priests and other men in the village would then drink kava together. The rootstock was prepared by grinding, not mastication, and the drink was infused in lead lines holes in the ground, in shallow wooden bowls that were sometimes human or animal in shape, of in plain clay vessels. Early fijians folders their kava by pouring it through bunches of backen fern leaves in a wooden canister like device, rather then using a stronger of hibiscus tiliaceus bark as is common in Polynesia. Fijians also did not drink our of coconut shells as they do today, but instead right out of the container.

In traditional samoan preperation, a young girl chased and served kava. The girl was preferably a virgin, who purified herself for kava preparation by washing her hands and wrists. After chewing kava, she mixed and infused the macerated root in a kava bowl and filtered out the residue with a hibiscus bark strainer. Samoan ceremony required the girl to sit cross legged and bare breasted on a mat behind the kava bowl, with flowers carefully arranged in her hair and wearing a grass skirt. This presented an image of beauty that added to the aesthetic dimension of kava preparation.

It the banks island of northern Vanuatu, Kava drinkers traditionally split into 2 groups, And a person from each group prepare kava for the other. As on most of the northern Vanuatu islands, preparation in the banks group involved the grinding of fresh kava over a large wooden dish using an elongated coral abrading stone. The inner surfaces of these wooden dishes eventually became covered with a grayish-green deposit that is also found at the bottom of coconut shells used as drinking bowls. This deposit is a resinous kavalactone residue that contains the plants active ingredients in concentrated form. Some drinkers periodically scrape the resin from there dishes and mix this with fresh water tho obtain a brew with very powerful effects.

Western Preparation

Kava preparation in the western world outside of the islands is a climbing trend with the emergence of natural products becoming more and more popular. Kava has moved from a ceremonial sense to more of a medicine with ease of use, from extracts of all solvents to pharmaceutical tablets with kavalactones as there main ingredient. Although there's is still a big consumer base for the traditional frozen or dried kava rootstock and is prepared in a semi traditional way.

In Western countries, kava is usually made from kava root powder or extracts. Generally, 2 tablespoons of powder is added per 8 oz. of water, but multiple tablespoons per 16 oz. of water to increase potency. The powder is then put into a muslin bag or nylon sock and soaked in water for about 30 minutes to allow the water to completely soak through the powdered fibers, after a thorough soaking the rootstock is then massaged for a few minutes under the water for a few minutes with breaks to squeeze the powder dry and repeating till the water is a creamy brown color.Lecithin is often added to aid in the process of emulsifying the kavalactones with water.

Another popular method is blending. Blended in a blender for several minutes then strained into a straining cloth; Nylon, cheesecloth, and silk screen are common materials for straining. The remaining liquid is squeezed from the pulp and then the process is repeated until one last strain and squeeze of the pulp and the rest is discarded. Often, coconut water, coconut milk, lemongrass, cocoa, sugar, or soy milk is added to improve flavor, and most of the time lecithin granules or some form of lecithin is added to aid in emulsifying of the water and better leaching of the kavalactones.

DMT Nexus refrences:

https://www.dmt-nexus.me/forum/default.aspx?g=posts&t=35465

Pills and extracts

Pharmaceutical and herbal supplement companies extract kavalactones from the kava plant using solvents such as supercritical carbon dioxide, acetone and ethanol to produce pills standardized with between 30% and 90% kavalactones. Some kava herbal supplements have been accused of contributing to very rare but severe hepatotoxic reactions (see section on safety) such may have been due to the use of plant parts other than the root, such as stems or peelings that are known to have been exported to European manufacturers. A kava pill usually has anywhere from 60 mg to 150 mg of kavalactones. By comparison the typical bowl of traditionally prepared kava beverage has around 250 mg of kavalactones.

Other then pills there is many places that sell extracts extracted from solvents such as supercritical carbon dioxide, acetone and ethanol. Carbon dioxide is showing to be the most preferred and most safe due to liver toxicity and more potent then the other solvent extracted products.

Chemistry and active principles

Kavalactones are the main principle chemicals that give the desired effects from kava.

Lactones

These chemicals are mostly, if not entirely, contained in its resin. These molecules are a series of lactones-that is, organic compounds containing oxygen, with similar structures. These are alpha- pyrones bearing a methoxyl group at carbon 4 and an aromatic styryl moiety at carbon 6.

Butyrolactone, an example of a lactone ring.

The skeletons of the lactonic molecules isolated from kava rootstock are generally 4- methoxy-2- pyrones with phenyl or styryl substitutions at the 6- position. They consider of 13 carbon atoms, 6 of which from a benzene ring attached by a double bond to an unsaturated lactone. 15 lactones have been isolated from kava rootstock, 9 of which have been fully identified.

The following 6 compounds are present in the highest concentrations: yangonin, methysticin, dihydromethystic, kavain, dihydrokavain, and demethoxy-yangonin. 9 other compounds are of minor importance in the rootstock: dehydrokavain, cis-5-hydroxy-kavain, 7,8-dihydroyangonin, 5,6-dihydroyangonin, 5,6-dehydro-methysticin, 11-methoxy-yangonin, 11-hydroxy-yangonin, 11-methoxy-12-hydroxy-dehydro-kavain, and 10-methoxy-yangonin.

Some researchers have tried to classify kavalactones by reference to common characteristics. The simplest method of grouping is one suggested by hänsel, which supports the molecules according to the presence or absence of double bonds at the 5,6 and 7,8 positions and divided them into 2 major groups: the enolides, with 1 double bond, and the dienolides, with 2 double bonds. This system recognizes that primary chemical differences among the kavalactones involve the presence or absence of these double bonds as well as the presence or absence of substituent groups in the phenyl ring.

Kavain, one of the active kavalactones present in Kava Kava root

Flavokavains and other compounds

3 flavokavains labeled A, B , and C, have been identified in kava rootstock. Flavokavain C structure and synthesis were analyzed by a Indian team in 1976. Other substances isolated from the kava plant include an alcohol, ketones, a phytosterol, and organic acids.

Chemotypes

In 1984 Lebot and Lévesque initiated a research program to address 2 questions about the chemistry of kava. First, are the chemical composition and total kavalactone content of a plant dependent on the cultivator, the age of the plant, specific environmental factors, or a combination of these variables? And second, when a sport of a cultivator presents a new, desirable chemical composition, is it possible to preserve this composition by cloning? Lebot and Lévesque's identification of a number of kava chemotype groups also provides additional insights into the pre history of distribution of the plant. Their findings showed that chemotypes are genetically controlled and therefore constitute a genetic fingerprint for each cultivar, and that species domestication involved preservation of selected chemotypes by cloning.

Lebot and Lévesque divided the active principles into 2 main groups-major and minor kavalactones-and demonstrated that the former for approximately 96% of the lipid extract. They therefore numbered and only used the major kavalactones (1 = demethoxy-yangonin, DMY; 2 = dihydrokavain, DHK; 3 = yangonin, y; 4 = kavain, k; 5 = dihydromethystic, DHM; and 6 = methysticin M) to define cultivar chemotypes. These 6 active substances comprise a natural "cocktail" that induces different physiological effects according to the particular kavalactone mixture. To identify the different mixtures offered by various cultivars, chemical compositions were coded by listing in decreasing order of proportion the 6 major kavalactones in the extract; this coded description is called a chemotype. For example, if the chemotype of a cultivar is 521364, this indicates that kavalactone number 5 (DHM) has the highest content of the 6 lactones in that cultivar, kavalactone number 2 (DHK) has the second highest content, and so on. Chemotype 521634 produced distinct physiological effects that differ from those of the other chemotypes. The first 3 kavalactones in the code usually represent 70% of the total. These 3, therefore, are typically the most important for characterizing the chemotype. In some cultivars, the percentage of each of the 3 major kavalactones is about the same.

Pharmacodynamics

Effects of kavalactones include mild sedation, a slight numbing of the gums and mouth, and vivid dreams. Kava has been reported to improve cognitive performance and promote a cheerful mood. Kava has similar effects to benzodiazepine medications, including muscle relaxant, anaesthetic, anticonvulsive and anxiolytic effects. They are thought to result from direct interactions of kavalactones with voltage-gated ion channels. Research currently suggests kavalactones potentiate GABAA activity, but do not alter levels of dopamine and serotonin in the CNS. It is thought to do this via modulating GABA activity via altering the lipid membrane structure and sodium channel function. However, it has also been shown that administration of the GABA antagonist Flumazenil does not have an antagonistic effect on kavalactones, suggesting that an alternative pathway may be involved. Heavy, long-term kava use does not cause any reduction of ability in saccade and cognitive tests, but is associated with elevated liver enzymes.

Desmethoxyyangonin, one of the six major kavalactones, is a reversible MAO-B inhibitor (Ki 280 nM) and is able to increase dopamine levels in the nucleus accumbens. This finding might correspond to the slightly euphoric action of kava.

Kavain, in both enantiomeric forms, inhibits the reuptake of noradrenalin at the transporter (NAT), but not of serotonin. An elevated extracellular noradrenalin level in the brain may account for the reported enhancement of attention and focus.

Effects

A moderately potent kava drink causes effects within 10–20 minutes that last for about two and a half hours, but can be felt for up to eight hours. Some report longer-term effects up to two days after ingestion, including a feeling of mental clarity, patience, and an ease of acceptance. The effects of kava are most often compared to alcohol, or benzodiazepines.

The sensations, in order of appearance, are slight tongue and lip numbing, mildly talkative and sociable behavior, clear thinking, calmness, relaxed muscles, and a sense of well-being. The numbing of the mouth is caused by the two kavalactones kavain and dihydrokavain, which cause the contraction of the blood vessels in these areas, acting as a local topical anesthetic.

The effects of a kava drink vary widely with the particular chemotype of kava plant and amount. A potent drink results in a faster onset with a lack of stimulation; the user's eyes become more sensitive, the person soon becomes somnolent. Sleep is often restful and pronounced periods of sleepiness correlate to the amount and potency of kava consumed. Many people reportedly experience deep sleep and rather vivid dreams after drinking moderate amounts of kava.

side effects

Side effects include, but are not limited to, loss of motor control, nausea, pupil dilation and tiredness. Do not operate a motor vehicle while under the influence, and some drugs could interact such as, both prescription and nonprescription – including, but not limited to, anticonvulsants, alcohol, antianxiety medications (CNS depressants such as benzodiazepines), antipsychotic medications, levodopa, diuretics, and drugs metabolized by the liver.

Kava in traditional pharmacopoeia and medicine

Condition	Medical treatment
Inflammation of the urogenital	Drinking macerated stump and young kava shoots
Gonorrhea and chronic cystitis	Drinking prepared kava
Difficulties in urinating	Drinking macerated stump
Female puberty syndromes	Drinking masticated kava
Menstrual dysmenorrhea	Drinking kava
Vaginal prolapsus	Application of macerated kava
Provoke an abortion	Kava leaves in vagina
Menstrual migraine	Drinking masticated kava
Headaches	Masticated root tissues, eaten or drunk as infusion
General weakness	Drinking of masticated, macerated kava diluted in water and boiled
Chills	Drinking macerated kava; fumigation with the leaves
Sleeping problems	Drinking of masticated, macerated kava diluted in water and boiled
General treatment of diseases	Fumigation of the leaves
To prevent infection	Drinking masticated kava
Rheumatism	Drinking of macerated stump
Weight gain	Drinking of macerated stump
Gastrointestinal upsets	Drinking of macerated stump mixed with other medicinal plants
Repository tract irritation	Drinking of macerated stump
Asthma	Drinking of macerated stump
Pulmonary pains	Drinking masticated kava
Tuberculosis	Drinking juice extracted from the stump
Leprosy	External application of masticated stump
Skin diseases	Application of masticated stump in a poultice
Certain skin diseases	Kava cure to cause desquamations, New healthy skin is formed
To prevent suppuration	Application of masticated stump in a poultice
To calm nervous children	Drinking of kava prepared from the nene variety

Recent research indicates that the chemical properties of kavalactones in the rootstock of kava and alkaloids in the leaves may explain much of its usefulness in traditional medicine, although not all its applications can be accounted for scientifically (e.g, those for menstrual ailments). For example, the bactericidal or bacteriostatic activity of kavalactones underlies kava's reputation as a remedy for urogenital infections. It's traditional perceived analgesic properties make it a common remedy for various aches and pains. It's diuretic effects may relieve symptoms of gonorrhea. Traditional uses of the plant as a contraceptive, abortifacient, or stimulant remain to be scientifically verified and explained, perhaps by research to identify physiological active compounds other then kavalactones. Some reliance on kava within folk medicinal systems no doubt reflects its symbolic rather than chemical attributes. Use of kava to induce women's beast milk flow, for example, May relate to the general symbolic appreciation of kava as a fertile fluid.

Traditional medicinal uses by region

New Guinea

In Irian Jaya, the internal part of P. Methysticin bark is used for toothache. In Papa New Guinea, scrapped bark and masticated roots are used to relieve sore throats, and the juice from the leaves is used to treat cuts and is imbibed as a general tonic. Women drink fresh masticated as an anesthetic when they are being tattooed. Women in some areas of this country also reportedly drink large quantities when they are pregnant, especially just before delivery, to stimulate milk production.

Vanuatu

The soporific properties of kava have been known in Vanuatu for many generations. Garanger provides some remarkable evidence of this. Archeological excavation of the burial site of Roy Mata, a chief who reigned over the Shephard Islands and Efate in the 13th century, uncovered male skeletons in positions suggesting they had been buried alive in a peaceful state of mind, whereas the position of associated female skeletons suggests they put up a struggle. According to oral tradition, the men interred alive were under the influence of kava but their wives were not allowed the soporific portion.

Today on Mota Lava, in the Banks Islands of Vanuatu, Kava is used in a drink tho treat constipation. It is also used to treat conjunctivitis: the eyes are washed with water mixed with juice squeezed from the leaves. In Melsisi, on Pentecost, juice expressed from kava leaves is dropped into ears to treat ear ache.A. Walter noted a similar use of kava in Vansemakul, another apma - speaking village in the same area. Also on Pentecost, a plaster made from heated and pounded kava leaves is applied to the abdomen to relieve an upset stomach. For feverish coughing, a handful of bark is ground up in a small amount of water, which the patient drinks in small doses. To relieve sickness characterized by fever followed by asthenia, sufferers drink half a glass of juice extracted from the kava leaves. To burst a boil, people grind kava leaves and heat them over the fire. The warm leaves are then pressed, and the juice obtained is applied to the boil, which is also covered with pulverized kava leaves and held in place with another leaf. For headaches, hot leaves are placed on the head. A sickness known in the Apma region bears a generic name of kava (sini); symptoms include swollen legs followed by fever. Sini is treated by bathing with a maceration of 4 leaves from the sini bo cultivar ground in a bowl of water. A poultice made from four sini bo leaves heated in the fire is also applied to swollen legs associated with a similar illness.

On Tongoa, to treat general indisposition and lack of energy, juice is extracted from ground kava leaves, mixed in cold water, and applied by massage of the body.

On Erromango,a complex preparation containing kava is reputed to act against not asthma and tuberculosis. The ingredients of the asthma remedy include leaves of Compositae (Crassocephalum crepidioides), locally referred to as sarndoo; a Papilionaceae (Arbus precatorius) called tamsi; 2 cultivars of Musceae (Heliconia indica, var. Indica), mevong and mevong netukus; and kava, called naghave (or nagave according to Lynch). These leaves are pressed and the juice extracted and drink. The sick person is restricted a salt free diet (no sea water) throughout coarse of treatment. This medicine is not administered to pregnant or menstruating women. On Tanna, however, juiceextracted from the leaves of kava and a Cyperaceae species (Fimbristylis cymosa) is given to pregnant women who are approaching their delivery date, "when the baby has to turn round," to be sure it presents itself favorably for birth.

There are Erromango tales of kava syndrome called naghave, attributed to sorcery performed with various leaves. The symptoms of the illness are blurred vision and dizziness those of an overdose of kava (these symptoms simply be from jaundice).

Fiji

In the early part this century, Rougier recorded several medicinal uses of kava in Fiji. For example, a sickness characterized by a pain inside the head and both ears associated with "blurred vision" that "sometimes disappears at high tide, and in other cases sunset," was treated various remedies, one of which contained leaves of Ipomea peltata and kava. Rougier also reported that "the best sedative drug is a draught prepared by scraping and pounding the kava root," and that "there were various means of contraception, one of which was masticating and swallowing kava leaves."