The Kavalactones Of Kava Kava (Plant Adaptogens)

The Kavalactones Of Kava Kava (Plant Adaptogens)


Drug (noun): a drug is any chemical substance that causes a change in an organism’s physiology or psychology when consumed. Drugs are typically distinguished from food and substances that provide nutritional support.


Plant Medicine (noun): a type of medicine that uses roots, stems, leaves, flowers, or seeds of plants to improve health, prevent disease, and treat illness. Herbal medicine is the study of pharmacognosy and the use of medicinal plants, which are a basis of traditional medicine. There is generally limited scientific evidence for the safety and efficacy of plants used in 21st century herbalism, due to a lack of standardisation for purity and dosage.



What Is Kava Kava?

While ‘The Kavalactones of Kava Kava’ could be the title of a cosmic science fiction novel, kava has its origins firmly grounded in the earth.

Kava kava (often shorted to ‘kava’) is made from the roots of the Piper methysticum plant – a member of the pepper family that also includes black pepper. It is often processed as a tea, powdered supplement or extract.

Traditionally, people made a paste from the plant’s root and mixed it with water or coconut milk to create a drink; The name has its roots in ‘bitter’, ‘sour’ or ‘acrid’ to the taste. Some sources claim that people native to the South Pacific islands use kava brew during cultural and religious ceremonies to create states of altered consciousness.

For example in Vanuatu, a strong kava drink is normally followed by a hot meal or tea. The meal traditionally follows some time after the drink so the psychoactives are absorbed into the bloodstream quicker. Here, no flavouring is added.

Fijians commonly share a drink called ‘grog’ made by pounding sun-dried kava root into a fine powder, straining and mixing it with cold water. Grog is drunk from the shorn half-shell of a coconut, called a bilo. The brew is especially popular among young men and often brings people together for storytelling and socialising. In this instance, it is typically followed by a chaser or a sweet snack.


Is Kava Legal?

Kava is legal in most countries and is often regulated as a dietary supplement. Whereas medicines are regulated as unsafe until proven safe, dietary supplements are regulated as relatively safe until proven otherwise.

Despite this, the FDA recommend that kava is a supplement that is limited to personal use. This is because it is not GRAS approved (Generally Recognised as Safe), therefore it cannot be added to over the counter foods or beverages as an ingredient.

Moderate consumption of kava in its traditional form (as a water-based suspension of kava roots) has been deemed to present an ‘acceptably low level of health risk’ by the World Health Organisation.


What Is Kava Used For?

In the health and wellness world, kava is being touted as a reliever of stress and anxiety. The most common actions of the extract are relaxation and euphoria, depending on the circumstances of ingestion, whereas higher doses cause sleepiness and skeletal muscle relaxation.

In a randomised controlled trial from 2013, scientists gave 75 people with anxiety disorders either kava extract or a placebo drug over 6 weeks. At the end of the study, they found that kava had a small but significant effect on reducing anxiety symptoms. Aside from headaches, the participants did not report liver problems or other side effects.

Kava’s relaxing effects are similar to alcohol, lending it to related recreational and anxiolytic uses. This is due to the kavalactones it contains – although the exact mechanisms are unknown, these demonstrate indirect effects on GABA and benzodiazepine receptors, as well as stimulation of the limbic system, and an ability to antagonise clonic strychnine convulsions.

Kava extract also contains kavapyrones, which have well-known psychotropic properties (affecting one’s mental state). There is some evidence that the relaxing and slightly euphoric actions may be caused by the activation of the mesolimbic dopaminergic neurones; With changes to the activity of 5-HT neurones providing the sleep-inducing action.


Dosing and Side-effects

Kava’s effects on dopamine and serotonin receptors have been inconsistent, but some activity has been noted, including an increase in parkinson-like symptoms in recipients taking high-dose kava.

There are no standard dosing guidelines, and peritoneal administration of aqueous extracts of kava has led to tolerance in animal models, suggesting that higher doses are required over time in order to achieve the same effects. Despite this, there is no evidence that people who regularly use kava become physiologically dependent on the drug, and are unlikely to experience withdrawal symptoms.

When injected straight into the abdomen in various animal studies, a ‘small dose’ is considered to be around 20mg/kg body weight, with ‘higher doses’ being set at 120 mg/kg body weight. Some research suggests that the optimum dose may be under 250mg of kava per day – but bioavailability will also depend on preparation and processing.

Like many other plant medicines that are processed by the liver, research suggests that continuous high doses can be hepatotoxic, meaning that it can damage liver cells. This has brought kava products under scrutiny and there have been over 100 reports of spontaneous adverse hepatic effects. However alcohol is often co-ingested in kava hepatotoxicity cases.

Many mechanisms have been postulated to explain the unexpected toxicity, one being pharmacokinetic interactions between kavalactones and co-administered drugs involving the cytochrome P450 enzyme system. Anything that affects this enzyme in the liver (including alcohol and grapefruit juice) affects metabolic rate, leading to higher or lower levels of the substance in the blood, possibly leading to an ‘over-dose’.

Adverse effects are also dependent on the quality of the product. In recent years, government regulatory bodies and non-profit NGOs have been set up with the declared aim of monitoring kava quality, producing regular reports, certifying vendors selling proper kava cultivars, and warning customers against products that may contain other varieties.

review from 2011 reported that while kava may show some evidence of improving stress and anxiety, more research about the safety and effectiveness is needed before it becomes a recommended therapy. kava can also interact with several other drugs, such as benzodiazepines and anti-depressants. For this reason, it is important to consult a doctor before making the decision to integrate it into your routine.


Kava Preparation

Scholars make a distinction between the so-called ‘noble’ and non-noble Kava cultivars. The latter category comprises the ‘tudei’ (or ‘two-day’) kavas, medicinal kavas, and wild kava (Piper wichmanii, the ancestor of domesticated Piper methysticum.)

Traditionally, only noble kavas have been used for regular consumption, due to their more favourable composition of kavalactones and other compounds that produce more pleasant effects and have lower potential for causing negative side-effects, such as nausea or ‘kava hangover‘ and tolerance.

More recently, it has also been suggested that the widespread use of tudei cultivars in the manufacturing of several kava products might have been the key factor contributing to the rare reports of adverse reactions to kava observed among the consumers of kava-based products in Europe.

The concerns about the adverse effects of non-noble varieties, produced by their undesirable composition of kavalactones and high concentrations of potentially harmful compounds (flavokavains), which are not present in any significant concentration in the noble varieties, has led to legislation prohibiting exports from countries such as Vanuatu.

Kava root is generally made into a paste and mixed with water or boiled into a tea. It is also possible to buy pre-made Kava tea from some stores. The plant can come in a liquid extract form to be mixed with other drinks for taste, and there are also tablets and capsules of powdered kava available.

In the pharmaceutical and herbal supplement markets, kavalactones may extracted from the kava plant using solvents such as supercritical CO2, acetone, and ethanol to produce pills standardised with between 30-90% kavalactones.

There are some concerns about some of these modern extraction methods, for instance, when compared with water extraction, organic solvents extract vastly larger amounts of flavokavains – compounds associated with adverse reactions to kava that are present in very low concentrations in noble kava, but significant in non-noble.

When choosing how to prepare kava, you may want to consider what you find easiest to measure and dose, as well as how small amounts have varying effects on your personal biochemistry – depending on the format and route of administration. It is also generally advised not to ‘mix medicines’.

While kava is showing promise in placebo-controlled studies as having some effect on the treatment of anxiety, stress, mood and insomnia, medicines can only do so much if the root causes are also linked to lifestyle and environmental factors that need to change in tandem.