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Kava-Kava (Piper Methysticum)


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Kava-Kava (Piper Methysticum)


Kava-Kava is a plant from the Western Pacific also known as Piper methysticum, which means 'intoxicating pepper'. The effects of kava-kava can be relaxing, sedating, and euphoric. Kava-kava contains kavalactrones, the psychoactive substance responsible for these effects. They interact with the GABAA receptor, as is the case with Alcohol and GHB.



Introduction to Kava-Kava


Kava-Kava comes from the plant Piper methysticum, which means 'intoxicating pepper'. ..................Kava-kava was the 25th most used herbal medicine in the world in 2002. Reports of liver toxicity of kava-kava may have led to a decline in use in recent years. (US National Institute of Health, 2003) ......


Using Kava-Kava


Traditionally, kava-kava root is ground up and soaked in water. The water extracts kavalactones from the kava-kava..............Kavalactones are chemically considered a-pyrones.



It's thought that the active kavalactones found in kava-kava include dihydrokawain, kawain, dihydromethysticin, methysticin, dihydroyangonin, and yangonin. The complete pharmacology of kavalactones is still being characterized and it's speculated that complex interactions may be seen when kava-kava is combined with other drugs. (Schelosky, 1995)


Ways of administration


Kava-kava is traditionally taken orally as a cold water-extracted tea, but pill form of kava-kava is available. Extracts of kava-kava are also widely sold.

Effects of Kava-Kava


Kava-kava is primarily known for it's anti-anxiety effects and has been used as a social lubricant among indigenous populations for centuries. (Pittler, 2000)


Kava-kava acts on neuronal voltage-dependent ion channels to decrease neuron firing. This action on neurons leads to kava-kava having anti-anxiety, muscle relaxant, anti-convulsant, and anesthetic properties.


Upon drinking a kava-kava tea, many people report a numbing effect on the mouth and throat. This effect has led to kava-kava being used for the treatment of sore-throats.

Combinations with Kava-Kava


Due to the complex pharmacological profile of the kavalactones, it is not recommended to combine kava-kava with other drugs. The kavalactones are primarily metabolized by the cytochrome P450 isozyme 2D6. Other drugs that are metabolized by the CYP 2D6 isozyme may interfere with the metabolism of kava-kava leading to possibly detrimental effects. ..................



The dangers of Kava-Kava


When parts of the plant other than the root is taken, kava-kava can create potentially fatal damage to the liver. Extracts of kava-kava made with acetone or ethanol also seem to increase the likelihood of liver damaging effects. (Ernst, 2007)


Kava-kava also contains some kavalactones which are known MAOI's, or more specifically MAO-B inhibitors. The MAOI activity is relatively weak, but users should be aware of it. Kava-kava combined with drugs which increase synaptic serotonin do pose a potential risk for serotonin syndrome, a potentially fatal condition requiring immediate medical attention. ..............



Legal status of Kava-Kava


Kava-kava is legal in many places, but may be regulated in others.

Kava-kava and kava-kava containing products are banned in Canada, France, Netherlands, and other places.


The UK and Australia both have restrictions on the sale, importation, and use of kava-kava.


One should check the laws in their locality regarding kava-kava........


.....In more recent years, use of kava-kava has expanded to the general population. The drink made from kava-kava is now widespread in many areas of the pacific islands and replaces alcohol consumption in some localities. This has caused some legal trouble for kava users, as liquor industries have fought to make kava-kava illegal. The use of kava-kava as a replacement inebriant for alcohol cuts into the profits of liquor merchants.


In other places, such as Vanuatu, kava bars have opened and the drink is served commercially in much the same way a typical bar serves alcohol.


One should note here that the traditional preparation of kava-kava, by using only the roots and soaking them in water, eliminates the potential risk of liver damage from the use of kava-kava.





What Are the Dangers of Kava Kava?


Kava kava is an herb used for its sedating and muscle-relaxing properties. It is often marketed as a natural remedy for insomnia, anxiety and some types of muscle pain and has been used in the Pacific Islands as an alcohol-like drink for centuries. Despite its natural origins, kava can cause dangerous side effects in some instances. Understanding the dangers of kava kava can help consumers weigh the risks and benefits of the supplement before using it.


Cognitive Impairment


Kava's main effects involve the central nervous system and include sedation, slowed cognitive functioning and mental relaxation. While these effects can be desirable in someone with anxiety or insomnia, they can be dangerous when performing potentially hazardous tasks like driving. Dizziness, drowsiness and loss of coordination are relatively common side effects of kava.


According to RxList, citations have been issued to people whose driving abilities were impaired by drinking kava tea. Do not drive or engage in other potentially dangerous activities while under the influence of kava. Taking kava close to bedtime may help minimize the risks associated with cognitive impairment.


Liver Damage


Liver damage is among the most serious adverse effects associated with kava. According to the Centers for Disease Control, people in several countries have experienced liver failure while taking kava supplements. As a result, Canada, Switzerland, Germany and several other countries have banned the sale of kava until more is known about its effects on the liver. While liver damage is considered a rare side effect, consumers should be aware of the possibility when using kava. Avoid taking kava with substances like acetaminophen or alcohol, and only buy brands that bear the U.S. Pharmacopeia safety seal.


Drug Interactions


Like other supplements, kava can cause dangerous interactions when taken with some herbs and medications . Mixing kava with alcohol, opiates or benzodiazepines can magnify their depressant effects, leading to an increased risk for cardiac arrest, respiratory depression and death. Kava may also decrease the effectiveness of levodopa, a drug used to treat Parkinson's disease. Other potential interactions include anti-convulsants, phenothiazines and some antipsychotic drugs.




While rare, kava overdose can be extremely dangerous. According to eMedTV, symptoms of overdose include body spasms, red eyes, dry mouth and signs of liver damage, such as yellowing of the skin or eyes. If you suspect an overdose, seek immediate medical attention to avoid serious health consequences.






Science News


Kava Linked To Liver Damage, New Evidence Shows


ScienceDaily (Feb. 23, 2008) — Scientists have found new evidence, using innovative techniques, to support the growing body of literature that indicates kava may have a negative effect on the liver. Kava is a plant native to the South Pacific. ....................... In recent years, serious concerns about the dangers of kava and the effects on the liver have resulted in regulatory agencies, such as the US Food and Drug Administration and Australia's Therapeutic Goods Administration, banning or restricting the sale of kava and kava products.


Originally from Fiji, where kava drinking is common, Professor Iqbal Ramzan, Dean of Pharmacy at the University of Sydney, Australia, had previously published articles on the adverse effects of kava, and wanted to investigate further the effects kava had on the liver.


Leading a team of researchers from the University of Sydney, Professor Ramzan spent one year investigating the cellular effects of kava on the liver. Kava has been used in ceremonies and for recreational and social purposes in the South Pacific since ancient times, much like alcohol, tea or coffee is in other societies today.


In the 1980s other medicinal uses for kava began to emerge and it was marketed in herbal form as a natural way to treat conditions such as anxiety, insomnia, tension and restlessness, particularly in Europe and North America.


More recently, evidence began to emerge about the adverse affect kava could have on the liver.


To test these theories, the University of Sydney study focused on the major kavalactone (the ingredient in kava believed to affect the liver) -- kavain -- and investigated the effects it had on the ultrastructure (or biological structure) of the liver.


This required the use of electron microscopes (which enable the examination of the interior of cells) provided by the Australian Key Centre for Microscopy and Microanalysis at the University of Sydney under the direction of its Deputy Director, Professor Filip Braet.


The study found that following kavain treatment the liver tissue displayed an overall change in structure, including the narrowing of blood vessels, the constriction of blood vessel passages and the retraction of the cellular lining.


Interestingly, kavain also adversely affected certain cells which function in the destruction of foreign antigens (such as bacteria and viruses), which make up part of the body's immune system.


In other words, the kavain treatment disturbed the basic structure of the liver, consequently seriously impacting the normal functioning of the liver.


The results of the University of Sydney's study clearly support earlier literature observations on kava's adverse affects on the functioning of the liver in general.


However, additional investigations into the effects of other major kavalactones on the liver, as well as studies on whether the effects of kava are reversible, are urgently needed.


Journal reference: Fu S, Korkmaz E, Braet F, Ngo Q, Ramzan I. Influence of kavain on hepatic ultrastructure. World J Gastroenterol 2008 January 28; 14(4): 541-546 http://www.wjgnet.com/1007-9327/14/541.aps







Kava Kava Knocked By FDA


Kava kava has been much advertised as a sedative, muscle relaxant and diuretic and, in recent years, has become very popular. It is sold without a prescription. Some while ago MedicineNet carried a couple of stories about the dangers of kava kava. One story was titled Kava Kava - Herb Hurts Liver. The other was called Rhubarb - Over Kava Kava Alert.


To my mind, medicinal herbs such as kava kava should be regulated by the FDA just like prescription drugs in the US. It is impossible for anyone to remember all the different health warnings about different herbs. Why not have the FDA protect us from adverse herb effects?


Frederick Hecht, MD, FAAP

Associate Chief Medical Editor, MedicineNet.com







March 27, 2002 - The Food and Drug Administration (FDA) is advising consumers of the potential risk of severe liver injury associated with the use of kava-containing dietary supplements. Kava (Piper methysticum) is a plant indigenous to the islands in the South Pacific where it is commonly used to prepare a traditional beverage. Supplements containing the herbal ingredient kava are promoted for relaxation (e.g., to relieve stress, anxiety, and tension), sleeplessness, menopausal symptoms and other uses. FDA has not made a determination about the ability of kava dietary supplements to provide such benefits.


Liver-related risks associated with the use of kava have prompted regulatory agencies in other countries, including those in Germany, Switzerland, France, Canada, and the United Kingdom, to take action ranging from warning consumers about the potential risks of kava use to removing kava-containing products from the marketplace. Although liver damage appears to be rare, FDA believes consumers should be informed of this potential risk.


Kava-containing products have been associated with liver-related injuries - including hepatitis, cirrhosis, and liver failure -- in over 25 reports of adverse events in other countries. Four patients required liver transplants. In the U.S., FDA has received a report of a previously healthy young female who required liver transplantation, as well as several reports of liver-related injuries.


Given these reports, persons who have liver disease or liver problems, or persons who are taking drug products that can affect the liver, should consult a physician before using kava-containing supplements.


Consumers who use a kava-containing dietary supplement and who experience signs of illness associated with liver disease should also consult their physician. Symptoms of serious liver disease include jaundice (yellowing of the skin or whites of the eyes) and brown urine. Non-specific symptoms of liver disease can include nausea, vomiting, light-colored stools, unusual tiredness, weakness, stomach or abdominal pain, and loss of appetite.[/i]


FDA urges consumers and their health care professionals to report any cases of liver and other injuries that may be related to the use of kava-containing dietary supplements. Adverse events associated with the use of dietary supplements should be reported as soon as possible to FDA's MedWatch program by calling their toll-free number (1-800-332-1088) or through the Internet (http://www.fda.gov/medwatch).


The presence of kava in a supplement should be identified on the product label in the "Supplement Facts" box. The following are commonly used names for kava:



ava pepper


intoxicating pepper


kava kava

kava pepper

kava root



kawa kawa



Piper methysticum

Piper methysticum Forst.f.

Piper methysticum G. Forst.







FDA will continue to investigate the relationship, if any, between the use of dietary supplements containing kava and liver injury. The agency's investigation includes attempting to determine a biological explanation for the relationship and to identify the different sources of kava in the U.S. and Europe. The agency will alert consumers, and if warranted, take additional action as more information becomes available.


(Source: http://www.cfsan.fda.gov/)

Last Editorial Review: 3/27/200





Pharmacopsychiatry. 1998 Sep;31(5):187-92.


Inhibition of platelet MAO-B by kava pyrone-enriched extract from Piper methysticum Forster (kava-kava).


Uebelhack R, Franke L, Schewe HJ.


Department of Psychiatry, Humboldt-Universität zu Berlin (Charité), Germany.




Kava-kava, a psychoactive beverage, induces relaxation, improves social interaction, promotes sleep and plays an important role in the sociocultural life in the islands of the South Pacific. On the other hand, standardized extracts of kava-kava roots are used for the therapy of anxiety, tension and restlessness. Kava pyrones, the major constituents of kava kava, are generally considered to be responsible for the pharmacological activity in humans and animals. To obtain more information on the mechanisms by which kava-kava exerts psychotropic properties we investigated the in vitro effects of kava-kava extract and pure synthetic kava pyrones on human platelet MAO-B, in comparison to amitriptyline, imipramine and brofaromine.


Kava-kava extract was found to be a reversible inhibitor of MAO-B in intact platelets (IC50 24 microM) and disrupted platelet homogenates (IC50 1.2 microM). Structural differences of kava pyrones resulted in a different potency of MAO-B inhibition. The order of potency was desmethoxyyangonin > (+/-)-methysticin > yangonin > (+/-)-dihydromethysticin > (+/-)- dihydrokavain > (+/-)-kavain. The two most potent kava pyrones, desmethoxyyangonin and (+/-)-methysticin displayed a competetive inhibition pattern with mean Ki 0.28 microM and 1.14 microM respectively. The inhibition of MAO-B by kava pyrone-enriched extracts might be an important mechanism for their psychotropic activity.




[PubMed - indexed for MEDLINE]

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  • 1 year later...

I slept 8 hours straight last night!!! And had zero AM anxiety. For the first time since July, when, on vacation, I slept normally for a couple of weeks and had no anxiety.


Part of it could be that I just went through a period of stress and anxiety because of a job offer, and yesterday I declined the job. But it could also be that I had a cup of Yogi Stress Relief tea that has kava extract in it. I'm leary of trying it again, but I thought the effects were interesting.


I didn't drink it specifically to sleep well... I was at a friend's house and we were going to have tea and I asked that it not have caffeine and not have valerian. She said she had some calming tea, and though I was a bit afraid, since I avoid all those things for fear of paradoxical reactions, I thought I'd try it since I was a mess already anyway. I had a small cup made with one tea bag for three cups of tea.


I felt the effect within minutes of drinking the tea. I felt cool and collected, but aware and in control. Almost everything I've taken before to "calm down", such as valerian, xanax, clonazepam, antihistamines, etc., made me feel fuzzy-headed and like it was drugging me but not getting at the source of the anxiety. For example, antihistamines could sometimes help me sleep in the morning, but the anxiety was just as present as ever, trying to burst through through my dreams. Like it affected my front brain, but not the deeper part where the exaggerated alerting was coming from. (There is only one benzodiazepine that I've tried that really worked, but can't recall the name now. I'm curious to know the mechanism of action, as maybe it holds clues to what is going on in my brain.)


The kava, on the other hand, really felt like it hit the source of the anxiety itself. And then I slept 8 hours! (I went to bed about 2 and a half hours after drinking the tea). Maybe it's because I was exhausted anyway, but it's so rare for me to be able to sleep like that no matter how exhausted I am.


I don't feel great this morning... feel a bit strange, like my sense of self is off and I don't feel centered, but I've felt that the past few days anyway. Part of not feeling great could also be because I was so excited to be able to sleep, that even after the 8 hours I stayed in bed for two more dozing. I think I overdid it.


What have other people's experiences been with kava kava? I might reserve it for emergency use!

'94-'08 On/off ADs. Mostly Zoloft & Wellbutrin, but also Prozac, Celexa, Effexor, etc.
6/08 quit Z & W after tapering, awful anxiety 3 mos. later, reinstated.
11/10 CTed. Severe anxiety 3 mos. later & @ 8 mos. much worse (set off by metronidazole). Anxiety, depression, anhedonia, DP, DR, dizziness, severe insomnia, high serum AM cortisol, flu-like feelings, muscle discomfort.
9/11-9/12 Waves and windows of recovery.
10/12 Awful relapse, DP/DR. Hydrocortisone?
11/12 Improved fairly quickly even though relapse was one of worst waves ever.

1/13 Best I've ever felt.

3/13 A bit of a relapse... then faster and shorter waves and windows.

4/14 Have to watch out for triggers, but feel completely normal about 80% of the time.

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I've had a few very good responses (internal calm but not sedated) to Kava Kava and several nonresponses. This was years ago using capsules from different sources. I never used it regularly.


I know people who get fresh Kava Kava from the Pacific Northwest. I havent checked into it.


Glad to hear you had a good night of sleep. I look forward to input from others.

Pristiq tapered over 8 months ending Spring 2011 after 18 years of polydrugging that began w/Zoloft for fatigue/general malaise (not mood). CURRENT: 1mg Klonopin qhs (SSRI bruxism), 75mg trazodone qhs, various hormonesLitigation for 11 years for Work-related injury, settled 2004. Involuntary medical retirement in 2001 (age 39). 2012 - brain MRI showing diffuse, chronic cerebrovascular damage/demyelination possibly vasculitis/cerebritis. Dx w/autoimmune polyendocrine failure.<p>2013 - Dx w/CNS Sjogren's Lupus (FANA antibodies first appeared in 1997 but missed by doc).

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I have friends (never had withdrawal syndrome) who swear by kava-kava.

This is not medical advice. Discuss any decisions about your medical care with a knowledgeable medical practitioner.

"It has become appallingly obvious that our technology has surpassed our humanity." -- Albert Einstein

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OK, nevermind. I had one of my worst nights ever last night, with terrible anxiety, random bombardment of memories this morning. Not sure if it has anything to do with having taken the kava tea the other night, but it's enough to scare me away.

'94-'08 On/off ADs. Mostly Zoloft & Wellbutrin, but also Prozac, Celexa, Effexor, etc.
6/08 quit Z & W after tapering, awful anxiety 3 mos. later, reinstated.
11/10 CTed. Severe anxiety 3 mos. later & @ 8 mos. much worse (set off by metronidazole). Anxiety, depression, anhedonia, DP, DR, dizziness, severe insomnia, high serum AM cortisol, flu-like feelings, muscle discomfort.
9/11-9/12 Waves and windows of recovery.
10/12 Awful relapse, DP/DR. Hydrocortisone?
11/12 Improved fairly quickly even though relapse was one of worst waves ever.

1/13 Best I've ever felt.

3/13 A bit of a relapse... then faster and shorter waves and windows.

4/14 Have to watch out for triggers, but feel completely normal about 80% of the time.

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