Kratom |
| Kratom | |||||||||||||||||||||||||||
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| Chemical Nomenclature | |||||||||||||||||||||||||||
| Common names | Mitragyna speciosa, กระท่อม (Thai), ketum, kratom or kratum | ||||||||||||||||||||||||||
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| Psychoactive class | Depressant | ||||||||||||||||||||||||||
| Chemical class | Indole alkaloid | ||||||||||||||||||||||||||
| Routes of Administration | |||||||||||||||||||||||||||
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| Summary sheet: Kratom |
Kratom, or Mitragyna speciosa, is a tree from Indonesia that produces psychoactive leaves. The leaf of the kratom tree is known to produce a full spectrum of typical opioid effects which can range from stimulation to sedation, and even both. It is commonly used as a substitute for pain medication, easing sleep and recreational usage.
There are a variety of strains of kratom; some of which have a much stronger opioid characteristic, causing sedation, while others are considered similar to a pleasant caffeine stimulation. As a general rule, kratom is more stimulating at lower doses, but becomes more sedating as the dosage is increased.
Kratom has a long history of human usage and is legal in many countries. It is commonly sold online and is also available within certain head shops and gas stations.
Contents
Chemistry
There are more than 40 compounds in M. speciosa leaves,[1] including many indole alkaloids such as mitragynine (once thought to be the primary active constituent), mitraphylline, and 7-hydroxymitragynine (which is currently the most likely candidate for the primary active chemical in the plant).[2][3] Other active chemicals in M. speciosa include raubasine, rhynchophylline and corynantheidine among many others.[4]
The amount of active chemicals within the leaves depends highly on many factors. One major factor is the location of the tree. When trees are grown in Southeast Asia, the levels tend to be higher but when grown elsewhere (even in greenhouses) the levels tend to be low or non-existent.[5] One analysis of products marketed as kratom leaf found mitragynine at levels of 1–6% and 7-hydroxymirtrogynine at levels of 0.01–0.04%.[6]
Pharmacology
Kratom behaves as an opioid receptor agonist similar in function to morphine and other opiates, although its pharmacological action and subjective effects differ significantly from those of traditional opiates.[7]
Opioids exert their effects by binding to and activating the opioid receptors. They structurally mimic endogenous endorphins which are naturally found within the body and also work upon the opioid receptor system. The way in which opioids structurally mimic these natural endorphins results in their euphoria, pain relief and anxiolytic effects. This is because endorphins are responsible for reducing pain, causing sedation, and feelings of pleasure. They can be released in response to pain, strenuous exercise, orgasm, or general excitement.
One of the primary pharmacological differences between kratom and traditional opiates is that at lower dosages, mitragynine alkaloids preferentially bind to delta opioid receptors, while opiates such as morphine and heroin preferentially bind to μ-opioid receptors.
At higher doses, however, mitragynine increasingly acts upon μ-opioid in a similar manner to traditional opioids. This is speculated to be one of the reasons that kratom has a stimulating effect at lower doses and sedating effects at higher doses.[8] Unlike most other opioids, kratom also presents affinity for the κ-opioid[9], norepinephrine and serotonin[10] receptor systems where it functions as an agonist. Its action on norepinephrine and serotonin also likely contributes to kratom's stimulating properties.
Alongside of this, kratom also contains alkaloids (rhynchophylline and mitraphylline) which function as NMDA receptor antagonists.[11] This may be responsible for the mild dissociating effects which occur at heavy doses.
Subjective effects
The effects listed below are based upon the subjective effects index and personal experiences of PsychonautWiki contributors. The listed effects will rarely (if ever) occur all at once, but heavier dosages will increase the chances and are more likely to induce a full range of effects.
Physical effects
- Stimulation and/or Sedation - An aspect of kratom that one may experience is the change from stimulating to sedating qualities as the dosage increases. Depending on the strain, the sedating and stimulating effects may occur simultaneously in a contradictory manner resulting in the sensation that one is both energized and relaxed. The sedation and stimulation effects may also occur at different times during the experience; a person may feel stimulated during the come up and sedated during the come down. Kratom is considerably more stimulating than that of all other opiates including oxycodone, heroin, or codeine.
- Euphoria - In comparison to other opioids, this particular substance can be considered as less intense in its physical euphoria when compared with that of morphine or heroin. The sensation itself can be described as extreme feelings of intense physical comfort, warmth, love and blissful euphoria.
- Nausea - If the dose is even slightly too high, one may feel quite ill and the nausea can last upwards of two days at the worst. For this reason, a light and healthy diet is recommended in the days prior to consuming higher doses of kratom.
- Pain relief
- Itchiness
- Constipation
- Difficulty urinating
- Pupil constriction
- Cough suppression
- Body odor alteration - Kratom can potentially leave a very distinct and unpleasant odor within one's urine for a small subset of people.
- Decreased libido
Cognitive effects
- Euphoria - In comparison to other opioids, this particular substance can be considered as less intense in its cognitive euphoria when compared with that of morphine or heroin. The sensation itself can be described as powerful and overwhelming feeling of emotional bliss, contentment, and happiness.
- Motivation enhancement
- Thought acceleration
- Anxiety suppression
Visual effects
The visual effects of kratom are unusually strong compared to other opioids of its class. They can be broken down into several components which progressively intensify proportional to dosage.
- Visual acuity suppression
- Double vision
- Visual disconnection - A sense of subtle disconnection from visual input is often experienced with high dosage kratom. This is similar to a low level version of the same effect universally experienced with dissociatives and may well be a result of the NMDA antagonist effects of kratom's active molecules.
- Internal hallucinations - The internal hallucinations of kratom can be described as more solid than psychedelics and do not seem to be composed of visual geometry. The most common way in which they manifest themselves are through hypnagogic scenarios. They are most common during high dosages and can be comprehensively described through their variations as lucid in believability, fixed in style, autonomous in controllability, and equal in new experiences and memory replays in content.
Strains
Similar to cannabis, there are many different strains of Mitragyna speciosa available from vendors. The strains below have varying degrees of depressant, stimulating, and opioid characteristics. The strains are named and identified after the country/region where the Mitragyna speciosa tree originated as well as the colour of the veins of the leaf (red, green, or white).
Below are the general effects and similarities of the various vein colours. Note that the effects vary across all strains and that the effects are dependent on the dose taken. Not all white strains, for example, will produce the same effects and each strain may work differently in one individual than it does on another.
- White Vein: Leaves with a white vein are generally reported to be energetic and stimulating, promoting alertness, motivation, and wakefulness in low to moderate doses.
- Red Vein: Red vein kratom is generally sedating and relaxing, making it a good choice for those with insomnia or pain.
- Green Vein: Green vein strains are a mix of both. They are not as stimulating as white vein nor as sedating as red vein.
Usage
There are several different ways that kratom is typically ingested:[12]
- Traditionally, kratom users in Thailand would commonly chew whole kratom leaves in order to achieve its stimulating and pain-relieving effects during manual labor. However, the amount of leaves needed to be chewed to induce optimal effects is quite high. In addition, kratom leaves are very bitter and few users would find this method bearable.
- Kratom tea is one popular method of consumption. Powdered or crushed kratom leaves are steeped in hot water to extract the alkaloids. Many users choose to place the leaf matter directly into the water without using a tea bag as it ensures that no alkaloids are wasted. Kratom tea is very bitter, so flavorings like honey, peppermint oil, or lemon juice can be added to mask the bitterness.
- Toss and wash is done by placing kratom powder in the back of the mouth, avoiding contact with the taste buds as much as possible, and washing the powder down with a drink. A sweet or acidic drink is typically used to mask the bitter taste of the kratom. Since kratom powder is fairly hydrophobic, it will not always be washed down perfectly with the liquid, which can leave a bitter taste and residual kratom powder in the back of the mouth. This can cause coughing or choking if not done correctly, although most people can perform this without any issues.
- Mixing with olive oil is a method that some users have found particularly helpful using powdered kratom. Kratom dissolves very easily in olive oil, and the lipids in the oil suppress the bitter taste of the kratom. Due to the fact that this method dissolves the majority of the powder, the chances of accidentally inhaling the powder or having it get stuck in the throat are minimal.
- Placing kratom in gelatin capsules is a good ingestion method for avoiding the bitter taste of kratom. Typically, "00" size gelatin or vegetable capsules are filled with kratom powder. This is normally done using a capsule making machine so that many capsules can be made at once. This also makes it easier to pack the powder down into the capsules, allowing around 0.5 grams of powder in each capsule. Some users dislike having to swallow a large amount of capsules when dosing, but this is an effective method for users who cannot tolerate kratom's bitter taste.
Smoking, vaporizing, or insufflating kratom is not seen as a viable means of administration, as the amount of alkaloids needed to produce effects would only be obtained by smoking or snorting an excessive amount of leaf material. In addition, certain kratom alkaloids may be destroyed during the process of combustion.
Potentiation
The effects of kratom can be potentiated using the techniques below.
- Antacids / tums - Taking up to four 750mg antacid tablets approximately 30 - 60 minutes before dosing kratom increases its intensity. This works because antacids raise the pH level in the stomach, which improves the absorption of kratom.[13]
- Tumeric / curcumin and black pepper - A tablespoon or 7 grams of tumeric and a large pinch of black pepper will greatly increase the potency of kratom as well as lengthening its duration if taken approximately 1 hour before ingestion. This works because tumeric functions as an MAOI. Although tumeric is mostly inactive by itself, black pepper increases its bioavailability by 2000% percent.[13]
- Grapefruit juice - Drinking a large glass of grapefruit juice approximately 2 hours before ingesting kratom can greatly potentiate its intensity.[13] This works because grapefruit juice functions as a CYP3A4 enzyme inhibitor which results in altered drug metabolism.[14]
- DXM - Taking 30 - 60 mg of DXM approximately 45 - 60 minutes before ingesting kratom is said to potentiate its effects.
- Watercress - Ingesting watercress approximately 45 minutes before kratom is said to potentiate its effects. This works because watercress functions as a cytochrome P450 CYP2E1 enzyme inhibitor which results in altered drug metabolism.[15]
Toxicity and harm potential
Like most opioids, safe usage of kratom does not cause any dangerous long-term complications. Heavy dosages of kratom can result in respiratory depression, leading onto fatal or dangerous levels of anoxia (oxygen deprivation). This is significantly less powerful than that of morphine or heroin's respiratory depression. It occurs because the breathing reflex is suppressed by agonism of µ-opioid receptors proportional to the dosage consumed. However, this is likely impossible to achieve this using kratom in its standard leaf form as the nausea ceiling makes it difficult to consume high enough dosages without vomiting. A pure extract or tincture however may be potent enough to cause lethal respiratory depression at appropriate dosages, although oral administration of pure mitragynine to mice in dosages up to 920mg/kg did not produce lethal respiratory depression.[16] This can become potentially fatal when kratom is combined with other depressants such as alcohol or benzodiazepines.
Kratom has a low toxicity relative to dose. As with all opioids, long-term effects can vary but can include diminished libido, apathy and memory loss.
It is strongly recommended that one use harm reduction practices when using this drug.
Side effects associated with chronic kratom use include loss of appetite and weight loss, constipation, and darkening of the skin colour of the face. Chronic use has been associated with bowel obstruction.[17][18]
Lethal dosage
The lethal dosage of kratom is unknown but thought to be far above the active dosage. The precise dosage likely depends on a variety of factors including strain, potency, tolerance and method of consumption. It is unlikely that one could ingest a lethal dosage of kratom powder as the nausea will force one to vomit at around 8 - 9 grams; however, it could be possible to ingest a lethal dosage of a kratom if purer forms such as a resin or pure alkaloids are used.
Only three case reports document deaths involving kratom. Other drugs were used in all cases, and in one, kratom was speculated to possibly be the primary cause of death.[19][20][21]
Tolerance and addiction potential
As with other opioids, the chronic use of kratom can be considered moderately addictive with a high potential for abuse and is capable of causing psychological dependence among certain users. When addiction has developed, cravings and withdrawal symptoms may occur if a person suddenly stops their usage.[22]
Tolerance to many of the effects of kratom develops with prolonged and repeated use. The rate at which this occurs develops at different rates for different effects, with tolerance to the constipation-inducing effects developing particularly slowly for instance. This results in users having to administer increasingly large doses to achieve the same effects. After that, it takes about 3 - 7 days for the tolerance to be reduced to half and 1 - 2 weeks to be back at baseline (in the absence of further consumption). kratom presents cross-tolerance with all other opioids, meaning that after the consumption of kratom all opioids will have a reduced effect.
Unlike a lot of other opioid related substances, kratom shows far less dependence and abuse potential. This may also be a result of the "nausea ceiling" most people will discover, to their dismay. If the dose is slightly too high, one may feel quite ill and the nausea can last upwards of two days at the worst.
Legal issues
- Thailand: Possession of kratom leaves is illegal in Thailand, despite the tree being native to the country. The Thai government passed the Kratom Act 2486 which made planting the tree illegal and requires existing trees to be cut down. As of October 2, 2013 the justice ministry of Thailand suggested removal of Kratom from the narcotic drug list relating to Category 5 of the Narcotic Drug Law of 1979, though still recommended regulating kratom in other ways.[24]
- Malaysia: The use of kratom leaves is prohibited in Malaysia under Section 30 (3) Poisons Act 1952 and the user may be penalized with a maximum compound of MYR 10,000 (USD 3,150) or up to 4 years imprisonment.[25]
- United States: Kratom itself is not regulated by the United States federal government, but it is regulated in the states of Tennessee, Vermont, Arkansas, Indiana[26] Iowa,[27] and Wisconsin.
- Latvia: Kratom and its primary active constituent mitragynine are Schedule I controlled substances according to an amendment on August 16th, 2012.[28]
- United Kingdom - It is illegal to produce, supply, or import this drug under the Psychoactive Substance Act, which came into effect on May 26th, 2016.[29]
Preparation methods
Preparation methods for this compound within our tutorial index include:
Experience reports
Anecdotal reports which describe this compound within our experience index include:
See also
External links
References
- ↑ Mitragyna speciosa, a psychoactive tree from Southeast Asia with opioid activity (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/21050173
- ↑ The neuromuscular blockade produced by pure alkaloid, mitragynine and methanol extract of kratom leaves (Mitragyna speciosa Korth (ScienceDirect) | http://www.sciencedirect.com/science/article/pii/S0378874110002102
- ↑ Pharmacology of kratom: an emerging botanical agent with stimulant, analgesic and opioid-like effects (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/23212430
- ↑ Studies on the synthesis and opioid agonistic activities of mitragynine-related indole alkaloids: discovery of opioid agonists structurally different from other opioid ligands (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/11960505
- ↑ Herbal medicines for the management of opioid addiction: safe and effective alternatives to conventional pharmacotherapy? (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/22133323
- ↑ Kikura-Hanajiri, Ruri; Kawamura, Maiko; Maruyama,Takuro;Kitajima, Mariko;
- ↑ Herbal medicines for the management of opioid addiction: safe and effective alternatives to conventional pharmacotherapy? (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/22133323
- ↑ Mitragyna speciosa Korthals - Kratom Usage | www.mitragyna.com/usage
- ↑ Partial agonistic effect of 9-hydroxycorynantheidine on μ-opioid receptor in the guinea-pig ileum | www.sciencedirect.com/science/article/pii/S0024320505010659 / http://sci-hub.cc/10.1016/j.lfs.2005.09.030
- ↑ Central antinociceptive effects of mitragynine in mice: contribution of descending noradrenergic and serotonergic systems (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/8982722 / http://sci-hub.cc/10.1016/S0014-2999(96)00714-5
- ↑ Mitragyna alkaloids: the structure of stipulatine (ScienceDirect) | http://www.sciencedirect.com/science/article/pii/S0040403901907464
- ↑ http://kratomsources.com/2011/01/23/10-ways-how-to-take-kratom/
- ↑ 13.0 13.1 13.2 How To Make Kratom Stronger: Kratom Potentiators | http://www.politiquessociales.net/how-to-make-kratom-stronger-kratom-potentiators/
- ↑ Grapefruit juice–drug interactions (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pmc/articles/PMC1873672/
- ↑ Inhibition of chlorzoxazone metabolism, a clinical probe for CYP2E1, by a single ingestion of watercress (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pubmed/9728894
- ↑ Kratom and Other Mitragynines: The Chemistry and Pharmacology of Opioids from a Non-Opium Source (first search result) - https://books.google.fr/books?hl=en&lr=&id=BtPMBQAAQBAJ&oi=fnd&pg=PA195&dq=mitragynine+respiratory&ots=JbvmS24yEo&sig=tW0crj7Jqhj-4S9JOFCpwxN25nY#v=snippet&q=respiratory&f=false
- ↑ Mitragyna speciosa, a psychoactive tree from Southeast Asia with opioid activity (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/21050173
- ↑ From Kratom to mitragynine and its derivatives: physiological and behavioural effects related to use, abuse, and addiction (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/23206666
- ↑ A drug fatality involving Kratom (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/23082895
- ↑ A drug toxicity death involving propylhexedrine and mitragynine (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/21219704
- ↑ Unintentional fatal intoxications with mitragynine and O-desmethyltramadol from the herbal blend Krypton (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/21513619
- ↑ Here Today, Gone Tomorrow…and Back Again? A Review of Herbal Marijuana Alternatives (K2, Spice), Synthetic Cathinones (Bath Salts), Kratom, Salvia divinorum, Methoxetamine, and Piperazines (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3550220/
- ↑ Kratom Legality Map | http://speciosa.org/kratom-legality-map/
- ↑ Kratom in Thailand: Decriminalization and Community Control? | http://www.tni.org/sites/www.tni.org/files/download/kratom-briefing-dlr13.pdf
- ↑ "Utusan Malaysia: Pinda akta daun ketum kepada Akta Dadah Berbahaya | http://translate.google.com/translate?hl=en&sl=auto&tl=en&prev=_dd&u=http%3A%2F%2Fwww.utusan.com.my%2Futusan%2FParlimen%2F20121213%2Fpa_02%2FPinda-akta-daun-ketum-kepada-Akta-Dadah-Berbahaya
- ↑ Bill Text: IN HB1196 | 2012 | Regular Session | Enrolled | http://legiscan.com/IN/text/HB1196/id/603106
- ↑ Bill Text: LA SB130 | 2012 | Regular Session | Chaptered | http://legiscan.com/LA/text/SB130/id/651753
- ↑ Noteikumi par Latvijā kontrolējamajām narkotiskajām vielām, psihotropajām vielām un prekursoriem (I saraksts) | http://likumi.lv/doc.php?id=121086
- ↑ Psychoactive Substances Act 2016 (Legislation.gov.uk) | http://www.legislation.gov.uk/ukpga/2016/2/contents/enacted