Search

Kratom is an evergreen tree that is native to Southeast Asia. Its leafs are traditionally used as a stimulant, a remedy for various health problems and for religious purposes. Especially in the US (in a lesser extent also in Europe) kratom use is significantly prevalent. In Western countries, kratom is used predominantly as an analgesic and stimulant, for the treatment of opioid use disorders, and for improving mental health (e. g., in depression, anxiety disorders). Main molecular constituents of kratom are alkaloids of which mitragynine and 7-hydroxymitragynine appear to be most important. Pharmacodynamics and -kinetics of kratom are complex and insufficiently studied. It is known that mitragynine and 7-hydroxymitragynine are partial agonist at human μ-opioid receptors and antagonists at κ- and δ-opioid receptors with additional effects at other central receptors. Tolerability of kratom is presumably better than that of classical opioids; this is probably due to missing effects of kratom on β-arrestin and discussed as a starting point for the development of opioids with improved tolerability. Some alkaloids of kratom are inhibitors of CYP26 and to a somewhat lesser degree of CYP2C19 and CYP3A4. The addictive potential of kratom appears to be lower than that of classical opioids; however, corresponding data is limited and kratom use disorders appear to occur primarily in Western countries. Several cases of severe health-related problems and deaths are known in the US; in these cases, however, polysubstance use was usually present. Kratom use is likely associated with hepatotoxicity and cardiotoxicity. Kratom-associated mortality and morbidity in Western countries are quantitatively significantly different from Southeast Asia, where kratom use is no public health problem. The reasons for this may be the combined use of substances (which is more prevalent in Western countries), higher dosages of consumed kratom, adulterations and contaminations of commercially available kratom in Western countries, pharmacokinetic interactions, and higher concentrations of 7-hydroxymitragynine in dried kratom leafs (that are typically consumed in Western countries) in comparison to fresh leafs (that are typically consumed in Southeast Asia)., Competing Interests: Der Autor erklärt, dass keine Interessenkonflikte vorliegen,, (Thieme. All rights reserved.)