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The Worldwide Spread of ‘Herbal Highs’
Published in Ornella Corazza, Andres Roman-Urrestarazu, Handbook of Novel Psychoactive Substances, 2018
Jessica Neicun, Darshan Singh, Eduardo Cinosi
Also, in Western countries, kratom appears to be used for both therapeutic and recreational purposes, largely in the frame of polydrug intake (Cinosi et al., 2015). Studies report that kratom is used as a substitute or in combination with classic drugs and various other natural or synthetic NPSs (Boyer et al., 2008; Hillebrand, Olszewski, & Sedefov, 2010; Warner, Kaufman, & Grundmann, 2016). In the context of unregulated medical use, Kratom is ingested to treat acute or chronic pain, is considered a less expensive alternative treatment for opioid withdrawal symptoms, and is used as a substitute in the context of a prescription medicine dependency (Grundmann, 2017; Singh, Müller, Vicknasingam, & Mansor, 2015; Singh et al., 2016). Furthermore, an online survey recently carried out in the USA among kratom users showed that kratom is also currently used to self-medicate mental health conditions, such as depression, anxiety, and PTSD (Grundmann, 2017; Swogger & Walsh, 2018). This new and concerning pattern of kratom use raises further questions regarding mechanisms of action of its constituents, mainly mitragynine and 7-hydroxymitragynine (Grundmann, 2017). It seems that kratom has great medicinal value. However, more controlled clinical studies are yet urgently needed to investigate the safety profile of kratom use in humans.
Long-term buprenorphine treatment for kratom use disorder: A case series
Published in Substance Abuse, 2022
Viktoriya R. Broyan, Jessica K. Brar, Tristen Allgaier, Student, Jeffrey T. Allgaier
Kratom is composed of a number of different compounds, but the ones of major significance are mitragynine and 7-hydroxymitragynine. Mitragynine has been shown to be a partial agonist at the mu-opioid receptors and a competitive antagonist at the kappa- and delta-opioid receptors.7,8 Similarly, 7-hydroxymitragynine acts as an opioid receptor agonist and antagonist at the mu- and kappa-opioid receptors, respectively.8 Other compounds in kratom have been identified to contribute to anti-inflammatory and anti-depressant effects, in addition to treating musculoskeletal pain.9 The estimated half-life of kratom is approximately 23 hours.10 However, there are conflicting reports of the half-life of mitragynine being as short as 3 hours.11 It has been suggested that due to kratom’s lipophilic nature, it could be stored in fatty tissue, thereby increasing the duration that kratom is present in the body.12 It should be mentioned that most of these findings are based on animal models, as human pharmacokinetics of kratom have not yet been fully explored.12
Is kratom (Mitragyna speciosa Korth.) use associated with ECG abnormalities? Electrocardiogram comparisons between regular kratom users and controls
Published in Clinical Toxicology, 2021
Mohammad Farris Iman Leong Abdullah, Kok Leng Tan, Suresh Narayanan, Novline Yuvashnee, Nelson Jeng Yeou Chear, Darshan Singh, Oliver Grundmann, Jack E. Henningfield
Kratom (Mitragyna speciosa Korth.) is a tropical plant commonly used as a traditional medicine in Southeast Asia. It has recently become the subject of research interest worldwide because of its alleged pain-relieving medicinal value [1,2]. Rural populations in Malaysia and Thailand have used kratom for centuries to treat various common health maladies, such as pain, fever, and diarrhoea, as a mood enhancer and as a stimulant drug for increasing work productivity [3]. To date, only a limited number of alkaloids have been isolated from kratom. Among these, mitragynine and 7-hydroxymitragynine possess unique opioid-like activity [4]. Both of these alkaloids act as partial agonists at the mu-opioid receptor and as competitive antagonists at the kappa and delta-opioid receptors. They are noted to be G protein-biased partial agonists at the mu-opioid receptor, which likely contributes to their low addictive potential and muted respiratory depressant effect [4,5]. Mitragynine alkaloids, therefore, exhibit a different pharmacological profile than classical opioids [4].
Home induction and outpatient treatment of kratom use disorder with buprenorphine-naloxone: A case report in a young adult
Published in Substance Abuse, 2020
Kelsey K. Schmuhl, Spencer M. Gardner, Casey B. Cottrill, Andrea E. Bonny
Kratom (Mitragyna speciosa) is a botanical drug that has been linked to a number of deaths in recent years and demonstrates opioid-like physiological dependence.1–3 Kratom is a tree native to Southeast Asia that has been used for centuries as a natural remedy to alleviate symptoms of opioid withdrawal. Many see kratom as a weaker, safer alternative to opioids. At lower doses, kratom tends to be used as a stimulant, while at higher doses its analgesic effects predominate.1 The leaves contain the alkaloids mitragynine and 7-hydroxymitragynine, which are believed to be responsible for the psychoactive effects. Three-dimensional modeling has shown that mitragynine and 7-hydroxymitragynine are structurally similar to opioids and agonize the mu receptor. These compounds also antagonize the delta receptor, which may explain the concurrent stimulating effects of kratom.1Mitragynine and 7-hydroxymitragynine are physiologically addictive with a number of documented deaths related to their use.2,3 Additionally, when use is acutely discontinued, opioid-like withdrawal symptoms can occur. There are both serum and urine tests available to screen for the presence of mitragynine,4 but these are not typically utilized in current routine toxicology screening.