2022
DOI: 10.1002/jcph.2001
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Clinical Pharmacology of the Dietary Supplement Kratom (Mitragyna speciosa)

Abstract: Kratom (Mitragyna speciosa) consists of over 40 alkaloids, with 2 of them, mitragynine and 7-OH-mitragynine (7-OH-MG) being the main psychoactive compounds. Mitragynine and 7-OH-mitragynine each target opioid receptors and have been referred to as atypical opioids. They exert their pharmacologic effects on the mu, delta, and kappa opioid receptors. In addition, they affect adrenergic, serotonergic, and dopaminergic pathways. Kratom has been touted as an inexpensive, legal alternative to standard opioid replace… Show more

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Cited by 16 publications
(28 citation statements)
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References 151 publications
(523 reference statements)
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“…Die Plasmaeiweißbin dung liegt bei > 90 %, bei schwacher Hemmung von PGlykoprote in [67]. Eine Modulation der UridinDiphopshatGlucoronyltrans ferase durch Kratom wurde auch beschrieben [68]. Ergebnisse von in vitro Studien (auch an humanen Zellen) fanden, dass Extrakte von Kratom starke Inhibitoren von Cytochrom P450 (CYP) 2D6 (vor allem durch Mitragynin und Corynantheidin, geringer auch Spe ciociliatein und Paynanthein [69]) und geringer auch CYP2C19 (vor allem Speciociiatin, Mitragynin und Speciogynin [69]) 3A4 sind [69][70][71], wobei in vivo Untersuchungen dazu fehlen.…”
Section: Pharmakokinetische Merkmaleunclassified
“…Die Plasmaeiweißbin dung liegt bei > 90 %, bei schwacher Hemmung von PGlykoprote in [67]. Eine Modulation der UridinDiphopshatGlucoronyltrans ferase durch Kratom wurde auch beschrieben [68]. Ergebnisse von in vitro Studien (auch an humanen Zellen) fanden, dass Extrakte von Kratom starke Inhibitoren von Cytochrom P450 (CYP) 2D6 (vor allem durch Mitragynin und Corynantheidin, geringer auch Spe ciociliatein und Paynanthein [69]) und geringer auch CYP2C19 (vor allem Speciociiatin, Mitragynin und Speciogynin [69]) 3A4 sind [69][70][71], wobei in vivo Untersuchungen dazu fehlen.…”
Section: Pharmakokinetische Merkmaleunclassified
“…Pharmacological classes found were stimulants (68 findings, 16 substances, in 22 patients) vastly dominated by synthetic cathinones and also represented by 3F‐phenmetrazine and ethylphenidate (the latter in the absence of methylphenidate indicating that it was not a metabolite of methylphenidate and ethanol); sedatives/hypnotics that were all benzodiazepines (44 findings, 5 substances, in 25 patients); synthetic cannabinoids (16 findings, 4 substances, in 6 patients); and potent opioids in the form of isotonitazene and four different fentanyl derivatives (13 findings, 5 substances, in 5 patients). In addition, the following substances were found: 3‐methoxy‐PCP, a dissociative hallucinogenic phencyclidine derivative 35 ; cyproheptadine, a sedating antihistamine with low abuse potential 36 but possibly self‐administered as a remedy against serotonergic, including sexual side effects of other substances 37 ; mitragynine, a stimulant at low doses but opioid‐like at high doses 38 ; and tianeptine, an atypical antidepressant with known abuse potential and opioid effects at high doses 39,40 . Of the 85 patients, 17 (20%) were positive for more than one NPS; 5 (6%) and 2 (2%) of these individuals were positive for NPS from two and three pharmacological NPS classes, respectively.…”
Section: Resultsmentioning
confidence: 99%
“…3-methoxy-PCP, a dissociative hallucinogenic phencyclidine derivative 35 ; cyproheptadine, a sedating antihistamine with low abuse potential 36 but possibly selfadministered as a remedy against serotonergic, including sexual side effects of other substances 37 ; mitragynine, a stimulant at low doses but opioid-like at high doses 38 ; and tianeptine, an atypical antidepressant with known abuse potential and opioid effects at high doses. 39,40 Of the 85 patients, 17 (20%) were positive for more than one NPS; 5 (6%) and 2 (2%) of these individuals were positive for NPS from two and three pharmacological NPS classes, respectively.…”
Section: Nps Findingsmentioning
confidence: 99%
“…Mitragynine and 7‐hydroxy mitragynine being the main phytoconstituents of kratom are atypical opioids. Each act on opioid receptors and impacts adrenergic, serotonergic, and dopaminergic pathways [85] . Several informal reports have recorded the administration of kratom preparations to attenuate opioid intake by decreasing withdrawal symptoms [86,87] .…”
Section: Resultsmentioning
confidence: 99%
“…β‐arrestin recruitment causes unfavourable central nervous system effects such as the risk of respiratory depression, sedation and constipation. These adverse effects are usually associated with traditional opioid replacement medications [85,88,89] . Mitragynine activates α‐2 adrenergic postsynaptic receptors, that regulate the decreasing pain pathways [88,90] .…”
Section: Resultsmentioning
confidence: 99%