Pharmacokinetics of mitragynine, a major analgesic alkaloid in kratom (Mitragyna speciosa): A systematic review.

@article{Ya2019PharmacokineticsOM,
  title={Pharmacokinetics of mitragynine, a major analgesic alkaloid in kratom (Mitragyna speciosa): A systematic review.},
  author={Kimheang Ya and Wimonchat Tangamornsuksan and C Norman Scholfield and Janthima Methaneethorn and MANUPAT LOHITNAVY},
  journal={Asian journal of psychiatry},
  year={2019},
  volume={43},
  pages={
          73-82
        }
}
Pharmacokinetics and Safety of Mitragynine in Beagle Dogs.
TLDR
The results provide the first detailed pharmacokinetic information for mitragynine in a non-rodent species (the dog) and therefore provide significant information for allometric scaling and dose predictions when designing clinical studies.
Development of a Physiologically Based Pharmacokinetic Model of Mitragynine, Psychoactive Alkaloid in Kratom (Mitragyna Speciosa Korth.), In Rats and Humans
TLDR
A physiologically based pharmacokinetic (PBPK) model that predicts mitragynine concentrations in plasma and organ of interests in rats and humans was developed and may be used to guide optimal mitragyna speciosa Korth dosing regimens.
Clinical Pharmacology of the Dietary Supplement Kratom (Mitragyna speciosa)
TLDR
Until studies are conducted that define kratom's role in treating opioid withdrawal and/or other central nervous system conditions, kratom will likely remain available as a dietary supplement for the foreseeable future.
The Chemical and Pharmacological Properties of Mitragynine and Its Diastereomers: An Insight Review
TLDR
The present data have shown that mitragynine is able to bind to opioid receptors, particularly MOR, to exhibit the analgesic effect and the updated pharmacological and toxicological properties of mitragyna speciosa and its diastereomers are discussed to render a comprehensive understanding of the pharmacological properties.
DARK Classics in Chemical Neuroscience: Kratom.
TLDR
The traditional and medicinal uses of kratom are reviewed along with the synthesis of its bioactive ingredients, their pharmacology, metabolism, and structure-activity relationships, and the importance in society of this currently controversial substance are discussed.
Current perspectives on the impact of Kratom use
TLDR
It is notable that Kratom can cause herb–drug interactions, especially with other central nervous system -active substances, and consumers may be exposed to adulterated or contaminated products, especially if purchased through websites or the darknet.
Kratom (Mitragyna Speciosa) Liver Injury: A Comprehensive Review
TLDR
Kratom likely causes liver injury based on the totality of low-quality human evidence, and, in the context of epidemiologic, animal, and mechanistic studies, it remains unclear which subgroups of users are at heightened risk.
Kratom—Pharmacology, Clinical Implications, and Outlook: A Comprehensive Review
TLDR
This manuscript will discuss the most current epidemiology, pharmacology, toxicity, and management related to kratom, while seeking to provide a contemporary perspective on the issue and its role in the greater context of the opioid epidemic.
Is kratom (Mitragyna speciosa Korth.) use associated with ECG abnormalities? Electrocardiogram comparisons between regular kratom users and controls
TLDR
There was no link between regular kratom use and electrocardiographic abnormalities with an estimated average daily intake of 434.28 mg of mitragynine, and there were no differences in the odds of having prolonged QTc intervals between kratom users and controls.
Mitragynine: A review of its extraction, identification, and purification methods
TLDR
Insight is provided on how the methods of extraction, purification, and identification of mitragynine have been developed over the last few decades and points out the facts that different methods gave different yields of the compound.
...
...

References

SHOWING 1-10 OF 54 REFERENCES
Pharmacokinetics of mitragynine in man
TLDR
The first pharmacokinetic study in humans, which demonstrated linearity and was consistent with the oral two-compartment model with a terminal half-life of about 1 day, suggests there is a possibility for it to be developed medically as a pain killer or better opioid substitute in the future.
The pharmacology and toxicology of kratom: from traditional herb to drug of abuse
TLDR
There are currently no standard analytical screening techniques for mitragynine and its metabolites following ingestion limiting its detection to more sophisticated techniques like liquid chromatography-mass spectrometry to determine kratom use.
Studies on the metabolism of mitragynine, the main alkaloid of the herbal drug Kratom, in rat and human urine using liquid chromatography-linear ion trap mass spectrometry.
TLDR
The seven identified phase I metabolites indicated that MG was metabolized by hydrolysis of the methylester in position 16, O-demethylation of the 9-methoxy group and of the 17-mETHoxy group, followed, via the intermediate aldehydes, by oxidation to carboxylic acids or reduction to alcohols and combinations of some steps.
Physicochemical Characterization of Mitragyna speciosa Alkaloid Extract and Mitragynine using In Vitro High Throughput Assays.
TLDR
The obtained ADME and cytotoxicity data demonstrated that both MSAE and mitragynine have poor bioavailability and have the potential to be significantly cytotoxic.
Pharmacology of Kratom: An Emerging Botanical Agent With Stimulant, Analgesic and Opioid-Like Effects
TLDR
Analyses of the medical literature and select Internet sites indicate that individuals in the United States are increasingly using kratom for the self-management of pain and opioid withdrawal.
In vitro effect of mitragynine on activity of drug metabolizing enzymes, n-demethylase and glutathione s-transferase in streptozotocin-induced diabetic rats
TLDR
This study indicates that the aminopyrine N-demethylase enzyme induction and GST activity inhibition by mitragynine is not influenced by sex.
Understanding the Physicochemical Properties of Mitragynine, a Principal Alkaloid of Mitragyna speciosa, for Preclinical Evaluation
TLDR
The determined physicochemical properties of mitragynine will provide a basis for developing a suitable formulation to further improve its solubility, stability and oral absorption for better assessment of this compound in preclinical studies.
Analysis of mitragynine and metabolites in human urine for detecting the use of the psychoactive plant kratom.
TLDR
Both ultra-high-performance liquid chromatography-tandem mass spectrometry methods have been developed and validated for monitoring the major alkaloids and metabolites found in urine following kratom use and the presence of analytes is confirmed by an information-dependent acquisition-enhanced product ion procedure generating full fragmentation data used to positively identify detected analytes.
...
...