Pharmacokinetics and Safety of Mitragynine in Beagle Dogs.

Planta medica
Elizabeth A MaxwellAbhisheak Sharma

Abstract

Mitragynine is the most abundant psychoactive alkaloid derived from the leaves of Mitragyna speciosa (kratom), a tropical plant indigenous to regions of Southeast Asia. Mitragynine displays a moderate affinity to opioid receptors, and kratom is often self-prescribed to treat pain and/or opioid addiction. The purpose of this study was to investigate the safety and pharmacokinetic properties of mitragynine in the dog. Single dose oral (5 mg/kg) and intravenous (0.1 mg/kg) pharmacokinetic studies of mitragynine were performed in female beagle dogs. The plasma concentrations of mitragynine were measured using ultra-performance liquid chromatography coupled with a tandem mass spectrometer, and the pharmacokinetic properties were analyzed using non-compartmental analysis. Following intravenous administration, mitragynine showed a large volume of distribution (Vd, 6.3 ± 0.6 L/kg) and high clearance (Cl, 1.8 ± 0.4 L/h/kg). Following oral mitragynine dosing, first peak plasma (Cmax, 278.0 ± 47.4 ng/mL) concentrations were observed within 0.5 h. A potent mu-opioid receptor agonist and active metabolite of mitragynine, 7-hydroxymitragynine, was also observed with a Cmax of 31.5 ± 3.3 ng/mL and a Tmax of 1.7 ± 0.6 h in orally dosed dogs wh...Continue Reading

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Citations

Apr 14, 2021·European Journal of Drug Metabolism and Pharmacokinetics·Elizabeth A MaxwellAbhisheak Sharma
Jul 4, 2021·Drug and Alcohol Dependence·Kirsten E SmithOliver Grundmann
Jul 27, 2021·Human Psychopharmacology·Elisabeth PreveteJohannes Gerardus Ramaekers
Dec 22, 2020·ACS Pharmacology & Translational Science·Shyam H KambleChristopher R McCurdy
Nov 17, 2021·Journal of Medicinal Chemistry·Soumen ChakrabortySusruta Majumdar

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