Patterns and reasons for kratom (Mitragyna speciosa) use among current and former opioid poly-drug users

Singh, Darshan; Chear, Nelson Jeng Yeou; Narayanan, Suresh; León, Francisco; Sharma, Abhisheak; McCurdy, Christopher R.; Avery, Bonnie A.; Vicknasingam, Balasingam

doi:10.1016/j.jep.2019.112462

Cited by 69 publications

(56 citation statements)

References 37 publications

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“…A limitation of this report is the individual nature of the consumption setting, in that Kratom is not consumed for the wide spread instrumentalization goals of recreation or work performance enhancement, but for pain self-medication. However, several case studies confirm a problematic use of Kratom as a pain self-medication in the context of opiate ( Boyer et al., 2007 ; Singh et al., 2020 ) or alcohol self-withdrawal ( Havemann-Reinecke, 2011 ). Some large-scale studies also suggest a rather successful, i.e.…”

Section: Discussionmentioning

confidence: 99%

Kratom instrumentalization for severe pain self-treatment resulting in addiction – A case report of acute and chronic subjective effects

Müller

Hillemacher

Müller

2020

Heliyon

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Background Kratom is a Southeast Asian plant, which is widely used in this region, and making an increasing appearance in Europe and the US. Case report We present the case of a 26-year-old man in Substitol-assisted treatment of excessive Kratom and Tilidin use expressing the wish for a drug-free management of a chronic pain condition. After an accidental calcaneus impression fracture, the patient was suffering from severe chronic pain and anxiety of further accidents. This was managed initially with Tilidin. Resulting from the wish to self-manage the pain condition in a way that permitted continuation of a job, the patient searched for a ‘natural’ treatment alternative obtained from an Internet vendor. He successfully instrumentalized Kratom for 3 years with daily consumption intermixed with occasional Tilidin for pain management. However, the dose of Kratom was increased considerably up to a level of effect reversal, when no analgesic and behaviorally activating effects occurred any more, but only intense drowsiness. The patient was treatment seeking and subsequently detoxified from Kratom and Tilidin. Pain management was shifted to retarded morphine. Conclusion Kratom instrumentalization for pain management might appear to be more problematic for addiction development than when its use is established for other consumption motives.

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Section: Discussionmentioning

confidence: 99%

Kratom instrumentalization for severe pain self-treatment resulting in addiction – A case report of acute and chronic subjective effects

Müller

Hillemacher

Müller

2020

Heliyon

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“…Due to the higher polar surface area of the molecule, 7-hydroxymitragynine has a more limited ability to cross the blood-brain barrier when compared to mitragynine, and it is further converted to even more potent and efficacious metabolite, mitragynine pseudoindoxyl specifically in human plasma [8,9]. Levels of 7-hydroxymitragynine in Malaysian street samples and other freshly prepared extracts are below the lower limit of quantification (0.01 %w/w) of analytical methods, but in commercial kratom products in the United States was present up to 2 %w/w [1,10]. According to our experience with freshly prepared kratom samples, 7-hydroxymitragynine is not produced by the plant but rather, oxidation of mitragynine occurs post-harvest during the drying, transportation, and/or manufacturing processes.…”

Section: Kratom Alkaloids and Therapeutic Potentialmentioning

confidence: 99%

“…Kratom is a psychotropic plant from the coffee family, Rubiaceae, and like coffee, brewed tea made from the freshly harvested leaves has been consumed customarily by the native users in Malaysia and Thailand. In the traditional use, it is consumed to treat pain, boost endurance, enhance mood, and to mitigate opioid withdrawal symptoms [1]. Many countries in Southeast Asia have a large Muslim population for whom alcohol is forbidden, so instead, they drink brewed kratom leaf tea recreationally.…”

Section: Introductionmentioning

confidence: 99%

Assessing the therapeutic potential and toxicity of Mitragyna speciosa in opioid use disorder

Sharma

McCurdy

2020

Expert Opinion on Drug Metabolism & Toxicology

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“…Furthermore, mitragynine administration resulted in a reduction of morphine and heroin intake in rodents and therefore may be of therapeutic value for opiate addiction and withdrawal. Dependency on kratom has been described after heavy use in humans [17,18], even so, it has potential to treat opioid and methamphetamine dependency [19]. Only limited studies of mitragynine pharmacokinetics and metabolism have been conducted to date, with even less information concerning penetrance and distribution of the parent drug and metabolites into tissues [20].…”

Section: Introductionmentioning

confidence: 99%

Pharmacokinetics and Safety of Mitragynine in Beagle Dogs

et al. 2020

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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 while its plasma concentrations were below the lower limit of quantification (1 ng/mL) for the intravenous study. The absolute oral bioavailability of mitragynine was 69.6%. Administration of mitragynine was well tolerated, although mild sedation and anxiolytic effects were observed. These results provide the first detailed pharmacokinetic information for mitragynine in a non-rodent species (the dog) and therefore also provide significant information for allometric scaling and dose predictions when designing clinical studies.

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Patterns and reasons for kratom (Mitragyna speciosa) use among current and former opioid poly-drug users

Cited by 69 publications

References 37 publications

Kratom instrumentalization for severe pain self-treatment resulting in addiction – A case report of acute and chronic subjective effects

Kratom instrumentalization for severe pain self-treatment resulting in addiction – A case report of acute and chronic subjective effects

Assessing the therapeutic potential and toxicity of Mitragyna speciosa in opioid use disorder

Pharmacokinetics and Safety of Mitragynine in Beagle Dogs

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