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Preclinical Antidepressant-Like Effects of Terpenes, Polyphenolics, and Other Non-Flavonoid Phytochemicals
Published in Scott Mendelson, Herbal Treatment of Major Depression, 2019
Mitragynine is a complex indole alkaloid extracted from Mitragyna speciosa Korth. This plant from Southeast Asia is more commonly known as kratom. Mitragynine acts, at least in part, as a μ-opioid receptor agonist.132 However, there is also evidence of monoaminergic effects.133 The leaves of Mitragyna speciose are commonly used to treat pain and as a minor stimulant among natives of Thailand and surrounding areas. More recently it has been used in treating opiate addiction.
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
The phytochemicals isolated from various parts of the kratom tree include over 40 structurally related alkaloids (Dargan & Wood, 2013) of which mitragynine is the most represented (up to 66% purity in the extract of leaves from Thailand). This alkaloid is thought to be partly responsible for the analgesic activity that has been linked to Kratom use, mostly because of its potent opioid agonist property (Takayama, 2004). Although mitragynine can act on the kappa (κ), mu (μ), and delta (δ) opioid receptors, it is structurally different from morphine or classic opioids, and it has been suggested that mitragynine might present a broader receptor binding activity (Thongpradichote et al., 1998).
Comparison of biochemical and safety parameters of regular kratom (Mitragyna speciosa Korth.) users at two different time periods
Published in Journal of Substance Use, 2023
Dinesh Sangarran Ramachandram, Kow Chia Siang, Rini R
To date, kratom consumption has not been linked to any adverse health problems among kratom users in traditional settings (Singh et al., 2014; Vicknasingam et al., 2010; Vicknasingam et al., 2020). The use of kratom leaf powder is said to be associated with detrimental health eventualities in the West (Anwar et al., 2016; Dorman et al., 2015; Kapp et al., 2011). Existing findings showed that crude extracts of M. speciosa and its principal alkaloid mitragynine were toxic in rats (Harizal et al., 2010; Sabetghadam et al., 2013). However, the toxic effects were only found to be associated with higher mitragynine dose (100 mg/kg) and with chronic administration in rats (Harizal et al., 2010; Ilmie et al., 2015; Sabetghadam et al., 2013). Kapp et al. (2011) found short-term use (2 weeks) of kratom powder via oral route could cause jaundice and pruritus in the absence of other causative agents. In the West, most of the uneventful health incidents occurred due to chronic kratom, (Cumpston et al., 2018) or when kratom is being administered together with other illicit substances and alcohol, (Drago et al., 2017; Forrester, 2013) and with the use of adulterated kratom products (Lydecker et al., 2016). It is reported that kratom users normally experience abdominal pain after ingesting kratom leaf powder (Cumpston et al., 2018; Kapp et al., 2011).
Exploring the self-reported motivations of kratom (Mitragyna speciosa Korth.) use: a cross-sectional investigation
Published in The American Journal of Drug and Alcohol Abuse, 2022
Oliver Grundmann, Charles A. Veltri, Diana Morcos, David Knightes, Kirsten E. Smith, Darshan Singh, Ornella Corazza, Eduardo Cinosi, Giovanni Martinotti, Zach Walsh, Marc T. Swogger
Kratom (Mitragyna speciosa Korth.) is a tree from Southeast Asia, whose leaves contain pharmacologically active constituents, most notably mitragynine (1). In Thailand, kratom use typically involves ingestion of the plant’s raw leaves or consumption of teas that are prepared from fresh leaves (1). Ingesting kratom leaves produces complex dose-dependent stimulant and opioid-like analgesic effects, and the dried powdered kratom leaf is frequently used to enhance overall feelings of well-being, increased energy, and alertness (2,3). Low to moderate doses (1–5 g) of leaves and dried powdered products produce mild stimulant effects, whereas moderate-to-high doses (5–15 g) are reported to have opioid-like effects. In these doses, kratom has been used for the management of pain, diarrhea, anxiety, and to attenuate opioid withdrawal symptoms (4). Very high doses (>15 g) of kratom tend to be sedating and can induce stupor, mimicking higher opioid-dose effects (1,5). More recent research indicates that stimulant and sedative effects may be felt at all doses of kratom depending on the mitragynine content (6). Self-report and initial human study data suggest between 1 and 5 grams per dose is shown to be efficacious in treating acute and chronic pain (3,7–10).
Characterization of urinary protein profile in regular kratom (Mitragyna speciosa korth.) users in Malaysia
Published in Journal of Addictive Diseases, 2022
Rana Khudhair Jasim, Zurina Hassan, Darshan Singh, Edward Boyer, Lay-Harn Gam
Since it is increasingly used to self-manage substance use disorder (SUD),10 further studies have also been conducted to characterize kratom’s pharmacological properties,11–13 and its side-effects.14,15 Of the dozens of alkaloids, mitragynine is the most abundant alkaloid, and its metabolite 7-hydroxymitragynine, is reported to have unique opioid and non-opioid like-effects since it binds to opioid and adrenergic receptors.12,16 Initial laboratory findings indicate that mitragynine has the potential to reduce opioid intake and treat opioid use disorder.11,17 Moreover, its beneficial effects in mitigating opioid use disorder and withdrawal, and mental health symptoms among prescription and illicit opioid users in the U.S especially, have also been documented.6–8