Abuse Potential of Cathinones in Humans: A Systematic Review

Poyatos, Lourdes; Torres, A Acuna; Papaseit, Esther; Pérez‐Mañá, Clara; Hladun, Olga; Núñez-Montero, Melani; Rosa, Georgina de la; Torrens, Marta; Fuster, Daniel; Muga, Roberto; Farré, Magı́

doi:10.3390/jcm11041004

Cited by 16 publications

(8 citation statements)

References 63 publications

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“…Methylone exhibited an effect profile comparable to that of MDMA, with a faster onset and earlier disappearance of subjective effects than MDMA. Typically, the abuse potential of methylone follows the trend of other cathinones, such as natural cathinone and mephedrone (Poyatos et al, 2022b). MDMA exhibited effects similar to those previously reported in other published human studies (Camí et al, 2000;Kirkpatrick et al, 2014;Papaseit et al, 2016;Kuypers et al, 2017;Holze et al, 2020;Studerus et al, 2021).…”

Section: Discussionsupporting

confidence: 80%

Pharmacological effects of methylone and MDMA in humans

et al. 2023

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Methylone is one of the most common synthetic cathinones popularized as a substitute for 3,4-methylenedioxymethamphetamine (MDMA, midomafetamine) owing to its similar effects among users. Both psychostimulants exhibit similar chemistry (i.e., methylone is a β-keto analog of MDMA) and mechanisms of action. Currently, the pharmacology of methylone remains scarcely explored in humans. Herein, we aimed to evaluate the acute pharmacological effects of methylone and its abuse potential in humans when compared with that of MDMA following oral administration under controlled conditions. Seventeen participants of both sexes (14 males, 3 females) with a previous history of psychostimulant use completed a randomized, double-blind, placebo-controlled, crossover clinical trial. Participants received a single oral dose of 200 mg of methylone, 100 mg of MDMA, and a placebo. The variables included physiological effects (blood pressure, heart rate, oral temperature, pupil diameter), subjective effects using visual analog scales (VAS), the short form of the Addiction Research Center Inventory (ARCI), the Evaluation of Subjective Effects of Substances with Abuse Potential questionnaire (VESSPA-SSE), and the Sensitivity to Drug Reinforcement Questionnaire (SDRQ), and psychomotor performance (Maddox wing, psychomotor vigilance task). We observed that methylone could significantly increase blood pressure and heart rate and induce pleasurable effects, such as stimulation, euphoria, wellbeing, enhanced empathy, and altered perception. Methylone exhibited an effect profile similar to MDMA, with a faster overall onset and earlier disappearance of subjective effects. These results suggest that abuse potential of methylone is comparable to that of MDMA in humans.Clinical Trial Registration:https://clinicaltrials.gov/ct2/show/NCT05488171; Identifier: NCT05488171.

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Section: Discussionsupporting

confidence: 80%

Pharmacological effects of methylone and MDMA in humans

et al. 2023

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“…In addition, when any drug induces desirable, euphoric and reinforcing effects, it may, to some extent, result in abuse and addictive potential. Regarding the sympathomimetics mentioned in this work, while cocaine addictive potential is recognized for several years [ 190 ], a new vision on cathinones has emerged with recent studies that recognize their abuse and addictive potential [ 177 , 222 ]. Actually, the addictive potential of some of these compounds adds another danger to the equation as chronic use will be likely and the set of toxic effects will increase.…”

Section: Discussionmentioning

confidence: 99%

Natural Sympathomimetic Drugs: From Pharmacology to Toxicology

Costa

Grando²,

Milandri³

et al. 2022

Biomolecules

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Sympathomimetic agents are a group of chemical compounds that are able to activate the sympathetic nervous system either directly via adrenergic receptors or indirectly by increasing endogenous catecholamine levels or mimicking their intracellular signaling pathways. Compounds from this group, both used therapeutically or abused, comprise endogenous catecholamines (such as adrenaline and noradrenaline), synthetic amines (e.g., isoproterenol and dobutamine), trace amines (e.g., tyramine, tryptamine, histamine and octopamine), illicit drugs (e.g., ephedrine, cathinone, and cocaine), or even caffeine and synephrine. In addition to the effects triggered by stimulation of the sympathetic system, the discovery of trace amine associated receptors (TAARs) in humans brought new insights about their sympathomimetic pharmacology and toxicology. Although synthetic sympathomimetic agents are mostly seen as toxic, natural sympathomimetic agents are considered more complacently in the terms of safety in the vision of the lay public. Here, we aim to discuss the pharmacological and mainly toxicological aspects related to sympathomimetic natural agents, in particular of trace amines, compounds derived from plants like ephedra and khat, and finally cocaine. The main purpose of this review is to give a scientific and updated view of those agents and serve as a reminder on the safety issues of natural sympathomimetic agents most used in the community.

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“…This study showed that several drugs, including diethylpropion, lead to undesirable effects that can cause dependence and abuse. The authors point to the need for future research to prevent negative manifestations in the treatment of patients [ 59 ].…”

Section: Novel Drugs In Obesity Treatmentmentioning

confidence: 99%

Pharmacological Treatments and Natural Biocompounds in Weight Management

et al. 2023

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The obesity pandemic is one of society’s most urgent public health concerns. One-third of the global adult population may fall under obese or overweight by 2025, suggesting a rising demand for medical care and an exorbitant cost of healthcare expenditure in the coming years. Generally, the treatment strategy for obese patients is largely patient-centric and needs dietary, behavioral, pharmacological, and sometimes even surgical interventions. Given that obesity cases are rising in adults and children and lifestyle modifications have failed to produce the desired results, the need for medical therapy adjunct to lifestyle modifications is vital for better managing obesity. Most existing or past drugs for obesity treatment target satiety or monoamine pathways and induce a feeling of fullness in patients, while drugs such as orlistat are targeted against intestinal lipases. However, many medications targeted against neurotransmitters showed adverse events in patients, thus being withdrawn from the market. Alternatively, the combination of some drugs has been successfully tested in obesity management. However, the demand for novel, safer, and more efficacious pharmaceutical medicines for weight management does exist. The present review elucidates the current understanding of the available anti-obesity medicines of synthetic and natural origin, their main mechanisms of action, and the shortcomings associated with current weight management drugs.

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Abuse Potential of Cathinones in Humans: A Systematic Review

Cited by 16 publications

References 63 publications

Pharmacological effects of methylone and MDMA in humans

Pharmacological effects of methylone and MDMA in humans

Natural Sympathomimetic Drugs: From Pharmacology to Toxicology

Pharmacological Treatments and Natural Biocompounds in Weight Management

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