Mephedrone – a synthetic derivative of cathinone

Abstract

Novel psychoactive substances (NPS) are a very diverse group of recreational drugs that mimic effects of classic drugs of abuse and, at least at the beginning, are not usually prohibited. Representative of this group is mephedrone – a cathinone derivative. It is widely used as a recreational drug, particularly among club guests. Mephedrone`s effects are compared to effects of cocaine and MDMA but are more short-lived and include: psychostimulation, enhanced empathy, reduced feeling of tiredness, euphoria, hallucinations. This drug also exerts adverse effects, such as: anxiety, delusions, paranoia, psychosis, increased body temperature, elevated blood pressure, sleep disturbances. According to surveys performed on mephedrone users, it may be addictive. Those findings confirms a growing number of behavioural and molecular studies on animals. Mephedrone acts mainly via increasing monoamine transmission through increasing release of dopamine, serotonin and noradrenaline into synaptic cleft, inhibiting their re-uptake and reducing their metabolism. However, participation of other transmitters, modulators and pathways are investigated, including glutamate and nitric oxide. Favorable routes of administering mephedrone is intranasal and per os. Moreover, most often drug users use it in a binge way, e.g. taking repeated doses of a drug in a short period of time. According to animal studies, this pattern of mephedrone use leaves more neural injuries than taking it regularly, but in smaller doses. Our aim was to present a short, but essential, overview of the current knowledge on mephedrone, focusing on its effects, mechanism of action, animal studies evaluating its influence on the brain structures, toxicity and pharmacokinetics.

Structure–Activity Relationship of Synthetic Cathinones: An Updated Review

“…84 However, not all the effects are only related to cathinone use, as polysubstance abuse (for example with alcohol, tobacco, MDMA, cannabis, and cocaine) is very common among those taking synthetic cathinones. 1,84 In addition, synthetic cathinones are often found in powders or pills resembling one another, potentially leading consumers to be unaware of the specific stimulant or combination of substances they are using. Adulteration by both substitution and addition is particularly relevant in this family of substances, as these mixtures increase the risk for consumers to encounter unforeseen adverse effects and potential harm.…”

“…89,90 Moreover, 4-MMC users reported a prolonged feeling of activity compared to cocaine. 1,81,84 Both animal and human studies have also suggested that methylone may possess an addiction potential like or greater than MDMA, although results suggested a lower potential for abuse and compulsive use than cocaine, methamphetamine, and 4-MMC. 42,79,91 On the other hand, an observational-naturalistic study conducted in humans to evaluate the acute pharmacological effects of methylone oral self-administration, showed that methylone was able to induce the prototypical psychostimulant and empathogenic effects generally associated with MDMA, although with lower intensity.…”

“…The term "new", does not necessarily refer to new inventions but to substances that have recently become available. 1 According to the United Nations Office on Drugs and Crime (UNODC), NPS can be classified into six groups based on their mode of action: stimulants, synthetic cannabinoid receptor agonists, dissociatives, sedatives/hypnotics, synthetic opioids and classic hallucinogens. 2 The proliferation of NPS in the illicit market presents a significant Public Health concern due to the rapid increase in their chemical diversity.…”