Abstract
Mephedrone (4-methylmethcathinone) is a synthetic cathinone with psychostimulant properties which remains one of the most popular new psychoactive substances (NPS). It is frequently used orally and/or intranasally. To date, no studies have evaluated the acute effects and pharmacokinetics after self-administration of mephedrone orally (ingestion) and intranasally (insufflation) in naturalistic conditions. An observational study was conducted to assess and compare the acute pharmacological effects, as well as the oral fluid (saliva) concentrations of mephedrone self-administered orally and intranasally. Ten healthy experienced drug users (4 females and 6 males) self-administered a single dose of mephedrone, orally (n = 5, 100–200 mg; mean 150 mg) or intranasally (n = 5, 50–100 mg, mean 70 mg). Vital signs (blood pressure, heart rate, and cutaneous temperature) were measured at baseline (0), 1, 2, and 4 h after self-administration. Each participant completed subjective effects questionnaires: A set of Visual Analogue Scales (VAS), the 49-item Addiction Research Centre Inventory (ARCI), and Evaluation of the Subjective Effects of Substances with Abuse Potential (VESSPA-SSE) at baseline, 1, 2, and 4 h after self-administration. Oral fluid and urine were collected during 4 h. Both routes of mephedrone self-administration enhanced ratings of euphoria and well-being effects and increased cardiovascular effects in humans. Although it was at times assessed that the oral route produced greater and larger effects than the intranasal one, concentrations of mephedrone in oral fluid and also the total amount of mephedrone and metabolites in urine showed that concentrations of mephedrone are considerably higher when self-administered intranasally in comparison to orally. Controlled clinical trials are needed to confirm our observational results.
Highlights
Mephedrone (4-methylmethcathinone) is considered to be the most popular synthetic cathinone drug, resembling the designer drug 3,4-methylenedioxymethamphetamine (MDMA, ecstasy) [1]
Mephedrone acts as a releaser of monoamines similar to MDMA, but with greater relative potency to release dopamine versus serotonin compared with MDMA [4,5], indicating
The main objective of the present study was to compare the acute effects after self-administration of oral and intranasal mephedrone in observational naturalistic conditions
Summary
Mephedrone (4-methylmethcathinone) is considered to be the most popular synthetic cathinone drug, resembling the designer drug 3,4-methylenedioxymethamphetamine (MDMA, ecstasy) [1]. Users sometimes reported mixing oral and nasal routes, and re-dosing during single-use sessions in which the total doses per session typically reached 0.5–2 g, usually taken in every one or two hours [10]. In this respect, in regular mephedrone recreational users, mephedrone induces some undesirable sub-acute effects such as negative mood, fatigue, and physical symptoms [11].
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