Mephedrone (4-methylmethcathinone; ‘meow meow’): chemical, pharmacological and clinical issues

Schifano, Fabrizio; Albanese, Anthony A.; Fergus, Suzanne; Stair, Jacqueline L.; Deluca, Paolo; Corazza, Ornella; Davey, Zoe; Corkery, John; Siemann, Holger; Scherbaum, Norbert; Farré, Magı́; Torrens, Marta; Demetrovics, Zsolt; Ghodse, A. Hamid

doi:10.1007/s00213-010-2070-x

Cited by 280 publications

(265 citation statements)

References 38 publications

Supporting

Mentioning

246

Contrasting

Unclassified

Order By: Relevance

“…The rapid rise in popularity of mephedrone may reflect growing user dissatisfaction with the purity and availability of MDMA (ecstasy) or its chemical precursors and cocaine. Mephedrone appears to be used by several population groups, including people involved in the dance and music scene, as well as mainstream young adults, and adolescents (Schifano et al 2011).…”

Section: Introductionmentioning

confidence: 99%

Mephedrone pharmacokinetics after intravenous and oral administration in rats: relation to pharmacodynamics

et al. 2013

View full text Add to dashboard Cite

Rationale Mephedrone (4-methylmethcathinone) is a still poorly known drug of abuse, alternative to ecstasy or cocaine.Objective The major aims were to investigate the pharmacokinetics and locomotor activity of mephedrone in rats and provide a pharmacokinetic/pharmacodynamic model. MethodsMephedrone was administered to male Sprague-Dawley rats intravenously (10 mg/kg) and orally (30 and 60 mg/kg). Plasma concentrations and metabolites were characterized by LC/MS and LC-MS/MS fragmentation patterns. Locomotor activity was monitored for 180-240 min.Results Mephedrone plasma concentrations after i.v. administration fit to a twocompartment model (α=10.23 h -1 and β=1.86 h -1 ). After oral administration, peak mephedrone concentrations were achieved between 0.5-1 h, and declined to undetectable levels at 9 h. Absolute bioavailability of mephedrone was of about 10% and the percentage of mephedrone protein binding was of 21.59 ± 3.67%. We have identified five Phase I metabolites in rat blood after oral administration. The relationship between brain levels and free plasma concentration was 1.85 ± 0.08.Mephedrone induced a dose-dependent increase in locomotor activity, which lasted up to 2 h. The pharmacokinetic-pharmacodynamic model successfully describes the relationship between mephedrone plasma concentrations and its psychostimulant effect. ConclusionsWe suggest a very important first-pass effect for mephedrone after oral administration and an easy access to the central nervous system. The model described might be useful in the estimation and prediction of the onset, magnitude and time course of mephedrone pharmacodynamics as well as to design new animal models of mephedrone addiction and toxicity.

show abstract

Section: Introductionmentioning

confidence: 99%

Mephedrone pharmacokinetics after intravenous and oral administration in rats: relation to pharmacodynamics

et al. 2013

View full text Add to dashboard Cite

show abstract

“…Users describe this feeling as the drug being very "moreish", meaning that it causes the user to want to ingest more shortly after use [11,28,61], and call taking multiple doses in succession "fiending" [62].…”

Section: Addiction and Withdrawalmentioning

confidence: 99%

The Toxicology of Bath Salts: A Review of Synthetic Cathinones

2011

View full text Add to dashboard Cite

Synthetic cathinones have recently emerged and grown to be popular drugs of abuse. Their dramatic increase has resulted in part from sensationalized media attention as well as widespread availability on the Internet. They are often considered "legal highs" and sold as "bath salts" or "plant food" and labeled "not for human consumption" to circumvent drug abuse legislation. Cathinone is a naturally occurring beta-ketone amphetamine analogue found in the leaves of the Catha edulis plant. Synthetic cathinones are derivatives of this compound. Those that are being used as drugs of abuse include butylone, dimethylcathinone, ethcathinone, ethylone, 3-and 4-fluoromethcathinone, mephedrone, methedrone, methylenedioxypyrovalerone (MDPV), methylone, and pyrovalerone. Synthetic cathinones are phenylalkylamines derivatives, and are often termed "bk-amphetamines" for the beta-ketone moiety. They may possess both amphetaminelike properties and the ability to modulate serotonin, causing distinct psychoactive effects. Desired effects reported by users of synthetic cathinones include increased energy, empathy, openness, and increased libido. Cardiac, psychiatric, and neurological signs and symptoms are the most common adverse effects reported in synthetic cathinone users who require medical care. Deaths associated with use of these compounds have been reported. Exposure to and use of synthetic cathinones are becoming increasingly popular despite a lack of scientific research and understanding of the potential harms of these substances. The clinical similarities to amphetamines and MDMA specifically are predictable based on the chemical structure of this class of agents. More work is necessary to understand the mechanisms of action, toxicokinetics, toxicodynamics, metabolism, clinical and psychological effects as well as the potential for addiction and withdrawal of these agents.

show abstract

“…It has been reported that mephedrone is sometimes sold in some countries as either ecstasy or 'synthetic' cocaine (Deluca et al, 2009;Schifano et al, 2011). Furthermore, it may be found mixed with adulterants, such as caffeine, paracetamol and even cocaine, amphetamine and ketamine (Camilleri et al, 2010), as well as with other methcathinones (as revealed by information supplied to the National Programme on Substance Abuse Deaths by coroners -see below).…”

Section: Chemistrymentioning

confidence: 99%

Mephedrone-Related Fatalities in the United Kingdom: Contextual, Clinical and Practical Issues

Corkery¹,

Schifano²,

Ghodse³

2012

Pharmacology

Self Cite

View full text Add to dashboard Cite

Mephedrone (4-methylmethcathinone; ‘meow meow’): chemical, pharmacological and clinical issues

Cited by 280 publications

References 38 publications

Mephedrone pharmacokinetics after intravenous and oral administration in rats: relation to pharmacodynamics

Mephedrone pharmacokinetics after intravenous and oral administration in rats: relation to pharmacodynamics

The Toxicology of Bath Salts: A Review of Synthetic Cathinones

Mephedrone-Related Fatalities in the United Kingdom: Contextual, Clinical and Practical Issues

Contact Info

Product

Resources

About