Behavioral pharmacology of designer cathinones: A review of the preclinical literature

Gregg, Ryan A.

doi:10.1016/j.lfs.2013.10.033

Cited by 41 publications

(32 citation statements)

References 50 publications

(78 reference statements)

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“…The term NPS includes a wide range of substances, including synthetic cannabinoids, phenethylamines, cathinones, piperazines, ketamine, tryptamines and other plant-based psychoactive substances (i.e., Kratom, Salvia divinorum Epling & Játiva) [2]. Synthetic cathinone abuse may produce severe side effects such as tachycardia, hyperthermia, delusions and violent behavior [2][3][4][5][6][7]. In 2011 in USA, mephedrone (4-methylmethcathinone), methylone (3,4-methylenedioxymethcathinone) and 3,4-methylenedioxypyrovalerone (MDPV) were classified as schedule I controlled substances [8].…”

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confidence: 99%

In Vitro, in Vivo and In Silico Metabolic Profiling of α-Pyrrolidinopentiothiophenone, A Novel Thiophene Stimulant

et al. 2015

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Background: Little or no pharmacological or toxicological data are available for novel psychoactive substances when they first emerge, making their identification and interpretation in biological matrices challenging. Materials & methods: A new synthetic cathinone, α-pyrrolidinopentiothiophenone (α-PVT), was incubated with hepatocytes and samples were analyzed using liquid chromatography coupled to a Q Exactive TM Orbitrap mass spectrometer. Authentic urine specimens from suspected α-PVT cases were also analyzed. Scans were data mined with Compound Discoverer™ for identification and structural elucidation of metabolites. Results/conclusion: Seven α-PVT metabolites were identified in hepatocyte incubations, and in the authentic urine samples, also with an additional monohydroxylated product and a glucuronide of low intensity. α-PVT dihydroxypyrrolidinyl, α-PVT 2-ketopyrrolidinyl, α-PVT hydroxythiophenyl and α-PVT thiophenol had the most intense in vivo signals.

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In Vitro, in Vivo and In Silico Metabolic Profiling of α-Pyrrolidinopentiothiophenone, A Novel Thiophene Stimulant

et al. 2015

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“…Un reciente cuerpo de evidencia está emergiendo, relacionada específicamente con las catinonas sintéticas, su toxicidad bioquímica y neurológica, sus consecuencias conductuales y sus efectos fisiológicos y psiquiátricos (Gregg y Rawls, 2014;Weaver, Hopper y Gunderson, 2015). Sin embargo, dada su novedad, la mayoría de los datos proporcionados por esta investigación están relacionados con las consecuencias agudas del consumo.…”

Section: Discussionunclassified

Síntomas psicóticos persistentes después del uso abusivo prolongado de mefedrona: una serie de dos casos

Barrio

Gaskell²,

Goti

et al. 2016

Adicciones

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Mephedrone (4-methylmethcathinone) is a synthetic stimulant drug of the cathinone class. Similar effects to those of cocaine and ecstasy are reported by users, with a high addictive potential. Given its increasing rate of consumption in Europe, it is getting more and more attention from the addiction field. In spite of that, little is known about the long-term consequences of prolonged heavy use. The two following cases might depict some of them.Case 1 was a middle-age man who reported three years of intravenous use of mephedrone. He used to binge for several days in a row.Psychotic symptoms appeared after a few months, especially paranoid delusions. Sent to aftercare in a therapeutic community, delusions kept reappearing after prolonged abstinence. A good response to risperidone was observed.Case 2 was a young man who used mephedrone heavily for two years, always snorted. Upon admission to the therapeutic community, the patient reported auditory hallucinations that partially remitted with olanzapine. Both cases showed a good insight and no personality deterioration.Given its similarities to other substances that are known to induce psychotic symptoms, and the increasing consumption of mephedrone around Europe, similar cases are expected in the near future. Conventional antipsychotic treatment seems a reasonable pharmacological approach.Keywords: mephedrone; cathinone; drug dependence; psychosis; heavy use; new psychoactibe substances.La mefedrona (4-methylmethcathinone) es un estimulante sintético del grupo de las catinonas. Los usuarios refieren efectos similares a los de la cocaína y el éxtasis, con un potencial adictivo elevado. Dada la creciente tasa de consumo en Europa, cada vez recibe más atención desde el campo de las adicciones. No obstante, poco se sabe sobre las consecuencias a largo plazo de su consumo abusivo. Los dos siguientes casos pueden servir para mostrar alguna de ellas.El caso 1 es un hombre de mediana edad, quien refería un consumo intravenoso de mefedrona de 3 años de duración. Su patrón de uso consistía en atracones que duraban varios días. Tras varios meses de consumo, aparecieron síntomas psicóticos, especialmente delirios paranoides. Tras ser enviado a una comunidad terapéutica, los síntomas psicóticos se continuaron produciendo pese a mantener una abstinencia prolongada. Se observó una buena respuesta a la risperidona. El caso 2 es un hombre joven, con un consume abusivo de 2 años de duración, vía nasal. A su llegada a la comunidad terapéutica, el paciente refirió alucinaciones auditivas que remitieron parcialmente con olanzapina. Ambos casos mostraron una buena conciencia de enfermedad, así como ausencia de deterioro en su personalidad.Dadas las similitudes bioquímicas con otras sustancias con potencial para inducir síntomas psicóticos, y el creciente consumo de mefedrona en Europa, casos similares son esperables en un futuro cercano. El uso de antipsicóticos convencionales parece una estrategia razonable de tratamiento.Palabras clave: mefedrona; catinona; dependencia a sustancias; ...

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“…Whilst mephedrone and MDPV have behavioural effects, respectively, similar to methamphetamine and cocaine, methylone's effects are closer to those of MDMA [69]. Individual cathinones have variable effects and potency levels on the DA, NE, and 5-HT pathways, but all typically possess sympathomimetic and/or amphetamine-like effects [70,71].…”

Section: Pharmacology/neuropharmacologymentioning

confidence: 99%

NPS: Medical Consequences Associated with Their Intake

Schifano

Orsolini

Papanti

et al. 2016

Current Topics in Behavioral Neurosciences

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Over the last decade, the 'traditional' drug scene has been supplemented - but not replaced - by the emergence of a range of novel psychoactive substances (NPS), which are either newly created or existing drugs, including medications, now being used in novel ways. By the end of 2014, in excess of 500 NPS had been reported by a large number of countries in the world. Most recent data show, however, that synthetic cathinones, synthetic cannabinoids, and psychedelics/phenethylamines account for the largest number of NPS.The present chapter aims at providing an overview of the clinical and pharmacological issues relating to these most popular NPS categories. Given the vast range of medical and psychopathological issues associated with the molecules here described, it is crucial for health professionals to be aware of the effects and toxicity of NPS. A general overview of the acute management of NPS adverse events is provided as well, although further studies are required to identify a range of evidence-based, index molecule-focused, treatment strategies. The rapid pace of change in the NPS online market constitutes a major challenge to the provision of current and reliable scientific knowledge on these substances.

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Behavioral pharmacology of designer cathinones: A review of the preclinical literature

Cited by 41 publications

References 50 publications

In Vitro, in Vivo and In Silico Metabolic Profiling of α-Pyrrolidinopentiothiophenone, A Novel Thiophene Stimulant

In Vitro, in Vivo and In Silico Metabolic Profiling of α-Pyrrolidinopentiothiophenone, A Novel Thiophene Stimulant

Síntomas psicóticos persistentes después del uso abusivo prolongado de mefedrona: una serie de dos casos

NPS: Medical Consequences Associated with Their Intake

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