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Novel psychoactive substances and inhalants
Published in Ilana B. Crome, Richard Williams, Roger Bloor, Xenofon Sgouros, Substance Misuse and Young People, 2019
3,4-methylenedioxypyrovalerone (MDPV) is a synthetic cathinone which is marketed under a variety of names including bath salts, Ivory Wave, plant fertiliser, Vanilla Sky, Explosion, Blow, Recharge, Energy-1, or Monkey Dust. It was classified as a Class B drug in 2010 in the UK and, since 2012, is a Schedule 1 drug in the USA.
NPS
Published in Ornella Corazza, Andres Roman-Urrestarazu, Handbook of Novel Psychoactive Substances, 2018
Máté Kapitány-Fövény, Aviv M. Weinstein, Zsolt Demetrovics
In comparison to mephedrone and other cathinones, MDPV contains a pyrrolidine ring in its chemical structure, which gives MDPV potent actions, blocking the uptake at dopamine and norepinephrine transporters (Marusich et al., 2014). In some studies (Cameron et al., 2013), MDPV was found to be more potent than cocaine, with longer lasting effects as well. Users often call it ‘MP4’ or ‘music’, street names of this substance. 4-MEC, a ‘second-generation’ mephedrone analogue, also became popular after the legislative ban on mephedrone. 4-MEC produces large increases in extracellular 5-HT (5-hydroxytryptamine: serotonin) (Saha et al., 2015); however, alongside methylone, it was found to be less potent than other cathinones (Araújo et al., 2015). After the zenith of mephedrone’s and MDPV’s popularity, pentedrone became the most frequently used cathinone, cited as ‘crystal’ or ‘penta crystal’ by its users. It acts as a reuptake inhibitor for dopamine and norepinephrine, the same mechanism of action as methylphenidate (Simmler, Rickli, Hoener, & Liechti, 2014), the chemical compound of ADHD-medication: Ritalin and Concerta. However, in the case of synthetic cathinones, potential “off-target” sites of neuropharmacological action are still underexplored (Baumann et al., 2014). Considering further effects of synthetic cathinone-derivatives, human studies are still lacking, as the majority of the published papers are using animal models. Nevertheless, MDPV is considered to create cocaine-like psychoactive effects, lasting for about three to four hours (Baumann et al., 2013), with severe and hardly tolerable comedown effects and adverse symptoms, including suicidality and disturbing hallucinations. Subjective effects of methylone include euphoria, alertness, enhanced empathy, restlessness (Karila, Megarbane, Cottencin, & Lejoyeux, 2015), thought acceleration, reduced fatigue, and increased locomotor activity (Karila, Billieux, Benyamina, Lançon, & Cottencin, 2016).
Comparison of clinical characteristics between meth/amphetamine and synthetic cathinone users presented to the emergency department
Published in Clinical Toxicology, 2022
Te-I Weng, Hsien-Yi Chen, Lengsu W. Chin, Hsin-Hui Chou, Meng-Huan Wu, Guan-yuan Chen, Ju-Yu Chen, Chia-Pang Shih, Chih-Chuan Lin, Cheng-Chung Fang
O’Connor et al. compared 19 users of SC with users of other stimulants, including 55 meth/amphetamine users and 9 cocaine users. They observed an increased risk of rhabdomyolysis and severe rhabdomyolysis in cathinone users [10]. In this cohort, there were 12 and 7 users of MDPV and α-pyrrolidinovalerophenone (α-PVP). MDPV and α-PVP are both N-pyrrolidine derivatives of cathinones, which are considered more potent than other cathinone derivatives [24]. N-pyrrolidine derivatives of cathinones are thought to more easily penetrate the blood-brain barrier as they have reduced hydrophilic properties conferred by the β-ketone moiety [33] and show similar pharmacodynamics to cocaine [34]. Severe and even fatal intoxications after MDPV abuse are not uncommon due to their high potency [35]. In our study, the patients used a wide range of cathinones of which mephedrone and eutylone were most frequently detected. Despite the less common of our patients used cathinones belonging to N-pyrrolidine derivatives, cathinone users showed a higher frequency of muscular injury and rhabdomyolysis as compared with meth/amphetamine users. The adverse muscular effects seem a general clinical feature of SC, not limited only to N-pyrrolidine derivatives.
Fetal death associated with the use of 3,4-MDPHP and α-PHP
Published in Clinical Toxicology, 2019
The toxicity of 3,4-MDPHP and α-PHP have not been studied and an exact toxic dosage and concentrations are unknown. The obtained results in the presented case can, however, be compared to the concentrations of MDPV and α-PVP because the doses and action of these compounds are similar. Concentrations of MDPV determined in blood in fatal cases were mostly in the range of 440–1090 ng/mL. Fatalities with lower concentrations, even at the level of 20 ng/mL, were also reported. Nevertheless, often this compound was not the sole cause of death and other substances were also present in these cases [26]. Similarly, in the majority of fatalities involving α-PVP, other substances were also present. The blood concentrations of α-PVP in the fatal cases were in the range of 1.1–6200 ng/mL; however, in most of these cases this compound was not the cause of death [27].
“Marvin, the Paranoid Android”: The Case of an Alpha-PVP User in the Expanding Galaxy of NPS
Published in Journal of Psychoactive Drugs, 2018
Simonato Pierluigi, Bulsis Laura, Negri Attilio, Bansal Gurjeet K, Pessa Gloria, Mioni Davide, Giuseppe Borgherini, Martinotti Giovanni, Schifano Fabrizio, Giulia Perini, Corazza Ornella
Alpha-PVP is a central nervous system (CNS) stimulant, chemically related to pyrovalerones (e.g., methylenedioxypyrovalerone; MDPV), belonging to the synthetic cathinones constellation (Katselou et al. 2016; Sauer et al. 2009). It was first synthetized approximately 50 years ago, but recently gained popularity as a recreational NPS. Due to its similarity to MDPV, this compound was suggested to be a norepinephrine-dopamine reuptake inhibitor (Kolanos et al., 2015; Smith et al. 2016), but with an unclear pharmacological profile. A recent study (Kaizaki, Tanaka, and Numazawa 2014) investigated the effects of Alpha-PVP in comparison to methamphetamine on the CNS of mice. The results concluded an earlier and stronger locomotor activity, and a rapid and shorter increase of dopamine in the striatum (D1 and D2 receptors). Further studies have suggested that Alpha-PVP acts as a dopamine-releasing agent (Aarde et al. 2015; Kaizaki, Tanaka, and Numazawa 2014; Smith et al. 2016), the main mechanism being responsible for CNS stimulation and psychopathological consequences.