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Synthetic Cathinones and Related Fatalities in the United Kingdom
Published in Ornella Corazza, Andres Roman-Urrestarazu, Handbook of Novel Psychoactive Substances, 2018
John M. Corkery, Christine Goodair, Hugh Claridge
Some synthetic cathinones remain licenced for medicinal use. For instance, bupropion (Amfebutamone, Zyban, Wellbutrin), which is primarily used as an antidepressant and a smoking cessation aid, has also been used for recreational purposes because of its cocaine-like effects (McCormick, 2002; Vento et al., 2013). Pyrovalerone, structurally related to MDPV, because of its stimulant effects, has been used in the clinical treatment of lethargy and chronic fatigue (Gardos & Cole, 1971). It has also been employed as an appetite suppressant and anorectic in France and elsewhere. However, problems with abuse and dependence mean it has not often been prescribed in recent years (Deniker, Lôo, Cuche, & Roux, 1975). Pyrovalerone is covered by Schedule IV of the United Nations (UN) 1971 Convention on Psychotropic Substances. In the UK, it was controlled as a Class C drug under the Misuse of Drugs Act 1971, prior to the inclusion of additional cathinones, e.g., mephedrone, in April 2010. Amfepramone was also categorized as a Class C drug.
Pulmonary hypertension induced by drugs and toxins
Published in Philippe Camus, Edward C Rosenow, Drug-induced and Iatrogenic Respiratory Disease, 2010
Kim Bouillon, Yola Moride, Lucien Abenhaim, Marc Humbert
Diethylpropion (amfepramone) is structurally related to amphetamines (see Fig. 29.2) and is a sympathomimetic stimulant. The implication of diethylpropion in the development of PAH is not clear because only a small number of patients were exclusively exposed to this drug. Between 1995 and 2003, only two cases of diethylpropion-associated PAH have been reported.47,48 The first case was observed in the United Kingdom. A 22-year-old woman was prescribed diethylpropion for 3–5 months. Breathlessness on exertion developed when she was 27, and the diagnosis of PAH was made 4 years later.47 The second case was observed in Belgium. A 27-year-old woman took diethylpropion during two courses of 4 and 5 weeks, respectively 3.5 and 1.5 years before onset of symptoms.48 Interestingly, a mutation of the BMPR2 was found in the second case of PAH associated with diethylpropion.
Blood concentrations of synthetic cathinones
Published in Clinical Toxicology, 2021
Data collection was based on a search of PubMed (U.S. National Library of Medicine) with mainly (but not only) each of the compound names (acronyms) listed in Table 1 as keywords (as well as their other synonyms and chemical names). The list of synthetic cathinones searched for was based on lists of substances monitored by EMCDDA. Licit medicinal drugs (e.g. bupropion, amfepramone) were excluded from the study. Found papers were checked carefully in order to identify any additional publications missed during the initial search. The Google search engine was used likewise, in particular for less popular compounds. All available data was from articles and reports written mainly in English, published from 2010 to the beginning of 2020 (one paper was from 2005 [124]). Cases where synthetic cathinone concentrations in humans had been measured in whole blood, serum or plasma were included in the data analysis. The cases were divided into two categories: non-fatal cases (including drug use, driving under the influence of drugs cases, non-fatal intoxication cases as well as a few human experimental studies) and fatal (autopsy) cases (from all fatal cases, including fatal intoxications as well as deaths due to other reasons). To simplify, the term “blood” is used synonymously for serum, plasma and whole blood in this report.
The problem of racemization in drug discovery and tools to predict it
Published in Expert Opinion on Drug Discovery, 2019
Andrew Ballard, Stefania Narduolo, Hiwa O. Ahmad, David A. Cosgrove, Andrew G. Leach, Niklaas J. Buurma
Amfepramone (19) is a stimulant that can be used as an appetite suppressant and is usually used as a racemate [30,37]. The rate of racemization was studied as buffer strength, ionic strength, temperature, and drug concentration were varied. The dependence on pH and on buffer strength revealed non-linear relationships. Cyclodextrin additives were also investigated for their ability to suppress racemization but showed mixed results with most examples actually promoting racemization while only a small number were protective. In human plasma, the half-life for racemization was measured to be 23–25 min but this is much lower than the known in vivo half-life following oral dosing of 1.5 to 2 h. Studies in phosphate buffers at a range of pHs and buffer strengths support a general-base-catalyzed reaction (Figure 3(a)) for 19 and the analogous primary amine.
Synthetic cathinones: an evolving class of new psychoactive substances
Published in Critical Reviews in Toxicology, 2019
João L. Gonçalves, Vera L. Alves, Joselin Aguiar, Helena M. Teixeira, José S. Câmara
During the second half of the twentieth century, other SCat continued to appear as potential medicines. Diethylcathinone, also known as amfepramone or diethylpropion, was introduced in 1958 as an appetite suppressant (Angrist and Sudilovsky 2012). Shortly after being patented in 1961 (Werke 1961), reports of its abuse began to emerge (Clein and Benady 1962; Kuenssberg 1962). In 1971, amfepramone was included in the list of controlled substances by the UN Convention on Psychotropic Substances (UN 1975).