Carlier J, Giorgetti R, Varì M R, Pirani F, Ricci G, Busardò F P
Unit of Forensic Toxicology, Sapienza University of Rome, Rome, Italy.
Eur Rev Med Pharmacol Sci. 2019 Jan;23(1):3-15. doi: 10.26355/eurrev_201901_16741.
In the last decades, several cognitive-enhancing drugs have been sold onto the drug market. Methylphenidate and analogs represent a sub-class of these new psychoactive substances (NPS). We aimed to review the use and misuse of methylphenidate and analogs, and the risk associated. Moreover, we exhaustively reviewed the scientific data on the most recent methylphenidate analogs (methylphenidate and ethylphenidate excluded).
Literature search was performed on methylphenidate and analogs, using specialized search engines accessing scientific databases. Additional reports were retrieved from international agencies, institutional websites, and drug user forums.
Methylphenidate/Ritalin has been used for decades to treat attention deficit disorders and narcolepsy. More recently, it has been used as a cognitive enhancer and a recreational drug. Acute intoxications and fatalities involving methylphenidate were reported. Methylphenidate was scheduled as an illegal drug in many countries, but NPS circumventing the ban and mimicking the psychostimulant effects of methylphenidate started being available: ethylphenidate, 3,4-dichloromethylphenidate, 3,4-dichloroethylphenidate, 4-fluoromethylphenidate, 4-fluoroethylphenidate, methylnaphthidate, ethylnaphthidate, isopropylphenidate, propylphenidate, 4-methylmethylphenidate, and N-benzylethylphenidate have been available in the past few years. Only little data is currently available for these substances. Many intoxications involving methylphenidate analogs were reported. To date, ethylphenidate was involved in 28 fatalities, although it was reportedly directly related to the cause of death in only 7 cases; 3,4-dichloroethylphenidate was involved in 1 death.
The rapid expansion of methylphenidate analogs onto the drug market in the past few years makes likely the occurrence of intoxications and fatalities in the next years. Careful monitoring and systematic control of methylphenidate analogs should be undertaken to reduce the uprising threat, and education efforts should be made among high-risk populations.
在过去几十年中，几种认知增强药物已投放市场。哌醋甲酯及其类似物是这些新型精神活性物质（NPS）的一个子类。我们旨在综述哌醋甲酯及其类似物的使用和滥用情况以及相关风险。此外，我们详尽回顾了关于最新的哌醋甲酯类似物（不包括哌醋甲酯和乙哌醋甲酯）的科学数据。
使用访问科学数据库的专业搜索引擎对哌醋甲酯及其类似物进行文献检索。从国际机构、机构网站和吸毒者论坛获取了其他报告。
哌醋甲酯/利他林已被用于治疗注意力缺陷障碍和发作性睡病数十年。最近，它被用作认知增强剂和娱乐性药物。有涉及哌醋甲酯的急性中毒和死亡报告。哌醋甲酯在许多国家被列为非法药物，但规避该禁令并模仿哌醋甲酯精神兴奋作用的新型精神活性物质开始出现：乙哌醋甲酯、3,4 - 二氯哌醋甲酯、3,4 - 二氯乙哌醋甲酯、4 - 氟哌醋甲酯、4 - 氟乙哌醋甲酯、萘哌醋甲酯、萘乙哌醋甲酯、异丙基哌醋甲酯、丙基哌醋甲酯、4 - 甲基哌醋甲酯和N - 苄基乙哌醋甲酯在过去几年中已出现。目前关于这些物质的数据很少。有许多涉及哌醋甲酯类似物的中毒报告。迄今为止，乙哌醋甲酯涉及28例死亡，尽管据报道仅7例与死亡原因直接相关；3,4 - 二氯乙哌醋甲酯涉及1例死亡。
过去几年哌醋甲酯类似物在药物市场的迅速扩张使得未来几年中毒和死亡事件有可能发生。应仔细监测并系统控制哌醋甲酯类似物以降低不断上升的威胁，并且应在高危人群中开展教育工作。
