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Stimulants: cocaine, amphetamines and party drugs
Published in Berry Beaumont, David Haslam, Care of Drug Users in General Practice, 2021
Methylphenidate (Ritalin) is prescribed for the treatment of attention deficit hyperactivity disorder (ADHD). It can be diverted and abused, orally, by snorting or by injection. This is a recognised problem in the USA and New Zealand in particular but is beginning to happen in the UK as well. It is of similar potency to dexamphetamine and has similar effects.2
Attention-Deficit Hyperactivity Disorder
Published in Quentin Spender, Niki Salt, Judith Dawkins, Tony Kendrick, Peter Hill, David Hall, Jackie Carnell, Child Mental Health in Primary Care, 2018
Quentin Spender, Niki Salt, Judith Dawkins, Tony Kendrick, Peter Hill, David Hall, Jackie Carnell
The same principles can be applied to dexamphetamine. The small number of children under six years who are treated with this drug can start with dexamphetamine or methylphenidate 2.5 mg. (Dexamphetamine is licensed for this and methylphenidate is not, but we find methylphenidate to be more effective and less prone to side-effects.)
Sympathomimetic Amines: Actions and Uses
Published in Kenneth J. Broadley, Autonomic Pharmacology, 2017
Amphetamine was found to promote weight loss when used in patients suffering from narcolepsy (prolonged bouts of sleepiness). Dexamphetamine (DexedrineR) has been used in the treatment of obesity, the weight loss being due to suppression of appetite rather than an effect on energy expenditure. Its effect is short-lived since tolerance develops and there are risks of hypertension and sleep disturbances. Amphetamine and related agents [phentermine (Ionamin, Duramine, FastinUS), diethylpropion (Tenuate DospanR), pheadimetrazine (PlegineUS), benzphetamine (DidrexUS), methamphetamine (DesoxynUS)] have psychostimulant properties and have potential for abuse and habituation. They have therefore been largely replaced by non-stimulant derivatives such as fenfluramine (PonderaxR) and its dextro isomer, dexfenfluramine (AdifexR). Whereas amphetamines are indirectly acting sympathomimetic amines releasing noradrenaline from nerve endings, fenfluramine releases 5-HT and is sedative rather than stimulant; in fact depression is a potential adverse effect. Mazindol (TeronacUK, MazanorUS) is a tricyclic antidepressant, structurally unrelated to amphetamine, which is an inhibitor of neuronal uptake. It supresses appetite and will interact with antihypertensives (eg neurone blockers).
Neurotoxic and cardiotoxic effects of N-methyl-1-(naphthalen-2-yl)propan-2-amine (methamnetamine) and 1-phenyl-2-pyrrolidinylpentane (prolintane)
Published in Drug and Chemical Toxicology, 2023
Sohee Jeong, Kyung Sik Yoon, Jin-Moo Lee, Eun Sung Jo, Dojung Kim, Sun Ok Choi
Amphetamine has been regulated by all 183 states since 1971 by the United Nations Convention on Psychotropic Substances (UNODC 2007). Due to these regulations, illegal drug users have started to use NPS (Ministry of Health, Labor and Welfare 2015). Methamphetamine, one of the amphetamine substitute drugs, is a compound with a similar structure to 1-(benzofuran-5-yl)-N-methylpropan-2-amine (5-MAPB) and, thus, prohibited in Japan. Animal experiments conducted using positive control drugs or central stimulants, such as amphetamine, significantly contributed to developing drug regulations. Prolintane is also a CNS stimulant with similar structural and pharmacological properties to d-amphetamine (Hollister and Gillespie 1970). The side-effects of d-amphetamine include insomnia, nervousness, irritability, and dizziness (Martinez-mir et al. 1997). The overuse of prolintane can cause hallucination, substance use disorder, and schizophrenia and, eventually, death (Kyle and Daley 2007). However, the data on the toxicity and carcinogenicity of many NPSs are minimal. Particularly, there is a lack of research exploring the CNS and cardiovascular system (ICH 1997). Safety abbreviations have regulated the medicines related to NPSs through guidelines established by the International Conference on Harmonization of technical requirements for registration of pharmaceuticals for human use. Safety pharmacology tests can be used to screen any issues with human organs, including the nervous, cardiovascular, and respiratory systems.
Clinical guidance on pharmacotherapy for the treatment of attention-deficit hyperactivity disorder (ADHD) for people with intellectual disability
Published in Expert Opinion on Pharmacotherapy, 2020
Jonjo Miller, Bhathika Perera, Rohit Shankar
Dexamphetamine works by increasing synaptic extracellular dopamine and norepinephrine levels in the prefrontal cortex [53]. Though dexamphetamine are first-line ADHD medications [16], the evidence base in the ID population has been limited. The sole result was a Cochrane review of amphetamine in ADHD in ID published in 2009 [54]. Within this, the only paper meeting inclusion criteria was a double-blind RCT of amphetamine vs MPH vs placebo [38], in 15 children (mean age 7.9) with fragile x-syndrome and mean IQ of 58. Dexamphetamine 0.2 mg/kg given once daily was found to cause no significant improvement vs placebo in ADHD symptoms as assessed by Conners’ parents/teachers questionnaire and ACTRS.
Successes, failures, and future prospects of prodrugs and their clinical impact
Published in Expert Opinion on Drug Discovery, 2019
Attention deficit hyperactivity disorder (ADHD) is one of the most common childhood psychiatric conditions that often persists into adulthood [31]. Pharmacological treatment of ADHD commonly involves amphetamine derivatives such as dexamphetamine and methylphenidate. Lisdexamphetamine is an orally administered inactive prodrug of dexamphetamine. Following oral administration, the amide linkage between dexamphetamine and L-lysine is enzymatically hydrolysed by plasma esterases. This long-acting prodrug formulation produces sustained plasma concentrations of dexamphetamine thus eliminating the need for administration of drugs in a school environment [32].