Novel psychoactive substances (designer drugs): overview and pharmacology of modulators of monoamine signalling
Swiss Medical Weekly January 11, 2015 DOI: 10.4414/smw.2015.14043 (opens in new tab)
Study at a glance
AI-extracted from the abstract| Characteristics | Review Peer reviewed |
|---|---|
| Topics | Serotonin |
| Keywords | Pharmacology Designer drug Monoamine neurotransmitter Receptor |
| Citations | 188 |
| Key findings | The ratio of serotonergic to dopaminergic activity helps predict the psychotropic effects, toxicity, and addiction potential of novel psychoactive substances. |
Abstract
Novel psychoactive substances are newly used designer drugs ("internet drugs", "research chemicals", "legal highs") potentially posing similar health risks to classic illicit substances. Chemically, many novel psychoactive substances can be classified as phenethylamines, amphetamines, synthetic cathinones, piperazines, pipradrols/piperidines, aminoindanes benzofurans, and tryptamines. Pharmacologically, these substances interact with various monoaminergic targets. Typically, stimulants inhibit the transport of dopamine and noradrenaline (pipradrols, pyrovalerone cathinones) or induce the release of these monoamines (amphetamines and methamphetamine-like cathinones), entactogens predominantly enhance serotonin release (phenylpiperazines, aminoindanes, para-substituted amphetamines, and MDMA-like cathinones) similar to MDMA (ecstasy), and hallucinogens (tryptamines, hallucinogenic phenethylamines) are direct agonists at serotonergic 5-HT2A receptors. Synthetic cannabinoids are another group of novel substances which all act as agonists at the cannabinoid CB1 receptor similar to THC but are chemically diverse. In particular, the relative serotonergic vs dopaminergic activity (determined by the dopamine/serotonin transporter inhibition ratio in vitro) can be helpful to predict the desired psychotropic but also the toxic effects of novel substances as well as their potential for addiction. Although the use of novel psychoactive substances mostly produces minor or moderate poisonings, serious complications occur. Serotonergic drugs (entactogens and hallucinogens) are associated with acute serotonin syndrome, hyperthermia, seizures, and hyponatremia. Dopaminergic drugs are highly addictive and acute toxicity includes prolonged stimulation, insomnia, agitation, and psychosis. Agitation, anxiety, paranoia, hypertension, and rarely myocardial infarction and renal failure are seen with synthetic cannabinoids. Treatment is supportive.
Comparable studies
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Citations in the library
Cited by 50
- Receptor interaction profiles of novel psychoactive tryptamines compared with classic hallucinogens. European Neuropsychopharmacology May 20, 2016
- Neuropharmacology of New Psychoactive Substances (NPS): Focus on the Rewarding and Reinforcing Properties of Cannabimimetics and Amphetamine-Like Stimulants Frontiers in Neuroscience April 19, 2016
- Direct comparison of the acute subjective, emotional, autonomic, and endocrine effects of MDMA, methylphenidate, and modafinil in healthy subjects Psychopharmacology May 27, 2017
- Pharmacological profile of novel psychoactive benzofurans British Journal of Pharmacology March 13, 2015
- The effects of MDMA on socio-emotional processing: Does MDMA differ from other stimulants? Journal of Psychopharmacology August 26, 2016
and 45 more in the library
Cites 20
- Amphetamine-type central nervous system stimulants release norepinephrine more potently than they release dopamine and serotonin Synapse 2000
- Beyond THC: The New Generation of Cannabinoid Designer Drugs Frontiers in Behavioral Neuroscience 2011
- MDMA enhances emotional empathy and prosocial behavior Social Cognitive and Affective Neuroscience October 4, 2013
- Clinical toxicology of newer recreational drugs Clinical Toxicology October 1, 2011
- Duloxetine Inhibits Effects of MDMA (“Ecstasy") In Vitro and in Humans in a Randomized Placebo-Controlled Laboratory Study PLoS One May 4, 2012
and 15 more in the library