Article ; Online: Modafinil, an atypical CNS stimulant?
Advances in pharmacology (San Diego, Calif.)
2023 Volume 99, Page(s) 287–326
Abstract: Modafinil is a central nervous system stimulant approved for the treatment of narcolepsy and sleep disorders. Due to its wide range of biochemical actions, modafinil has been explored for other potential therapeutic uses. Indeed, it has shown promise as ... ...
Abstract | Modafinil is a central nervous system stimulant approved for the treatment of narcolepsy and sleep disorders. Due to its wide range of biochemical actions, modafinil has been explored for other potential therapeutic uses. Indeed, it has shown promise as a therapy for cognitive disfunction resulting from neurologic disorders like ADHD, and as a smart drug in non-medical settings. The mechanism(s) of actions underlying the therapeutic efficacy of this agent remains largely elusive. Modafinil is known to inhibit the dopamine transporter, thus decreasing dopamine reuptake following neuronal release, an effect shared by addictive psychostimulants. However, modafinil is unique in that only a few cases of dependence on this drug have been reported, as compared to other psychostimulants. Moreover, modafinil has been tested, with some success, as a potential therapeutic agent to combat psychostimulant and other substance use disorders. Modafinil has additional, but less understood, actions on other neurotransmitter systems (GABA, glutamate, serotonin, norepinephrine, etc.). These interactions, together with its ability to activate selected brain regions, are likely one of the keys to understand its unique pharmacology and therapeutic activity as a CNS stimulant. In this chapter, we outline the pharmacokinetics and pharmacodynamics of modafinil that suggest it has an "atypical" CNS stimulant profile. We also highlight the current approved and off label uses of modafinil, including its beneficial effects as a treatment for sleep disorders, cognitive functions, and substance use disorders. |
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MeSH term(s) | Humans ; Modafinil/pharmacology ; Modafinil/therapeutic use ; Central Nervous System Stimulants/therapeutic use ; Central Nervous System Stimulants/pharmacokinetics ; Benzhydryl Compounds/pharmacology ; Benzhydryl Compounds/therapeutic use ; Dopamine ; Substance-Related Disorders/drug therapy |
Chemical Substances | Modafinil (R3UK8X3U3D) ; Central Nervous System Stimulants ; Benzhydryl Compounds ; Dopamine (VTD58H1Z2X) |
Language | English |
Publishing date | 2023-11-22 |
Publishing country | United States |
Document type | Journal Article |
ISSN | 1557-8925 |
ISSN (online) | 1557-8925 |
DOI | 10.1016/bs.apha.2023.10.006 |
Database | MEDical Literature Analysis and Retrieval System OnLINE |
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