Practical Use and Risk of Modafinil, a Novel Waking Drug

Kim, Dongsoo

doi:10.5620/eht.2012.27.e2012007

Cited by 65 publications

(41 citation statements)

References 60 publications

(92 reference statements)

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“…For conciseness, we did not compare the effect of modafinil with other central nervous system stimulants, such as methylphenidate and amphetamines. A descriptive review by Kim discusses the neural mechanisms and cognitive effects of amphetamine and caffeine and compares it to modafinil (Kim, 2012). Similar effectiveness was found.…”

Section: Discussionsupporting

confidence: 67%

Modafinil effects on cognition and emotion in schizophrenia and its neurochemical modulation in the brain

2013

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Section: Discussionsupporting

confidence: 67%

Modafinil effects on cognition and emotion in schizophrenia and its neurochemical modulation in the brain

2013

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“…Modafinil was first approved by the US Food and Drug Administration (FDA) in 1998 and marketed as the racemic mixture of R- and S-enantiomers (2) and later as a formulation containing only the R-enantiomer, which is pharmacokinetically distinct from the S-enantiomer in humans (3) as described later (4). It has been viewed throughout its history (5–7) as a “novel” wake-promoting therapeutic, and apparently is still viewed in the same manner to this day (8). The fact that this mainstream therapeutic agent is still thought of as novel presumably stems from some unique pharmacological and clinically relevant properties of modafinil relative to other wake-promoting agents.…”

Section: Introductionmentioning

confidence: 99%

Modafinil as a Catecholaminergic Agent: Empirical Evidence and Unanswered Questions

Wisor¹

2013

Front. Neurol.

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Modafinil, in its two clinical formulations (Provigil® and Nuvigil®), is a widely prescribed wake-promoting therapeutic agent. It binds competitively to the cell-membrane dopamine (DA) transporter and is dependent on catecholaminergic (dopaminergic and adrenergic) signaling for its wake-promoting effects. The clinical spectrum of effects for modafinil is distinct from the effects seen with other catecholaminergic agents. Relative to other commonly used agents that act through catecholaminergic mechanisms, modafinil has a relatively low abuse potential, produces wakefulness with an attenuated compensatory sleep recovery thereafter, and does not ameliorate cataplexy in narcolepsy. These clinically relevant phenomenological differences between modafinil and agents such as amphetamines and cocaine do not eliminate catecholaminergic effects as a possible mediator of its wake-promoting action; they merely reflect its unique pharmacological profile. Modafinil is an exceptionally weak, but apparently very selective, DA transporter inhibitor. The pharmacodynamic response to modafinil, as measured by DA levels in brain microdialyzate, is protracted relative to other agents that act via catecholaminergic mechanisms. The conformational constraints on the interaction of modafinil with the DA transporter – and probably, as a consequence, its effects on trace amine receptor signaling in the catecholaminergic cell – are unique among catecholaminergic agents. These unique pharmacological properties of modafinil should be considered both in seeking to thoroughly understand its putatively elusive mechanism of action and in the design of novel therapeutic agents.

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“…First, it has been reported that modafinil blocks dopamine transporter in animals and human brain resulted in inhibition of dopamine reuptake 17 . Inhibition of dopamine reuptake increases the extracellular levels of dopamine in the brain leading to disrupting wake-promoting actions in knock-out mice 17 . Blocking the dopamine reuptake may increase dopamine in the nucleus accumbens and can be connected to the drug abuse.…”

Section: Modafinil Tolerancementioning

confidence: 99%