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Modafinil is generally well-tolerated but can have potential risks and side effects. Common adverse effects of modafinil, experienced by less than 10% of users, include headaches, nausea, and reduced appetite. [92] [93] [20] Anxiety, insomnia, dizziness, diarrhea, and rhinitis are also reported in 5% to 10% of users. [20]
A Cephalon-founded study in which patients were administered modafinil, methylphenidate, and a placebo found that modafinil produces "psychoactive and euphoric effects and feelings consistent with [methylphenidate]." [12] Like modafinil, armodafinil is an inhibitor and/or inducer of certain cytochrome P450 enzymes.
Modafinil is a drug that helps keep people awake and alert (wakefulness-promoting agent or "eugeroic"). [ 1 ] [ 2 ] Most of the listed modafinil analogues are drugs that specifically target dopamine reuptake (reabsorption of a neurotransmitter by a neurotransmitter transporter ) with stronger effects ( selective DRIs with improved potency ...
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The drug has been found to block the dopamine transporter (DAT) by 83%, to a greater extent than methylphenidate without unfavorable concomitant adrenergic effects. [8] The drug is an atypical DRI similarly to modafinil. [11] [1] [9] The affinities for the DAT of flmodafinil's enantiomers and modafinil have also been studied.
The pharmaceutical company Cephalon, the original United States market rights holder of modafinil, has demonstrated initiative in the development of a successor to the prototypical eugeroic. [25] Of the more than twenty compounds preclinically tested in Cephalon's three-part drug discovery series, the compound fluorenol was selected as a lead. [26]
Approved for treating narcolepsy, obstructive sleep apnea, and shift work sleep disorder, modafinil is a wakefulness-promoting drug used to decrease fatigue, increase vigilance, and reduce daytime sleepiness. [1] Modafinil improves alertness, attention, long-term memory, and daily performance in people with sleep disorders. [1] [18]
Both enantiomers of modafinil preferentially bind to the DAT in an inward facing conformation that is associated with atypical dopamine reuptake inhibitor (DRI) profiles. [ 5 ] [ 6 ] Esmodafinil and armodafinil are said to have equipotent pharmacological effects but differing pharmacokinetics (see below).
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