Mechanism of Action

Modafinil's mechanism of action is not fully understood, but it is thought to activate orexin/hypocretin neurons in the hypothalamus, which are responsible for maintaining wakefulness (10). Its wakefulness-promoting effects may also be related to a reduction in gamma aminobutyric acid-ergic transmission and some potentiation of dopaminergic and noradrenergic function. An intact noradrenergic system is essential for the optimal wakefulness-promoting effects from modafinil, although it does not seem to have direct alpha-1 adrenergic agonist effects and it does not inhibit monoamine oxidase (10).

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