Wakefulness-promoting agents

Engber T. M., Koury E. J., Dennis S. A. et al. (1998). Differential patterns of regional c-Fos induction in the rat brain by amphetamine and the novel wakefulness-promoting agent modafinil. Neurosci. Lett. 241, 95-8. 

Prior to the use of wakefulness-promoting agents, and in some pediatric patients, maintenance of wakefulness is dependent on stimulant medications and antidepressants. The safety of such medications during reproductive years and the risk of driving accidents without medication are typically handled during discussions between the prescribing practitioner and the patient. Irritability, anxiety, and erectile or ejaculatory dysfunction have been reported with these medications (78). The costs of newly approved medications for the treatment of narcolepsy,... 

Wake-promoting Agents (Stimulants) (See Also Chap. 20)... 

For military operations, the ideal wake-promoting agent would restore cognitive readiness to well-rested levels with few side effects (to include minimal interfer-... 

Engber, T.M., Dennis, S.A., Jones, B.E., Miller, MS, Contreras, PC. Brain regional substrates for the actions of the novel wake-promoting agent modafinil in the rat comparison with amphetamine. Neuroscience 1998 87(4) 905-911. 

Whatever the reason for insufficient sleep, the sleepiness and neurobehav-ioral consequences seem inevitable. Prevention of sleep deprivation through lifestyle management, and perhaps with hypnotics, would be first- and second-line recommendations for most situations. However, there are instances in which sleepiness cannot be managed with those approaches. Wake-promoting agents would seem very appropriate for use in some of these situations. It should be noted that the use of medications to modulate the effects of lifestyle is not unique to sleep medicine. The use of artificial sweeteners or lipid-lowering agents, often to correct the effect of inappropriate nutritional choices, has become an acceptable part of daily food selection as well as medical practice. 

Gallopin T, Luppi PH, Rambert FA, Frydman A, Fort P (2004) Effect of the wake-promoting agent modafinil on sleep-promoting neurons from the ventrolateral preoptic nucleus an in vitro pharmacologic study. Sleep 27 19-25... 

Modafinil another wakefulness promoting agent with an unknown mechanism of action used for narcolepsy in adults and being studied for use in children at present dose range is 1 Of MOO mg/day divided bid. Side effects include headaches, anxiety, nausea and nervousness. 

Modafinil is a wake-promoting agent whose specific biochemical mechanism of action is obscure. It increases brain concentrations of dopamine after chronic administration in animals but has no overtly stimulant effect like amphetamines. It appears to have a slow onset and its action lasts 8-12 h abuse potential is very low. Modafinil is used in narcolepsy and other hypersomnias and has also been studied in normal people who need to stay awake for long periods and fimction well. 

Modafinil is a benzhydrylsulfinylacetamide wake-promoting agent for oral administration (1). It selectively targets neuronal pathways in the sleep/wake centers of the brain. It is well absorbed and its half-life is about 12-15 hours, which largely reflects the half-life of its levorotatory enantiomer. It... 

We are interested in developing H3 antagonists as potential wake promoting agents and recently described a new series of H3 antagonists derived from the natural product Conessine, a known H3 antagonist. While compounds from this series showed excellent potency and selectivity for the H3 receptor, their pharmacokinetic (PK) profiles and structural complexity prompted us to study other chemical scaffolds. 

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