Eugeroics (originally "eugrégorique" or "eugregoric"),[1] also known as wakefulness-promoting agents and wakefulness-promoting drugs, are a class of drugs that promote wakefulness and alertness.[2][3] They are medically indicated for the treatment of certain sleep disorders including excessive daytime sleepiness (EDS) in narcolepsy or obstructive sleep apnea (OSA).[2][3] Eugeroics are also often prescribed off-label for the treatment of EDS in idiopathic hypersomnia.[4] In contrast to classical psychostimulants, such as methylphenidate and amphetamine, which are also used in the treatment of these disorders, eugeroics typically do not produce marked euphoria, and, consequently, have a lower addictive potential.[2][3][5]
| Eugeroic | |
|---|---|
| Drug class | |
 The chemical structure of modafinil, the prototypical drug of this class | |
| Class identifiers | |
| Synonyms | Wakefulness-promoting agent Wakefulness-promoting drug |
| Use | Promote wakefulness and alertness |
| ATC code | N06B |
| Legal status | |
| In Wikidata | |
Modafinil and armodafinil are each thought to act as selective, weak, atypical dopamine reuptake inhibitors (DRI),[2][3] whereas adrafinil acts as a prodrug for modafinil. Other eugeroics include solriamfetol, which acts as a norepinephrine–dopamine reuptake inhibitor (NDRI),[6][7] and pitolisant, which acts as a histamine 3 (H3) receptor antagonist/inverse agonist.[8][9][10]
Recent research edit
Cephalon, the original U.S. market rights holder of modafinil, has demonstrated initiative in the development of a successor to the prototypical eugeroic.[11] Of the more than twenty compounds preclinically tested in Cephalon's three-part drug discovery series, the compound fluorenol was selected as a lead. Fluorenol was found to induce wakefulness to a greater degree than modafinil, despite possessing a lower affinity for the dopamine transporter.[12]
All currently marketed eugeroics are classified as central nervous system stimulants and possess some (attenuated) stimulant-like properties.[13][14] It is expected that future developments will further distinguish eugeroics from classical CNS stimulants.[15][11]
Examples edit
Marketed edit
- Armodafinil (Nuvigil)
- Modafinil (Provigil)
- Pitolisant (Wakix)[16]
- Solriamfetol (Sunosi)[14]
Discontinued edit
- Adrafinil (Olmifon)
Never marketed edit
- Flmodafinil (CRL-40,940)
- Fluorafinil (CRL-40,941)
- Fluorenol
- Methylbisfluoromodafinil
In development edit
- Selective orexin receptor agonists (two are currently under development by Takeda, danavorexton and TAK-994)[17]
- CE-123 is under patent by Red Bull.[18]