Talk:Eugeroic

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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 used medically for the treatment of certain sleeping disorders, such as excessive daytime sleepiness and narcolepsy.[2][3] Unlike traditional stimulants, they generally have a low addictive potential.[2][3]

The prototypical and most widely known eugeroic is modafinil. Other substances in the class include armodafinil, its enantiopure formulation, and adrafinil, a modafinil prodrug. Modafinil and armodafinil have been found to act as selective, weak, atypical dopamine reuptake inhibitors.[2][3]

Subjective effects

Disclaimer: The effects listed below are taken from the subjective effect index, which is based on anecdotal reports and the personal experiences of PsychonautWiki contributors. As a result, they should be treated with a healthy degree of skepticism. It is worth noting that these effects will rarely (if ever) occur all at once, although higher doses will increase the chances of inducing a full range of effects. Likewise, adverse effects become much more likely on higher doses and may include serious injury or death.

These effects are listed and defined in detail within their own dedicated articles below:

Secondary effects include:

Examples

See also

Literature

  • Engber TM, Koury EJ, Dennis SA, Miller MS, Contreras PC, Bhat RV (January 1998). "Differential patterns of regional c-Fos induction in the rat brain by amphetamine and the novel wakefulness-promoting agent modafinil". Neurosci. Lett. 241 (2-3): 95–8. PMID 9507929. https://doi.org/10.1016/s0304-3940(97)00962-2.
  • Darwish, M.; Kirby, M.; Hellriegel, E. T.; Robertson Jr, P. (2009). "Armodafinil and Modafinil Have Substantially Different Pharmacokinetic Profiles Despite Having the Same Terminal Half-Lives". Clinical Drug Investigation. 29 (9): 613–623. PMID 19663523. https://doi.org/10.2165/11315280-000000000-00000.
  • Milgram, Norton W.; Callahan, Heather; Siwak, Christina (2006). "Adrafinil: A Novel Vigilance Promoting Agent". CNS Drug Reviews. 5 (3): 193–212. https://doi.org/10.1111/j.1527-3458.1999.tb00100.x.

External links

References

  1. Milgram, Norton W.; Callahan, Heather; Siwak, Christina (2006). "Adrafinil: A Novel Vigilance Promoting Agent". CNS Drug Reviews. 5 (3): 193–212. doi:10.1111/j.1527-3458.1999.tb00100.x.
  2. 2.0 2.1 2.2 2.3 "Provigil: Prescribing information" (PDF). United States Food and Drug Administration. Cephalon, Inc. January 2015. Retrieved 16 August 2015.
  3. 3.0 3.1 3.2 3.3 "Nuvigil: Prescribing information" (PDF). United States Food and Drug Administration. Cephalon, Inc. April 2015. Retrieved 16 August 2015.

Notes

A wakefulness-promoting agent (or wakefulness-promoting drug), also known as a eugeroic (originally "eugrégorique" or "eugregoric"), is a type of drug which specifically improves wakefulness and alertness.

They are used mainly in the treatment of sleeping disorders, excessive daytime sleepiness and narcolepsy. They are also used to counteract fatigue and lethargy and to increase motivation and productivity.[medical citation needed] Wakefulness-promoting agents are said to have a low or very low addictive potential. Eugeroic simply means “good arousal,” but eugeroics form a unique class of drugs, which contain only two at present, those being adrafinil and modafinil, (both of which have been developed by Lafon Laboratories of France).

The basis of their uniqueness lies in their ability to only “stimulate when stimulation is required.” As a result, the “highs and lows” associated with other stimulants such as amphetamine, are absent with eugeroics.

Their initial use often produces comments such as, “I can’t tell any difference.” But it is only several hours later, when one realizes that attention and awakeness are the same as earlier, that one is made fully aware of their benefit.

Eugeroics have been designed to treat narcolepsy (sleeping in the day), hypersomnia (excessive sleep) and cataplexy, (a condition of sudden muscular weakness or fatigue).

Yet eugeroics don’t affect normal sleep patterns, nor are they addictive and they Eugeroic simply means “good arousal,” but eugeroics form a unique have far fewer side effects than the current prescribed stimulants.

Modafinil’s Unique Stimulation

One study, (5) on rats suggested that one possible vigilance enhancing property of modafinil was its ability to inhibit the release of GABA, through an action on 5HTP serotonin receptors. However, the doses used were far higher than normal therapeutic doses. So meanwhile, most clinical studies point to modafinil as a unique and highly selective agonist of brain postsynaptic receptor sites called, alpha-1 adrenergic (1,2,7,8,9,10).

These alpha-1 sites are receptive to the neurotransmitter- Norepinephrine (NE). The central function of NE is a fairly recent discovery, it appears to regulate alertness and the waking/ sleep cycle and has a role in the maintenance of attention, memory, learning, cerebral plasticity and even has neuro-protection qualities (2).

Central nervous stimulants (CNS), such as amphetamine or pemoline are the most widely used drugs to treat narcolepsy, hypersomnia and cataplexy, but these have a number of well documented problems, particularly cardiovascular side effects, interference with sleep, psychiatric disturbances and addiction.

Two studies, (3,10) directly compared the affects of modafinil and the “classic” stimulant, d-amphetamine on sleep. Both double blind controls involved about twelve individuals, one study was undertaken with individuals whose mean age was 68, the other on much younger volunteers. They utilized 100mg or 200mg of modafinil, or 10mg or 20mg of d-amphetamine, or a placebo. All the drugs were administered orally and sleep scales, awakening quality and psychometric tests were completed in the morning.

The outcome of both tests showed that d-amphetamine caused a dose dependant impairment of sleep maintenance, but modafinil did not. Here in lies a problem for those who have difficulty staying alert and awake during the day. The use of “classic” stimulants, such as amphetamines, threatens to reduce total sleep time and REM sleep, and this will ultimately mean higher and higher doses are required, thus creating a vicious circle.

On the other hand, modafinil has not been shown to interfere with night time sleep, thus clearly indicating that the two compounds operate by different methods.

The prototypical eugeroic is modafinil, and others.