Eugeroic Explained

Synonyms:Wakefulness-promoting agent
Wakefulness-promoting drug
Use:Promote wakefulness and alertness
Atc Prefix:N06B

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. They are medically indicated for the treatment of certain sleep disorders including excessive daytime sleepiness (EDS) in narcolepsy or obstructive sleep apnea (OSA). Eugeroics are also often prescribed off-label for the treatment of EDS in idiopathic hypersomnia.[2] 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.[3]

Modafinil and armodafinil are each thought to act as selective, weak, atypical dopamine reuptake inhibitors (DRI),[4] [5] 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

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] It is expected that future developments will further distinguish eugeroics from classical CNS stimulants.[14]

Examples

Marketed

Discontinued

Never marketed

In development

Notes and References

  1. Milgram. Norton W.. Callahan. Heather. Siwak. Christina. Adrafinil: A Novel Vigilance Promoting Agent. CNS Drug Reviews. 5. 3. 2006. 193–212. 1080-563X. 10.1111/j.1527-3458.1999.tb00100.x. free.
  2. Web site: Practice Parameters for the Treatment of Narcolepsy and other Hypersomnias of Central Origin. September 2007. American Academy of Sleep Medicine (AASM).
  3. Taneja . Indu . Haman . Kirsten . Shelton . Richard C. . Robertson . David . February 2007 . A randomized, double-blind, crossover trial of modafinil on mood . Journal of Clinical Psychopharmacology . 27 . 1 . 76–79 . 10.1097/jcp.0b013e31802eb7ea . 0271-0749 . 17224718. 40801601 .
  4. Web site: Provigil: Prescribing information. United States Food and Drug Administration. Cephalon, Inc. 16 August 2015. January 2015.
  5. Web site: Nuvigil: Prescribing information. United States Food and Drug Administration. Cephalon, Inc. 16 August 2015. April 2015.
  6. Stahl . Stephen M. . Pradko . James F. . Haight . Barbara R. . Modell . Jack G. . Rockett . Carol B. . Learned-Coughlin . Susan . 2004-08-13 . A Review of the Neuropharmacology of Bupropion, a Dual Norepinephrine and Dopamine Reuptake Inhibitor . The Primary Care Companion to the Journal of Clinical Psychiatry . 06 . 4 . 159–166 . 10.4088/PCC.v06n0403 . 1523-5998 . 514842 . 15361919.
  7. Book: Stahl, Stephen M. . Stahl's Illustrated Antidepressants . 2009-03-02 . Cambridge University Press . 978-0-521-75852-9 . en.
  8. Schwartz . Jean-Charles . The histamine H3 receptor: from discovery to clinical trials with pitolisant: H3 Receptor: from discovery to clinical trials . British Journal of Pharmacology . 2011 . en . 163 . 4 . 713–721 . 10.1111/j.1476-5381.2011.01286.x. 21615387 . 3111674 .
  9. Kollb-Sielecka . Marta . Demolis . Pierre . Emmerich . Joseph . Markey . Greg . Salmonson . Tomas . Haas . Manuel . The European Medicines Agency review of pitolisant for treatment of narcolepsy: summary of the scientific assessment by the Committee for Medicinal Products for Human Use . Sleep Medicine . 2017 . en . 33 . 125–129 . 10.1016/j.sleep.2017.01.002. 28449891 .
  10. Inocente . Clara . Arnulf . Isabelle . Bastuji . Hélène . Thibault-Stoll . Anne . Raoux . Aude . Reimão . Rubens . Lin . Jian-Sheng . Franco . Patricia . Pitolisant, an Inverse Agonist of the Histamine H3 Receptor: An Alternative Stimulant for Narcolepsy-Cataplexy in Teenagers With Refractory Sleepiness . Clinical Neuropharmacology . 2012 . en . 35 . 2 . 55–60 . 10.1097/WNF.0b013e318246879d . 22356925 . 36336966 . 0362-5664.
  11. Dunn . Derek . Hostetler . Greg . Iqbal . Mohamed . Messina-McLaughlin . Patricia . Reiboldt . Alyssa . Lin . Yin Guo . Gruner . John . Bacon . Edward R. . Ator . Mark A. . Chatterjee . Sankar . 2012-03-15 . Wake-promoting agents: search for next generation modafinil: part I . Bioorganic & Medicinal Chemistry Letters . 22 . 6 . 2312–2314 . 10.1016/j.bmcl.2011.12.099 . 1464-3405 . 22264475.
  12. Dunn . Derek . Hostetler . Greg . Iqbal . Mohamed . Marcy . Val R. . Lin . Yin Guo . Jones . Bruce . Aimone . Lisa D. . Gruner . John . Ator . Mark A. . Bacon . Edward R. . Chatterjee . Sankar . 2012-06-01 . Wake promoting agents: Search for next generation modafinil, lessons learned: Part III . Bioorganic & Medicinal Chemistry Letters . 22 . 11 . 3751–3753 . 10.1016/j.bmcl.2012.04.031 . 22546675 . 0960-894X.
  13. Inocente . Clara . Arnulf . Isabelle . Bastuji . Hélène . Thibault-Stoll . Anne . Raoux . Aude . Reimão . Rubens . Lin . Jian-Sheng . Franco . Patricia . 2012 . Pitolisant, an inverse agonist of the histamine H3 receptor: an alternative stimulant for narcolepsy-cataplexy in teenagers with refractory sleepiness . Clinical Neuropharmacology . 35 . 2 . 55–60 . 10.1097/WNF.0b013e318246879d . 1537-162X . 22356925. 36336966 .
  14. Kim . Dongsoo . 2012-02-22 . Practical Use and Risk of Modafinil, a Novel Waking Drug . Environmental Health and Toxicology . 27 . e2012007 . 10.5620/eht.2012.27.e2012007 . 2233-6567 . 3286657 . 22375280.
  15. Web site: How WAKIX Works WAKIX® (pitolisant) tablets. wakix.com. 2020-01-03.
  16. Web site: What is SUNOSI® (solriamfetol) Treatment ? SUNOSI® for Patients. www.sunosi.com. en. 2020-01-03.
  17. Web site: New Data Presented at World Sleep Congress Demonstrate Early Signs of Efficacy for TAK-925, a Selective Orexin Type-2 Receptor (OX2R) Agonist, in Patients with Narcolepsy Type 1. www.takeda.com. en. 2019-12-06.
  18. Web site: Thiazole and diphenyl substituted sulfoxides for use in improving cognition functions and against addictions to substances. - Patent EP-3792252-A1 - PubChem . 2022-09-26 . pubchem.ncbi.nlm.nih.gov.

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