MODAFINIL FOR EXCESSIVE DAYTIME SLEEPINESS: MECHANISM OF ACTION, DOSAGE, AND BENEFITS
July 24, 2021Dave
If you have suffered from excessive daytime sleepiness (EDS), it might be a cause of obstructive sleep apnea (OSA), myotonic dystrophy, shift work disorder, and narcolepsy. Even if you sleep adequately at night, you feel increased fatigue during the daytime, causing impaired physical performance and decreased quality of life. If you’re consuming drugs like neuroleptics, antihistamines, or sedatives, you might also suffer from EDS.
This article explains the effectiveness of modafinil for treating daytime sleepiness and its mechanism of action.
Optimal Treatment Option for EDS:
Modafinil is a stimulant and wakefulness-promoting agent approved by the US Food and Drug Administration (FDA). If you're a patient with obstructive sleep apnea (OSA), modafinil is prescribed along with positive airway pressure treatment. Your brain contains several chemicals that control sleep and wakefulness. Modafinil changes the amount of these chemicals to prevent EDS. It has also been used in the treatment of some neurodegenerative illnesses as a eugeroic medication. (1)
Unlike other stimulants like amphetamines, modafinil possesses minimal side effects (dependence or hyperarousal) and is considered safe. It comes under different brand names like Provigil® and is quite affordable. (2)
The orexins are sleep-suppressing peptides and wakefulness-promoting peptides, the dysfunction of which causes narcolepsy. It activates the neurons of orexins with the symptoms of euphoria and psychoactivation. If you’re a patient of hypersomnia, this medicine can be really helpful with no complaints of fatigue and lack of energy. (3)
Modafinil’s Mechanism of Action:
The way modafinil acts in your brain is still unclear. However, various studies have shown that modafinil has a binding affinity for different receptors at different locations. These receptors or neurotransmitters include angiotensin, glycine, dopamine, neurotensin, GABA, and serotonin. (4)
Various in vitro studies have reported that modafinil increases extracellular dopamine by the interaction with the dopamine reuptake pump, thereby inhibiting the dopamine reuptake. Modafinil has also been proved to inhibit GABA and activate glutamatergic circuits. It also stimulates different receptors because of its alpha 1B-adrenergic agonist effects. (5)
Your body is prepared for action when norepinephrine (a neurotransmitter) is activated. Its reuptake is inhibited by modafinil and increases its concentration because norepinephrine is associated with alertness and wakefulness. (6)
Benefits of Modafinil:
Here are some of the incredible benefits of modafinil based on scientific research:
Enhanced Wakefulness: By affecting many neurotransmitter systems, modafinil decreases EDS and promotes wakefulness in patients with OSA, narcolepsy, and work shift disorder. Modafinil also increases focus and concentration, makes you alert, and reduces daytime sleepiness. (7)
Improved Cognitive Function in Non-Sleep Deprived Adults: The efficacy of modafinil is not limited to only wakefulness; it also boosts cognitive performance in individuals who are non-sleep deprived. As a potent nootropic, modafinil has been linked with improvements in visual processing, decision-making skills, spatial planning, and visual pattern recognition. (8)
Improved Mood and Memory: The nootropic effects of modafinil have also been associated with improvements in performance for both episodic and working memory tasks. Modafinil also has a small effect on improving mood. The benefits of modafinil on improving mood are great for depressed people who describe their mood improvements as “euphoria.” (9,10)
Hangover Cure: Hangovers often result in wasting the day being unmotivated and tired. Modafinil is the hangover cure because it kills the hangover and makes you more focused, alert, and productive.
How to Use Modafinil?
You can take modafinil to treat OSA or narcolepsy with or without food. Modafinil, as approved by the FDA, usually comes in the form of capsules.
For work shift sleep disorder, it is recommended to take it 1 hour before starting your work shift.
The recommended dose of modafinil is 100-200mg taken every morning to promote wakefulness. If you feel well-rested with modafinil, you should continue its use. It is important to note that modafinil is not a cure for your sleep disorder; it only decreases your excessive sleepiness. (11)
A sudden stop to modafinil consumption may cause withdrawal symptoms like shakiness, sweating, dizziness, chills, and confusion. Talk to your doctor If you experience these symptoms.
Modafinil has minimal side effects like anxiety, nausea, fever, restlessness, dizziness, diarrhea, and headaches. Although very few people experience these side effects, awareness of side effects is good. (12)
Easow Mathew M, Biswas T, Fahad S, Patnaik M. Modafinil for excessive daytime sleepiness. Cochrane Database Syst Rev [Internet]. 2017 Jan 20 [cited 2021 May 23];2017(1). Available from: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6464806/
Valentino RM, Foldvary-Schaefer N. Modafinil in the treatment of excessive daytime sleepiness. Cleve Clin J Med. 2007 Aug;74(8):561–6, 568–71.
Modafinil [Internet]. [cited 2021 May 23]. Available from: https://go.drugbank.com/drugs/DB00745
Tobin ML. Why Choose Modafinil for Excessive Daytime Sleepiness? Issues Ment Health Nurs. 2007 Jan 1;28(3):313–7.
Gerrard P, Malcolm R. Mechanisms of modafinil: A review of current research. Neuropsychiatr Dis Treat. 2007 Jun;3(3):349–64.
Modafinil: A Review of Neurochemical Actions and Effects on Cognition | Neuropsychopharmacology [Internet]. [cited 2021 May 23]. Available from: https://www.nature.com/articles/1301534
Effects of Modafinil on Cognitive Performance and Alertness Durin...: Ingenta Connect [Internet]. [cited 2021 May 23]. Available from: https://www.ingentaconnect.com/content/ben/cpd/2006/00000012/00000020/art00002
Cognitive enhancing effects of modafinil in healthy volunteers | SpringerLink [Internet]. [cited 2021 May 23]. Available from: https://link.springer.com/article/10.1007/s00213-002-1250-8
Effect of Pharmacological Enhancement on the Cognitive and C... : Annals of Surgery [Internet]. [cited 2021 May 23]. Available from: https://journals.lww.com/annalsofsurgery/fulltext/2012/02000/effect_of_pharmacological_enhancement_on_the.8.aspx
Modafinil: past, present and future: Expert Review of Neurotherapeutics: Vol 2, No 4 [Internet]. [cited 2021 May 23]. Available from: https://www.tandfonline.com/doi/abs/10.1586/14737126.96.36.1999
Modafinil Oral: Uses, Side Effects, Interactions, Pictures, Warnings & Dosing - WebMD [Internet]. [cited 2021 May 23]. Available from: https://www.webmd.com/drugs/2/drug-16962/modafinil-oral/details
Modafinil: MedlinePlus Drug Information [Internet]. [cited 2021 May 23]. Available from: https://medlineplus.gov/druginfo/meds/a602016.html