What is modafinil actually and how does it work?

Modafinil is a wakefulness-promoting drug that is used to treat excessive sleepiness caused by narcolepsy, shift work sleep disorder, and obstructive sleep apnea/hypopnea syndrome. It is also used as a cognitive enhancer to boost memory and attention.

Modafinil may decrease the effectiveness of hormonal birth control (pills, patches, rings, injections). Use an alternate form of birth control while taking this medication and for 1 month afterward.

How Does Modafinil Work?

For people with narcolepsy and other sleep disorders, Modafinil 200 Australia helps to reduce excessive daytime sleepiness. However, it does not treat the underlying cause. It is important to continue to get enough good quality sleep, and to use any other treatments (such as the CPAP machine or mouth device) that your doctor has recommended.

Like other stimulants, Modafinil makes you feel awake and alert. But it is different from amphetamines in that it does not increase heart rate or blood pressure. It is also thought to have less of a potential for abuse. It does this by inhibiting the dopamine reuptake pump and by activating glutamatergic circuits while inhibiting GABA.

Studies of healthy individuals have found that Modafinil enhances cognitive performance. It improves digit span, visual recognition memory, and spatial planning. In addition, it appears to improve working memory and inhibit pre-potent responding. Several studies of patients with narcolepsy have shown similar results.

It is a central nervous system stimulant, and it can cause side effects such as headache, nausea, dizziness, difficulty sleeping and mental/mood changes (including agitation, confusion, hallucinations). Therefore, women who take this medication should use another method of contraception.

Modafinil Mechanism of Action

Modafinil has been shown to increase wakefulness in patients with narcolepsy, allowing them to stay awake longer and complete tasks they normally find difficult or impossible. It also improves memory and enhances cognitive control processes. These effects are attributed to its ability to interact with certain neurotransmitter systems, particularly those in the frontal cortex.

Modafinil is able to reduce symptoms of fatigue and enhance performance in conditions such as narcolepsy, jet lag, and ADHD. It is also used as a study drug to help people concentrate for long periods of time, such as high school students taking exams or college students studying for finals.

It has been suggested that Modawake 200 mg induces alertness via direct inhibition of dopamine reuptake and indirect inhibition of noradrenalin reuptake in the VLPO. It also increases histamine release from the hypothalamus and causes an indirect increase in glutamate in the medial prefrontal cortex by inhibiting GABA reuptake (Stowe et al., 1995).

Another proposed mechanism is that Modafinil acts as an orexin receptor agonist to stimulate sleep-promoting activities in narcoleptic patients. This idea is supported by the fact that Modafinil increases Fos-immunoreactivity in orexin cells within the perifornical area of narcoleptic mice and rats, and also has partial wake-promoting activity in orexin receptor knockout animals (Chemelli et al., 1999).

It has been shown that Modafinil also interacts with the catecholamine transporters DAT and NET with modest potency. It has been found that Modafinil inhibits the reuptake of DA, NE and 5HT with equal potency to amphetamine and methylphenidate. In addition, it can cause significantly elevated extracellular levels of DA, NE and 5HT in the brain.

Modafinil Effects on the Brain

Modafinil has a modest affinity for DAT but does not appear to bind to a wide range of other monoamine and neuropeptide receptors, transporters or nerve membrane ion channels. It also does not appear to exert direct effects on second messenger systems.

Modafinil causes dose-dependent increases in the performance of rats on a delayed nonmatching to position task, with performance improving even after a delay (Ward et al, 2004). It also has a positive effect on a serial reversal discrimination task and increases levels of plasma corticosterone in response to stress, which is inversely correlated with working memory performance.

It increases dopamine release from the hypothalamus and medial preoptic area (Ferraro et al, 1999) but not from the striatum or nucleus acumens (Ferraro et al, 1992). However, in narcoleptic patients treated with Modafinil for 3 weeks, a doubling of the dosage was associated with a decline in prefrontal cortex activity as measured by scalp EEG, which correlated with performance on the Pauli test.

Modafinil acts as a wakefulness-promoting agent by activating a family of wakefulness-promoting and sleep-suppressing peptides in the prefrontal cortex, including orexin neurons. It also has stimulant-like effects in humans, causing arousal and increasing levels of cerebral blood flow. It enhances vigilance in subjects with chronic fatigue syndrome and improves narcolepsy in those with dysfunction of the orexin system (Rambert et al, 2000).

Interestingly, it has been found to increase performance on a digit symbol substitution task in schizophrenia patients with prominent negative symptoms when added to an antipsychotic regimen (Spence et al, 2005). This effect is associated with increased activation of the dorsolateral cingulate cortex.

Modafinil Side Effects

Modafinil is known to reduce fatigue in a variety of neurological and medical illnesses, including multiple sclerosis, idiopathic Parkinson’s disease, chronic fatigue syndrome, fibromyalgia, HIV infection and post-anaesthetic sedation. It is also known to have improved cognitive function, particularly in tasks requiring attention and concentration. These effects are believed to be mediated by its actions on the frontal cortex.

Despite its wide use and apparent safety, it is important to note that Modafinil may have serious side effects. It is therefore important to discuss its risks with your doctor before starting this medication. Tell your doctor if you have:

Cardiovascular disease: If you have heart problems (including high blood pressure, a history of heart attack or stroke), a personal or family history of psychiatric disorders, or a history of using amphetamines/stimulant medications, you should be closely monitored for adverse cardiovascular events while taking Modafinil.

Psychosis/mania: If you have a history of psychotic disorder or mania, you should not take this medication. People with a history of these disorders should be carefully monitored for symptoms such as hallucinations, delusions, aggression and suicidal thoughts while taking Modafinil.