Modafinil

What is Modafinil?

Modafinil, also known by its brand name Provigil, is a prescription medication classified as a central nervous system (CNS) stimulant and a "wakefulness-promoting agent" or "eugeroic." It is primarily used to treat excessive daytime sleepiness associated with specific sleep disorders. It is not an amphetamine, but it does have some similarities to traditional stimulants.

Other Names

• Brand Names: Provigil

• Other designations: CRL-40476, CRC-40476

Side Effects and Benefits

Benefits:

• Promotes Wakefulness: Modafinil is highly effective at promoting wakefulness in people with narcolepsy, obstructive sleep apnea, and shift work sleep disorder.

• Improved Cognition: It is often used "off-label" as a "smart drug" or nootropic. Studies have shown it can improve "higher" brain functions like decision-making and planning, particularly during complex, long-duration tasks.

• Mood-Brightening Effects: Some individuals report an improvement in mood while taking modafinil.

• Less Jitteriness: Compared to traditional stimulants like amphetamines, modafinil is generally associated with less jitteriness, anxiety, and rebound effects.

• Memory Enhancement: It has been shown to enhance short-term memory.

Side Effects:

• Common Side Effects: The most common side effects are headache and nausea. Others include nervousness, anxiety, and trouble sleeping.

• Serious Side Effects: Although rare, modafinil can cause serious side effects, including:

  • Severe mental health changes (hallucinations, aggression, suicidal thoughts).

  • Severe skin reactions, such as Stevens-Johnson syndrome, which can be fatal.

  • Heart problems, including chest pain and a faster-than-normal heartbeat.

  • Dependence and misuse, especially with higher dosages.

Pros and Cons

Pros:

• Effective for its intended use: It is a well-validated treatment for sleep disorders like narcolepsy.

• Taken once a day: Its long half-life allows for convenient once-daily dosing.

• Less Jittery: It may cause less anxiety and a "jittery" feeling than other stimulants.

• Cognitive Enhancement: It has been shown to improve cognitive functions in both sleep-deprived and healthy individuals.

Cons:

• Controlled Substance: It is a Schedule IV controlled substance in the U.S., meaning there are specific rules for its prescription and dispensing.

• Potential for Abuse: While its potential for abuse is considered relatively low compared to other stimulants, it can still lead to dependence due to its effect on dopamine levels.

• Long-term effects: Long-term, non-medical use can potentially disrupt natural sleep patterns and may have unknown effects on the brain.

• Serious Side Effects: There is a risk of rare but severe side effects, including psychiatric and dermatological reactions.

Dosage and Frequency

The typical dosage of modafinil is 200 mg, taken orally once a day. The timing depends on the condition being treated:

• Narcolepsy and Obstructive Sleep Apnea: The dose is usually taken in the morning.

• Shift Work Sleep Disorder: The dose is taken about one hour before the start of the work shift.

For people with severe liver problems or who are over 65, a lower dosage (e.g., 100 mg per day) may be recommended. Doses up to 400 mg per day have been used, but there's no consistent evidence that higher doses offer more benefit than 200 mg.

Half-Life and Detection Time

• Half-Life: The effective half-life of modafinil is about 15 hours. The half-life of its metabolites can be longer. This means it takes approximately 15 hours for the body to eliminate half of the drug from the bloodstream.

• Detection Time: The detection time for modafinil can vary depending on the type of test:

  • Blood: Up to 24 hours.

  • Saliva: Up to 48 hours.

  • Urine: Up to 11 days, as the metabolites (like modafinil acid) can be detected for a longer period.

Sterogenic, Progestronic, and Prolactin Effects

• Prolactin: A study in healthy volunteers found that modafinil caused a reduction in prolactin levels.

• Estrogenic and Progestogenic: There is no significant evidence that modafinil has direct estrogenic or progestogenic effects. The drug's primary mechanism of action involves neurotransmitters like dopamine and norepinephrine, not sex hormones.

Anabolic Androgenic Ratio

Modafinil is a central nervous system stimulant, not an anabolic-androgenic steroid. Therefore, it does not have an anabolic-androgenic ratio. This ratio is a measure used for steroids to compare their muscle-building (anabolic) and masculinizing (androgenic) effects. Modafinil's mechanism of action is completely different and does not involve these pathways.