Modafinil is a drug used to treat sleepiness due to narcolepsy, sleep disturbances due to shift work, or obstructive sleep apnea. It is also used off-label for the alleged improvement of cognitive abilities. However, its efficacy for this application has not been confirmed. It is taken by mouth.
The exact mechanism of action is not fully understood. Modafinil is thought to inhibit the reuptake of dopamine by binding to the dopamine reuptake pump, leading to an increase in extracellular dopamine. Modafinil also activates glutamate receptors while inhibiting GABA channels. Modafinil has less abuse potential than other stimulants (Adderall, Ritalin) because it does not induce significant euphoric effects.
Modafinil is rapidly absorbed in the gastrointestinal tract. Plasma protein binding is approximately 60%. Modafinil is metabolized in the liver and 90% is excreted in the urine. The half-life is between 23 and 215 hours.
Concomitant administration of Modafinil with opioids such as hydrocodone, oxycodone, and fentanyl, as well as various other drugs, may result in a decrease in plasma concentrations.
Common side effects include headache, anxiety, sleep disturbances, and nausea.
Severe side effects may include allergic reactions such as anaphylaxis, Stevens-Johnson syndrome, and hallucinations. The dose may need to be adjusted in people with kidney or liver problems.
It is not recommended in cardiac arrhythmias, significant hypertension, or left ventricular hypertrophy.
There are no data on the safety of modafinil during pregnancy and lactation, so the drug should not be taken during this time.
LD50 (mouse, i.v.): > 800 mg-kg-1
| ATC Code | N06BA07 |
| Formula | C15H15NO2S |
| Molar Mass (g·mol−1) | 273,35 |
| Physical State | solid |
| Density (g·cm−3) | 1,342 |
| Melting Point (°C) | 164–166 |
| CAS Number | 68693-11-8 |
| PUB Number | 4236 |
| Drugbank ID | DB00745 |
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