Modafinil
Wake-promoting agents and narcolepsy drugs
Wake-promoting agents and narcolepsy drugs
A wake-promoting drug for excessive sleepiness in narcolepsy, sleep apnoea and shift work. It blocks dopamine reuptake; serious rashes are rare but dangerous.
Quick facts
- Group
- Wake-promoting agents and narcolepsy drugs
- Target
- Dopamine transporter (DAT)
- Used for
- Excessive sleepiness in narcolepsy
- Key effects
- Headache · Nausea · Nervousness and anxiety
- Monitor
- Daytime sleepiness and safety to drive · Skin rash
- ATC
- N06BA07
No doses: the clinician sets them by the current guideline.
Mechanism of action
Its exact mechanism is not known. Modafinil binds the dopamine transporter and blocks dopamine reuptake, so dopamine stays longer in the synapse in wake-promoting circuits; it is not a direct dopamine receptor agonist.
- Binds the dopamine transporter (DAT)
- Less dopamine is taken back into the neuron
- Wake-promoting signalling increases; daytime sleepiness falls
Indications
- Excessive sleepiness in narcolepsy Narcolepsy →
- Residual sleepiness in obstructive sleep apnoea (with airway treatment) Obstructive sleep apnoea →
- Shift work disorder
Adverse effects
Common
- Headache
- Nausea
- Nervousness and anxiety
- Insomnia
- Dizziness and rhinitis
Contraindications
- Known hypersensitivity to modafinil or armodafinil
Key interactions
- Hormonal contraceptives
- Less effective; another method is used during treatment and for one month after stopping
- Cyclosporine
- Lower cyclosporine levels
- CYP2C19 substrates (phenytoin, diazepam, omeprazole)
- Higher levels of these drugs
What is monitored
- Daytime sleepiness and safety to drive
- Skin rash, mood and psychiatric symptoms
- Heart rate and blood pressure in heart disease
Administration and safety
- Given by mouth in the morning, or before the shift in shift work disorder
- Controlled medicine (Schedule IV in the United States)
Pregnancy and breastfeeding
Animal data suggest possible fetal harm; it also makes hormonal contraception unreliable.
Nursing care
- Teach to stop the drug and seek care at the first rash, blisters or mouth sores
- Counsel on a non-hormonal or added contraceptive method
- Ask about psychosis, depression, mania and heart disease
- Remind that it does not replace CPAP in sleep apnoea
Pharmacokinetics
- Metabolism
- Mostly in the liver (about 90%); it induces CYP3A4 and inhibits CYP2C19
- Elimination
- Metabolites in the urine; less than 10% as unchanged drug
- Half-life
- About 15 hours after repeated doses
Test yourself
Think of the answer, then tap the question to see it.
Which transporter does modafinil block?
The dopamine transporter (DAT).
Why is contraception counselling part of modafinil treatment?
It lowers the effectiveness of hormonal contraceptives, during treatment and for a month after.
Does modafinil treat the airway in obstructive sleep apnoea?
No. It treats the residual sleepiness; the airway treatment continues.
Connections
← Back to the class: Wake-promoting agents and narcolepsy drugs
Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.
Sources: DailyMed - MODAFINIL tablet (DailyMed (U.S. National Library of Medicine), 2026); ATCDDD - ATC/DDD Index (WHO Collaborating Centre for Drug Statistics Methodology, 2026).
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Representative model, for educational purposes only.