Armodafinil
Wake-promoting agents and narcolepsy drugs
Wake-promoting agents and narcolepsy drugs
The R-enantiomer of modafinil, used for the same kinds of excessive sleepiness. It shares modafinil's rash and contraceptive warnings.
Quick facts
- Group
- Wake-promoting agents and narcolepsy drugs
- Target
- Dopamine transporter (DAT)
- Used for
- Excessive sleepiness in narcolepsy
- Key effects
- Headache · Nausea · Dizziness
- Monitor
- Daytime sleepiness and safety to drive
- ATC
- N06BA13
No doses: the clinician sets them by the current guideline.
Mechanism of action
Armodafinil is the R-enantiomer of modafinil. Its wake-promoting mechanism is not fully known; it acts as an indirect dopamine agonist by binding the dopamine transporter and blocking dopamine reuptake.
- Binds the dopamine transporter, like modafinil
- Dopamine reuptake falls and synaptic dopamine rises
- Wakefulness improves through the day
Indications
- Excessive sleepiness in narcolepsy Narcolepsy →
- Residual sleepiness in obstructive sleep apnoea Obstructive sleep apnoea →
- Shift work disorder
Adverse effects
Common
- Headache
- Nausea
- Dizziness
- Insomnia
Contraindications
- Known hypersensitivity to modafinil or armodafinil
Key interactions
- Hormonal contraceptives
- Less effective during treatment and for one month after
- Cyclosporine
- Lower cyclosporine levels
- CYP2C19 substrates (omeprazole, phenytoin, diazepam)
- Higher levels of these drugs
What is monitored
- Daytime sleepiness and safety to drive
- Rash and psychiatric symptoms
Administration and safety
- Given by mouth once a day, in the morning or before the work shift
- Controlled medicine (Schedule IV in the United States)
- Look-alike name with modafinil: they are not given together
Pregnancy and breastfeeding
Animal studies showed developmental toxicity and human data are limited.
Nursing care
- Teach to stop it and seek care at the first rash, blisters or mouth sores
- Counsel on added or non-hormonal contraception
- Watch mood and signs of misuse
Pharmacokinetics
- Metabolism
- Mainly amide hydrolysis; CYP3A4/5 forms a sulfone metabolite
- Half-life
- About 15 hours
Test yourself
Think of the answer, then tap the question to see it.
How is armodafinil related to modafinil?
It is modafinil's R-enantiomer.
Which contraindication do modafinil and armodafinil share?
Known hypersensitivity to either drug.
Which enzyme family forms armodafinil's sulfone metabolite?
CYP3A4/5.
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 - ARMODAFINIL 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.