armodafinil

N06BA13

Forms & Strengths

Adult Dosing

Narcolepsy: 150 to 250 mg once daily in the morning
Obstructive Sleep Apnea (OSA): 150 to 250 mg once daily in the morning
Shift Work Disorder (SWD): 150 mg once daily approximately 1 hour prior to work shift start
Hepatic impairment: Reduce dose by 50% in severe hepatic impairment
Renal impairment: Safety and efficacy not adequately studied in severe renal impairment

Pediatric Dosing

Children and adolescents (< 18 years): Not recommended due to lack of safety and efficacy data, and risk of serious psychiatric and dermatological adverse reactions

Indications

Improve wakefulness in adult patients with excessive daytime sleepiness associated with narcolepsy
Improve wakefulness in obstructive sleep apnea (OSA) as an adjunct to standard treatment(s) for obstruction
Improve wakefulness in shift work disorder (SWD)

Mechanism of Action

R-enantiomer of modafinil (eugeroic)
Binds to the dopamine transporter (DAT) and inhibits dopamine reuptake, increasing extracellular dopamine levels
Mechanism of wake-promoting action is not fully understood; distinct from sympathomimetic stimulants

Contraindications

Known hypersensitivity to armodafinil, modafinil, or any formulation components
History of rash associated with modafinil or armodafinil use (e.g., Stevens-Johnson syndrome)

Adverse Reactions

Common: Headache, nausea, dizziness, insomnia, dry mouth, anxiety, diarrhea
Serious: Severe rash (Stevens-Johnson syndrome, toxic epidermal necrolysis, DRESS)
Serious: Psychiatric symptoms (mania, delusions, hallucinations, suicidal ideation)
Serious: Cardiovascular events (chest pain, palpitations, hypertension, tachycardia)

Drug Interactions

CYP3A4/5 substrates: Armodafinil is a weak inducer of CYP3A4/5, potentially decreasing concentrations of drugs like oral contraceptives, cyclosporine, and midazolam
CYP2C19 substrates: Inhibits CYP2C19, potentially increasing concentrations of substrates like omeprazole, phenytoin, and diazepam
CYP1A2 inducers/inhibitors: Co-administration with strong CYP3A4/5 and CYP2C19 inducers or inhibitors may alter armodafinil clearance
CNS stimulants: May enhance stimulant effects, increasing risk of adverse cardiovascular and psychiatric events
Hormonal contraceptives: May reduce effectiveness; alternative or additional non-hormonal contraception recommended during treatment and for one month after discontinuation

Curated Content: Needs Vetting Before Put to Clinical Use