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NERVOUS SYSTEM › PSYCHOANALEPTICS › PSYCHOSTIMULANTS, AGENTS USED FOR ADHD AND NOOTROPICS › Other psychostimulants and nootropics
adrafinil
N06BX17
Forms & Strengths
- Oral capsules: 300 mg
- Oral tablets: 300 mg
Adult Dosing
- Initial dose: 600 mg to 900 mg orally once daily in the morning
- Maintenance dose: 300 mg to 900 mg daily based on clinical response and tolerance
- Maximum recommended dose: 900 mg daily
- Hepatic/Renal impairment: Use with caution and consider lower doses
Pediatric Dosing
- Safety and efficacy in pediatric patients have not been established
- Not recommended for use in children under 18 years of age
Indications
- Excessive daytime sleepiness associated with narcolepsy (off-label or unregulated in many jurisdictions)
- Shift work sleep disorder and chronic fatigue states (unofficial uses)
Mechanism of Action
- Prodrug for modafinil; metabolized in the liver primarily to modafinil and modafinil acid
- Acts as an atypical, weak dopamine reuptake inhibitor
- Increases extracellular dopamine levels in the brain
- Modulates wakefulness-promoting centers in the hypothalamus
Contraindications
- Known hypersensitivity to adrafinil, modafinil, or any components of the formulation
- History of left ventricular hypertrophy or ischemic heart disease
- Mitral valve prolapse with previous stimulants
- Severe hepatic or renal impairment (relative contraindication)
Adverse Reactions
- Common: Headache, insomnia, nervousness, anxiety, nausea, dry mouth
- Cardiovascular: Palpitations, tachycardia, hypertension
- Dermatological: Severe skin rashes, including Stevens-Johnson syndrome (rare, class effect with modafinil)
- Psychiatric: Agitation, irritability, confusion, mania (rare)
Drug Interactions
- CYP3A4/5 inducers (e.g., carbamazepine, phenobarbital): May decrease plasma concentrations of the active metabolite modafinil
- CYP2C19 substrates (e.g., omeprazole, phenytoin): May inhibit their metabolism, increasing their exposure
- Contraceptives: May decrease the efficacy of steroidal contraceptives via CYP3A4 induction
- Central nervous system stimulants: Increased risk of CNS overstimulation, tachycardia, and insomnia
Curated Content: Needs Vetting Before Put to Clinical Use