Pharmaceutical

Armodafinil

(R)-2-(Diphenylmethylsulfinyl)acetamide

Evidence TierAWADA PROHIBITED

tuneTypical Dose

150 mg

watchEffect Window

Peaks within 2 hours. Half-life is approximately 15 hours.

lockCompliance

WADA PROHIBITED

Overview

Clinical Summary

Armodafinil is the R-enantiomer of modafinil and a prescription wakefulness agent. It treats excessive sleepiness disorders and supports sustained alertness during the day.

Clinical trials show improved wakefulness and reduced daytime sleepiness in narcolepsy, shift work disorder, and sleep apnea-related sleepiness. Cognitive benefits are most apparent under sleep deprivation, improving vigilance and reaction time. Minority studies examine fatigue in neurologic disease and depression, with variable results depending on underlying cause and baseline sleepiness.

R-enantiomer of modafinil. Weak atypical dopamine reuptake inhibitor that elevates hypothalamic histamine and orexin. Longer half-life (~15h) than racemic modafinil (~12h).

Outcomes

What This Is Expected To Influence

Primary Outcomes

  • Reverses cognitive decline and fatigue from sleep deprivation with longer duration than modafinil
  • Highly effective treatment for narcolepsy and shift-work sleep disorder

Secondary Outcomes

  • Improved sustained attention in healthy adults (off-label)
  • Better afternoon alertness maintenance vs racemic modafinil

Safety

Contraindications and Interactions

Contraindications

  • Severe hepatic impairment
  • History of Stevens-Johnson Syndrome
  • Severe cardiac conditions (LVH, mitral valve prolapse)
  • History of psychosis or mania

Side effects

  • Headache
  • Nausea
  • Dizziness
  • Insomnia
  • Anxiety
  • Stevens-Johnson Syndrome (very rare, potentially fatal)

Interactions

  • Hormonal contraceptives (reduced efficacy via CYP3A4 induction)
  • Warfarin (altered INR)
  • Cyclosporine (reduced levels)
  • High-dose caffeine (additive stimulation)

Avoid if

  • History of psychosis or mania
  • Severe anxiety disorders
  • Unstable cardiovascular disease
  • Pregnancy
  • Lactation

Evidence

Study-level References

armodafinil-SRC-001RCT
Sourceopen_in_new

Czeisler CA, et al. "Armodafinil for treatment of excessive sleepiness associated with shift work disorder: a randomized controlled study." Mayo Clin Proc. 2009.

Population: Patients with shift work disorder

Key findings: Armodafinil 150 mg significantly improved wakefulness, overall clinical condition, and long-term memory in patients with excessive sleepiness associated with shift work disorder.

Paper content

Armodafinil 150 mg significantly improved wakefulness, overall clinical condition, and long-term memory in patients with excessive sleepiness associated with shift work disorder.

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