Armodafinil and Modafinil Have Substantially Different Pharmacokinetic Profiles Despite Having the Same Terminal Half-Lives

  title={Armodafinil and Modafinil Have Substantially Different Pharmacokinetic Profiles Despite Having the Same Terminal Half-Lives},
  author={Mona Darwish and Mary Kirby and Edward T. Hellriegel and Philmore Jr. Robertson},
  journal={Clinical Drug Investigation},
AbstractBackground and objective: Armodafinil, a non-amphetamine, wakefulness-promoting medication, is the R- and longer-lasting isomer of racemic modafinil. [] Key Method Non-compartmental pharmacokinetic parameters were assessed. Results: Armodafinil and modafinil both had a mean single-dose terminal elimination half-life of∼13 hours, with similar mean maximum plasma drug concentration (Cmax) and median time to Cmax values.

Systemic Exposure to Armodafinil and Its Tolerability in Healthy Elderly versus Young Men

Systemic exposure following administration of armodafinil is increased in the elderly in comparison with younger subjects, particularly in those aged ≥75 years, and consideration should be given to the use of lower dosages of armo-sleepiness for the management of excessive sleepiness in older patients, particularly the very elderly.

Armodafinil and Modafinil in Patients With Excessive Sleepiness Associated With Shift Work Disorder: A Pharmacokinetic/Pharmacodynamic Model for Predicting and Comparing Their Concentration‐Effect Relationships

Armodafinil, the longer lasting R‐isomer of racemic modafinil, improves wakefulness in patients with excessive sleepiness associated with shift work disorder (SWD). Pharmacokinetic studies suggest

Population Pharmacokinetic Modeling of Armodafinil and Its Major Metabolites

These population pharmacokinetic models were from the largest population of adults reported to date and provide a robust characterization of the pharmacokinetics of armodaf inil, R‐modafinil acid, and modafinIL sulfone in adults.

Pharmacokinetic evaluation of armodafinil for the treatment of bipolar depression

Armodafinil is well tolerated and presents a possible new treatment option for bipolar depression, however, further investigation is still needed in order to confirm its efficacy and to clarify its role in the treatment of bipolar depression.

Armodafinil versus Modafinil in Patients of Excessive Sleepiness Associated with Shift Work Sleep Disorder: A Randomized Double Blind Multicentric Clinical Trial

Armodafinil was found to be safe and effective in the treatment of SWSD in Indian patients and the study did not demonstrate any difference in efficacy and safety of armodaf inil 150 mg and modafinils 200 mg.

Investigation of a Possible Interaction Between Quetiapine and Armodafinil in Patients With Schizophrenia: An Open‐Label, Multiple‐Dose Study

The data do not suggest that the observed decrease in systemic exposure to quetiapine was associated with a change in disease state, but patients with schizophrenia should be monitored during combination therapy with quet iapine and armodafinil.

Armodafinil in the treatment of excessive sleepiness

  • R. Bogan
  • Medicine, Biology
    Expert opinion on pharmacotherapy
  • 2010
Armodafinil is a useful therapy for the treatment of excessive sleepiness arising from a number of clinical conditions and has a low potential for abuse or tolerance.

Safety and Efficacy of Armodafinil in the Treatment of Excessive Sleepiness

Current evidence suggests that armodafinil significantly improves wakefulness in patients with excessive sleepiness in studies up to 12 weeks, and should be considered safe for use and monitored for adverse effects, particularly cardiovascular complications.



Comparison of Steady-State Plasma Concentrations of Armodafinil and Modafinil Late in the Day Following Morning Administration

At steady state, armodaf inil produces consistently higher plasma drug concentrations late in the day than modafinil when compared on a milligram- to-milligram basis following once-daily administration.

Clinical Pharmacokinetic Profile of Modafinil

The results show that modafinil is a moderately long-lived drug that is well absorbed and extensively metabolised, and has potential to affect the pharmacokinetics of drugs that are metabolised by certain CYP enzymes.

The efficacy and safety of armodafinil as treatment for adults with excessive sleepiness associated with narcolepsy*

Armodafinil significantly improved ability to sustain wakefulness throughout the day in patients with narcolepsy and also significantly improved overall clinical condition, memory, attention, and fatigue when compared with placebo.

Pharmacodynamic effects on alertness of single doses of armodafinil in healthy subjects during a nocturnal period of acute sleep loss*

Armodafinil improved alertness at all doses studied and both drugs were well tolerated; however, further research on the efficacy, safety, and tolerability of armodaf inil in patients with disorders of excessive sleepiness (ES) is required.

Dosing Regimen Effects of Modafinil for Improving Daytime Wakefulness in Patients With Narcolepsy

Modafinil significantly improved patients' ability to sustain wakefulness, as demonstrated by mean sleep latency at week 3 compared with placebo at baseline, and a split-dose 400-mg regimen may be superior to once-daily dosing for sustaining wakefulness throughout the entire waking day.

Effects of Modafinil on Wakefulness and Executive Function in Patients With Narcolepsy Experiencing Late-Day Sleepiness

For patients with residual late-day sleepiness associated with narcolepsy, an additional 200-mg dose of modafinil taken at midday was effective in sustaining wakefulness throughout the entire waking day.

Open‐Label, Single‐Dose Pharmacokinetic Study of Modafinil Tablets: Influence of Age and Gender in Normal Subjects

Results from this study indicated that there were age and gender effects on modafinil clearance processes, and the clearance rate in males decreased with age while young females cleared modaf inil at a faster rate than young males.

Dose effects of modafinil in sustaining wakefulness in narcolepsy patients with residual evening sleepiness.

In patients who experience excessive sleepiness in the late afternoon/evening, despite satisfactory treatment earlier in the day, a split dose of modafinil may promote wakefulness throughout the waking day.

Armodafinil improves wakefulness and long-term episodic memory in nCPAP-adherent patients with excessive sleepiness associated with obstructive sleep apnea

Adjunct treatment with armodafinil significantly improved wakefulness, long-term memory, and patients’ ability to engage in activities of daily living in nCPAP-adherent individuals with ES associated with OSA.