Armodafinil

Trade Names:
Nuvigil
- Tablets 50 mg
- Tablets 150 mg
- Tablets 250 mg

Pharmacology

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Wakefulness-promoting agent; however, the precise mechanism is unknown.

Pharmacokinetics

Absorption

Readily absorbed after oral administration. C _max approximately 2 h. Food delays T _max approximately 2 to 4 h. Steady state is reached within 7 days of dosing.

Distribution

Vd is approximately 42 L. Binding to plasma protein, primarily albumin, is 60%.

Metabolism

Undergoes hydrolytic deamidation (with sulfone formation by CYP3A4/5), S-oxidation, and aromatic ring hydroxylation, with subsequent glucuronide conjugation of the hydroxylated products.

Elimination

Terminal t _½ is approximately 15 h. Oral CrCl is approximately 33 mL/min. Mainly eliminated by hepatic metabolism with less than 10% excreted in the urine.

Indications and Usage

Improve wakefulness in patients with excessive sleepiness associated with obstructive sleep apnea/hypopnea syndrome, narcolepsy, and shift work sleep disorder.

Contraindications

Hypersensitivity to modafinil or armodafinil or any component of the product.

Dosage and Administration

PO 150 or 250 mg as a single dose in the morning.

PO 150 mg daily approximately 1 h prior to the start of work shift.

General Advice

• Consider dosage adjustments for drugs that are substrates for CYP3A4/5.

Storage/Stability

Store at 68° to 77°F.

Drug Interactions

Plasma concentration may be elevated by armodafinil, increasing the risk of adverse reactions. Dosage reduction of these agents may be necessary.

Plasma concentrations may be reduced by armodafinil, decreasing efficacy.

Armodafinil concentrations may be reduced, decreasing efficacy.

Armodafinil concentrations may be elevated, increasing the risk of adverse reactions.

Laboratory Test Interactions

None well documented.

Adverse Reactions

Cardiovascular

Palpitations (2%); increased heart rate (1%).

CNS

Headache (23%); insomnia (6%); dizziness (5%); anxiety (4%); depression (3%); fatigue (2%); agitation, attention disturbance, decreased appetite, depressed mood, migraine, nervousness, paresthesia, pyrexia, thirst, tremor (1%).

Dermatologic

Rash (4%); contact dermatitis, hyperhidrosis (1%).

GI

Nausea (9%); dry mouth (7%); diarrhea (4%); dyspepsia, upper abdominal pain (2%); anorexia, constipation, loose stools, vomiting (1%).

Lab Tests

Increased gamma-glutamyltransferase (1%).

Respiratory

Dyspnea (1%).

Miscellaneous

Influenza-like illness, pain, seasonal allergy (1%).

Precautions

Pregnancy

Category C .

Lactation

Undetermined.

Children

Safety and efficacy not established in patients younger than 17 yr of age.

Elderly

Consider using lower doses in elderly patients because of possible reduced drug elimination.

Hypersensitivity

Rare cases of angioedema, anaphylactoid reactions, and multiorgan hypersensitivity have been reported.

Hepatic Function

Reduce dose in patients with severe hepatic function impairment.

CNS

Psychotic episodes have been reported.

CV system

Use with caution in patients with recent history of MI or unstable angina. Avoid use in patients with history of left ventricular hypertrophy or in patients with mitral valve prolapse who have experienced mitral valve prolapse syndrome with previously administered CNS stimulants.

Drug abuse

Because of psychoactive and euphoric effects, armodafinil has potential for abuse.

Persistent sleepiness

Wakefulness may not return to normal.

Severe rash

Life-threatening rash, including Stevens-Johnson syndrome, toxic epidermal necrolysis, and drug rash with eosinophilia and systemic symptoms may occur.

Patient Information

• Advise patient to read the patient information leaflet before using product the first time and with each refill.
• Advise patients that the drug affects the CNS and may impair judgment or thinking skill, and to use caution while driving, riding a bike, or performing other tasks until they are certain that therapy will not adversely affect their ability to engage in such activities.
• Advise patients that drug may improve, but not eliminate, abnormal tendency to fall asleep.
• Inform patients to take their previously prescribed treatments.
• Advise patients to notify health care provider if they experience anxiety, chest pain, depression, or signs of psychosis or mania.
• Advise patients to notify health care provider if they develop blisters, hives, mouth sores, peeling skin, rash, trouble swallowing or breathing, or a related allergic phenomenon.
• Advise women who become pregnant or intend to become pregnant during therapy to notify health care provider.
• Advise women who are breast-feeding to notify health care provider.
• Advise patients to avoid alcohol while taking this medication.

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