Modalert is a prescription medication containing modafinil, a wakefulness-promoting agent indicated for the improvement of wakefulness in patients with excessive sleepiness associated with narcolepsy, obstructive sleep apnea (OSA), and shift work sleep disorder (SWSD). It is classified as a Schedule IV controlled substance in the United States due to its potential for dependence. This product card provides a comprehensive, expert-level overview of its specifications, therapeutic benefits, and essential safety information for healthcare professionals and informed patients. Its primary mechanism of action is not fully understood but is believed to involve the selective activation of specific wake-promoting neuronal systems, including those utilizing dopamine, norepinephrine, and orexin/hypocretin, without widespread generalized CNS stimulation.

Features

• Active Ingredient: Modafinil (100 mg or 200 mg tablets)
• Drug Class: Eugeroic (Wakefulness-Promoting Agent) / Central Nervous System Stimulant
• Dosage Form: Oral tablet
• Bioavailability: High, with peak plasma concentrations occurring within 2-4 hours post-administration.
• Half-Life: Approximately 15 hours, allowing for once-daily dosing.
• Metabolism: Primarily hepatic, via CYP3A4/5-mediated pathways, with subsequent renal excretion.
• Schedule: C-IV Controlled Substance (US)

Benefits

• Promotes sustained wakefulness and alertness, enabling patients with sleep disorders to maintain normal daytime function.
• Improves objective measures of attention, including ability to sustain focus and reduce lapses in attention during monotonous tasks.
• May enhance certain aspects of cognitive function, such as working memory and executive function, in individuals with sleep deprivation.
• Offers a favorable side effect profile compared to traditional stimulants like amphetamines, with a lower incidence of euphoria, rebound hypersomnia, and significant cardiovascular effects.
• Once-daily dosing regimen supports patient adherence and consistent therapeutic coverage throughout the waking day.

Common use

Modalert (modafinil) is FDA-approved for the treatment of excessive sleepiness associated with:

• Narcolepsy: A chronic neurological disorder characterized by overwhelming daytime drowsiness and sudden attacks of sleep.
• Obstructive Sleep Apnea (OSA): As adjunctive therapy to standard treatment (e.g., continuous positive airway pressure, CPAP) for residual excessive sleepiness. It is not a treatment for the underlying airway obstruction.
• Shift Work Sleep Disorder (SWSD): For individuals who experience insomnia during scheduled sleep periods or excessive sleepiness during scheduled wake periods due to a work schedule that overlaps with the typical sleep period.

Its use for cognitive enhancement in healthy individuals (“off-label” use) is not approved by regulatory agencies and is not recommended due to a lack of long-term safety data and potential risks.

Dosage and direction

• The recommended dose for narcolepsy and OSA is 200 mg administered orally once daily in the morning.
• The recommended dose for SWSD is 200 mg administered orally approximately 1 hour prior to the start of the work shift.
• Doses of 400 mg daily have been well-tolerated but demonstrate no consistent additional benefit.
• For patients with severe hepatic impairment, a reduced dose of 100 mg daily is recommended.
• The tablet should be swallowed whole with a glass of water. It may be taken with or without food, although a slight delay in absorption may occur if taken with a high-fat meal.
• Dosing should be individualized based on clinical response and tolerability.

Precautions

• Potential for Dependence: Although the risk is lower than with amphetamines, Modalert has a known potential for psychological or physical dependence. Caution is advised in patients with a history of drug or alcohol abuse.
• Cardiovascular Effects: Increases in blood pressure and heart rate have been observed. Patients, especially those with underlying hypertension or cardiovascular disease, should have their blood pressure monitored regularly.
• Psychiatric Symptoms: New or exacerbated psychiatric symptoms, including anxiety, mania, depression, hallucinations, and psychosis, have been reported. Use with caution in patients with a history of psychosis, depression, or mania.
• Serious Skin Reactions: Rare but serious skin reactions, including Stevens-Johnson Syndrome (SJS), Toxic Epidermal Necrolysis (TEN), and Drug Reaction with Eosinophilia and Systemic Symptoms (DRESS) have been reported. The drug should be discontinued at the first sign of rash.
• Pregnancy and Lactation: Modalert is Pregnancy Category C. There are no adequate and well-controlled studies in pregnant women. It should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. It is not known if modafinil is excreted in human milk; a decision should be made to discontinue nursing or discontinue the drug.

Contraindications

Modalert is contraindicated in patients with:

• Known hypersensitivity to modafinil, armodafinil, or any inactive ingredient in the formulation.
• History of left ventricular hypertrophy or ischemic ECG changes, chest pain, arrhythmias, or other clinically significant manifestations of mitral valve prolapse in association with CNS stimulant use.

Possible side effect

Common side effects (≥1%) include:

• Headache
• Nausea
• Nervousness
• Anxiety
• Insomnia
• Dizziness
• Diarrhea
• Dry mouth
• Rhinitis

Less common but serious side effects require immediate medical attention:

• Severe skin rash or blistering
• Symptoms of psychosis (e.g., hallucinations, delusions)
• Symptoms of heart problems (e.g., chest pain, palpitations, shortness of breath)
• Symptoms of allergic reaction (e.g., swelling of face, eyes, lips, tongue, or throat; difficulty swallowing or breathing; hives)

Drug interaction

Modalert has the potential for several significant drug interactions:

• CYP3A4 Inducers/Inhibitors: Drugs that induce CYP3A4 (e.g., carbamazepine, phenobarbital, rifampin) may decrease modafinil plasma concentrations. Drugs that inhibit CYP3A4 (e.g., ketoconazole, itraconazole) may increase modafinil plasma concentrations.
• CYP2C19 Substrates: Modalert is a weak inducer of CYP2C19. It may decrease the plasma concentrations of drugs metabolized by this enzyme (e.g., diazepam, phenytoin, propranolol, omeprazole).
• Hormonal Contraceptives: Modalert can significantly reduce the effectiveness of ethinyl estradiol-containing oral contraceptives, implants, and patches by inducing their metabolism. Women of childbearing potential should use an alternative or additional method of contraception while taking modafinil and for one month after discontinuation.
• Warfarin (Coumadin): Modalert may alter the metabolism of warfarin. Prothrombin time (INR) should be monitored more frequently during and for up to two months after discontinuing modafinil therapy.
• Cyclosporine: Blood concentrations of cyclosporine may be reduced; monitoring of levels is recommended.
• Other CNS Active Drugs: The combined use with other psychoactive drugs may produce additive effects. Caution should be exercised when modafinil is given in combination with other CNS stimulants or MAO inhibitors.

Missed dose

If a dose is missed, it should be taken as soon as possible on the same day. However, if it is late in the day, the missed dose should be skipped to prevent nighttime insomnia. Do not double the next dose.

Overdose

• Symptoms: Overdose may manifest as excitation or agitation, insomnia, anxiety, slight-to-moderate elevations in hemodynamic parameters (heart rate, blood pressure), and other CNS effects. In massive overdoses, more severe symptoms could theoretically occur.
• Management: There is no specific antidote for modafinil overdose. Management consists of instituting supportive care aimed at stabilizing the patient. This includes cardiovascular monitoring and symptomatic treatment. The long half-life of the drug should be considered when determining the duration of monitoring.

Storage

• Store at room temperature between 20°C to 25°C (68°F to 77°F).
• Excursions permitted between 15°C and 30°C (59°F and 86°F).
• Keep in the original container, tightly closed, and out of reach of children and pets.
• Protect from excessive moisture and light.

Disclaimer

This information is for educational and informational purposes only and is not a substitute for professional medical advice, diagnosis, or treatment. Always seek the advice of your physician or other qualified health provider with any questions you may have regarding a medical condition or before starting any new treatment. Never disregard professional medical advice or delay in seeking it because of something you have read here. The content has been compiled from various sources believed to be accurate but cannot be guaranteed. The manufacturer and publisher are not liable for any errors or omissions or for any consequences resulting from the use of this information.

Reviews

• Clinical Studies: Large-scale, randomized, double-blind, placebo-controlled trials have consistently demonstrated the efficacy of modafinil in improving measures of wakefulness (e.g., Maintenance of Wakefulness Test), reducing excessive sleepiness (e.g., Epworth Sleepiness Scale), and improving overall clinical condition in patients with narcolepsy, OSA, and SWSD. It is considered a first-line therapeutic option for these indications.
• Patient Reported Outcomes: Many patients report a significant subjective improvement in their ability to stay awake and alert during the day, leading to improved quality of life, productivity, and social functioning. Common feedback highlights the clear-headed nature of the wakefulness it promotes, distinct from the jitteriness associated with traditional stimulants. The most frequently cited negative aspect is the occurrence of headache, which often diminishes with continued use.