VIGINIL

Modafinil is a stimulant drug marketed as a'wakefulness promoting agent'and is one of the stimulants used in the treatment of narcolepsy.

Narcolepsy is caused by dysfunction of a family of wakefulness-promoting and sleep-suppressing peptides, the orexins, whose neurons are activated by modafinil.

The prexin neuron activation is associated with psychoactivation and euphoria.

The exact mechanism of action is unclear, although in vitro studies have shown it to inhibit the reuptake of dopamine by binding to the dopamine reuptake pump, and lead to an increase in extracellular dopamine.

Modafinil activates glutamatergic circuits while inhibiting

To improve wakefulness in patients with excessive daytime sleepiness (EDS) associated with narcolepsy.

Modafinil is a stimulant drug marketed as a'wakefulness promoting agent'and is one of the stimulants used in the treatment of narcolepsy.

Narcolepsy is caused by dysfunction of a family of wakefulness-promoting and sleep-suppressing peptides, the orexins, whose neurons are activated by modafinil.

The prexin neuron activation is associated with psychoactivation and euphoria.

Modafinil is not indicated for complaints of lack of energy or fatigue; but it appears to be very helpful for some patients.

Also, it has been used in the treatment of hypersomnia, a disorder in which patients lack the capacity for meaningful sleep and may require ten or more hours per day. Recent studies have have found that modafinil may help recovering cocaine addicts fight their addiction.

Rapid following oral administration.

Hepatic Hover over products below to view reaction partners Modafinil modafinil acid.

The major route of elimination is metabolism (~90%), primarily by the liver, with subsequent renal elimination of the metabolites.

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In clinical trials, a total of 151 protocol-specified doses ranging from to 1600 mg/day (5 to 8 times the recommended daily dose of modafinil) have been administered to 32 subjects, including 13 subjects who received doses of 1000 or 1200 mg/day for to 21 consecutive days.

In addition, several intentional acute overdoses occurred; the two largest being 4500 mg and 4000 mg taken by two subjects participating in foreign depression studies.

None of these study subjects experienced any unexpected or life-threatening effects.

Adverse reactions that were reported at these doses included excitation or agitation, insomnia, and slight or moderate elevations in hemodynamic parameters.

Other observed high-dose effects in clinical studies have included anxiety, irritability, aggressiveness, confusion, nervousness, tremor, palpitations, sleep disturbances, nausea, diarrhea, and decreased prothrombin time.

From postmarketing experience, there have been reports of fatal overdoses involving modafinil alone or in combination with other drugs.

Symptoms most often accompanying modafinil overdose, alone or in combination with other drugs have included insomnia; central nervous system symptoms such as restlessness, disorientation, confusion, agitation, anxiety, excitation, and hallucination; digestive changes such as nausea and diarrhea; and cardiovascular changes such as tachycardia, bradycardia, hypertension, and chest pain.

Cases of accidental ingestion/overdose have been reported in children as young as 11 months of age.

The highest reported accidental ingestion on a mg/kg basis occurred in a three-year-old boy who ingested to 1000 mg (50 to 63 mg/kg) of modafinil.

The child remained stable.

The symptoms associated with overdose in children were similar to those observed in adults.

No specific antidote exists for the toxic effects of a modafinil overdose.

Such overdoses should be managed with primarily supportive care, including cardiovascular monitoring.

Modafinil is contraindicated in patients with known hypersensitivity to modafinil or armodafinil or its inactive ingredients.

Modafinil is contraindicated in patients with known hypersensitivity to modafinil or armodafinil.

• Narcolepsy or OSA: 200 mg once a day in the morning.

• SWD: 200 mg once a day, taken approximately one hour prior to start of the work shift.

• Severe Hepatic Impairment: reduce dose to half the recommended dose.

• Geriatric Patients: consider lower dose. 2.1 Dosage in Narcolepsy and Obstructive Sleep Apnea (OSA) The recommended dosage of modafinil tablets for patients with narcolepsy or OSA is 200 mg taken orally once a day as a single dose in the morning.

Doses up to 400 mg/day, given as a single dose, have been well tolerated, but there is no consistent evidence that this dose confers additional benefit beyond that of the 200 mg/day dose. 2.2 Dosage in Shift Work Disorder (SWD) The recommended dosage of modafinil tablets for patients with SWD is 200 mg taken orally once a day as a single dose approximately 1 hour prior to the start of their work shift. 2.3 Dosage Modifications in Patients with Severe Hepatic Impairment In patients with severe hepatic impairment, the dosage of modafinil tablets should be reduced to one-half of that recommended for patients with normal hepatic function. 2.4 Use in Geriatric Patients Consideration should be given to the use of lower doses and close monitoring in geriatric patients.

Modafinil tablets

USP, 200 mg are white to off white colored capsule shaped tablets debossed with ‘M’ on one side and 200 MG on other side with a breakline between and MG. 30s count HDPE container NDC 68788-8280-3 60s count HDPE container NDC 68788-8280-6 90s count HDPE container NDC 68788-8280-9 16.2 Storage Store at 20° to 25°C (68° to 77°F). .

There are no adequate and well-controlled studies of modafinil in pregnant women.

Intrauterine growth restriction and spontaneous abortion have been reported in association with modafinil (a mixture of R - and S-modafinil) and armodafinil (the R-enantiomer of modafinil).

Although the pharmacology of modafinil is not identical to that of the sympathomimetic amines, it does share some pharmacologic properties with this class.

Certain of these drugs have been associated with intrauterine growth restriction and spontaneous abortions.

Whether the cases reported with modafinil are drug-related is unknown.

In studies of modafinil and armodafinil conducted in rats (modafinil, armodafinil) and rabbits (modafinil), developmental toxicity was observed at clinically relevant plasma exposures.

Modafinil should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Modafinil (50, 100, or 200 mg/kg/day) administered orally to pregnant rats throughout organogenesis caused, in the absence of maternal toxicity, an increase in resorptions and an increased incidence of visceral and skeletal variations in the offspring at the highest dose tested.

The higher no-effect dose for embryofetal developmental toxicity in rats (100 mg/kg/day) was associated with a plasma modafinil AUC less than that in humans at the recommended human dose (RHD) of modafinil (200 mg/day).

However, in a subsequent study of up to 480 mg/kg/day of modafinil, no adverse effects on embryofetal development were observed.

Oral administration of armodafinil (60, 200, or 600 mg/kg/day) to pregnant rats throughout organogenesis resulted in increased incidences of fetal visceral and skeletal variations and decreased fetal body weight at the highest dose tested.

The highest no-effect dose for embryofetal developmental toxicity in rats (200 mg/kg/day) was associated with a plasma armodafinil AUC less than that in humans at the RHD of modafinil.

Modafinil administered orally to pregnant rabbits throughout organogenesis at doses of up to 100 mg/kg/day had no effect on embryofetal development; however, the doses used were too low to adequately assess the effects of modafinil on embryofetal development.

In a subsequent developmental toxicity study evaluating doses of 45, 90, and 180 mg/kg/day in pregnant rabbits, the incidences of fetal structural alterations and embryofetal death were increased at the highest dose.

The highest no-effect dose for developmental toxicity (100 mg/kg/day) was associated with a plasma modafinil AUC similar to that in humans at the RHD of modafinil.

Modafinil administration to rats throughout gestation and lactation at oral doses of up to 200 mg/kg/day resulted in decreased viability in the offspring at doses greater than 20 mg/kg/day, a dose resulting in a plasma modafinil AUC less than that in humans at the RHD of modafinil.

No effects on postnatal developmental and neurobehavioral parameters were observed in surviving offspring.

It is not known whether modafinil or its metabolites are excreted in human milk.

Because many drugs are excreted in human milk, caution should be exercised when modafinil is administered to a nursing woman.

Safety and effectiveness in pediatric patients have not been established.

Modafinil is not approved in this population for any indication.

Serious skin rashes, including erythema multiforme major (EMM) and Stevens-Johnson Syndrome (SJS) have been associated with modafinil use in pediatric patients.

In a controlled 6 week study, 165 pediatric patients (aged to 17 years) with narcolepsy were treated with modafinil (n=123), or placebo (n=42).

There were no statistically significant differences favoring modafinil over placebo in prolonging sleep latency as measured by MSLT, or in perceptions of sleepiness as determined by the clinical global impression-clinician scale (CGI-C).

In the controlled and open-label clinical studies, treatment emergent adverse reactions of the psychiatric and nervous system included Tourette’s syndrome, insomnia, hostility, increased cataplexy, increased hypnagogic hallucinations, and suicidal ideation.

Transient leukopenia, which resolved without medical intervention, was also observed.

In the controlled clinical study, 3 of 38 girls, ages 12 or older, treated with modafinil experienced dysmenorrhea compared to of 10 girls who received placebo.

There were three to 9 week, double-blind, placebo-controlled, parallel group studies in children and adolescents (aged to 17 years) with Attention-Deficit Hyperactivity Disorder (ADHD).

Two of the studies were flexible-dose studies (up to 425 mg/day), and the third was a fixed-dose study (340 mg/day for patients <30 kg and 425 mg/day for patients ≥30 kg).

Although these studies showed statistically significant differences favoring modafinil over placebo in reducing ADHD symptoms as measured by the ADHD-RS (school version), there were 3 cases of serious rash including one case of possible SJS among 933 patients exposed to modafinil in this program.

Modafinil is not approved for use in treating ADHD.

In clinical trials, experience in a limited number of modafinil-treated patients who were greater than 65 years of age showed an incidence of adverse reactions similar to other age groups.

In elderly patients, elimination of modafinil and its metabolites may be reduced as a consequence of aging.

Therefore, consideration should be given to the use of lower doses and close monitoring in this population.