Armodafinil

Armodafinil is a prescription medicine used in the treatment of excessive daytime sleepiness (narcolepsy), obstructive sleep apnea (OSA), and shift work disorder (SWD). It improves wakefulness and helps you stay awake.

Armodafinil is the R-enantiomer of Modafinil (which is a 1:1 mixture of R- and S-enantiomers). It binds to the dopamine transporter and inhibits dopamine reuptake, increasing neuronal activity in the hypothalamus and enhancing activity in the hypothalamic wakefulness center (TMN).

Common side effects include headache, nausea, dizziness, and insomnia.

• Obstructive sleep apnea (OSA) - to improve wakefulness in adults
• Narcolepsy - to improve wakefulness in adults
• Shift work disorder (SWD) - to improve wakefulness in adults

Armodafinil is an indirect dopamine receptor agonist. This is the R-enantiomer of Modafinil which is a 1:1 mixture of the R- and S-enantiomers.

Armodafinil binds to the dopamine transporter and inhibits dopamine reuptake. As a result, it increases neuronal activity in the hypothalamus and enhances activity in hypothalamic wakefulness center (TMN, tuberomammillary nucleus) within the hypothalamic sleep wake switch.

Armodafinil binds to the dopamine transporter and inhibits dopamine reuptake, increasing dopamine levels in the synaptic cleft. This enhances wakefulness-promoting neuronal activity in the hypothalamus and reduces GABA-mediated neurotransmission, improving wakefulness.

Adults:

• Obstructive Sleep Apnea & Narcolepsy: 150-250 mg as a single dose in the morning
• Shift Work Disorder: 150 mg as a single dose approximately 1 hour prior to the start of work shift

Elderly: Consider lower initial dose (elimination may be reduced due to aging)

Hepatic Impairment: Reduce dose in severe hepatic impairment

Renal Impairment: Safety and efficacy not established in severe renal impairment

Children: Safety and efficacy not established in patients <17 years

Take this medicine in the dose and duration as advised by your doctor. Swallow the tablet whole - do not chew, crush or break. May be taken with or without food, preferably in the morning at a fixed time.

If you miss a dose, skip it and continue with your normal schedule. Do not double the dose.

• Headache
• Dizziness
• Nausea
• Insomnia (difficulty in sleeping)
• Excitation or agitation

Serious Rare:

• Stevens-Johnson syndrome
• Angioedema and anaphylactic reactions
• Multi-organ hypersensitivity reactions
• Psychiatric symptoms
• Cardiovascular events

Serious Precautions:

• Patients should be cautioned about operating automobiles or hazardous machinery until reasonably certain that therapy will not adversely affect ability
• Caution in patients with history of psychosis, depression or mania - consider discontinuation if psychiatric symptoms develop
• Monitor heart rate and blood pressure - caution in cardiovascular disease
• Do not use in uncontrolled moderate to severe hypertension or cardiac arrhythmias
• May reduce effectiveness of contraceptive pills - use additional contraception methods
• Inform doctor if you develop suicidal thoughts, mood changes, rash, itching, or breathing problems
• Long-term use may have addiction/dependence potential
• Do not stop suddenly without consulting your doctor
• Not a replacement for a good sleep routine

• Known hypersensitivity to Armodafinil or any excipient
• Uncontrolled moderate to severe hypertension or cardiac arrhythmias
• History of left ventricular hypertrophy or ischaemic ECG changes, chest pain, any clinical signs of mitral valve prolapse

• CYP3A4/CYP3A5 substrates (e.g., steroidal contraceptives, cyclosporine, midazolam, triazolam): Armodafinil increases clearance → lower systemic exposure → dose adjustment needed
• CYP2C19 substrates (e.g., phenytoin, diazepam, propranolol, omeprazole, clomipramine): Armodafinil prolongs elimination → higher systemic exposure → dose adjustment needed
• Warfarin: More frequent monitoring of prothrombin time/INR
• MAO Inhibitors: Caution when co-administered
• CYP3A4 inhibitors: Levels/effects may be increased
• CYP3A4 inducers: Levels/effects may be reduced
• Alcohol: Avoid

[UNSAFE] It is unsafe to consume alcohol with Armodafinil. Alcohol may increase side effects.

[CONSULT YOUR DOCTOR] Armodafinil may be unsafe to use during pregnancy (Pregnancy Category C). Animal studies have shown harmful effects on the developing baby. Your doctor will weigh the benefits and potential risks before prescribing. Use only if potential benefit justifies the potential risk to the fetus.

[CONSULT YOUR DOCTOR] It is not known whether Armodafinil or its metabolites are excreted in human milk. Caution should be exercised when administered to a nursing woman.

Safety and effectiveness in pediatric patients less than 17 years of age have not been established.

In elderly patients, elimination of Armodafinil and its metabolites may be reduced due to aging. Consider lower doses and close monitoring.

[CONSULT YOUR DOCTOR] There is inadequate information to determine safety and efficacy of dosing in patients with severe renal impairment.

[CONSULT YOUR DOCTOR] In patients with severe hepatic impairment, Armodafinil should be administered at a reduced dose.

There were no overdoses reported in clinical studies. Symptoms of overdose are likely similar to Modafinil - excitation or agitation, insomnia, and slight elevations in hemodynamic parameters. No specific antidote. Manage with primary supportive care.

Keep below 25°C, away from light & moisture. Keep out of reach of children.