Armodafinil

Oral
Narcolepsy, Obstructive sleep apnoea

Oral
Shift-work sleep disorder

Severe: Dose reduction may be required.

Hypersensitivity. Pregnancy.

Patient with a history of psychosis, mania or depression; history of drug abuse; history of angina or MI, Tourette syndrome and other tic disorders. Not recommended for use in patients with history of left ventricular hypertrophy or in patients with mitral valve prolapse who have developed mitral valve prolapse syndrome induced by previous CNS stimulant use. When used for obstructive sleep apnoea: Not indicated as treatment for underlying obstruction; if continuous positive airway pressure (CPAP) is the treatment of choice, maximal effort to treat using CPAP for an adequate period must be made before starting therapy. Avoid abrupt withdrawal following chronic use. Hepatic impairment. Elderly. Lactation.

Significant: Agitation, anxiety, depression, mania, hallucinations, irritability, nervousness, suicidal thoughts, delusions, aggression; persistent sleepiness.
Cardiac disorders: Palpitations.
Gastrointestinal disorders: Diarrhoea, dry mouth, nausea, vomiting, thirst, dyspepsia, upper abdominal pain, constipation.
General disorders and administration site conditions: Fatigue, pain, fever, flu-like symptoms.
Immune system disorders: Seasonal allergy.
Investigations: Increased heart rate, increased gamma-glutamyl transferase.
Metabolism and nutrition disorders: Anorexia, decreased appetite.
Nervous system disorders: Headache, dizziness, disturbance in attention, migraine, paraesthesia, tremor.
Psychiatric disorders: Nervousness, depressed mood, insomnia.
Renal and urinary disorders: Polyuria.
Respiratory, thoracic and mediastinal disorders: Dyspnoea.
Skin and subcutaneous tissue disorders: Rash, contact dermatitis, hyperhidrosis.
Potentially Fatal: Rarely, serious dermatologic reactions (e.g. Stevens-Johnson syndrome, toxic epidermal necrolysis), drug rash with eosinophilia and systemic symptoms (DRESS) or multi-organ hypersensitivity, anaphylaxis, angioedema.

This drug may alter thinking, judgment and motor skills, if affected, do not drive or operate machinery.

Completely evaluate sleepiness prior to treatment. Assess pregnancy status before initiating treatment. Monitor blood pressure, heart rate; signs of drug abuse, hypersensitivity, rash, psychiatric symptoms. Re-assess the degree of sleepiness frequently.

May alter serum concentration with potent CYP3A4/5 inducers (e.g. carbamazepine, oxcarbazepine, phenytoin, phenobarbital, rifampicin, rifabutin) or CYP3A4/5 inhibitors (e.g. protease inhibitors [e.g. indinavir, nelfinavir, ritonavir, saquinavir], erythromycin, clarithromycin, chloramphenicol, ketoconazole, itraconazole, nefazodone, verapamil, diltiazem). May decrease serum concentration of drugs that are substrates for CYP3A enzymes (e.g. ciclosporin, steroidal contraceptives, midazolam, triazolam) and quetiapine. May increase serum concentration of some drugs that are substrates for CYP2C19 (e.g. diazepam, phenytoin, propranolol, clomipramine, omeprazole).

May alter serum concentration with St. John's wort. May delay absorption, affect bioavailability (minimal), onset and time course with food.

Description:
Mechanism of Action: Armodafinil, an R-enantiomer of modafinil, has unknown exact mechanism of action. It appears to bind to the dopamine transporter and suppress dopamine reuptake, resulting in increased extracellular dopamine levels in the brain. However, it is not a dopamine receptor agonist and does not seem to bind or suppress most of the hormones, enzymes or receptors that are believed to be involved in the sleep-wake cycle.
Pharmacokinetics:
Absorption: Readily absorbed. Food may delay absorption, affect bioavailability (minimal), onset and time course. Time to peak plasma concentration: Approx 2 hours.
Distribution: Enters breast milk. Volume of distribution: Approx 42 L. Plasma protein binding: Approx 60%, mainly albumin (based on modafinil).
Metabolism: Metabolised in the liver via multiple pathways including amine hydrolysis and sulfone formation by CYP3A4/5, into metabolites (e.g. R-modafinil acid and modafinil sulfone).
Excretion: Mainly via urine (based on modafinil: 80% as metabolites, <10% as unchanged drug). Elimination half-life: Approx 15 hours.

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 9690109, Armodafinil. https://pubchem.ncbi.nlm.nih.gov/compound/Armodafinil. Accessed Aug. 25, 2021.

Store between 20-25°C.

Thuốc TKTW khác & thuốc trị rối loạn tăng động giảm chú ý

N06BA13 - armodafinil ; Belongs to the class of centrally-acting sympathomimetics. Used as CNS stimulant.

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Anon. Armodafinil. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 05/07/2021.

Armodafinil. Gold Standard Drug Database in ClinicalKey [online]. Elsevier Inc. https://www.clinicalkey.com. Accessed 05/07/2021.

Buckingham R (ed). Armodafinil. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 09/07/2021.

Nuvigil 150 mg and 250 mg Tablet (Teva Pharma [Thailand] Co., Ltd.). MIMS Thailand. http://www.mims.com/thailand. Accessed 09/07/2021.

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