Armodafinil

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Armodafinil
Armodafinil.svg
Systematic (IUPAC) name
(–)-2-[(R)-(diphenylmethyl)sulfinyl]acetamide
Clinical data
Trade names Nuvigil
AHFS/Drugs.com monograph
MedlinePlus a602016
Pregnancy cat. C
Legal status Schedule IV (US) Prescription only
Dependence liability Very Low
Routes Oral
Pharmacokinetic data
Metabolism Hepatic, including CYP3A4 and other pathways
Half-life 12-15 hrs
Excretion Urine (as metabolites)
Identifiers
CAS number 112111-43-0 N
ATC code N06BA07
PubChem CID 9690109
ChemSpider 7962943 YesY
UNII V63XWA605I YesY
KEGG D03215 YesY
ChEBI CHEBI:77590 N
ChEMBL CHEMBL1201192 N
Chemical data
Formula C15H15NO2S 
Mol. mass 273.351
 N (what is this?)  (verify)

Armodafinil (Nuvigil) is the enantiopure of the vigilance-promoting drug,[1] or eugeroic, Modafinil (Provigil). It consists of just the (−)-(R)-enantiomer of the racemic Modafinil. Armodafinil is produced by the pharmaceutical company Cephalon Inc.[2] and was approved by the U.S. Food and Drug Administration (FDA) in June 2007.[3][4]

Although they have similar half lives, armodafinil reaches its peak concentration in the blood later after administration than modafinil does, which may make it more effective at improving wakefulness in patients with excessive daytime sleepiness.[5]

Mechanism of action[edit]

The mechanism of action of armodafinil is poorly understood, but it has been shown to act as both an indirect dopamine receptor agonist and a dopamine reuptake inhibitor.[2]

Medical uses[edit]

Armodafinil is currently FDA-approved to treat excessive daytime sleepiness associated with obstructive sleep apnea, narcolepsy, and shift work disorder.[2] It is commonly used off-label to treat attention deficit hyperactivity disorder, chronic fatigue syndrome, and major depressive disorder. It has been shown to improve vigilance in air traffic controllers.[6]

Sleep disorders[edit]

Armodafinil is approved by the U.S. FDA for the treatment of narcolepsy and shift work sleep disorder, and as an adjuvant therapy for obstructive sleep apnea.[7] For narcolepsy and obstructive sleep apnea, armodafinil is taken as a once daily 150 mg or 250 mg dose in the morning. For shift work sleep disorder, 150 mg of armodafinil are taken one hour prior to starting work. Slow dose titration is needed to mitigate some side effects.[7]

Schizophrenia[edit]

In June, 2010, it was revealed that a phase II study of armodafinil as an adjunctive therapy in adults with schizophrenia had failed to meet the primary endpoints, and the clinical program was subsequently terminated.[8] However, a study published later that year showed that schizophrenic patients treated with armodafinil showed fewer of the negative symptoms of schizophrenia.[9]

Jet lag[edit]

On March 30, 2010, the FDA declined to approve use of Nuvigil to treat jet lag.[10][11]

Adverse effects[edit]

In placebo-controlled studies, the most commonly observed side effects were headache, nausea, dizziness, and insomnia.[2][12]

Availability[edit]

Armodafinil is sold under a wide variety of brand names world wide.

  • Waklert - India (also Armod, Armod)

See also[edit]

References[edit]

  1. ^ Ferraro L, Antonelli T, Tanganelli S, O'Connor WT, Perez de la Mora M, Mendez-Franco J, Rambert FA, Fuxe K (April 1999). "The vigilance promoting drug modafinil increases extracellular glutamate levels in the medial preoptic area and the posterior hypothalamus of the conscious rat: prevention by local GABAA receptor blockade". Neuropsychopharmacology (Free full text) 20 (4): 346–56. doi:10.1016/S0893-133X(98)00085-2. PMID 10088135. 
  2. ^ a b c d http://www.nuvigil.com/PDF/Full_Prescribing_Information.pdf
  3. ^ "CDER Drug and Biologic Approvals for Calendar Year 2007". Retrieved 2008-01-21. 
  4. ^ "Search results from the "OB_Rx" table for query on "021875."", Orange Book (U.S. Food and Drug Administration), March 2012, retrieved April 30, 2012 
  5. ^ Darwish, M.; Kirby, M.; Hellriegel, E. T.; Robertson Jr, P. (2009). "Armodafinil and Modafinil Have Substantially Different Pharmacokinetic Profiles Despite Having the Same Terminal Half-Lives". Clinical Drug Investigation 29 (9): 613–623. doi:10.2165/11315280-000000000-00000. PMID 19663523.  edit
  6. ^ Phillips, J. B.; Simmons, R. G.; Arnold, R. D. (2011). "A single dose of armodafinil significantly promotes vigilance 11 hours post-dose". Military medicine 176 (7): 833–839. PMID 22128728.  edit
  7. ^ a b RXList-nuvigil
  8. ^ "Cephalon Provides Clinical Update on Phase II Study of NUVIGIL as an Adjunctive Therapy in Adults with Schizophrenia,". Retrieved 2011-08-21. 
  9. ^ Kane, J. M.; d'Souza, D. C.; Patkar, A. A.; Youakim, J. M.; Tiller, J. M.; Yang, R.; Keefe, R. S. E. (2010). "Armodafinil as Adjunctive Therapy in Adults with Cognitive Deficits Associated with Schizophrenia". The Journal of Clinical Psychiatry 71 (11): 1475–1481. doi:10.4088/JCP.09m05950gry. PMID 20816042.  edit
  10. ^ Pollack, Andrew (January 6, 2010). "A Drug’s Second Act: Battling Jet Lag". The New York Times. Retrieved 2010-03-30. 
  11. ^ Pollack, Andrew (March 29, 2010). "Regulators Reject a Drug Maker’s Plan to Use Its Alertness Pill to Overcome Jet Lag". The New York Times. Retrieved 2010-03-30. 
  12. ^ http://www.rxlist.com/nuvigil-drug/side-effects-interactions.htm

External links[edit]