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Vilazodone
Systematic (IUPAC) name
5-(4-[4-(5-cyano-1H-indol-3-yl)butyl]piperazin-1-yl)benzofuran-2-carboxamide
Identifiers
CAS number 163521-12-8
ATC code none
PubChem 6918313
Chemical data
Formula C26H27N5O2
Mol. mass 441.524 g/mol
SMILES eMolecules & PubChem
Pharmacokinetic data
Half life 20-24 hours
Therapeutic considerations
Pregnancy cat.  ?
Legal status Uncontrolled
Routes Oral

Vilazodone (EMD-68,843, SB-659,746-A) is an antidepressant and anxiolytic of the piperazine chemical class. It is currently under development by Clinical Data for the treatment of major depressive disorder, and as of 2009 has completed two phase III clinical trials with positive results.[1] An NDA is currently pending confirmation by the FDA which, if approved, will likely precede vilazodone's availability on the market by the end of 2010.[2]

Contents

Pharmacology

Vilazodone acts as a serotonin reuptake inhibitor (IC50 = 0.5 nM) and 5-HT1A receptor partial agonist (IC50 = 0.2 nM; IA = ~60-70%).[3][4] It has negligible affinity for other serotonin receptors such as 5-HT1D, 5-HT2A, and 5-HT2C.[3][4]

Efficacy and tolerability

According to an eight-week, randomized, double-blind, placebo-controlled trial, vilazodone was reported to elicit an antidepressant response after 1 week of treatment. After 8 weeks, subjects assigned to vilazodone experienced a significantly higher response rate than the group given placebo. At a dose of 40mg per day, it's considered to be well tolerated and reported adverse effects ranged from mild to moderate in intensity; side effects included diarrhea, nausea, and somnolence.[5]

See also

References

  1. ^ de Paulis T (March 2007). "Drug evaluation: Vilazodone--a combined SSRI and 5-HT1A partial agonist for the treatment of depression". IDrugs : the Investigational Drugs Journal 10 (3): 193–201. PMID 17351874. 
  2. ^ "Clinical Data, Inc. - Clinical Data, Inc. Announces Positive Results from Second Phase III Trial of Vilazodone for Depression". http://investor.clda.com/releasedetail.cfm?ReleaseID=387284. 
  3. ^ a b Page ME, Cryan JF, Sullivan A, et al. (September 2002). "Behavioral and neurochemical effects of 5-(4-[4-(5-Cyano-3-indolyl)-butyl)-butyl-1-piperazinyl)-benzofuran-2-carboxamide (EMD 68843): a combined selective inhibitor of serotonin reuptake and 5-hydroxytryptamine(1A) receptor partial agonist"]. The Journal of Pharmacology and Experimental Therapeutics 302 (3): 1220–7. doi:10.1124/jpet.102.034280. PMID 12183683. http://jpet.aspetjournals.org/cgi/pmidlookup?view=long&pmid=12183683. 
  4. ^ a b Hughes ZA, Starr KR, Langmead CJ, et al. (March 2005). "Neurochemical evaluation of the novel 5-HT1A receptor partial agonist/serotonin reuptake inhibitor, vilazodone". European Journal of Pharmacology 510 (1-2): 49–57. doi:10.1016/j.ejphar.2005.01.018. PMID 15740724. http://linkinghub.elsevier.com/retrieve/pii/S0014-2999(05)00041-5. 
  5. ^ Rickels K, Athanasiou M, Robinson DS, Gibertini M, Whalen H, Reed CR (March 2009). "Evidence for efficacy and tolerability of vilazodone in the treatment of major depressive disorder: a randomized, double-blind, placebo-controlled trial". The Journal of Clinical Psychiatry 70 (3): 326–33. PMID 19284933. http://article.psychiatrist.com/?ContentType=START&ID=10003992. 







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