Vilazodone

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Vilazodone
Systematic (IUPAC) name
5-(4-[4-(5-cyano-1H-indol-3-yl)butyl]piperazin-1-yl)benzofuran-2-carboxamide
Clinical data
Trade namesViibryd
AHFS/Drugs.comConsumer Drug Information
MedlinePlusa611020
Licence dataUS Daily Med:link
Pregnancy cat.C (US)
Legal status-only (US)
RoutesOral
Pharmacokinetic data
Bioavailability72% (Oral, with food)[1]
MetabolismHepatic via CYP3A4[1]
Half-life25 hours[1]
ExcretionFaecal and renal[1]
Identifiers
CAS number163521-12-8 N
ATC codeN06AX24
PubChemCID 6918313
ChemSpider5293518 YesY
UNIIS239O2OOV3 YesY
KEGGD09698 YesY
ChEBICHEBI:70707 N
ChEMBLCHEMBL439849 YesY
Chemical data
FormulaC26H27N5O2 
Mol. mass441.524 g/mol
 N (what is this?)  (verify)
 
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Vilazodone
Systematic (IUPAC) name
5-(4-[4-(5-cyano-1H-indol-3-yl)butyl]piperazin-1-yl)benzofuran-2-carboxamide
Clinical data
Trade namesViibryd
AHFS/Drugs.comConsumer Drug Information
MedlinePlusa611020
Licence dataUS Daily Med:link
Pregnancy cat.C (US)
Legal status-only (US)
RoutesOral
Pharmacokinetic data
Bioavailability72% (Oral, with food)[1]
MetabolismHepatic via CYP3A4[1]
Half-life25 hours[1]
ExcretionFaecal and renal[1]
Identifiers
CAS number163521-12-8 N
ATC codeN06AX24
PubChemCID 6918313
ChemSpider5293518 YesY
UNIIS239O2OOV3 YesY
KEGGD09698 YesY
ChEBICHEBI:70707 N
ChEMBLCHEMBL439849 YesY
Chemical data
FormulaC26H27N5O2 
Mol. mass441.524 g/mol
 N (what is this?)  (verify)

Vilazodone (United States trade name Viibryd) is a serotonergic antidepressant developed by Clinical Data for the treatment of major depressive disorder. The chemical compound was originally developed by Merck KGaA (Germany).[2] By 2009 two phase III clinical trials with positive results had been completed.[3] Vilazodone was approved by the FDA for use in the United States to treat major depressive disorder on January 21, 2011.[4][5][6]

Medical uses[edit]

Major Depressive Disorder[edit]

According to two eight-week, randomized, double-blind, placebo-controlled trials in adults, vilazodone was reported to elicit an antidepressant response after one week of treatment. After eight weeks, subjects assigned to vilazodone 40mg daily dose (titrated over 2 weeks) experienced a significantly higher response rate than the group given placebo (44% vs 30%, P = .002). But, remission rates for vilazodone were not significantly different versus placebo.[7][8]

However, FDA staff called these claims into question in a September 2011 article that concluded "it is unknown whether [vilazodone] has any advantages compared to other drugs in the antidepressant class."[9]

Adverse Effects[edit]

After a 1 year, open-label study assessing the safety and tolerability of vilazodone in patients with major depressive disorder, the most common adverse effects were diarrhea (35.7%), nausea (31.6%), and headache (20.0%); greater than 90% of these adverse effects were mild or moderate.[10] In contrast to other SSRIs currently on the market, initial clinical trials showed that vilazodone did not cause significant decreased sexual desire/function as with many other antidepressants, which often cause people to abandon their use.[4]

Incidence of Adverse Effects[edit]

Sources:[1]

Very common adverse effects (incidence > 10%)
Common adverse effects (1-10% incidence)
Uncommon adverse effects (0.1-1% incidence)
Rare adverse effects (<0.1% incidence)
-Nausea
-Vomiting
-Mental status change (e.g. confusion, hallucinations, agitation, coma, stupor)
-Muscle rigidity
-Tremor
-Myoclonus
-Hyperreflexia — overresponsive/overactive reflexes.
-Hyperthermia — elevated body temperature.
-Autonomic instability (e.g. tachycardia, dizziness, abnormally excessive sweating, etc.)
Unknown incidence adverse effects

Overdose[edit]

Adverse reactions of VIIBRYD at doses of 200-280 mg included serotonin syndrome, lethargy, restlessness, hallucinations, and disorientation.

Pharmacology[edit]

Vilazodone acts as a serotonin reuptake inhibitor (IC50 = 2.1 nM; Ki = 0.1 nM) and 5-HT1A receptor partial agonist (IC50 = 0.2 nM; IA = ~60–70%).[14][15] It has negligible affinity for other serotonin receptors such as 5-HT1D, 5-HT2A, and 5-HT2C.[14][15]

It also exhibits negligible inhibitory activity at the norepinephrine and dopamine transporters (IC50 = 56 nM for NET and 37 nM for DAT).[1]

Partial agonism of the 5-HT1A receptor is a relatively novel mechanism of action and is also shared by the anxiolytic buspirone (Buspar), the atypical antipsychotics aripiprazole (Abilify) and lurasidone (Latuda) ,and the novel antidepressant vortioxetine (Brintellix).

Ingredients[edit]

Viibryd (US)[edit]

Viibryd is available in tablet form as the hydrochloride salt of vilazodone. Inactive ingredients include lactose monohydrate, microcrystalline cellulose, magnesium stearate, colloidal silicon dioxide, polyvinyl alcohol, titanium dioxide, polyethylene glycol, talc, and various FD&C colorings (Blue #1, Yellow #6, Red #40) depending on the dose.[1]


See also[edit]

References[edit]

  1. ^ a b c d e f g "VIIBRYD (vilazodone hydrochloride) tablet VIIBRYD (vilazodone hydrochloride) kit [Forest Laboratories, Inc.]". DailyMed. Forest Laboratories, Inc. December 2012. Retrieved 28 October 2013. 
  2. ^ Clinical Data's Vilazodone Patient Enrollment Over One Third Complete. August 17th, 2006[dead link]
  3. ^ 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. 
  4. ^ a b "FDA approves Clinical Data Inc's antidepressant". Reuters. January 22, 2011. 
  5. ^ "FDA approves Clinical Data Inc's antidepressant". Reuters. January 22, 2011. 
  6. ^ "Clinical Data, Inc. - Clinical Data, Inc. Submits New Drug Application for Vilazodone for the Treatment of Major Depressive Disorder". 
  7. ^ 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. 
  8. ^ USA (2013-01-30). "A randomized, double-blind, placebo-controlled, 8-week study of vilazodone, a serotonergic agent for the treatment of major depressive disorder". Ncbi.nlm.nih.gov. Retrieved 2013-02-28. 
  9. ^ Laughren TP, Gobburu J, Temple RJ, Unger EF, Bhattaram A, Dinh PV, Fossom L, Hung HM, Klimek V, Lee JE, Levin RL, Lindberg CY, Mathis M, Rosloff BN, Wang SJ, Wang Y, Yang P, Yu B, Zhang H, Zhang L, Zineh I (September 2011). "Vilazodone: clinical basis for the US Food and Drug Administration's approval of a new antidepressant". The Journal of Clinical Psychiatry 72 (9): 1166–73. doi:10.4088/JCP.11r06984. PMID 21951984. 
  10. ^ USA (2013-01-30). "A 1-year, open-label study assessing the safety and tolerability of vilazodone in patients with major depressive disorder". Ncbi.nlm.nih.gov. Retrieved 2013-02-28. 
  11. ^ a b Australian Medicines Handbook 2013. The Australian Medicines Handbook Unit Trust; 2013.
  12. ^ Taylor D, Paton C, Kapur S, Taylor D. The Maudsley prescribing guidelines in psychiatry. 11th ed. Chichester, West Sussex: John Wiley & Sons; 2012.
  13. ^ Wang Y-P, Chen Y-T, Tsai C-F, Li S-Y, Luo J-C, Wang S-J, et al. Short-Term Use of Serotonin Reuptake Inhibitors and Risk of Upper Gastrointestinal Bleeding. Am J Psychiatry [Internet]. 2013 Sep 13 [cited 2013 Oct 6]; Available from: http://ajp.psychiatryonline.org/article.aspx?articleid=1738031
  14. ^ 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. 
  15. ^ 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.