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that's only one (possibly proprietary) formulation; the article is about the API itself. Undid revision 575316361 by 4h8s (talk)
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* [[Syndrome of inappropriate antidiuretic hormone secretion]] (SIADH)
* [[Syndrome of inappropriate antidiuretic hormone secretion]] (SIADH)
* [[Hyponatraemia]] (a complication of the former)
* [[Hyponatraemia]] (a complication of the former)



== Ingredients ==
'''Active ingredient:''' vilazodone hydrochloride

'''Inactive ingredients:''' lactose monohydrate, microcrystalline cellulose, magnesium stearate, colloidal silicon dioxide, polyvinyl alcohol, titanium dioxide, polyethylene glycol, talc, and FD&C Blue #1 (40 mg only), FD&C Yellow #6 (20 mg only) and FD&C Red #40 (10 mg only)






Revision as of 19:24, 1 October 2013

Vilazodone
Clinical data
Trade namesViibryd
AHFS/Drugs.comConsumer Drug Information
MedlinePlusa611020
License data
Routes of
administration		Oral
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailability72% (Oral, with food)[1]
MetabolismHepatic [1] via CYP3A4[2]
Elimination half-life25 hours [1]
ExcretionFaecal and renal [1]
Identifiers
  • 5-(4-[4-(5-cyano-1H-indol-3-yl)butyl]piperazin-1-yl)benzofuran-2-carboxamide
CAS Number
PubChem CID
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC26H27N5O2
Molar mass441.524 g/mol g·mol−1
3D model (JSmol)
  • N#Cc1ccc2c(c1)c(cn2)CCCCN5CCN(c4cc3c(oc(c3)C(=O)N)cc4)CC5
  • InChI=1S/C26H27N5O2/c27-16-18-4-6-23-22(13-18)19(17-29-23)3-1-2-8-30-9-11-31(12-10-30)21-5-7-24-20(14-21)15-25(33-24)26(28)32/h4-7,13-15,17,29H,1-3,8-12H2,(H2,28,32) checkY
  • Key:SGEGOXDYSFKCPT-UHFFFAOYSA-N checkY
 ☒NcheckY (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).[3] By 2009 two phase III clinical trials with positive results had been completed.[4] Vilazodone was approved by the FDA for use in the United States to treat major depressive disorder on January 21, 2011.[5][6][7]

Pharmacology

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%).[8][9] It has negligible affinity for other serotonin receptors such as 5-HT1D, 5-HT2A, and 5-HT2C.[8][9]

It also exhibits negligible inhibitory activity at the norepinephrine and dopamine transporters (IC50 = 56 nM for NET and 37 nM for DAT).[10]

Partial agonism of the 5-HT1A receptor is a relatively novel mechanism of action and is also shared by the anxiolytic buspirone (Buspar), atypical antipsychotic aripiprazole (Abilify) and novel antidepressant vortioxetine (Brintellix). Mirtazapine (Remeron) also acts as partial 5-HT1A agonist, though its action is indirect.

Efficacy and tolerability

Vilazodone is approved in 10 mg, 20 mg, and 40 mg doses.

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. [11][12] 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.[13] In contrast to other SSRIs currently on the market, initial clinical trials showed that vilazodone did not cause significant weight gain or decreased sexual desire/function as with many other antidepressants, which often cause people to abandon their use.[5]

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." [14]

Incidence of Adverse Effects

Sources:[1][2]

Very common adverse effects (incidence > 10%)
  • Nausea
  • Diarrhoea
Common adverse effects (1-10% incidence)
  • Vomiting
  • Dry mouth
  • Dizziness
  • Insomnia
Uncommon adverse effects (0.1-1% incidence)
  • Somnolence
  • Paraesthesia
  • Tremor
  • Abnormal dreams
  • Libido decreased
  • Restlessness
  • Akathisia
  • Restless legs syndrome
  • Abnormal orgasms (male patients only)
  • Delayed ejaculations (male patients only)
  • Erectile dysfunction (male patients only)
  • Fatigue
  • Feeling jittery
  • Palpitations
  • Ventricular premature beats
  • Arthralgia
  • Increased appetite
Rare adverse effects (<0.1% incidence)
-Nausea
-Vomiting
-Mental status change (e.g. confusion, hallucinations, agitation, coma, stupor)
-Muscle rigidity
-Tremor
-Myoclonus
-Hyperreflexia
-Hyperthermia
-Autonomic instability (e.g. tachycardia, dizziness, abnormally excessive sweating, etc.)
Unknown incidence adverse effects


See also

References

  1. ^ a b c d e Truven Health Analytics, Inc. DRUGDEX® System (Internet) [cited 2013 Oct 1]. Greenwood Village, CO: Thomsen Healthcare; 2013.
  2. ^ a b VIIBRYD (vilazodone hydrochloride) tablet VIIBRYD (vilazodone hydrochloride) kit [Forest Laboratories, Inc.] [Internet]. DailyMed. 2012 [cited 2013 Oct 1]. Available from: http://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=4c55ccfb-c4cf-11df-851a-0800200c9a66
  3. ^ Clinical Data's Vilazodone Patient Enrollment Over One Third Complete. August 17th, 2006[dead link‍]
  4. ^ de Paulis T (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. {{cite journal}}: Unknown parameter |month= ignored (help)
  5. ^ a b "FDA approves Clinical Data Inc's antidepressant". Reuters. January 22, 2011.
  6. ^ "FDA approves Clinical Data Inc's antidepressant". Reuters. January 22, 2011.
  7. ^ "Clinical Data, Inc. - Clinical Data, Inc. Submits New Drug Application for Vilazodone for the Treatment of Major Depressive Disorder".
  8. ^ a b Page ME, Cryan JF, Sullivan A; et al. (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. {{cite journal}}: Explicit use of et al. in: |author= (help); Unknown parameter |month= ignored (help)CS1 maint: multiple names: authors list (link)
  9. ^ a b Hughes ZA, Starr KR, Langmead CJ; et al. (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. {{cite journal}}: Explicit use of et al. in: |author= (help); Unknown parameter |month= ignored (help)CS1 maint: multiple names: authors list (link)
  10. ^ "DRUGDEX Evaluations - Vilazodone".
  11. ^ Rickels K, Athanasiou M, Robinson DS, Gibertini M, Whalen H, Reed CR (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. {{cite journal}}: Unknown parameter |month= ignored (help)CS1 maint: multiple names: authors list (link)
  12. ^ 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.
  13. ^ 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.
  14. ^ 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 (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. PMID 21951984. {{cite journal}}: Unknown parameter |month= ignored (help)CS1 maint: multiple names: authors list (link)


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