Chonnam Med J.  2016 May;52(2):91-100. 10.4068/cmj.2016.52.2.91.

Vilazodone for the Treatment of Depression: An Update

• Wang SM
• Han C
• Lee SJ
• Patkar AA
• Masand PS
• Pae CU

• KMID: 2164318
• DOI: http://doi.org/10.4068/cmj.2016.52.2.91

Abstract

Vilazodone is a novel antidepressant having a selective serotonin (5-HT) reuptake inhibitor and 5-HT(1A) receptor partial agonist profile, so it has been regarded as a serotonin partial agonist-reuptake inhibitor (SPARI). We aimed to provide Vilazodone's clinical implications mainly by reviewing published clinical trials. Vilazodone has been speculated to have three potential benefits including faster onset of action, greater efficacy, and better tolerability owning to its SPARI properties. However, no studies conducted so far have directly proven the above speculations. Five initial phase II trials failed to distinguish vilazodone from placebo in the treatment of MDD, but 4 randomized clinical trials (RCT), 3 post-hoc or pooled analysis, 1 long-term open label study, and a meta-analysis showed vilazodone's superior efficacy over placebo. The studies also showed vilazodone is generally safe and tolerable. However, diarrhea, nausea, headache, dizziness, dry mouth, and insomnia warrant close attention in clinical practice because they have been constantly noted throughout the clinical studies. 2 RCTs recently documented the efficacy and safety of vilazodone in patients with generalized anxiety disorder, which could be a start of broadening vilazodone's usage or FDA approval in diverse anxiety disorders.

Keyword

Antidepressive agents; Anxiety disorders; 5-HT1 receptor agonists; Serotonin uptake inhibitors; Vilazodone hydrochloride

MeSH Terms

Antidepressive Agents
Anxiety Disorders
Depression*
Diarrhea
Dizziness
Headache
Humans
Mouth
Nausea
Receptor, Serotonin, 5-HT1A
Serotonin
Serotonin Uptake Inhibitors
Sleep Initiation and Maintenance Disorders
Vilazodone Hydrochloride*
Antidepressive Agents
Receptor, Serotonin, 5-HT1A
Serotonin
Serotonin Uptake Inhibitors
Vilazodone Hydrochloride

Figure

• 

  FIG. 1 Vilazodone's propsed mechanism of action.1325 1) Vilazodone can increase extra-neuronal serotonin by blocking SERT. 2) By acting only as a partial agonist at 5-HT1A autoreceptors, vilazodone may more rapidly desensitize 5-HT1A autoreceptors without causing excess activation of 5-HT1A autoreceptor-mediated serotonin inhibition. 3) Vilazodone binds to 5-HT1A With a higher affinity in a longer time than serotonin contributing to faster desensitization of 5-HT1A autoreceptors. 4) Vilazodone will enhance 5-HT by activating 5-HT1A postsynaptic receptors, and synergistic with its SSRI properties, vilazodone would yield even more serotonin release leading to greater efficacy. 5) Activating 5-HT1Apostsynaptic receptors increase dopamine release, which contribute to reduction in sexual dysfunction. 5HT: Serotonin, SERT: Serotonin transporter, SSRI: Selective serotonin reuptake inhibitor. Figure adapted from Wang et al.25

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