Vilazodone

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Vilazodone
Vilazodone2DACS4.svg
Vilazodone3Dan.gif
Systematic (IUPAC) name
5-(4-[4-(5-Cyano-1H-indol-3-yl)butyl]piperazin-1-yl)benzofuran-2-carboxamide
Clinical data
Trade names Viibryd
AHFS/Drugs.com Consumer Drug Information
MedlinePlus a611020
Licence data US Daily Med:link
Pregnancy
category
  • US: C (Risk not ruled out)
Legal status
Routes of
administration		 Oral
Pharmacokinetic data
Bioavailability 72% (Oral, with food)[1]
Metabolism Hepatic via CYP3A4[1]
Biological half-life 25 hours[1]
Excretion Faecal and renal[1]
Identifiers
CAS Number 163521-12-8 N
ATC code N06AX24 (WHO)
PubChem CID: 6918313
IUPHAR/BPS 7427
ChemSpider 5293518 YesY
UNII S239O2OOV3 YesY
KEGG D09698 YesY
ChEBI CHEBI:70707 N
ChEMBL CHEMBL439849 YesY
Chemical data
Formula C26H27N5O2
Molecular mass 441.524 g/mol
  • 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) YesY
  • Key:SGEGOXDYSFKCPT-UHFFFAOYSA-N YesY
 NYesY (what is this?)  (verify)

Vilazodone (United States trade name Viibryd VEYE-brid) 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] Vilazodone was approved by the FDA for use in the United States to treat major depressive disorder in 2011.[3][4][5]

Medical uses

According to two eight-week, randomized, double-blind, placebo-controlled trials in adults, vilazodone elicits an antidepressant response after one week of treatment. After eight weeks, subjects assigned to vilazodone 40 mg daily dose (titrated over two weeks) experienced a significantly higher response rate than the group given placebo (44% vs 30%, P = .002). Remission rates for vilazodone were not significantly different versus placebo.[6]

According to an article on the United States approval of vilazodone written by FDA staff, "it is unknown whether [vilazodone] has any advantages compared to other drugs in the antidepressant class."[7]

Adverse effects

After a one-year, open-label study assessing the safety and tolerability of vilazodone in people 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.[6] Whereas in randomized controlled trials these rates were 28%, 23.4% and 13.3%, respectively.[6] 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.[3]

Incidence of adverse effects

Incidence of adverse effects include:[1]

Very common adverse effects (incidence >10%)
  • Nausea
  • Diarrhea
  • Headache
Common adverse effects (1-10% incidence)

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Uncommon adverse effects (0.1-1% incidence)

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Rare adverse effects (<0.1% incidence)
  • Serotonin syndrome — a serious adverse effect characterised by:
    • 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.)
  • Mania/hypomania — a potentially dangerously elated/agitated mood. Every antidepressant has the potential to induce these psychiatric reactions. They are particularly problematic in those with a history of hypomania/mania such as those with bipolar disorder.[8]
Unknown-incidence adverse effects
  • Suicidal ideation — all antidepressants can cause suicidal ideation especially in young adults and adolescents under the age of 25.
  • Abnormal bleeding — the SSRIs are known for their ability to increase the incidence of gastrointestinal bleeds and other bleeding abnormalities.[8][9][10]
  • Seizures
  • Syndrome of inappropriate antidiuretic hormone secretion (SIADH) — a condition characterised by an abnormally excessive secretion of antidiuretic hormone causing potentially-fatal electrolyte abnormalities (such as hyponatraemia).
  • Hyponatraemia (a complication of the former) — low blood sodium.

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%).[6][11] It has negligible affinity for other serotonin receptors such as 5-HT1D, 5-HT2A, and 5-HT2C.[11][12] It also exhibits negligible inhibitory activity at the norepinephrine and dopamine transporters (IC50 = 56 nM for NET and 37 nM for DAT).[1]

See also

References

  1. ↑ 1.0 1.1 1.2 1.3 1.4 1.5 Lua error in package.lua at line 80: module 'strict' not found.
  2. ↑ Lua error in package.lua at line 80: module 'strict' not found.
  3. ↑ 3.0 3.1 Lua error in package.lua at line 80: module 'strict' not found.
  4. ↑ Lua error in package.lua at line 80: module 'strict' not found.
  5. ↑ Lua error in package.lua at line 80: module 'strict' not found.
  6. ↑ 6.0 6.1 6.2 6.3 Lua error in package.lua at line 80: module 'strict' not found.
  7. ↑ Lua error in package.lua at line 80: module 'strict' not found.
  8. ↑ 8.0 8.1 Australian Medicines Handbook 2013. The Australian Medicines Handbook Unit Trust; 2013.
  9. ↑ Taylor D, Paton C, Kapur S, Taylor D. The Maudsley prescribing guidelines in psychiatry. 11th ed. Chichester, West Sussex: John Wiley & Sons; 2012.
  10. ↑ 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
  11. ↑ 11.0 11.1 Lua error in package.lua at line 80: module 'strict' not found.
  12. ↑ Lua error in package.lua at line 80: module 'strict' not found.
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