Vilazodone Explained

Verifiedfields:changed
Watchedfields:changed
Verifiedrevid:470630135
Width:280
Pronounce:
Tradename:Viibryd
Dailymedid:Vilazodone
Routes Of Administration:By mouth
Class:Serotonin modulator
Atc Prefix:N06
Atc Suffix:AX24
Legal Br:C1
Legal Br Comment:[1]
Legal Ca:Rx-only
Legal Ca Comment:[2] [3]
Legal Us:Rx-only
Bioavailability:72% (oral, with food)
Metabolism:Liver via CYP3A4[4]
Elimination Half-Life:25 hours
Excretion:Faecal and renal
Index2 Label:as HCl
Cas Number:163521-12-8
Cas Number2:163521-08-2
Pubchem:6918314
Pubchem2:6918313
Iuphar Ligand:7427
Drugbank:DB06684
Drugbank2:DBSALT000187
Chemspiderid:5293518
Chemspiderid2:5293517
Unii:S239O2OOV3
Unii2:U8HTX2GK8J
Kegg:D09698
Kegg2:D09699
Chebi:70707
Chebi2:70705
Chembl:439849
Chembl2:1615374
Pdb Ligand:YG7
Synonyms:EMD-68843; SB-659746A
Drug Name:Vilazodone
Iupac Name:5-(4-[4-(5-Cyano-1''H''-indol-3-yl)butyl]piperazin-1-yl)benzofuran-2-carboxamide
C:26
H:27
N:5
O:2
Smiles:N#Cc5ccc4[nH]cc(CCCCN3CCN(c2ccc1oc(C(N)=O)cc1c2)CC3)c4c5
Stdinchi: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)
Stdinchikey:SGEGOXDYSFKCPT-UHFFFAOYSA-N

Vilazodone, sold under the brand name Viibryd among others, is a medication used to treat major depressive disorder. It is classified as a serotonin modulator and is taken by mouth.

Common side effects include nausea, diarrhea, and trouble sleeping. Serious side effects may include increased suicidal thoughts or actions in those under the age of 25, serotonin syndrome, bleeding, mania, pancreatitis, and SIADH. Vilazodone may cause less emotional blunting than typical SSRIs and SNRIs.[5] A withdrawal syndrome may occur if the dose is rapidly decreased. Use during pregnancy and breastfeeding is not generally recommended.[6] It is in the serotonin modulator class of medications and is believed to work both as an SSRI and activator of the 5-HT1A receptor.[7]

Vilazodone was approved for medical use in the United States in 2011[7] and in Canada in 2018.[8] In 2019, it was the 334th most commonly prescribed medication in the United States, with more than 900thousand prescriptions.[9] The drug lost patent protection in June 2022 for adults and in July 2023 for pediatrics.[10] Generic versions have been approved by the U.S. Food and Drug Administration (FDA).[11] [12]

Medical uses

Seven controlled efficacy trials were conducted of vilazodone for treatment of major depressive disorder (MDD).[13] Five of these trials showed no significant influence of vilazodone over placebo on depressive symptoms. In the remaining two trials, small but significant advantages of vilazodone over placebo were found. According to these two eight-week trials in adults, vilazodone has an antidepressant response after one week of treatment. After eight weeks it resulted in a 13% greater response than placebo. Remission rates, however, were not significantly different versus placebo.[14]

According to the US Food and Drug Administration (FDA) staff in 2011, "it is unknown whether vilazodone has any advantages compared to other drugs in the antidepressant class."[15] A 2019 review stated that "present studies do not suggest the superiority of vilazodone compared with other antidepressants."[16]

Development of vilazodone for generalized anxiety disorder (GAD) has been stopped as of 2017.[17] While there is tentative evidence of a small benefit in GAD, there is a high rate of side effects.[18]

Adverse effects

In September 2016, the FDA wrote a letter to Forest Labs requiring a new warning to be added to the label related to a link between the drug and acute pancreatitis and sleep paralysis.[19]

The most common adverse effects include nausea, diarrhea, vomiting, and insomnia.

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.[20] [14] In randomized controlled trials, meanwhile, these rates were 28%, 23.4% and 13.3%, respectively.[14] In contrast to other SSRIs, initial trials showed that vilazodone did not cause decreased sexual desire/function, which often cause people to abandon their use.[21] Additionally, vilazodone may cause less emotional blunting than typical SSRIs and SNRIs.[5]

Pregnancy

Antidepressant exposure (including vilazodone) is associated with shorter average duration of pregnancy (by three days), increased risk of preterm delivery (by 55%), lower birth weight (by 75 g), and lower Apgar scores (by <0.4 points).[22] [23] It is uncertain whether there is an increased rate of septal heart defects among children whose mothers were prescribed an SSRI in early pregnancy.[24] [25]

Pharmacology

Pharmacodynamics

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] [26] It has negligible affinity for other serotonin receptors such as 5-HT1D, 5-HT2A, and 5-HT2C,[26] [27] as well as the norepinephrine and dopamine transporters (Ki = 56 nM for NET and 37 nM for DAT). A small clinical study found occupancy of the 5-HT1A receptor with vilazodone, whereas occupancy of the SERT by vilazodone in humans does not seem to have been studied.[28] [29] [30]

Pharmacokinetics

Vilazodone is best absorbed with food and has a bioavailability of 72% under fed conditions. The Cmax increased between 147 and 160% and the AUC increased between 64 and 85% of vilazodone when it was administered with either a fatty or light meal.[31]

History

It was developed by Merck KGaA and licensed by Clinical Data, a biotech company purchased by Forest Laboratories in 2011.[32]

Notes and References

  1. Web site: Anvisa . Brazilian Health Regulatory Agency . March 31, 2023 . RDC Nº 784 - Listas de Substâncias Entorpecentes, Psicotrópicas, Precursoras e Outras sob Controle Especial . Collegiate Board Resolution No. 784 - Lists of Narcotic, Psychotropic, Precursor, and Other Substances under Special Control. live . https://web.archive.org/web/20230803143925/https://www.in.gov.br/en/web/dou/-/resolucao-rdc-n-784-de-31-de-marco-de-2023-474904992 . August 3, 2023 . August 16, 2023 . . pt-BR . April 4, 2023.
  2. Web site: Viibryd Product information . Health Canada . April 25, 2012 . June 10, 2022.
  3. Web site: Health Canada New Drug Authorizations: 2015 Highlights . . 4 May 2016 . 7 April 2024.
  4. Web site: Viibryd (vilazodone hydrochloride) tablet Viibryd (vilazodone hydrochloride) kit [Forest Laboratories, Inc.]]. DailyMed. Forest Laboratories, Inc.. December 2012. October 28, 2013. live. https://web.archive.org/web/20131029192518/http://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=4c55ccfb-c4cf-11df-851a-0800200c9a66. October 29, 2013.
  5. Hughes S, Lacasse J, Fuller RR, Spaulding-Givens J . Adverse effects and treatment satisfaction among online users of four antidepressants . Psychiatry Research . 255 . 78–86 . September 2017 . 28531820 . 10.1016/j.psychres.2017.05.021 . 4572360 .
  6. Web site: Vilazodone (Viibryd) Use During Pregnancy . Drugs.com . March 21, 2019 .
  7. Web site: Vilazodone Hydrochloride Monograph for Professionals . Drugs.com . American Society of Health-System Pharmacists . March 3, 2019 .
  8. Web site: Government of Canada . Health Canada . Drug Product Database Online Query . May 18, 2020 . April 25, 2012.
  9. Web site: Vilazodone - Drug Usage Statistics . ClinCalc . October 16, 2021 . July 8, 2020 . https://web.archive.org/web/20200708071359/https://clincalc.com/DrugStats/Drugs/VilazodoneHydrochloride . dead .
  10. Web site: Generic Viibryd Availability.
  11. Web site: Vilazodone: FDA-Approved Drugs.
  12. Web site: 2019 First Generic Drugs Approvals . U.S. Food and Drug Administration (FDA) . January 21, 2021 . June 10, 2022.
  13. Kirsch I . Antidepressants and the Placebo Effect . Zeitschrift für Psychologie . 222 . 3 . 128–134 . 2014 . 25279271 . 4172306 . 10.1027/2151-2604/a000176 .
  14. Wang SM, Han C, Lee SJ, Patkar AA, Masand PS, Pae CU . A review of current evidence for vilazodone in major depressive disorder . International Journal of Psychiatry in Clinical Practice . 17 . 3 . 160–169 . August 2013 . 23578403 . 10.3109/13651501.2013.794245 . 10702028 .
  15. 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 . Vilazodone: clinical basis for the US Food and Drug Administration's approval of a new antidepressant . The Journal of Clinical Psychiatry . 72 . 9 . 1166–1173 . September 2011 . 21951984 . 10.4088/JCP.11r06984 .
  16. Stuivenga M, Giltay EJ, Cools O, Roosens L, Neels H, Sabbe B . Evaluation of vilazodone for the treatment of depressive and anxiety disorders . Expert Opinion on Pharmacotherapy . 20 . 3 . 251–260 . February 2019 . 30475091 . 10.1080/14656566.2018.1549542 . Informa UK Limited . 1887/3630582 . 53773793 . free .
  17. Web site: New Medicines Newsletter . NHS . March 21, 2019 . March 21, 2019 . https://web.archive.org/web/20190321102419/https://www.sps.nhs.uk/wp-content/uploads/2018/01/New-Medicines-Newsletter-December-2017.pdf . dead .
  18. Zareifopoulos N, Dylja I . Efficacy and tolerability of vilazodone for the acute treatment of generalized anxiety disorder: A meta-analysis . Asian Journal of Psychiatry . 26 . 115–122 . April 2017 . 28483071 . 10.1016/j.ajp.2017.01.016 .
  19. Web site: SUPPLEMENT APPROVAL . U.S. Food and Drug Administration (FDA) .
  20. Robinson DS, Kajdasz DK, Gallipoli S, Whalen H, Wamil A, Reed CR . A 1-year, open-label study assessing the safety and tolerability of vilazodone in patients with major depressive disorder . Journal of Clinical Psychopharmacology . 31 . 5 . 643–6 . October 2011 . 21869687 . 10.1097/JCP.0b013e31822c6741 .
  21. News: FDA approves Clinical Data Inc's antidepressant . Reuters . January 22, 2011 . live . https://web.archive.org/web/20110127072759/http://www.reuters.com/article/idUSN2111362920110122 . January 27, 2011 .
  22. Ross LE, Grigoriadis S, Mamisashvili L, Vonderporten EH, Roerecke M, Rehm J, Dennis CL, Koren G, Steiner M, Mousmanis P, Cheung A . Selected pregnancy and delivery outcomes after exposure to antidepressant medication: a systematic review and meta-analysis . JAMA Psychiatry . 70 . 4 . 436–443 . April 2013 . 23446732 . 10.1001/jamapsychiatry.2013.684 . free .
  23. Lattimore KA, Donn SM, Kaciroti N, Kemper AR, Neal CR, Vazquez DM . Selective serotonin reuptake inhibitor (SSRI) use during pregnancy and effects on the fetus and newborn: a meta-analysis . Journal of Perinatology . 25 . 9 . 595–604 . September 2005 . 16015372 . 10.1038/sj.jp.7211352 . free .
  24. Pedersen LH, Henriksen TB, Vestergaard M, Olsen J, Bech BH . Selective serotonin reuptake inhibitors in pregnancy and congenital malformations: population based cohort study . BMJ . 339 . sep23 1 . b3569 . September 2009 . 19776103 . 2749925 . 10.1136/bmj.b3569 .
  25. Huybrechts KF, Palmsten K, Avorn J, Cohen LS, Holmes LB, Franklin JM, Mogun H, Levin R, Kowal M, Setoguchi S, Hernández-Díaz S . Antidepressant use in pregnancy and the risk of cardiac defects . The New England Journal of Medicine . 370 . 25 . 2397–2407 . June 2014 . 24941178 . 4062924 . 10.1056/NEJMoa1312828 .
  26. Hughes ZA, Starr KR, Langmead CJ, Hill M, Bartoszyk GD, Hagan JJ, Middlemiss DN, Dawson LA . Neurochemical evaluation of the novel 5-HT1A receptor partial agonist/serotonin reuptake inhibitor, vilazodone . European Journal of Pharmacology . 510 . 1–2 . 49–57 . March 2005 . 15740724 . 10.1016/j.ejphar.2005.01.018 .
  27. Page ME, Cryan JF, Sullivan A, Dalvi A, Saucy B, Manning DR, Lucki I . 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 . 1220–1227 . September 2002 . 12183683 . 10.1124/jpet.102.034280 . 12020750 .
  28. Dawson LA . The discovery and development of vilazodone for the treatment of depression: a novel antidepressant or simply another SSRI? . Expert Opinion on Drug Discovery . 8 . 12 . 1529–1539 . December 2013 . 24195711 . 10.1517/17460441.2013.855195 . 19662281 .
  29. Dawson LA, Watson JM . Vilazodone: a 5-HT1A receptor agonist/serotonin transporter inhibitor for the treatment of affective disorders . CNS Neuroscience & Therapeutics . 15 . 2 . 107–117 . 2009 . 19499624 . 6493994 . 10.1111/j.1755-5949.2008.00067.x .
  30. Choi E, Zmarlicka M, Ehret MJ . Vilazodone: a novel antidepressant . American Journal of Health-System Pharmacy . 69 . 18 . 1551–1557 . September 2012 . 22935937 . 10.2146/ajhp110374 .
  31. Cruz MP . Vilazodone HCl (Viibryd): A Serotonin Partial Agonist and Reuptake Inhibitor For the Treatment of Major Depressive Disorder . P & T . 37 . 1 . 28–31 . January 2012 . 22346333 . 3278186 .
  32. Web site: Xconomy: Blend Therapeutics Taps Former Clinical Data Chief Fromkin As New CEO. April 13, 2015. xconomy.com. May 6, 2018. live. https://web.archive.org/web/20170909234053/http://www.xconomy.com/boston/2015/04/13/blend-therapeutics-taps-former-clinical-data-chief-fromkin-as-new-ceo/. September 9, 2017.

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