Vilazodone
Clinical data
Pronunciation/vɪˈlæzədoʊn/
vi-LAZ-ə-dohn
Trade namesViibryd
Other namesEMD-68843; SB-659746A
AHFS/Drugs.comMonograph
MedlinePlusa611020
License data
Routes of
administration		By mouth
Drug classSerotonin modulator[1]
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailability72% (oral, with food)[4]
MetabolismLiver via CYP3A4[4]
Elimination half-life25 hours[4]
ExcretionFaecal and renal[4]
Identifiers
  • 5-(4-[4-(5-Cyano-1H-indol-3-yl)butyl]piperazin-1-yl)benzofuran-2-carboxamide
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
PDB ligand
Chemical and physical data
FormulaC26H27N5O2
Molar mass441.535 g·mol−1
3D model (JSmol)
  • N#Cc5ccc4[nH]cc(CCCCN3CCN(c2ccc1oc(C(N)=O)cc1c2)CC3)c4c5
  • 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, sold under the brand name Viibryd among others, is a medication used to treat major depressive disorder.[1] It is classified as a serotonin modulator[1] and is taken by mouth.[1]

Common side effects include nausea, diarrhea, and trouble sleeping.[1] Serious side effects may include increased suicidal thoughts or actions in those under the age of 25, serotonin syndrome, bleeding, mania, pancreatitis, and SIADH.[1] Vilazodone may cause less emotional blunting than typical SSRIs and SNRIs.[5] A withdrawal syndrome may occur if the dose is rapidly decreased.[1] 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.[1]

Vilazodone was approved for medical use in the United States in 2011[1] and in Canada in 2018.[7] In 2019, it was the 334th most commonly prescribed medication in the United States, with more than 900 thousand prescriptions.[8] The drug lost patent protection in June 2022 for adults and in July 2023 for pediatrics.[9] Generic versions have been approved by the U.S. Food and Drug Administration (FDA).[10][11]

Medical uses

Seven controlled efficacy trials were conducted of vilazodone for treatment of major depressive disorder (MDD).[12] Five of these trials showed no significant influence of vilazodone over placebo on depressive symptoms.[12] In the remaining two trials, small but significant advantages of vilazodone over placebo were found.[12] According to these two eight-week trials in adults, vilazodone has an antidepressant response after one week of treatment.[13] After eight weeks it resulted in a 13% greater response than placebo.[13] Remission rates, however, were not significantly different versus placebo.[13]

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."[14] A 2019 review stated that "present studies do not suggest the superiority of vilazodone compared with other antidepressants."[15]

Development of vilazodone for generalized anxiety disorder (GAD) has been stopped as of 2017.[16] While there is tentative evidence of a small benefit in GAD, there is a high rate of side effects.[17]

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.[18]

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.[13] In randomized controlled trials, meanwhile, these rates were 28%, 23.4% and 13.3%, respectively.[13] 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.[19] Additionally, vilazodone may cause less emotional blunting than typical SSRIs and SNRIs.[5] Incidence of adverse effects include:[4]

Very common adverse effects (incidence >10%)
  • Nausea
  • Diarrhea
  • Headache
Common adverse effects (1–10% incidence)
Uncommon adverse effects (0.1–1% incidence)
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.[20]
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.[20][21][22]
  • 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.

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).[23][24] It is uncertain whether there is an increased rate of septal heart defects among children whose mothers were prescribed an SSRI in early pregnancy.[25][26]

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%).[13][27] It has negligible affinity for other serotonin receptors such as 5-HT1D, 5-HT2A, and 5-HT2C,[27][28] as well as the norepinephrine and dopamine transporters (Ki = 56 nM for NET and 37 nM for DAT).[4] 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.[29][30][31]

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.[32]

History

It was developed by Merck KGaA and licensed by Clinical Data, a biotech company purchased by Forest Laboratories in 2011.[33]

References

  1. 1 2 3 4 5 6 7 8 9 "Vilazodone Hydrochloride Monograph for Professionals". Drugs.com. American Society of Health-System Pharmacists. Retrieved 3 March 2019.
  2. ↑ Anvisa (2023-03-31). "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] (in Brazilian Portuguese). Diário Oficial da União (published 2023-04-04). Archived from the original on 2023-08-03. Retrieved 2023-08-16.
  3. ↑ "Viibryd Product information". Health Canada. 25 April 2012. Retrieved 10 June 2022.
  4. 1 2 3 4 5 6 7 "Viibryd (vilazodone hydrochloride) tablet Viibryd (vilazodone hydrochloride) kit [Forest Laboratories, Inc.]". DailyMed. Forest Laboratories, Inc. December 2012. Archived from the original on 29 October 2013. Retrieved 28 October 2013.
  5. 1 2 Hughes S, Lacasse J, Fuller RR, Spaulding-Givens J (September 2017). "Adverse effects and treatment satisfaction among online users of four antidepressants". Psychiatry Research. 255: 78–86. doi:10.1016/j.psychres.2017.05.021. PMID 28531820. S2CID 4572360.
  6. ↑ "Vilazodone (Viibryd) Use During Pregnancy". Drugs.com. Retrieved 21 March 2019.
  7. ↑ "Drug Product Database Online Query". Health Canada. Government of Canada. 25 April 2012. Retrieved 18 May 2020.
  8. ↑ "Vilazodone - Drug Usage Statistics". ClinCalc. Archived from the original on 8 July 2020. Retrieved 16 October 2021.
  9. ↑ "Generic Viibryd Availability".
  10. ↑ "Vilazodone: FDA-Approved Drugs".
  11. ↑ "2019 First Generic Drugs Approvals". U.S. Food and Drug Administration (FDA). 21 January 2021. Retrieved 10 June 2022.
  12. 1 2 3 Kirsch I (2014). "Antidepressants and the Placebo Effect". Zeitschrift für Psychologie. 222 (3): 128–134. doi:10.1027/2151-2604/a000176. PMC 4172306. PMID 25279271.
  13. 1 2 3 4 5 6 Wang SM, Han C, Lee SJ, Patkar AA, Masand PS, Pae CU (August 2013). "A review of current evidence for vilazodone in major depressive disorder". International Journal of Psychiatry in Clinical Practice. 17 (3): 160–169. doi:10.3109/13651501.2013.794245. PMID 23578403. S2CID 10702028.
  14. ↑ Laughren TP, Gobburu J, Temple RJ, Unger EF, Bhattaram A, Dinh PV, et al. (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): 1166–1173. doi:10.4088/JCP.11r06984. PMID 21951984.
  15. ↑ Stuivenga M, Giltay EJ, Cools O, Roosens L, Neels H, Sabbe B (February 2019). "Evaluation of vilazodone for the treatment of depressive and anxiety disorders". Expert Opinion on Pharmacotherapy. Informa UK Limited. 20 (3): 251–260. doi:10.1080/14656566.2018.1549542. PMID 30475091. S2CID 53773793.
  16. ↑ "New Medicines Newsletter" (PDF). NHS. Archived from the original (PDF) on 21 March 2019. Retrieved 21 March 2019.
  17. ↑ Zareifopoulos N, Dylja I (April 2017). "Efficacy and tolerability of vilazodone for the acute treatment of generalized anxiety disorder: A meta-analysis". Asian Journal of Psychiatry. 26: 115–122. doi:10.1016/j.ajp.2017.01.016. PMID 28483071.
  18. ↑ "SUPPLEMENT APPROVAL" (PDF). U.S. Food and Drug Administration (FDA).
  19. ↑ "FDA approves Clinical Data Inc's antidepressant". Reuters. January 22, 2011. Archived from the original on January 27, 2011.
  20. 1 2 Australian Medicines Handbook 2013. The Australian Medicines Handbook Unit Trust; 2013.
  21. ↑ Taylor D, Paton C, Kapur S, Taylor D. The Maudsley prescribing guidelines in psychiatry. 11th ed. Chichester, West Sussex: John Wiley & Sons; 2012.
  22. ↑ 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
  23. ↑ Ross LE, Grigoriadis S, Mamisashvili L, Vonderporten EH, Roerecke M, Rehm J, et al. (April 2013). "Selected pregnancy and delivery outcomes after exposure to antidepressant medication: a systematic review and meta-analysis". JAMA Psychiatry. 70 (4): 436–443. doi:10.1001/jamapsychiatry.2013.684. PMID 23446732.
  24. ↑ Lattimore KA, Donn SM, Kaciroti N, Kemper AR, Neal CR, Vazquez DM (September 2005). "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. doi:10.1038/sj.jp.7211352. PMID 16015372.
  25. ↑ Pedersen LH, Henriksen TB, Vestergaard M, Olsen J, Bech BH (September 2009). "Selective serotonin reuptake inhibitors in pregnancy and congenital malformations: population based cohort study". BMJ. 339 (sep23 1): b3569. doi:10.1136/bmj.b3569. PMC 2749925. PMID 19776103.
  26. ↑ Huybrechts KF, Palmsten K, Avorn J, Cohen LS, Holmes LB, Franklin JM, et al. (June 2014). "Antidepressant use in pregnancy and the risk of cardiac defects". The New England Journal of Medicine. 370 (25): 2397–2407. doi:10.1056/NEJMoa1312828. PMC 4062924. PMID 24941178.
  27. 1 2 Hughes ZA, Starr KR, Langmead CJ, Hill M, Bartoszyk GD, Hagan JJ, 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.
  28. ↑ Page ME, Cryan JF, Sullivan A, Dalvi A, Saucy B, Manning DR, Lucki I (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): 1220–1227. doi:10.1124/jpet.102.034280. PMID 12183683. S2CID 12020750.
  29. ↑ Dawson LA (December 2013). "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. doi:10.1517/17460441.2013.855195. PMID 24195711. S2CID 19662281.
  30. ↑ Dawson LA, Watson JM (2009). "Vilazodone: a 5-HT1A receptor agonist/serotonin transporter inhibitor for the treatment of affective disorders". CNS Neuroscience & Therapeutics. 15 (2): 107–117. doi:10.1111/j.1755-5949.2008.00067.x. PMC 6493994. PMID 19499624.
  31. ↑ Choi E, Zmarlicka M, Ehret MJ (September 2012). "Vilazodone: a novel antidepressant". American Journal of Health-System Pharmacy. 69 (18): 1551–1557. doi:10.2146/ajhp110374. PMID 22935937.
  32. ↑ Cruz MP (January 2012). "Vilazodone HCl (Viibryd): A Serotonin Partial Agonist and Reuptake Inhibitor For the Treatment of Major Depressive Disorder". P & T. 37 (1): 28–31. PMC 3278186. PMID 22346333.
  33. ↑ "Xconomy: Blend Therapeutics Taps Former Clinical Data Chief Fromkin As New CEO". xconomy.com. 13 April 2015. Archived from the original on 9 September 2017. Retrieved 6 May 2018.
This article is issued from Wikipedia. The text is licensed under Creative Commons - Attribution - Sharealike. Additional terms may apply for the media files.