Vortioxetine

Vortioxetine
Clinical data
Pronunciation/vɔːrtiˈɒksətiːn/ vor-tee-OK-sə-teen
Trade namesTrintellix, Brintellix, others
Other namesLu AA21004, Vortioxetine hydrobromide (JAN JP), Vortioxetine hydrobromide (USAN US)
AHFS/Drugs.comMonograph
MedlinePlusa614003
License data
Pregnancy
category
Routes of
administration		By mouth
Drug classSerotonin modulator and stimulator (SMS)[3]
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailability75% (peak at 7–11 hours)[13]
Protein binding98–99%[13][11][14]
MetabolismLiver, primarily CYP2D6-mediated oxidation[13]
Elimination half-life66 hours[13]
Excretion59% in urine, 26% in feces[13]
Identifiers
  • 1-[2-(2,4-Dimethyl-phenylsulfanyl)phenyl]piperazine
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard100.258.748 Edit this at Wikidata
Chemical and physical data
FormulaC18H22N2S
Molar mass298.45 g·mol−1
3D model (JSmol)
  • CC(C=C(C)C=C1)=C1SC2=C(N3CCNCC3)C=CC=C2
  • InChI=1S/C18H22N2S/c1-14-7-8-17(15(2)13-14)21-18-6-4-3-5-16(18)20-11-9-19-10-12-20/h3-8,13,19H,9-12H2,1-2H3 ☒N
  • Key:YQNWZWMKLDQSAC-UHFFFAOYSA-N ☒N
  (verify)

Vortioxetine, sold under the brand name Trintellix (in the US) and Brintellix (in the EU) among others, is an antidepressant of the serotonin modulator and stimulator (SMS) class.[15][3] Its effectiveness is viewed as similar to that of other antidepressants.[15] It is taken orally.[15]

Common side effects include nausea, dry mouth, diarrhea, constipation, vomiting, and sexual dysfunction.[15][11] Serious side effects may include suicide in those under the age of 25, serotonin syndrome, bleeding, mania, and SIADH.[15] A withdrawal syndrome may occur if the medication is abruptly stopped or the dose is decreased.[15] Use during pregnancy and breastfeeding is not generally recommended.[16] Vortioxetine's mechanism of action is not entirely understood but is believed to be related to increasing serotonin levels and possibly interacting with certain serotonin receptors.[15][17][18]

It was approved for medical use in the United States in 2013.[15][19] In 2020, it was the 243rd most commonly prescribed medication in the United States, with more than 1 million prescriptions.[20][21]

  1. ^ "Brintellix (vortioxetine (as hydrobromide)) Product Information" (PDF). Therapeutic Goods Administration.
  2. ^ "Updates to the Prescribing Medicines in Pregnancy database". Therapeutic Goods Administration (TGA). Australian Government. 12 May 2022. Retrieved 13 May 2022.
  3. ^ a b "Vortioxetine Tablet - Uses, Side Effects, and More". WebMD. Retrieved 13 April 2024.
  4. ^ "FDA-sourced list of all drugs with black box warnings (Use Download Full Results and View Query links.)". nctr-crs.fda.gov. FDA. Retrieved 22 October 2023.
  5. ^ "Product Information Brintellix" (PDF). Therapeutic Goods Administration (TGA). Australian Government.
  6. ^ "AusPAR: Vortioxetine hydrobromide". Therapeutic Goods Administration (TGA). Australian Government.
  7. ^ "Prescription medicines: registration of new chemical entities in Australia, 2014". Therapeutic Goods Administration (TGA). 21 June 2022. Retrieved 10 April 2023.
  8. ^ Anvisa (31 March 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] (in Brazilian Portuguese). Diário Oficial da União (published 4 April 2023). Archived from the original on 3 August 2023. Retrieved 16 August 2023.
  9. ^ "Product monograph brand safety updates". Health Canada. 6 June 2024. Retrieved 8 June 2024.
  10. ^ "Brintellix tablets 5, 10 and 20mg - Summary of Product Characteristics (SmPC)". (emc). 11 April 2022. Archived from the original on 19 December 2022. Retrieved 19 December 2022.
  11. ^ a b c Cite error: The named reference Trintellix FDA label was invoked but never defined (see the help page).
  12. ^ "Brintellix EPAR". European Medicines Agency (EMA). 17 September 2018. Retrieved 15 January 2021.
  13. ^ a b c d e Cite error: The named reference pmid29189941 was invoked but never defined (see the help page).
  14. ^ Bundgaard C, Pehrson AL, Sánchez C, Bang-Andersen B (2 January 2015). "Case Study 2". Blood-Brain Barrier in Drug Discovery. Hoboken, NJ: John Wiley & Sons, Inc. pp. 505–520. doi:10.1002/9781118788523.ch23. ISBN 9781118788523.
  15. ^ a b c d e f g h "Vortioxetine Hydrobromide Monograph for Professionals". Drugs.com. American Society of Health-System Pharmacists. Retrieved 18 March 2019.
  16. ^ British national formulary : BNF 76 (76 ed.). Pharmaceutical Press. 2018. p. 376. ISBN 9780857113382.
  17. ^ Cite error: The named reference pmid25907797 was invoked but never defined (see the help page).
  18. ^ Cite error: The named reference pmid25562777 was invoked but never defined (see the help page).
  19. ^ Gibb A, Deeks ED (January 2014). "Vortioxetine: first global approval". Drugs. 74 (1): 135–145. doi:10.1007/s40265-013-0161-9. PMID 24311349. S2CID 5987668.
  20. ^ "The Top 300 of 2020". ClinCalc. Retrieved 7 October 2022.
  21. ^ "Vortioxetine - Drug Usage Statistics". ClinCalc. Retrieved 7 October 2022.