Vortioxetine

Vortioxetine
Clinical data
Pronunciation/vɔːrtiˈɒksətn/ 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)[12]
Protein binding98–99%[12][10][13]
MetabolismLiver, primarily CYP2D6-mediated oxidation[12]
Elimination half-life66 hours[12]
Excretion59% in urine, 26% in feces[12]
Identifiers
IUPAC name
  • 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
Chemical and physical data
FormulaC18H22N2S
Molar mass298.45 g·mol−1
3D model (JSmol)
SMILES
  • CC(C=C(C)C=C1)=C1SC2=C(N3CCNCC3)C=CC=C2
InChI
  • 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 medication of the serotonin modulator and stimulator (SMS) class used in the treatment of major depressive disorder.[14][3] Its effectiveness is viewed as similar to that of other antidepressants.[14] It is taken orally.[14]

Common side effects include nausea, dry mouth, diarrhea, constipation, vomiting (3-6% of people), and sexual dysfunction.[14][10] Serious side effects may include suicide in those under the age of 25, serotonin syndrome, bleeding, mania, and SIADH.[14] A withdrawal syndrome may occur if the medication is abruptly stopped or the dose is decreased.[14] Use during pregnancy and breastfeeding is not generally recommended.[15] 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.[14][16][17]

It was approved for medical use in the United States[18][14][19] and in the European Union in 2013.[11] 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. ^ "Product Information Brintellix" (PDF). Therapeutic Goods Administration (TGA). Australian Government.
  5. ^ "AusPAR: Vortioxetine hydrobromide". Therapeutic Goods Administration (TGA). Australian Government.
  6. ^ "Prescription medicines: registration of new chemical entities in Australia, 2014". Therapeutic Goods Administration (TGA). 21 June 2022. Retrieved 10 April 2023.
  7. ^ 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.
  8. ^ "Product monograph brand safety updates". Health Canada. 6 June 2024. Retrieved 8 June 2024.
  9. ^ "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.
  10. ^ a b c Cite error: The named reference Trintellix FDA label was invoked but never defined (see the help page).
  11. ^ a b "Brintellix EPAR". European Medicines Agency (EMA). 17 September 2018. Retrieved 15 January 2021.
  12. ^ a b c d e Cite error: The named reference pmid29189941 was invoked but never defined (see the help page).
  13. ^ 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.
  14. ^ 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.
  15. ^ British national formulary : BNF 76 (76 ed.). Pharmaceutical Press. 2018. p. 376. ISBN 9780857113382.
  16. ^ Cite error: The named reference pmid25907797 was invoked but never defined (see the help page).
  17. ^ Cite error: The named reference pmid25562777 was invoked but never defined (see the help page).
  18. ^ "Drug Approval Package: Brintellix (vortioxetine) Tablets NDA #204447". U.S. Food and Drug Administration (FDA). 30 October 2013. Archived from the original on 8 July 2016. Retrieved 10 December 2024.
  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.