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Vortioxetine information


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
  • US DailyMed: Vortioxetine
Pregnancy
category
  • AU: B3[1][2]
Routes of
administration
By mouth
Drug classSelective serotonin reuptake inhibitor (SSRI)[3]
ATC code
  • N06AX26 (WHO)
Legal status
Legal status
  • AU: S4 (Prescription only)[5][6][7]
  • BR: Class C1 (Other controlled substances)[8]
  • UK: POM (Prescription only)[9]
  • US: WARNING[4]Rx-only[10]
  • EU: Rx-only[11]
  • In general: ℞ (Prescription only)
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
  • 508233-74-7 checkY
PubChem CID
  • 9966051
IUPHAR/BPS
  • 7351
DrugBank
  • DB09068 checkY
ChemSpider
  • 8141643 checkY
UNII
  • 3O2K1S3WQV
  • as salt: TKS641KOAY
KEGG
  • D10184 checkY
  • as salt: D10185 checkY
ChEBI
  • CHEBI:76016 checkY
ChEMBL
  • ChEMBL2204360 checkY
CompTox Dashboard (EPA)
  • DTXSID80965062 Edit this at Wikidata
ECHA InfoCard100.258.748 Edit this at Wikidata
Chemical and physical data
FormulaC18H22N2S
Molar mass298.45 g·mol−1
3D model (JSmol)
  • Interactive image
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 names Trintellix and Brintellix among others, is an antidepressant of the serotonin modulator and stimulator (SMS) class.[14][3] Its effectiveness is viewed as similar to that of other antidepressants.[14] It is taken by mouth.[14]

Common side effects include nausea, vomiting, constipation, 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 receptors for serotonin.[14][16][17]

It was approved for medical use in the United States in 2013.[14][18] In 2020, it was the 243rd most commonly prescribed medication in the United States, with more than 1 million prescriptions.[19][20]

  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. ^ "Brintellix tablets 5, 10 and 20mg - Summary of Product Characteristics (SmPC)". (emc). 11 April 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. ^ "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. ^ 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.
  19. ^ "The Top 300 of 2020". ClinCalc. Retrieved 7 October 2022.
  20. ^ "Vortioxetine - Drug Usage Statistics". ClinCalc. Retrieved 7 October 2022.

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Vortioxetine

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Vortioxetine, sold under the brand names Trintellix and Brintellix among others, is an antidepressant of the serotonin modulator and stimulator (SMS) class...

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Serotonin modulator and stimulator

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describe the mechanism of action of the serotonergic antidepressant vortioxetine, which acts as a serotonin reuptake inhibitor (SRI), agonist of the 5-HT1A...

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Atypical antidepressant

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nefazodone, opipramol, tianeptine, and trazodone. The agents vilazodone and vortioxetine are partly atypical. Typical antidepressants include the SSRIs, SNRIs...

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Serotonin antagonist and reuptake inhibitor

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antagonist, acting solely as a 5-HT1A receptor partial agonist instead. Vortioxetine (Trintellix) – another closely related drug, could technically be considered...

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Antidepressants in Japan

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and long in clinical trials in Japan. Takeda and Lundbeck submitted vortioxetine (Trintellix) to the Ministry of Health, Labour and Welfare in Japan....

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Serotonin reuptake inhibitor

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Seproxetine ((S)-norfluoxetine) Trazodone (Desyrel) Vilazodone (Viibryd) Vortioxetine (Trintellix) Cianopramine (Ro 11-2465) Litoxetine (SL-810,385) Lubazodone...

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Dapoxetine

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(2020). "Antistress and antidepressant properties of dapoxetine and vortioxetine". Acta Neurobiologiae Experimentalis. 80 (3): 217–224. doi:10.21307/ane-2020-020...

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Selective serotonin reuptake inhibitor

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less with atypical antidepressants like bupropion, agomelatine, and vortioxetine. Higher doses of antidepressants seem to be more likely to produce emotional...

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List of antidepressants

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Toludesvenlafaxine (Ruoxinlin) Nefazodone (Serzone) Vilazodone (Viibryd) Vortioxetine (Trintellix, Brintellix) Nefazodone (Dutonin, Nefadar, Serzone) –...

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Tedatioxetine

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Cocaine

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MDMA

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Nitrous oxide

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Ketamine

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LSD

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Brazilian Controlled Drugs and Substances Act

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Serotonin receptor agonist

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Benzodiazepine

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List of psychotropic medications

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Antidepressant

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Sertraline

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Trazodone

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Escitalopram

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Piperazine

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Pregabalin

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Aripiprazole

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Dextromethorphan

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