Vortioxetine

Vortioxetine
Clinical data


Pronunciation	/vɔːrtiːˈoʊksətiːn/ vor-tee-OX-uh-teen
Trade names	Trintellix, Brintellix
License data	EU EMA: Brintellix US FDA: Vortioxetine
Pregnancy category	US: C (Risk not ruled out)
Routes of administration	By mouth (film-coated tablets)
ATC code	N06AX26 (WHO)
Legal status
Legal status	In general: ℞ (Prescription only)
Pharmacokinetic data
Bioavailability	75% (peak at 7–11 hours)
Protein binding	98%
Metabolism	Extensive hepatic, primarily CYP2D6-mediated oxidation
Biological half-life	66 hours
Excretion	59% in urine, 26% in feces
Identifiers
IUPAC name 1-[2-(2,4-Dimethyl-phenylsulfanyl)-phenyl]piperazine
Synonyms	Lu AA21004
CAS Number	508233-74-7^Y
PubChem CID	9966051
IUPHAR/BPS	7351
DrugBank	DB09068^N
ChemSpider	8141643^N
UNII	3O2K1S3WQV
KEGG	D10184^N
ChEBI	CHEBI:76016^N
Chemical and physical data
Formula	C₁₈H₂₂N₂S
Molar mass	298.45 g/mol (379.36 as hydrobromide)
3D model (Jmol)	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
^NY (what is this?)

Vortioxetine (trade names Trintellix, Brintellix) is an atypical antidepressant (a serotonin modulator and stimulator) made by Lundbeck and Takeda.

Vortioxetine is used as a treatment for major depressive disorder.

The most common side effects reported with vortioxetine are nausea, diarrhea, dry mouth, constipation, vomiting, flatulence, dizziness, and sexual dysfunction. Vortioxetine used alone in high dose or in combination with other medications, such as other antidepressants, can produce a potentially life-threatening drug reaction known as serotonin syndrome.

Incidence of sexual dysfunction is reportedly higher in patients taking vortioxetine than in people taking placebos but appears to be lower than in people taking other antidepressants

Vortioxetine is a so-called "serotonin modulator and stimulator". It has been shown to possess the following pharmacological actions:

* Human isoforms

Vortioxetine reaches peak plasma concentration (C_max) within 7 to 11 hours post-administration (T_max), and its mean terminal half-life ( ^T⁄_1/2) is ≈ 66 hours. Steady-state plasma concentrations are typically reached within two weeks. It has no active metabolites (i.e., it is not a prodrug).

Vortioxetine was discovered by scientists at Lundbeck who reported the rationale and synthesis for the drug (then called Lu AA21004) in a 2011 paper.

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