Vortioxetine, sold under the trade names Trintellix among others, is a medication used to treat major depressive disorder. Effectiveness is viewed as similar to that of other antidepressants. It is only recommended in people who have not improved sufficiently on two other antidepressants. It is taken by mouth.
|Trade names||Trintellix, Brintellix, others|
|By mouth (film-coated tablets)|
|Bioavailability||75% (peak at 7–11 hours)|
|Metabolism||Extensive Liver, primarily CYP2D6-mediated oxidation|
|Elimination half-life||66 hours|
|Excretion||59% in urine, 26% in feces|
|Chemical and physical data|
|Molar mass||298.45 g/mol (379.36 as hydrobromide) g·mol−1|
|3D model (JSmol)|
|(what is this?)|
Common side effects include constipation and nausea. Serious side effects may include suicide in those under the age of 25, serotonin syndrome, bleeding, mania, and SIADH. A withdrawal syndrome may occur if the dose is rapidly decreased. Use during pregnancy and breastfeeding is not generally recommended. It is classified as a serotonin modulator. How it works is not entirely clear but is believed to be related to increasing serotonin levels.
It was approved for medical use in the United States in 2013. A month supply in the United Kingdom costs the NHS about £27.72 as of 2019. In the United States the wholesale cost of this amount is about 368.40 USD. In 2016 it was the 260th most prescribed medication in the United States with more than a million prescriptions.
The most common side effects reported with vortioxetine are nausea, diarrhea, dry mouth, constipation, vomiting, flatulence, dizziness, and sexual dysfunction. However, with the singular exception of nausea, these side effects occurred in less than 10% of study participants given the active drug, with up to 8% of placebo-treated participants reporting the same side effects.
If vortioxetine is prescribed alongside traditional selective serotonin reuptake inhibitors (SSRIs), or other serotonergic drugs, this can induce the potentially life-threatening serotonin syndrome.
Incidence of sexual dysfunction is only slightly higher in patients taking vortioxetine than in people taking placebos and occurs in less than 10% of vortioxetine-treated patients. As such, vortioxetine may be appropriate for people who have suffered sexual side effects from other antidepressant medications.
It increases serotonin concentrations in the brain by inhibiting its reuptake in the synapse, and by modulating (activating certain receptors while blocking, or antagonizing, others) certain serotonin receptors. This puts it in the class of atypical antidepressants known as serotonin modulators and stimulators.
|Ki (nM)||IC50 / EC50 (nM)||IA (%)|
* Human isoforms
Steady-state mean Cmax values were 9, 18, and 33 ng/mL following doses of 5, 10, and 20 mg/day. Steady-state plasma concentrations are typically reached within two weeks.
In 2007, the compound was in Phase II clinical trials, and Lundbeck and Takeda entered into a partnership in which Takeda paid Lundbeck $40 million upfront, with promises of up to $345 million in milestone payments, and Takeda agreed to pay most of the remaining cost of developing the drug. The companies agreed to co-promote the drug in the US and Japan, and that Lundbeck would receive a royalty on all such sales. The deal included another drug candidate, tedatioxetine (Lu AA24530), and could be expanded to include two other Lundbeck compounds.
Society and cultureEdit
Vortioxetine was previously trademarked as Brintellix in the United States, but on May 2, 2016, the US FDA approved a name change to Trintellix in order to avoid confusion with the blood-thinning medication Brilinta (ticagrelor).
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The authors suggest that vortioxetine is currently a good second-line antidepressant option and shows promise, pending additional long-term data, to become a first-line antidepressant option.
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