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. In Britain, it is only recommended in people who have not improved sufficiently on two other antidepressants. It is taken by mouth. 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. In 2017, it was the 312th most commonly prescribed medication in the United States, with more than one million prescriptions.
Medical uses
Vortioxetine is used as a treatment for major depressive disorder. Effectiveness appear to be similar to other antidepressants. It may be used when other treatments have failed. Vortioxetine is also used off label for anxiety. A 2016 review found it was not useful in generalized anxiety disorder.
Adverse effects
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, 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.
Vortioxetine reaches peak plasma concentration within 7 to 11 hours post-administration, and its mean terminal half-life is ≈ 66 hours. 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. Vortioxetine's pKa values are determined to be 9.1 and 3.0 according to Australian Public Assessment Report for vortioxetine hydrobromide.
History
Vortioxetine was discovered by scientists at Lundbeck who reported the rationale and synthesis for the drug in a 2011 paper. 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, and could be expanded to include two other Lundbeck compounds. Vortioxetine was approved by the U.S. FDA for the treatment of major depressive disorder in adults in September 2013, and it was approved in Europe later that year.
Society and culture
It is made by the pharmaceutical companies Lundbeck and Takeda.
Names
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.
