Vortioxetine is an antidepressant that acts as a serotonin and noradrenaline reuptake inhibitor and modulates several serotonergic receptors. This drug improves neuronal transmission and has positive effects on cognitive symptoms of depression. Metabolization of vortioxetine mainly involves the CYP2D6 enzyme, and genetic variants in this gene can affect the plasma concentration of the drug.
Vortioxetine (Dosage)
Vortioxetine is an antidepressant that acts as a serotonin and noradrenaline reuptake inhibitor and modulates serotonergic receptors. This drug was licensed by the U.S. Food and Drug Administration (FDA) to treat depression in 2013.
MECHANISM OF ACTION
Its mechanism of action is multimodal. On the one hand, it increases the concentration of the neurotransmitters serotonin and noradrenaline in the synaptic cleft by blocking their reuptake, thus enhancing their transmission. On the other hand, it modulates postsynaptic serotonin receptors, either activating or blocking them.
Vortioxetine can influence the neurotransmission of several systems, such as serotonin, noradrenaline, dopamine, acetylcholine, histamine, glutamate and gamma-aminobutyric acid. This multimodal action, affecting different complex neuronal networks, may explain the improved efficacy in the treatment of cognitive symptoms of depression.
CONTRAINDICATIONS
Vortioxetine should not be used in patients with known hypersensitivity to this active ingredient or to any of its excipients. Concomitant use with selective or non-selective monoamine oxidase inhibitors is also not recommended due to the risk of serotonin syndrome.
Special caution is recommended in combination therapy with migraine medications such as triptans, other antidepressants and neuroleptics, or CYP2D6 inhibitors such as bupropion. Some supplements such as St. John's wort may also cause unwanted effects.
SIDE EFFECTS
The most common adverse effects of vortioxetine include nausea, dry mouth, dizziness, gastrointestinal problems such as constipation or diarrhea, sexual dysfunction, and vomiting.
BRAND NAMES
- Trintellix®
- Brintellix®
Genes analyzed
CYP2D6
Bibliography
Bousman CA, Stevenson JM, Ramsey LB, et al. Clinical Pharmacogenetics Implementation Consortium (CPIC) Guideline for CYP2D6, CYP2C19, CYP2B6, SLC6A4, and HTR2A Genotypes and Serotonin Reuptake Inhibitor Antidepressants. Clin Pharmacol Ther. 2023 Jul;114(1):51-68.
Chen G, Højer AM, Areberg J, et al. Vortioxetine: Clinical Pharmacokinetics and Drug Interactions. Clin Pharmacokinet. 2018 Jun;57(6):673-686.
Zhang X, Cai Y, Hu X, et al. Systematic Review and Meta-Analysis of Vortioxetine for the Treatment of Major Depressive Disorder in Adults. Front Psychiatry. 2022 Jun 24;13:922648.
