Products
Vortioxetine is commercially available as film-coated tablets and as an oral solution (drops). It was approved in the United States and the EU in 2013 and in many countries in 2016 (Brintellix, United States: Trintellix).
Structure and properties
Vortioxetine (C18H22N2S, Mr = 298.4 g/mol) is a piperazine derivative. It is present in the film-coated tablets as vortioxetine hydrobromide, a white to light beige powder that is sparingly soluble in water. The active ingredient belongs to the biarylsulfanyl antidepressants. Vortioxetine DL-lactate is present in the solution.
Effects
Vortioxetine (ATC N06AX26) has antidepressant and antianxiety properties and improves cognitive function. The effects are due to inhibition of the reuptake of serotonin into presynaptic nerve terminals. This increases the activity of serotonin in the central nervous system. Vortioxetine additionally also binds to various serotonin receptors as a partial agonist, as an agonist and antagonist. This exerts effects on various neurotransmitter systems. Vortioxetine has a long half-life of 66 hours.
Indications
For the treatment of depressive episodes in adults (major depressive episodes) and for subsequent maintenance therapy.
Dosage
According to the SmPC. Tablets or drops are taken once daily, independent of meals.
Contraindications
- Hypersensitivity
- Combination with non-selective MAO inhibitors or selective MAO-A inhibitors.
For complete precautions, see the drug label.
Interactions
Vortioxetine is metabolized by several CYP isozymes. Corresponding drug-drug interactions with CYP inhibitors and CYP inducers are possible. Other interactions have been described with serotonergic drugs, drugs that lower the seizure threshold, and MAO inhibitors, among others.
Adverse effects
The most common adverse effect observed is nausea.
