2014 issue 2

Back

Volume 30, issue 2

Review article

Selective or multimodal? The development of serotonin reuptake inhibitors – the case of vortioxetine

Przemysław Bieńkowski1, Łukasz Święcicki2
1. Instytut Psychiatrii i Neurologii w Warszawie, Zakład Farmakologii
2. Instytut Psychiatrii i Neurologii w Warszawie, II Klinika Psychiatryczna
Farmakoterapia w Psychiatrii i Neurologii, 2014, 2, 61–67
Keywords: vortioxetine, multimodal antidepressant drugs, serotonin receptors, depression

Abstract

The recent approval of vortioxetine in the USA and Europe adds a new medication to a group of multi-modal antidepressant drugs modulating both serotonin transporters and some serotonin receptors. Both in vitro and in vivo studies indicate that vortioxetine is a potent and relatively selective inhibitor of serotonin reuptake with marginal affi nity to norepinephrine and dopamine transporters. In addition, vortioxetine at the concentrations needed to inhibit serotonin transporters antagonize serotonin 5-HT3 (3.7 nM) and 5-HT7 (19 nM) receptors and stimulate serotonin 5-HT1A receptors (15 nM). The affi nity of vortioxetine to other serotonin receptors (5-HT1B, 5-HT1D) is weaker but can contribute to its clinical effects. The antidepressant effects of vortioxetine have been assessed in several clinical studies, in patients with a diagnosis of major depression according to the DSM-IV criteria. The drug exerted dose-dependent antidepressant effects comparable to those produced by the active comparators used in the study, duloxetine and venlafaxine. The authors of clinical reports concluded that the drug was safe and well tolerated. The most common side effects associated with vortioxetine administration were nausea and headache. The risk of sexual dysfunction in patients treated with vortioxetine was relatively low. The aim of this brief review is to familiarize psychiatrists with the most important features of vortioxetine, with special emphasis given to a possible relationship between its pharmacological properties and clinical indications.

Address for correspondence:
Prof. dr hab. n. med. Przemysław Bieńkowski
Instytut Psychiatrii i Neurologii, Zakład Farmakologii
ul. Sobieskiego 9, 02-957 Warszawa, Poland
e-mail: bienkow@ipin.edu.pl