VORTIOXETINE

Day 1: #vortioxetine is a unique antidepressant, discovered from exploring bis-aryl-sulfanyl amine compounds. It is categorised as a ‘serotonergic’ drug, acting both as an SSRI & as a serotonin receptor modulator. Approved for adults in the USA in 2013 & in Europe 2014

Day 2: Indication for #vortioxetine is major depressive disorder. Used when at least 2 other anti-depressants have not worked. Oral delivery 10mg od (5mg if >65) titrated to 20mg according to response (caution elderly >10mg). Continue minimum 6 months after symptoms resolve

Day 3: High but slow oral absorption, highly plasma protein bound & high Vd. Liver metabolism major via CYP2D6, minor 3A4/5 & 2C9. No active metabolites. 2/3 excretion urine, 1/3 faeces. T½ 66 hrs with around 2 weeks to steady state. No dose adjustment for renal/hepatic impairment, but this may be necessary for poor CYP2D6 metabolisers

Day 4: #vortioxetine has high affinity for the serotonin (5-HT) transporter & increases serotonin levels. It also acts as a 5-HT₃ & 5-HT₇ receptor antagonist & a 5-HT_1A agonist. Further, multiple neural pathways may be modulated, such as NE, dopamine, ACh, histamine, as well as modulation GABA & glutamate, but much remains poorly understood