| ATC Code | N06AX26 |
| CAS number | 508233-74-7 |
| PUB number | 9966051 |
| Drugbank ID | DB09068 |
| Empirical formula | C18H22N2S |
| Molar mass (g·mol−1) | 298,446 |
| Physical state | solid |
| Density (g·cm−3) | 1,2 |
| Boiling point (°C) | 424,8 |
| PKS value | 8,85 |
| Solubility | 0.00362 mg/mL |
Vortioxetine is an active ingredient for the treatment of depression and anxiety disorders. It belongs to the group of serotonin antagonist and reuptake inhibitors (SARI). Vortioxetine is available as a tablet or solution. It is a piperazine derivative and is usually available as vortioxetine hydrobromide. It is also a white to beige powder that is only slightly soluble in water. As a solution, the active ingredient is usually available as vortioxetine DL-lactate.
Vortioxetine works in several ways. By binding to the serotonin receptor, it blocks serotonin reuptake and the serotonin concentration in the central nervous system increases. It also acts as a partial agonist of the 5-HT1B receptor, as an agonist of 5-HT1A and as an antagonist of the 5-HT3, 5-HT1D and 5-HT7 receptors. Binding to these receptors results in the effects of various neurotransmitters. These include noradrenaline, dopamine, acetylcholine, histamine, glutamate and GABA.
Vortioxetine is a CYP450 isoenzyme substrate and is metabolized (converted) in the liver by various CYP enzymes (primarily by CYP2D6). The bioavailability, i.e. the percentage of the active ingredient that is available in the blood, is 75%. Food does not appear to have any influence on bioavailability. The half-life, i.e. the time the body needs to excrete half of the active ingredient, is around 66 hours. The maximum plasma concentration (Cmax), i.e. the maximum concentration of the active substance in the blood plasma (liquid cell-free part of the blood), is reached after about 7 to 11 hours.
Always take vortioxetine exactly as described in the package leaflet or as advised by your doctor.
The usual recommended dose for adults is initially 10 mg daily.
The recommended maintenance dose should be between 5-20 mg per day.
The maximum dose is 20 mg per day.
For patients over 65 years of age, the initial dose is 5 mg daily.
The following side effects may occur:
Very common:
Frequent:
Occasionally:
Rarely:
Frequency unknown:
Interactions may occur if the following medicines are taken at the same time:
Vortioxetine can react positively to methadone in a urine drug screen.
Vortioxetine must NOT be taken in the following cases
Vortioxetine should only be used from the age of 18. At the age of 7-11 years, the active substance is NOT recommended due to a lack of information. At the age of 12-17 years, the efficacy has NOT been proven.
Vortioxetine should NOT be used during pregnancy unless your doctor considers it absolutely necessary.
If taken in the last trimester of pregnancy, newborns may experience withdrawal symptoms. These can manifest themselves as breathing problems, seizures, vomiting, tremors, etc.
In such cases, consult a doctor IMMEDIATELY. Treatment with vortioxetine should always be discussed with a midwife or doctor. Therapy should only be started or stopped under medical supervision.
Vortioxetine should NOT be used during breastfeeding, as it is likely to pass into breast milk. Your doctor will decide whether you should breastfeed or discontinue treatment after weighing up the risks and benefits.
Vortioxetine was approved in the USA and the EU in 2013. Switzerland followed suit in 2016. Germany decided, also in 2016, that the active ingredient had no advantage over selective serotonin reuptake inhibitors (SSRIs) and was therefore withdrawn from the market. In addition, the active ingredient is sold at a high price compared to other antidepressants.
Thomas Hofko
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