Vortioxetine
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| Non-proprietary name | Vortioxetine | |||||||||||||||||||||
| other names |
1- {2 - [(2,4-Dimethylphenyl) sulfanyl] phenyl} piperazine ( IUPAC ) |
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| Molecular formula | C 18 H 22 N 2 S | |||||||||||||||||||||
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| Molar mass | 298,45 g · mol -1 | |||||||||||||||||||||
| pK s value |
9.1 (free base) |
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| As far as possible and customary, SI units are used. Unless otherwise noted, the data given apply to standard conditions . | ||||||||||||||||||||||
Vortioxetine is an antidepressant acting drug with multimodal mechanism of action. Vortioxetine is a so-called serotonin modulator and stimulator and is perorally effective.
In September 2013, the vortioxetine preparation was the company Lundbeck for the US market (as Trintellix ) and in December 2013 the European market (as Brintellix ) for the treatment of episodes of major depression admitted in adults. In Germany, Brintellix was available from May 2015 to August 2016. In Switzerland the drug is approved since 17 August 2016th
Mechanism of action
The mechanism of action of vortioxetine combines two complementary pharmacological modes of action: the inhibition of the 5-HT transporter and the direct modulation of the complex serotonergic receptor activity . Preclinical data indicate that vortioxetine
- antagonistic to the 5-HT 3 , 5-HT 7 , and 5-HT 1D receptors,
- partially agonistic at the 5-HT 1B receptor ,
- agonistic at the 5-HT 1A receptor
acts and is an inhibitor of the 5-HT transporter. Preclinical studies have also shown in vivo that vortioxetine modulates the neural firing rate and neurotransmitter release in various important systems, which leads to increased levels of serotonin, norepinephrine , dopamine , acetylcholine and histamine, as well as a reduction in GABA and an increase in glutamate in specific brain areas leads. This multimodal pharmacological profile of vortioxetine is held responsible for the antidepressant effects and the indications for improving cognitive performance in the context of the depressive episode, of learning and remembering.
Side effects and restrictions on use
The most common side effect is nausea, which was observed in over 10% of those treated. Vomiting, constipation, diarrhea, decreased appetite, dizziness and itching were also observed (in 1 to 10% of those treated). Vortioxetine is contraindicated with concomitant use of non-selective monoamine oxidase inhibitors (MAOIs) or selective MAO-A inhibitors.
Simultaneous use of drugs with a serotonergic effect ( e.g. tramadol , sumatriptan , other triptans) increases the risk of serotonin syndrome .
Chemical-pharmaceutical information
The vortioxetine be used pharmaceutically hydrobromide and Vortioxetin- DL - lactate . Both substances are a white to slightly beige, non- hygroscopic powder. The vortioxetine hydrobromide used in the Brintellix film tablets is soluble in methanol and ethanol , and sparingly soluble in water and aqueous systems with a pH between 2.0 and 8.3 appears in four polymorphic forms. The vortioxetine lactate used in the oral drip solution is soluble in polar solvents and in water and forms three polymorphic forms.
Trade names
Brintellix (EU), Trintellix ( CA , USA)
Withdrawal from the market in Germany
Lundbeck ceased sales in Germany on August 15, 2016. This was done because no agreement was reached in the price negotiations with the National Association of Health Insurance Funds after the active ingredient was not granted any additional benefit by the Federal Joint Committee . According to Lundbeck, the umbrella association was unwilling to compromise despite clear financial concessions and insisted on a price at a generic level, although the daily therapy costs for the health insurance companies would only have been in the range of 1 euro.
The German Society for Psychiatry and Psychotherapy, Psychosomatics and Neurology (DGPPN) has already criticized the result of the benefit assessment by the Institute for Quality and Efficiency in Health Care . In addition to the fundamental criticism of the procedure, the DGPPN pointed out that an evaluation had not taken place for methodological reasons. In addition, important factors such as side effects and quality of life did not play a role in the assessment of the drug for the patient.
Web links
- Product information on Brintellix on the website of the European Medicines Agency
- Vortioxetine in depression: no hint of added benefit. IQWIG press release of August 3, 2015.
Individual evidence
- ↑ ema.europa.eu: Brintellix, INN-vortioxetine , accessed on March 1, 2015.
- ↑ This substance has either not yet been classified with regard to its hazardousness or a reliable and citable source has not yet been found.
- ^ Jürgen Stoschek: Antidepressant Vortioxetine: Multimodal Activities. In: Deutsches Ärzteblatt , 2015; 112 (17): A-792 .
- ↑ Vortioxetine: New antidepressant from May. April 14, 2015, accessed February 11, 2019 .
- ↑ compendium.ch. In: compendium.ch. Archived from the original on August 24, 2016 ; accessed on August 22, 2016 .
- ↑ Doctors Zeitung: Profit margin too low: Lundbeck takes vortioxetine from the market. In: www.aerztezeitung.de. Retrieved July 8, 2016 .
- ↑ Doctors newspaper: Antidepressants: Vortioxetine from mid-August out of sales. In: www.aerztezeitung.de. Retrieved July 8, 2016 .
- ^ Written statement by the DGPPN. (pdf) August 24, 2015, accessed on February 11, 2019 .