Бринтелликс
Бринтелликс Uses, Dosage, Side Effects, Food Interaction and all others data.
Бринтелликс is an atypical antipsychotic and antidepressant indicated for the treatment of major depressive disorder (MDD). It is classified as a serotonin modulator and simulator (SMS) as it has a multimodal mechanism of action towards the serotonin neurotransmitter system whereby it simultaneously modulates one or more serotonin receptors and inhibits the reuptake of serotonin. More specifically, vortioxetine acts via the following biological mechanisms: as a serotonin reuptake inhibitor (SRI) through inhibition of the serotonin transporter, as a partial agonist of the 5-HT1B receptor, an agonist of 5-HT1A, and an antagonist of the 5-HT3, 5-HT1D, and 5-HT7 receptors. SMSs were developed because there are many different subtypes of serotonin receptors, however, not all of these receptors appear to be involved in the antidepressant effects of SRIs. Some serotonin receptors seem to play a relatively neutral or insignificant role in the regulation of mood, but others, such as 5-HT1A autoreceptors and 5-HT7 receptors, appear to play an oppositional role in the efficacy of SRIs in treating depression.
Бринтелликс binds with high affinity to the human serotonin transporter (Ki=1.6 nM), but not to the norepinephrine (Ki=113 nM) or dopamine (Ki>1000 nM) transporters. Бринтелликс potently and selectively inhibits reuptake of serotonin by inhibition of the serotonin transporter (IC50=5.4 nM). Specifically, vortioxetine binds to 5HT3 (Ki=3.7 nM), 5HT1A (Ki=15 nM), 5HT7 (Ki=19 nM), 5HT1D (Ki=54 nM), and 5HT1B (Ki=33 nM), receptors and is a 5HT3, 5HT1D, and 5HT7 receptor antagonist, 5HT1B receptor partial agonist, and 5HT1A receptor agonist.
| Trade Name | Бринтелликс |
| Availability | Prescription only |
| Generic | Vortioxetine |
| Vortioxetine Other Names | Vortioxetina, Vortioxétine, Vortioxetine, vortioxetinum |
| Related Drugs | Trintellix, Rexulti, sertraline, trazodone, Lexapro, Zoloft, citalopram, Cymbalta, Prozac |
| Type | |
| Formula | C18H22N2S |
| Weight | Average: 298.45 Monoisotopic: 298.15036989 |
| Protein binding | The plasma protein binding of vortioxetine in humans is 98%, independent of plasma concentrations. No apparent difference in the plasma protein binding between healthy subjects and subjects with hepatic (mild, moderate) or renal (mild, moderate, severe, ESRD) impairment is observed. |
| Groups | Approved, Investigational |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | Russia |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Бринтелликс is an atypical antipsychotic and antidepressant indicated for the treatment of major depressive disorder (MDD).
Бринтелликс is indicated for the treatment of major depressive disorder (MDD).
Бринтелликс is also used to associated treatment for these conditions: Major Depressive Disorder (MDD)
How Бринтелликс works
Бринтелликс is classified as a serotonin modulator and simulator (SMS) as it has a multimodal mechanism of action towards the serotonin neurotransmitter system whereby it simultaneously modulates one or more serotonin receptors and inhibits the reuptake of serotonin. More specifically, vortioxetine acts via the following biological mechanisms: as a serotonin reuptake inhibitor (SRI) through inhibition of the serotonin transporter, while also acting as a partial agonist of the 5-HT1B receptor, an agonist of 5-HT1A, and antagonist of the 5-HT3, 5-HT1D, and 5-HT7 receptors.
Toxicity
The most commonly reported adverse effects during clinical trials were nausea, diarrhea, and dry mouth. The FDA label includes a blackbox warning for the following risks and complications: serotonin syndrome, especially when combined with other serotonergic agents; increased risk of abnormal bleeding, especially when combined with NSAIDs, aspirin, or other drugs that affect coagulation; activation of mania/hypomania; hyponatremia; and suicidal thoughts and behaviour in children, adolescents, and young adults.
Food Interaction
- Avoid alcohol.
- Avoid St. John's Wort. When administered with vortioxetine, this herb may increase the risk of serotonin syndrome.
- Take with or without food.
[Moderate] GENERALLY AVOID: Alcohol may potentiate some of the pharmacologic effects of CNS-active agents.
Use in combination may result in additive central nervous system depression and
MANAGEMENT: Patients receiving CNS-active agents should be warned of this interaction and advised to avoid or limit consumption of alcohol.
Ambulatory patients should be counseled to avoid hazardous activities requiring complete mental alertness and motor coordination until they know how these agents affect them, and to notify their physician if they experience excessive or prolonged CNS effects that interfere with their normal activities.
Бринтелликс Drug Interaction
Major: amphetamine / dextroamphetamine, duloxetine, venlafaxine, escitalopram, desvenlafaxine, lisdexamfetamine, sertralineModerate: lamotrigine, pregabalin, methylphenidateUnknown: aripiprazole, lorazepam, lurasidone, esomeprazole, acetaminophen, quetiapine, acetaminophen, cyanocobalamin, cholecalciferol, alprazolam
Бринтелликс Disease Interaction
Moderate: depression, angle closure glaucoma, bleeding, hyponatremia, mixed/manic episode
Volume of Distribution
The apparent volume of distribution of vortioxetine is approximately 2600 L, indicating extensive extravascular distribution.
Elimination Route
The maximal plasma vortioxetine concentration (Cmax) after dosing is reached within 7 to 11 hours postdose. Absolute bioavailability is 75%. No effect of food on the pharmacokinetics was observed.
Half Life
Mean terminal halflife is approximately 66 hours
Elimination Route
Following a single oral dose of [14C]labeled vortioxetine, approximately 59% and 26% of the administered radioactivity was recovered in the urine and feces, respectively as metabolites. Negligible amounts of unchanged vortioxetine were excreted in the urine up to 48 hours.
Innovators Monograph
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