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Pharmacological properties


The mechanism of action of vortioxetine is believed to be associated with its multimodal activity, which is a combination of two pharmacological mechanisms: direct modulation of receptor activity and inhibition of the serotonin transporter (5-HT). Preclinical evidence suggests that vortioxetine is a 5-HT antagonist35-HT7 and 5-HT1Dpartial agonist 5-HT1B5-HT agonist1A a receptor and an inhibitor of the 5-HT transporter, modulates neurotransmission in several systems, including serotonin, norepinephrine, dopamine, histamine, acetylcholine, GABA, and glutamate. Such multimodal activity is believed to provide antidepressant and anxiolytic effects, and also helps to improve cognitive function, learning, and memory in preclinical studies of vortioxetine. Preclinical studies indicate that vortioxetine does not cause sexual dysfunction. The exact contribution of each component of this mechanism to the observed pharmacodynamic profile remains unclear, therefore, attention should be paid when extrapolating preclinical data directly to humans.

It was found that the capture of the serotonin transporter with the use of various daily doses of vortioxetine was approximately 50% at a dose of 5 mg, 65% at a dose of 10 mg and 80% at a dose of 20 mg. Vortioxetine clinically demonstrated an antidepressant effect when capturing the 5-HT transporter by 50%.

Clinical efficacy and safety. The effectiveness of vortioxetine increases with increasing dose. In addition, vortioxetine at doses of 5–20 mg / day has been shown to be effective in a wide range of depressive (according to the MADRS scale) and alarming (according to the HAM-A scale) symptoms of depression.

Relapse prevention. The duration of the antidepressant effect was demonstrated in a relapse prevention study in which the placebo group identified a twofold increase in the risk of relapse compared with the vortioxetine group.

Elderly patients. In the range of doses of vortioxetine 5–20 mg / day, the efficacy and tolerability in the elderly was consistent with the results of studies in the adult population.

Patients with severe depression or high levels of anxiety symptoms. Antidepressant efficacy has been demonstrated in patients with severe depression (≥30 points on the MADRS scale) and in patients with depression with high levels of anxiety symptoms (≥20 points on the HAM-A scale) in short-term studies, including studies involving elderly patients and long-term relapse prevention studies.

Patients with an inadequate response to treatment with selective serotonin / noradrenaline reuptake inhibitors (SSRIs / SSRIs). In a comparative study of the use of vortioxetine in flexible doses in patients with depression after an inadequate response to treatment with SSRIs / SSRIs, a higher statistically significant efficacy of vortioxetine in a daily dose of 10–20 mg was demonstrated compared with agomelatine in a dose of 25–50 mg (according to the MADRS scale) , Clinical Global Impression-Clinical Global Impression-I (CGI-I) and Sheehan Disability Scale (SDS) scaled clinical significance.

Cognitive dysfunction in depression. Studies of the effect of the drug on cognitive processes revealed that the effect of vortioxetine is mainly due to a direct effect on cognitive function, and not an indirect effect through a decrease in the severity of symptoms of depression.

Quality of life and overall functioning. Vortioxetine was superior to placebo in terms of assessing the quality of life, clinically significantly improving overall health (on the EQ-5D scale) and overall functioning (on the SDS scale - work, social and family life) compared with a placebo or reference drug (agomelatine).Moreover, the best placebo effects in terms of quality of life continued throughout the long-term relapse prevention study.

Portability and safety. The safety and tolerance of vortioxetine was evaluated in short and long-term studies for doses of 5–20 mg / day.

Vortioxetine did not increase the incidence of insomnia or drowsiness compared with placebo.

During a systematic assessment of potential withdrawal symptoms, there was no clinically significant difference between vortioxetine and placebo in the frequency and nature of withdrawal symptoms either after a short-term (6–12 week) or after a long-term (24–64 week) treatment period.

In clinical studies of vortioxetine, the frequency of reporting undesirable sexual reactions was low and similar to placebo, the incidence of sexual dysfunction associated with therapy, and overall ASEX scores showed no clinically significant difference with placebo regarding the symptoms of sexual dysfunction with the recommended dose of vortioxetine , but the use of the drug in high doses was associated with an increase in the number of cases of dysfunction.

In clinical trials, like placebo, vortioxetine did not affect body weight, heart rate, and blood pressure. There were no clinically significant changes in the evaluation of liver and kidney function.

Vortioxetine did not have any clinically significant effect on ECG parameters, including Q – T, Q – Tc, P – R, and QRS intervals, in patients with major depressive disorder. In a thorough study of Q – Tc in healthy volunteers with doses up to 40 mg / day, there was no potential to increase the Q – Tc interval.

Childhood. Clinical studies involving pediatric patients have not been conducted, therefore, the safety and effectiveness of Brintellix for patients under the age of 18 have not been established.


Absorption. Vortioxetine is slowly but well absorbed after oral administration and Cmax in blood plasma is reached within 7-11 hours. After repeated use of the drug in doses of 5; 10 or 20 mg / day, the average value of Cmax 9–33 ng / ml. Absolute bioavailability is 75%. There is no effect of food intake on pharmacokinetics.

Distribution. The average volume of distribution is 2600 L, which indicates a volumetric extravascular distribution. Vortioxetine strongly binds to plasma proteins (98–99%), and binding, apparently, does not depend on the concentration of vortioxetine in blood plasma.

Biotransformation. Vortioxetine is extensively metabolized in the liver, mainly by oxidation and subsequent conjugation with glucuronic acid. In vitro cytochrome P450 isoenzymes CYP 2D6, CYP 3A4 / 5, CYP 2C19, CYP 2C9, CYP 2A6, CYP 2C8 and CYP 2B6 are involved in the metabolism of vortioxetine. The inhibitory or inducing effect of vortioxetine in vitro on the isoenzymes of CYP 1A2, CYP 2A6, CYP 2B6, CYP 2C8, CYP 2C9, CYP 2C19, CYP 2D6, CYP 2E1 or CYP 3A4 / 5 is not noted. Vortioxetine is a weak substrate and inhibitor of P-glycoprotein. The main metabolite of vortioxetine is pharmacologically inactive.

Elimination. T½ - 66 hours. About ⅔ of the inactive metabolite of vortioxetine is excreted in the urine and around 1/3 - with feces. Only a small amount of vortioxetine is excreted in the feces. Stable plasma concentration is achieved after 2 weeks.

Linearity / nonlinearity. The pharmacokinetics are linear and time-independent in the range of doses studied (2.5–60 mg / day). Given the half-life, the accumulation index is 5 to 6 based on AUC0-24 after several doses of 5 to 20 mg / day.

Elderly patients. In healthy elderly volunteers (≥65 years; n = 20), the effect of vortioxetine is enhanced by 27% (Cmax and AUC) compared with young healthy control group volunteers (aged ≤45 years) after several doses of 10 mg / day. No dose adjustment is required.

Renal failure.After a single dose of vortioxetine at a dose of 10 mg for renal failure (according to the Cockroft-Gault formula of mild, moderate or severe severity; n = 8), a slight increase in exposure (up to 30%) was observed compared to that in the control group of healthy volunteers. In patients with end-stage renal failure, only a small fraction of vortioxetine was lost during dialysis (AUC and Cmax 13 and 27% lower; n = 8) after a single dose of vortioxetine in a dose of 10 mg. No dose adjustment is required.

Liver failure. The presence of mild or moderate hepatic insufficiency (on the Child-Pugh scale; n = 8 in each group) did not affect the pharmacokinetics of the drug with a single dose of 10 mg (AUC changes were 10%). No dose adjustment is required. Vortioxetine has not been studied in patients with severe hepatic insufficiency, therefore caution should be exercised when prescribing the drug in such patients.

Weak CYP 2D6 metabolizers. In weak CYP 2D6 metabolizers, the concentration of vortioxetine in the blood plasma is approximately 2 times higher than in extensive metabolizers. In the presence of potent CYP 3A4 / 2C9 inhibitors, the potential effect may be more pronounced. Depending on the individual reaction, dose adjustment may be required, as with other patients.


Treatment of major depressive disorder in adult patients.


Brintellix is ​​administered orally, regardless of the meal. initial and maintenance doses are 10 mg 1 time per day. depending on the individual sensitivity of the patient, the dose can be increased to a maximum of 20 mg / day, or reduced to a minimum of 5 mg / day.

After eliminating the symptoms of depression, it is recommended to continue treatment for ≥6 months to consolidate the antidepressant effect.

Discontinuation of treatment. Brintellix treatment can be stopped abruptly; there is no need for a gradual dose reduction.

Elderly patients. Dose adjustment for elderly patients is not required.

Inhibitors of cytochrome P450. Depending on the individual patient response, the use of vortioxetine in low doses should be considered if potent CYP 2D6 inhibitors are added to the therapy (for example, bupropion, quinidine sulfate, fluoxetine, paroxetine).

Inductors of cytochrome P450. Depending on the individual patient response, dose adjustment of vortioxetine should be considered if a cytochrome P450 inducer is added to therapy (e.g. rifampicin, carbamazepine, phenytoin).


Hypersensitivity to the active substance or any component of the drug. simultaneous use with non-selective MAO inhibitors or selective MAO-a inhibitors.

Side effects

The most common adverse reaction is nausea. usually mild or moderate adverse reactions occurred during the first 2 weeks of treatment. reactions were usually transient and usually did not require discontinuation of therapy. digestive reactions (e.g. nausea) were more common in women than in men.

Adverse reactions described below were defined as: very frequent (≥1 / 10), frequent (from ≥1 / 100 to 1/10), infrequent (from ≥1 / 1000 to 1/100), rare (from ≥1 / 10,000 to 1/1000), very rare (1/10 000) and unknown (the frequency cannot be determined from the available data).


System, organ, class Frequency Adverse reactions
Change in nutrition and metabolism Often Anorexia
From the psyche Often Pathological dreams
Infrequently Bruxism
From the nervous system Often Dizziness
From the cardiovascular system Infrequently Blush
From the digestive system Often Nausea
Often Diarrhea, constipation, vomiting
On the part of the skin and subcutaneous tissue Often Generalized itching
Infrequently Increased night sweats

special instructions

Use in pediatrics.Brintellix is ​​not recommended for the treatment of depression in patients aged 18 years, since safety and effectiveness for this age group have not been established. in clinical trials involving children who used other antidepressants, suicidal behavior (suicidal attempts and suicidal thoughts) and hostility (mainly aggression, opposition behavior, anger) were noted more often than in patients who used placebo.

Suicide / suicidal thoughts. Depression is associated with an increased risk of suicidal thoughts, self-harm, and suicide (events associated with suicide). This risk persists until significant remission is achieved. Since improvement may not occur during the first few weeks of treatment or longer, patients should be carefully monitored until remission. It is known from general clinical experience that the risk of suicide may increase in the early stages of recovery.

Patients with a history of suicidal history or with significant signs of suicidal thoughts before treatment are known to be at greater risk of suicidal thoughts or suicide attempts and need to be carefully monitored during treatment. A meta-analysis of placebo-controlled clinical trials of antidepressants in adult patients with mental disorders showed an increased risk of suicidal behavior compared with placebo in patients under 25 years of age. Strict observation of patients and, in particular, those at high risk should accompany treatment, especially at the beginning of therapy and

Tags: Brintellix® [Vortioxetine]