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Brintellix® [Vortioxetine]

Lundbeck AS
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Clinical Pharmacology

The mechanism of action of vortioxetine is believed to be related to 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 data show that vortioxetine is an antagonist of 5-HT 3, 5-HT 7, and 5-HT 1D receptors, a partial agonist of 5-HT 1B receptors, an agonist of 5-HT 1A receptors and an inhibitor of the 5-HT transporter, and 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 as well as improved cognitive function, learning and memory in the preclinical setting of vortioxetine. In addition, 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, so care should be taken when extrapolating preclinical data directly to humans. It was found that the seizure of the serotonin transporter by various daily doses of vortioxetine was approximately 50% at a dose of 5 mg, 65% at a dose of 10 mg, and more than 80% at a dose of 20 mg. Vortioxetine was clinically shown to have an antidepressant effect when up to 50% of the 5-HT transporter is captured.

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Brintellix® [Vortioxetine]

Dosage and Administration

Brintellix is ​​taken orally with or without food. The initial and maintenance doses are 10 mg once a day. Depending on the individual sensitivity of the patient, the dose can be increased to a maximum of 20 mg per day or reduced to at least 5 mg per day. After elimination of the symptoms of depression, it is recommended to continue treatment for another 6 months to strengthen the antidepressant effect. Termination of treatment. Treatment with Brintellix can be stopped abruptly, there is no need for a gradual dose reduction. Special patient groups. Elderly patients. No dose adjustment is required for elderly patients based solely on age. Inhibitors of cytochrome P450. Depending on the individual patient response, low-dose vortioxetine should be considered if potent CYP2D6 inhibitors (eg bupropion, quinidine, fluoxetine, paroxetine) are added to therapy. Cytochrome P450 inducers. Depending on the individual response of the patient, dose adjustment of vortioxetine should be considered if a cytochrome P450 inducer is added to therapy (for example, rifampicin, carbamazepine, phenytoin). Children. The safety and efficacy of Brintellix for the treatment of depression in patients under the age of 18 has not been established, therefore, its use is not recommended.

Adverse reactions

The most common adverse reaction was nausea. Adverse reactions were usually mild to moderate and were observed during the first two weeks of treatment. Reactions were usually transient and did not usually lead to discontinuation of therapy. Gastrointestinal disorders (eg nausea) were more common in women than in men.
The adverse reactions listed below are defined as:
very often (≥ 1/10),
often (≥ 1/100 to <1/10),
infrequent (≥ 1/1000 to <1/100),
rare (≥ 1/10 000 to <1/1000),
very rare (<1/10 000)
unknown (frequency cannot be determined from available data).
From the side of nutrition and metabolism:
Often: Decreased appetite
From the side of the psyche:
Often: Pathological dreams
Uncommon: Bruxism
From the nervous system:
Often: Dizziness
On the part of the cardiovascular system:
Uncommon: Blush
From the digestive system:
Very common: Nausea
Often: Diarrhea, constipation, vomiting
On the part of the skin and subcutaneous tissue:
Often: Generalized itching
Uncommon: Night sweats

Drug interactions

High levels of vitamin K in foods (spinach, broccoli, lettuce, and other leafy vegetables) can reduce the effect of Warfrex. However, one should not change the diet too abruptly, use vitamins and nutritional supplements without consulting a doctor. Smoking can reduce the anticoagulant effect of the drug. The effect of Warfarex can change under the influence of a large number of drugs. NSAIDs, dipyridamole, valproic acid, cytochrome P450 inhibitors, cimetidine, chloramphenicol, laxatives - increase the risk of bleeding. The combined use of these drugs and Varferex should be avoided (cimetidine can be replaced by ranitidine or famotidine). If treatment with chloramphenicol is necessary, anticoagulant therapy may be temporarily stopped. Diuretics can reduce the effect of anticoagulants (in the case of pronounced hypovolemic action, which can lead to an increase in the concentration of coagulation factors).Weaken the effect: barbiturates, vitamin K, gluthethimide, griseofulvin, dicloxacillin, carbamazepine, mianserin, paracetamol, retinoids, rifampicin, sucralfate, phenazone, cholestyramine. Enhance the action: allopurinol, amiodarone, anabolic steroids (alkylated at the C-17 position), acetylstechracidic acid and other NSAIDs, heparin, glibenclamide, glucagon, danazol, diazoxide, disopyramide, disulfiram, isoniazid, ketoconazole, clarithmicine, clarithimethyne, and disithiramide, disulfiram, isoniazid, ketoconazole, clarithmicine, and clarithimethyne, and disithiramide, disulfiram, isoniazid, ketoconazole, clarithmicine, and clarithimethyne, and disithiramide, disulfiram, isoniazid, ketoconazole, clarithmicine, and glycine chyne, and disithiramide, disulfiram, isoniazid, ketoconazole, clarithycidine, and glycine chyne, as well as glyphenyl acetate; miconazole, nalidixic acid, nilutamide, omeprazole, paroxetine, proguanil, oral hypoglycemic agents - sulfonamide derivatives, sulfonamides, tamoxifen, thyroxin, quinine, quinidine, fluvoxamine, fluconazole, fluorouracil, quinolone , Chloral hydrate, chloramphenicol, cephalosporins, cimetidine, erythromycin, ethacrynic acid, ethanol. When using Warfarex in combination with the above drugs, it is necessary to monitor the INR at the beginning and end of treatment and, if possible, 2-3 weeks from the start of therapy. When using drugs that can increase the risk of bleeding due to a decrease in normal coagulation (inhibition of blood coagulation factors or liver enzymes), the strategy of anticoagulant therapy should be determined by the possibility of carrying out laboratory monitoring. If frequent laboratory control is possible, then, if therapy with such means is necessary, the dose of Warfarex can be reduced by 5-10%. If carrying out laboratory control is difficult, then treatment with Varferex should be stopped if necessary, the appointment of these drugs.

Pregnancy and Lactation

Warfarex should not be prescribed to pregnant women in connection with the identified teratogenic effects, the development of bleeding in the fetus and his death. The drug is excreted with maternal milk in small quantities and has almost no effect on blood coagulation in a child, so this medicine can be used during lactation, but it is desirable to refrain from breastfeeding in the first 3 days of warfarin therapy.

Special instructions

Vortioxetine is metabolized in the liver mainly by oxidation and subsequent conjugation with glucuronic acid. In vitro, cytochrome P450 isoenzymes CYP2D6, CYP3A4 / 5, CYP2C19, CYP2C9, CYP2A6, CYP2C8 and CYP2B6 are involved in the metabolism of vortioxetine.
The influence of other drugs on the action of vortioxetine. Irreversible non-selective MAO inhibitors
Due to the risk of serotonin syndrome, vortioxetine is contraindicated in any combination with irreversible non-selective MAO inhibitors. Treatment with vortioxetine should not be started earlier than at least 14 days after discontinuation of treatment with irreversible non-selective MAO inhibitors. Vortioxetine should be discontinued at least 14 days before starting treatment with irreversible non-selective MAO inhibitors.
Reverse selective MAO-A inhibitor (moclobemide). The combination of vortioxetine with a reversible selective MAO-A inhibitor such as moclobemide is contraindicated. Careful monitoring of serotonin syndrome with simultaneous use is necessary.
Reverse non-selective MAO inhibitor (linezolid). The combination of vortioxetine with a weak reversible and non-selective MAO inhibitor such as the antibiotic linezolid is contraindicated. Careful monitoring of serotonin syndrome with simultaneous use is necessary.
Non-circulating selective MAO-B inhibitors (selegiline, rasagiline). Despite the lower (than with MAO-A inhibitors) the expected risk of serotonin syndrome, the combination of vortioxetine with irreversible MAO-B inhibitors, such as selegiline or rasagiline, must be carried out with caution. Careful monitoring of serotonin syndrome with simultaneous use is necessary.
Serotonergic drugs.
Concomitant administration with serotonergic drugs (for example, with tramadol, sumatriptan and other triptans) can lead to serotonin syndrome.
St. John's wort.
The simultaneous use of serotonergic antidepressants and herbal remedies containing St. John's wort can lead to an increase in the frequency of adverse reactions, including serotonin syndrome.
Medicines that lower the seizure threshold.
Serotonergic antidepressants can lower the seizure threshold. Caution is advised when concomitant use of other drugs that can lower the seizure threshold (such as antidepressants (TCAs, SSRIs, SIZZN), antipsychotics (phenothiazines, thioxanthenes, butyrophenones), mefloquine, tramadine, bibadamide).
ECT (electroconvulsive therapy).
There is no clinical experience with the simultaneous use of vortioxetine with ECT, therefore, caution is advisable.
Inhibitors of cytochrome P450.
When administered together with 150 mg of bupropion (a strong inhibitor of CYP2D6) twice a day for 14 days in healthy volunteers, the effect of vortioxetine increased 2.3 times for the AUC. Co-administration was more likely to increase the incidence of side effects with the addition of bupropion to vortioxetine than with the addition of vortioxetine to bupropion. Depending on the individual sensitivity of the patient, when adding strong inhibitors of CYP2D6 (for example, bupropion, quinidine, fluoxetine, paroxetine) to therapy, low-dose vortioxetine may be considered.
With the joint appointment of vortioxetine after 6 days of use of ketoconazole 400 mg per day (inhibitor of CYP3A4 / 5 and P-glycoprotein) or fluconazole 200 mg per day (inhibitor of CYP2C9, CYP2C19 and CYP3A4 / 5) in healthy volunteers, respectively, 1.3 and 1 were observed, 5-fold increase in the AUC of vortioxetine. No dose adjustment is required.
The effect of a single dose of 40 mg of omeprazole (a CYP2C19 inhibitor) on the pharmacokinetics of long-term use of vortioxetine in healthy volunteers was not observed.
The combination of potent inhibitors of CYP3A4 and CYP2C9 in patients with low CYP2D6 metabolism has not been studied, however, an increased effect of vortioxetine in such patients is likely to be expected.
Cytochrome P450 inducers.
With a single administration of 20 mg of vortioxetine together after 10 days of taking rifampicin 600 mg per day (inducer of CYP isoenzymes), healthy volunteers showed a 72% decrease in the AUC of vortioxetine. Depending on the individual patient's response, a dose adjustment may be required if a cytochrome P450 inducer (eg rifampicin, carbamazepine, phenytoin) is added to vortioxetine treatment.
Acetylsalicylic acid.
The effect of repeated intake of acetylsalicylic acid 150 mg per day on the pharmacokinetics of vortioxetine in healthy volunteers was not observed.
The effect of vortioxetine on the action of other drugs. Anticoagulants and antiplatelet agents. No significant effects of influence on the indices of the international normalized ratio, prothrombin or plasma R- / S-warfarin compared with placebo were observed when vortioxetine was co-administered with a fixed dose of warfarin in healthy volunteers.


Experience is limited. Taking vortioxetine in the dose range from 40 to 75 mg exacerbated the following side effects:
Postural vertigo
Abdominal discomfort
Generalized itching
Drowsiness and blush
Treatment should be symptomatic and include appropriate monitoring. Medical supervision in a specialized setting is recommended.
  • Brand name: Brintellix®
  • Active ingredient: Vortioxetine
  • Manufacturer: Lundbeck AS
  • Country of Origin: Denmark

Studies and clinical trials of Vortioxetine (Click to expand)

  1. A randomized, double-blind trial of 2.5 mg and 5 mg vortioxetine (Lu AA21004) versus placebo for 8 weeks in adults with major depressive disorder
  2. A Randomized Trial on the Acute and Steady-State Effects of a New Antidepressant, Vortioxetine (Lu AA21004), on Actual Driving and Cognition
  3. Vortioxetine (Lu AA21004) in generalized anxiety disorder: Results of an 8-week, multinational, randomized, double-blind, placebo-controlled clinical trial
  4. Vortioxetine: First Global Approval
  5. Pharmacokinetic Drug Interactions Involving Vortioxetine (Lu AA21004), a Multimodal Antidepressant
  6. Vortioxetine, but not escitalopram or duloxetine, reverses memory impairment induced by central 5-HT depletion in rats: Evidence for direct 5-HT receptor modulation
  7. On assessing potential efficacy for vortioxetine in generalized anxiety disorder
  8. The efficacy and safety of 5 mg/d Vortioxetine compared to placebo for major depressive disorder: A meta-analysis
  9. Vortioxetine (Lu AA21004) 5mg in generalized anxiety disorder: Results of an 8-week randomized, double-blind, placebo-controlled clinical trial in the United States
  10. P.2.b.011 Vortioxetine (Lu AA21004) 15 and 20 mg/day: open-label long-term safety and tolerability in major depressive disorder
  11. Relative Efficacy and Acceptability of Vortioxetine Versus Marketed Antidepressants
  12. Antidepressant and anxiolytic potential of the multimodal antidepressant vortioxetine (Lu AA21004) assessed by behavioural and neurogenesis outcomes in mice
  13. Vortioxetine dose-dependently reverses 5-HT depletion-induced deficits in spatial working and object recognition memory: A potential role for 5-HT1A receptor agonism and 5-HT3 receptor antagonism
  14. The Safety and Tolerability Profile of Vortioxetine in the Treatment of Patients With Major Depressive Disorder Aged 65 Years and Older
  15. P.2.e.003 Role of 5-HT3 receptors in the mechanism of action of the investigational antidepressant vortioxetine
  16. P.1.g.014 Vortioxetine, a novel multimodal antidepressant, modulates GABA and glutamate neurotransmission via serotonergic mechanisms
  17. P.2.f.029 A randomised, double-blind, study of vortioxetine versus agomelatine in adults with major depressive disorder (MDD) with inadequate response to SSRI/SNRI treatment
  18. P.1.g.013 Effects of vortioxetine versus paroxetine on polysomnography in man: a pharmacokinetic/pharmacodynamic study
  19. P.2.e.004 Vortioxetine (Lu AA21004) disinhibits pyramidal cell output and enhances theta rhythms and long-term plasticity in the hippocampus
  20. P.2.e.001 Single dose vortioxetine or ketamine but not fluoxetine increases expression of neuroplasticity related genes in the rat prefrontal cortex
  21. P.2.f.013 Clinical evidence for improvement in cognitive dysfunction in patients with major depressive disorder (MDD) after treatment with vortioxetine

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