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Brintellix - instructions for use, analogs, reviews and release forms (5 mg, 10 mg, 15 mg and 20 mg tablets) antidepressant medications for the treatment of depression and depressive episodes in adults, children and pregnancy. Composition and alcohol

Brintellix - instructions for use, analogs, reviews and release forms (5 mg, 10 mg, 15 mg and 20 mg tablets) antidepressant medications for the treatment of depression and depressive episodes in adults, children and pregnancy. Composition and alcohol

In this article, you can read the instructions for using the drug Brintellix. There are reviews of visitors to the site - consumers of this medication, as well as opinions of doctors specialists on the use of antidepressant Brintellix in their practice. A big request is to actively add their feedback on the drug: the medicine helped or did not help get rid of the disease, which were observed complications and side effects, possibly not declared by the manufacturer in the annotation. Analogues Brintellix in the presence of existing structural analogs.Use to treat depression and depressive episodes in adults, children, as well as during pregnancy and lactation. Composition and interaction of the drug with alcohol.

 

Brintellix antidepressant.

 

The mechanism of action is associated with its direct modulating serotonergic activity and inhibition of the serotonin transfer protein. Preclinical studies show that vortioxetine (the active ingredient of Brintellix) acts as an antagonist of 5-HT3-, 5-HT7- and 5-HT1D receptors, a partial agonist of 5-HT1B receptors and a complete 5-HT1A receptor agonist, and also inhibits the 5-HT transporter, thereby modulating neurotransmission in several systems, primarily serotonergic, but probably also noradrenergic, dopaminergic, neurotransmission mediated by histamine, acetylcholine, GABA and glutamate. Such multimodal pharmacological activity appears to underlie the antidepressant and anxiolytic properties of vortioxetine, and also determines the improvement in cognitive functions, learning and memory observed in animal studies.

 

However, since the individual contribution of each pharmacological target to the observed pharmacodynamic profile of vortioxetin remains unclear, extrapolation of the preclinical data to humans should be carried out with caution.

 

In two studies using positron emission tomography in humans to quantify the degree of occupancy of 5-HT carriers (using ligands 11C-MADAM or 11C-DASB), at different levels of dosing of vortioxetin, the following data were obtained: the average number of carriers of 5-HT, associated with vortioxetin, was approximately 50% at a dose of 5 mg per day, 65% at a dose of 10 mg per day, and increased to 80% with increasing doses to 20 mg per day.

 

Composition

 

Vortioxetin hydrobromide + excipients.

 

Pharmacokinetics

 

Vortoxyxine is slowly but well absorbed after oral administration. Eating does not affect the pharmacokinetics of the drug. The degree of binding to plasma proteins is high (98-99%) and, apparently, does not depend on the concentration of vortioxetin in the plasma. Vortioxetine is extensively metabolized in the liver mainly by oxidation with the help of the CYP2D6 isoenzyme and, to a lesser extent, isoenzymes CYP3A4 / 5 and CYP2C9 and subsequent conjugation with glucuronic acid.About 2/3 of the inactive metabolite of vortioxetin is excreted in the urine and about 1/3 - with feces. Only a small amount of vortioxetin is excreted with feces unchanged.

 

Indications

  • depression (major depressive episodes in adults).

 

Forms of release

 

Tablets coated with 5 mg, 10 mg, 15 mg and 20 mg.

 

Instructions for use and dosage

 

Inside, regardless of food intake.

 

Dosing regimen. The initial and recommended dose of Brintellix in adults younger than 65 years is 10 mg once a day. Depending on the individual reaction of the patient, the daily dose of vortioxetin can be increased to the maximum dose of 20 mg once a day or reduced to a minimum dose of 5 mg once a day. After completely resolving the symptoms of depression, it is recommended to continue treatment for at least 6 months to fix the antidepressant effect.

 

Termination of treatment. Patients receiving treatment with Brintellix can immediately stop taking it without the need for a gradual dose reduction and development of withdrawal syndrome.

 

Side effect

  • unusual dreams;
  • dizziness;
  • serotonin syndrome;
  • tides;
  • nausea, vomiting;
  • diarrhea, constipation;
  • itching, incl. generalized;
  • night sweats;
  • Large dosages can affect the potency and libido.

 

Contraindications

  • hypersensitivity to the active substance or to any component of the drug;
  • simultaneous use with nonselective monoamine oxidase (MAOI) inhibitors or selective MAOI A;
  • children and adolescents under 18 years of age (safety and efficacy not established).

 

Carefully:

  • severe renal and hepatic insufficiency;
  • mania and hypomania;
  • pharmacologically uncontrolled epilepsy, convulsive fits in the anamnesis;
  • pronounced suicidal behavior;
  • cirrhosis of the liver;
  • tendency to bleeding;
  • simultaneous administration with MAO B inhibitors (selegiline, rasagiline), serotonergic drugs, drugs that reduce the threshold of convulsive readiness, lithium, tryptophan, drugs containing St. John's wort, oral anticoagulants and drugs that affect platelet function, drugs that can cause hyponatremia , electroconvulsive therapy, advanced age.

 

Application in pregnancy and lactation

 

Data on the use of Brintellix in pregnant women are limited. Studies in animals have revealed reproductive toxicity of vortioxetine. In newborns whose mothers receive serotonergic drugs in late pregnancy, the following symptoms may occur: respiratory distress, cyanosis, apnea, convulsions, temperature instability, difficulty eating, vomiting, hypoglycemia, hypertension, hypotension, hyperreflexia, tremor, reflex excitability, irritability, lethargic sleep, constant crying, drowsiness and bad sleep. These symptoms can be associated with both withdrawal syndrome and excessive serotonergic activity. In most cases, such complications begin immediately or soon (less than 24 hours) after birth.

 

Data from epidemiological studies suggest that the use of SSRIs during pregnancy, especially in later life, may increase the risk of developing persistent pulmonary hypertension in newborns (PPHN). Although to date, the possibility of the relationship of this state with the use of vortioxetin is notwas studied, taking into account the mechanism of its action (increased concentration of serotonin), a possible risk can not be ruled out.

 

Brintellix should not be used during pregnancy unless the woman's clinical condition requires it.

 

Available pharmacodynamic and toxicological data in animals have shown that vortioxetin and its metabolites penetrate into breast milk. Probably, vortioxetin also penetrates into the human breast milk.

 

The risk to the child during breastfeeding can not be ruled out.

 

The decision to terminate breastfeeding or abstain from applying Brintellix should be made taking into account the assessment of the relative benefits of breastfeeding for the baby and the need for therapy for the mother.

 

Fertility. Fertility studies in male and female rats have shown that Brintellix does not affect fertility, sperm quality, or mating ability. The use of drugs in a person belonging to the corresponding pharmacological class of antidepressants (SSRIs) has shown an effect on the quality of sperm, which is reversible.Influence on fertility of the person for the present moment was not observed.

 

Use in children

 

Contraindicated in children and adolescents under the age of 18 years (safety and efficacy not established).

 

Application in elderly patients

 

In patients older than 65 years, the initial effective dose should always be the minimum effective dose of Brintellix 5 mg once daily. Care must be taken when treating patients older than 65 years with doses above 10 mg vortioxetin once daily, data on the use of the drug in this group of patients are limited.

 

special instructions

 

Use in children and adolescents under 18 years. Brintellix is ​​not recommended for treatment of depression in patients under the age of 18, since the safety and efficacy of Brintellix in this age group has not been established. In clinical trials in children and adolescents receiving other antidepressants, suicidal behavior (suicide attempts and suicidal thoughts) and hostility (with a predominance of aggressive behavior, a tendency to confrontation and irritation) were more frequent compared with those who received a placebo.

 

Suicide / suicidal thoughts or clinical impairment. Depression is associated with an increased risk of suicidal thoughts, self-injury and suicide (suicidal behavior). This risk persists until a marked remission occurs. Because the improvement may not be observed during the first few weeks of therapy or even a longer period of time, patients should be monitored continuously until their condition improves.

 

General clinical practice shows that in the early stages of recovery may increase the risk of suicide. Patients with a history of suicidal behavior or patients with a significant level of meditation on suicidal topics prior to the commencement of treatment are more likely to be at risk of suicidal thoughts or suicide attempts, so they should be closely monitored during treatment. A meta-analysis of placebo-controlled clinical trials of antidepressants with adult patients with mental disorders showed that when using antidepressants in patients younger than 25, there is an increased risk of suicidal behavior compared with placebo.

 

Patients should be closely monitored, especially for those who show a high suicide risk, especially at the beginning of treatment or when changing the dose of the drug. Patients (and their caregivers) should be warned about the need to monitor the signs of any clinical impairment, suicidal behavior and suicidal thoughts, and unusual behavioral changes and seek medical help immediately if any of these symptoms occur.

 

Convulsive seizures. There is a possible risk of developing seizures with the use of antidepressants. Therefore, Brintellix should be used with caution in patients with seizures in history or in patients with unstable epilepsy. If seizures occur or their frequency increases, treatment with vortioxetin should be discontinued.

 

Serotonin syndrome (SS) or malignant neuroleptic syndrome (CNS). MOP or ZNS are potentially life-threatening conditions and can occur when using the Brintellix preparation. The risk of CC or ZNS increases when combined with serotonergic drugs(including triptans), drugs that affect serotonin metabolism (including MAOI), antipsychotics, or other dopamine antagonists. Patients should be monitored for the appearance of objective and subjective symptoms of SS and ZNS.

 

CS symptoms include mental status changes (e.g., agitation, hallucinations, coma), autonomic instability (e.g., tachycardia, labile blood pressure, hyperthermia), neuromuscular abnormalities (e.g., hyperreflexia, coordination disorder) and / or gastrointestinal symptoms (for example, nausea, vomiting, diarrhea). In the event of such symptoms, Brintellics should immediately stop therapy and begin symptomatic treatment.

 

Mania / Hypomania. Brintellix should be used with caution in patients with episodes of mania / hypomania in an anamnesis. The drug should be discontinued when developing a manic condition.

 

Closed-angle glaucoma. Dilation of pupils, which occurs after taking many antidepressants, including. Brintelliksa and can provoke an attack of angle-closure glaucoma in patients with anatomically narrow angles of the anterior chamber, which was not carried out peripheral iridectomy.

 

Bleeding. Against the background of serotonergic antidepressants (SSRIs, SNRIs) have been observed rare cases of bleeding disorders, such as ecchymosis, purpura, gastrointestinal and gynecological bleeding. The drug is recommended to be used with caution in patients taking anticoagulants and / or agents affecting platelet function (e.g., atypical antipsychotics, phenothiazines, most tricyclic antidepressants, nonsteroidal anti-inflammatory drugs (NSAIDs) and acetylsalicylic acid), as well as in patients with a known tendency to bleeding / coagulation disorders.

 

Hyponatremia. Against the background of the use of antidepressants with serotonergic effect (SSRIs, SNRIs) reported rare cases of hyponatremia, probably due to the syndrome of inappropriate secretion of antidiuretic hormone. Caution should be exercised when applying vortioksetina in patients of high risk groups such as elderly patients, patients with hepatic cirrhosis or patients concurrently treated with drugs that may induce hyponatremia.It should be possible to cancel Brintellix in patients with symptomatic hyponatraemia and conduct appropriate medical interventions aimed at correcting their condition.

 

Elderly patients. Data on the use of Brintellix in elderly patients with a large depressive episode are limited. Therefore, care should be taken when treating patients older than 65 years using doses of vortioxetine above 10 mg once daily.

 

Impaired renal function. There are only limited data on the use of the drug in patients with severe renal failure. Therefore, care should be taken when treating these patients.

 

Dysfunction of the liver. Vortoxyxetin has not been studied in patients with severe hepatic insufficiency, so in such patients the drug should be used with caution.

 

Influence on ability to drive vehicles and work with mechanisms

 

Brintellix does not have or has very little effect on the ability to drive a car or machinery. However, patients should be careful when driving vehicles or when working with dangerous machinery,especially at the beginning of treatment with vortioxetine or with a change in its dose.

 

Drug Interactions

 

Possible effects of other drugs on the pharmacological action of Brintellix

 

Irreversible non-selective MAOIs. Because of the risk of serotonergic syndrome, vortioxetin is contraindicated in combination with irreversible non-selective MAOIs. Vortoxyxetin can be prescribed no earlier than 14 days after the cancellation of irreversible non-selective MAOIs.

 

Vortoxyxetin must be discontinued no less than 14 days before the application of irreversible non-selective MAOIs.

 

Reversible selective MAOA A (moclobemide). The simultaneous use of vortioxetine with reversible selective MAOA A, such as moclobemide, is contraindicated. In the case of the proven need for simultaneous use, the drug to be added should be used in minimal doses and with careful clinical observation for the onset of serotonin syndrome.

 

Reversible nonselective MAOI (linezolid). Simultaneous use of vortioxetine with a weak reversible non-selective MAOI, such as the antibiotic linezolid, is contraindicated.In case of the proven need for simultaneous use, the drug to be added should be used in minimal doses with careful clinical monitoring for the appearance of serotonin syndrome.

 

Irreversible selective MAOI B (selegiline, rasagiline). Although the risk of serotonin syndrome with the simultaneous use of vortoxyxine and selective MAOI B is lower than with the simultaneous use of vortioxetin and selective MAOA A, the combined use of vortioxetin with irreversible MAOI B, such as selegiline or rasagiline, should be carried out with caution. In the case of simultaneous use, careful monitoring of the patient for the appearance of serotonin syndrome is necessary.

 

Serotonergic drugs. The simultaneous use of vortioxetine and other drugs with a serotonergic effect (for example, tramadol, Sumatriptan and other tryptans) can lead to the development of serotonin syndrome.

 

Saint John's wort. Simultaneous use of antidepressants with a serotonergic effect with preparations containing St. John's wort (Hypericum perforatum)may lead to an increase in the incidence of adverse reactions, including serotonin syndrome.

 

Drugs that reduce the threshold of convulsive readiness. Antidepressants with a serotonergic effect can reduce the threshold of convulsive readiness. Simultaneous use with drugs that reduce the threshold of convulsive readiness (for example, antidepressants (TCAs, SSRIs, SSRIs), antipsychotics (phenothiazines, thioxanthenes, butyrophenones), mefloquine, bupropion, tramadol) should be carried out with caution.

 

Electroconvulsive therapy (ECT). Currently, the clinical experience of simultaneous use of vortioxetin and ECT is absent, therefore, with this application, care must be taken.

 

Inhibitors of the isoenzyme CYP2D6. In the case of vortoxyxine 10 mg / day, simultaneously with bupropion (a strong inhibitor of the isoenzyme CYP2D6) at a dose of 150 mg twice daily for 14 days in healthy subjects, the exposure of vortioxetin (AUC) increased 2.3-fold. Undesirable reactions were more often observed with the addition of bupropion to current therapy with vortioxetine than with the addition of vortioxetine to current therapy with bupropion.Depending on the individual reaction of the patient, when a strong inhibitor of the CYP2D6 isoenzyme (eg, bupropion, quinidine, fluoxetine, paroxetine) is added to the current therapy with vortioxetine, the possibility of reducing the dose of vortioxetin should be considered.

 

Inhibitors of isoenzymes CYP3A4 and CYP2C9. The addition of vortioxetine 6 days after initiation of Ketoconazole 400 mg / day (inhibitor of CYP3A4 / 5 and P-gp isoenzymes) or 6 days after the onset of Fluconazole 200 mg / day (inhibitor of isoenzymes CYP2C9, CYP2C19 and CYP3A4 / 5 ) in healthy subjects, the exposure (AUC) of vortioxetin increased by 1.3 and 1.5 times, respectively. Correction of the dose is not required.

 

Interactions in patients with a weak activity of the isoenzyme CYP2D6. Special studies of the use of vortioxetin concurrently with strong inhibitors of the isoenzyme CYP3A4 (such as itraconazole, voriconazole, clarithromycin, telithromycin, nefazodone, conivaptan and many HIV protease inhibitors) and inhibitors of the CYP2C9 isoenzyme (such as fluconazole and amiodarone) in patients with decreased activity of the CYP2D6 isoenzyme , it can nevertheless be expected that in these patients such an application will result in a more pronounced vortioxetin exposure compared to the moderate effect described above.The administration of a single dose of Omeprazole 40 mg (inhibitor of the isoenzyme CYP2C19) against the background of repeated doses of vortioxetin did not change the pharmacokinetics of the latter in healthy subjects.

 

Inductors of cytochrome P450. When a single dose of vortioxetin 20 mg was administered 10 days after the initiation of rifampicin at a dose of 600 mg / day (induction of CYP isoenzymes of a wide spectrum) in healthy subjects, the exposure (AUC) of vortioxetin decreased by 72%. Depending on the individual reaction of the patient, if a strong inductor of cytochrome P450 isoenzymes of a wide spectrum (eg, rifampicin, carbamazepine, phenytoin) is added to the current therapy with vortioxetine, the possibility of correcting the dose of vortioxetin should be considered.

 

Alcohol. At simultaneous administration of single doses of Brintellix (20 and 40 mg) and ethanol (alcohol) (0.6 g / kg), healthy subjects did not observe changes in the pharmacokinetics of vortioxetine or ethanol and significant impairment of cognitive functions compared with placebo. However, during therapy with antidepressants, alcohol intake is not recommended.

 

Acetylsalicylic acid. Multiple administration of Acetylsalicylic acid at a dose of 150 mg per day did not alter the pharmacokinetics of multiple dosesvortioxetine in healthy subjects.

 

Possible influence of Brintellix on the pharmacological action of other drugs

 

Anticoagulants and antiaggregants. There was no significant effect of vortioxetine versus placebo on prothrombin parameters, MHO, or R- / S-warfarin ratio in blood plasma, while using multiple doses of vortoxyxine with a fixed dose of Warfarin in healthy subjects. There was also no significant inhibitory effect of vortioxetin on platelet aggregation and the pharmacokinetics of acetylsalicylic and salicylic acid in comparison with placebo with simultaneous use of acetylsalicylic acid at a dose of 150 mg per day after repeated doses of vortioxetine in healthy subjects. Nevertheless, as with the use of other serotonergic drugs, caution should be exercised while using vortioxetine and oral anticoagulants or antiplatelet agents due to the potential risk of bleeding caused by pharmacodynamic interaction.

 

Substrates of cytochrome P450. Studies have not revealed in vortioxetine the ability to inhibit or induce isoenzymes of the cytochrome P450 system.After using multiple doses of vortioxetine in healthy subjects, its inhibitory effect on the activity of cytochrome P450 isoenzymes CYP2C19 (omeprazole, diazepam), CYP3A4 / 5 (ethinylestradiol, midazolam), CYP2B6 (bupropion), CYP2C9 (tolbutamide, S-warfarin) CYP1A2 (caffeine) or CYP2D6 (dextromethorphan). Pharmacodynamic interactions were also not observed. There was no significant cognitive impairment compared with placebo when vortioxetin was used in combination with a single dose of Diazepam 10 mg. There was no significant effect of vortioxetine compared with placebo on the level of sex hormones after its use in combination with a combined oral contraceptive (ethinylestradiol 30 μg + levonorgestrel 150 μg).

 

Lithium, tryptophan. In healthy subjects, no clinically significant changes were observed with simultaneous use of lithium and multiple doses of vortioxetine. However, since the cases of increasing the effect of serotonergic antidepressants with simultaneous use with lithium or tryptophan have been described, the use of vortioxetin in combination with these drugs should be carried out with caution.

 

Analogues of the drug Brintellix

 

Brintellix does not have structural analogs for the active substance.

 

Analogues for the pharmacological group (antidepressants):

  • Ademethionine;
  • Adress;
  • Azafen;
  • Alventa;
  • Aleval;
  • Amizole;
  • Amide;
  • Amitriptyline;
  • Anaphranil;
  • Asentra;
  • Valdoxane;
  • Velaxin;
  • Venlafaxine;
  • Heptor;
  • Heptral;
  • Daplex;
  • Depres;
  • Depenone;
  • Deprim;
  • Deprim forte;
  • Doxepine;
  • Duloxetine;
  • Zoloft;
  • Ixelles;
  • Kaliksta;
  • Clominal;
  • Clomipramine;
  • Coaxyl;
  • Lenuksin;
  • Maprotibene;
  • Maprotiline;
  • Melipramine;
  • Mirzaten;
  • Mirtazapine (hemihydrate);
  • Mirtalan;
  • Neuroplant;
  • Noxibel;
  • Newvelong;
  • Oprah;
  • Paxil;
  • Paroxetine;
  • Pipofezin;
  • Prozac;
  • Profluzak;
  • Rexetin;
  • Saroten retard;
  • Selektra;
  • Sirleft;
  • Sertraline;
  • Sinekwan;
  • Stimuloton;
  • Trittico;
  • Févarine;
  • Fluval;
  • Fluxonil;
  • Fluoxetine;
  • Framex;
  • Cipralex;
  • Citalopram;
  • Elivel;
  • Elicia;
  • Escitalopram;
  • Ephevelone.

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