Doses and method of administration
Orally, 1 time per day, regardless of meals.
Depressive episodes
The recommended dose is 10 mg per day.
Depending on the patient’s individual response, the dose can be increased to a maximum of 20 mg per day.
The antidepressant effect develops 2-4 weeks after the start of treatment. After the symptoms of depression disappear, therapy must be continued for at least 6 months. to consolidate the resulting effect.
To discontinue therapy with escitalopram, it is necessary to gradually reduce the dose over 1-2 weeks in order to reduce the risk of developing withdrawal syndrome.
Panic disorders (including agoraphobia)
5 mg/day during the first week, then 10-20 mg/day.
The maximum daily dose is 20 mg.
The maximum therapeutic effect is achieved approximately 3 months after the start of treatment.
Elderly patients (over 65 years old)
The recommended dose is 5 mg per day, the maximum daily dose is 10 mg per day.
Renal dysfunction
For mild or moderate renal failure (creatinine clearance (CC) more than 30 ml/min), no dose adjustment is required;
In severe renal failure (creatinine clearance less than 30 ml/min), the drug should be prescribed with caution.
Liver dysfunction
For liver dysfunction, the initial dose is 5 mg per day for 2 weeks. Depending on the patient's individual response, the dose may be increased to 10 mg per day;
In severe liver dysfunction, slower dose titration is recommended.
Reduced activity of the CYP2C19 isoenzyme
The recommended initial dose for the first 2 weeks is 5 mg per day; depending on the individual patient's response, the dose can be increased to 10 mg per day.
Elycea
Use during pregnancy and breastfeeding
Elicea® is not used during pregnancy (safety has not been established).
Due to the fact that escitalopram is secreted into breast milk, the use of the drug during breastfeeding is not recommended. If it is necessary to use Elicea® during lactation, breastfeeding should be discontinued.
Use for liver dysfunction
For liver dysfunction, the initial dose is 5 mg/day for 2 weeks. Depending on the patient's individual response, the dose may be increased to 10 mg/day. In severe liver dysfunction, slower dose titration is recommended.
Use for renal impairment
For mild or moderate renal failure (creatinine clearance more than 30 ml/min), no dose adjustment is required. In severe renal failure (creatinine clearance less than 30 ml/min), the drug should be prescribed with caution.
Use in children
The use of the drug in children under 18 years of age is contraindicated.
Use in elderly patients
The drug should be used with caution in elderly patients.
special instructions
You should stop using the drug Elitseya if convulsive disorders, epileptic seizures develop, or their frequency increases in case of pharmacologically uncontrolled epilepsy.
If a manic state develops, Elicea® should be discontinued.
Escitalopram may increase blood glucose concentrations in diabetes mellitus, which may require dose adjustments of oral hypoglycemic agents and/or insulin.
Hyponatremia associated with a decrease in ADH secretion occurs rarely with the use of Elitsey® (more often in older people, patients with cirrhosis of the liver, or constantly taking drugs that can cause hyponatremia) and usually disappears when the drug is discontinued.
If serotonin syndrome develops, the drug should be immediately discontinued and symptomatic treatment prescribed.
Escitalopram should be used with caution in patients with a history of mania/hypomania. If a manic state develops, escitalopram should be discontinued.
Neuroleptic malignant syndrome (NMS) is a rare, potentially dangerous condition associated with the use of antidepressants, incl. escitalopram. Symptoms of NMS: increased body temperature (hyperpyrexia), muscle rigidity, changes in mental status and instability of the autonomic nervous system (arrhythmia, blood pressure fluctuations, tachycardia, profuse sweating, cardiac arrhythmia). If NMS is detected, you must immediately stop using Elitsey®.
During the first two weeks, akathisia/psychomotor agitation may develop (subjectively unpleasant or irritating restlessness and the need to move, often combined with the inability to sit or stand quietly).
When using the drug Elitsey®, the development of skin hemorrhages (ecchymosis and purpura) is possible. Escitalopram should be used with caution in patients with a tendency to bleeding, as well as those taking indirect anticoagulants and other drugs that affect blood clotting.
The simultaneous use of escitalopram and ethanol is not recommended.
Clinical experience with electroconvulsive therapy and escitalopram is limited and caution is advised.
There is limited experience with the use of escitalopram in patients with coronary artery disease, so Elitseya® is recommended to be used with caution in this group of patients.
When escitalopram therapy is quickly discontinued, withdrawal syndrome often occurs: dizziness, sensory disturbances (including paresthesia), sleep disturbances (insomnia, unusual dreams), psychomotor agitation, anxiety, nausea and/or vomiting, tremor, confusion, sweating, headache, diarrhea, palpitations, emotional lability and visual disturbances. The severity of these reactions is usually mild or moderate and the duration is limited. In this regard, it is recommended to discontinue Elicea® gradually, reducing the dose over several weeks or months.
In children, adolescents and young adults (under 24 years of age) with depression and other mental disorders, antidepressants, compared with placebo, increase the risk of suicidal thoughts and suicidal behavior. Therefore, when using escitalopram or any other antidepressants in children, adolescents and young adults (under 24 years of age), the risk of suicide should be weighed against the benefits of their use. In short-term studies, the risk of suicide did not increase in people over 24 years of age, but it decreased slightly in people over 65 years of age. Any depressive disorder itself increases the risk of suicide. Therefore, during treatment with antidepressants, all patients should be monitored for early detection of disturbances or changes in behavior, as well as suicidality.
Impact on the ability to drive vehicles and operate machinery
During the treatment period, it is necessary to refrain from driving vehicles and engaging in potentially hazardous activities that require increased concentration and speed of psychomotor reactions due to the possibility of dizziness, hallucinations, confusion, depersonalization and other side effects.
Carefully
Pharmacologically uncontrolled epilepsy, history of mania/hypomania, diabetes mellitus, depression with suicidal attempts, old age, liver cirrhosis, chronic renal failure (creatinine clearance (CC) less than 30 ml/min), coronary heart disease (CHD), bleeding tendency ; simultaneous use of drugs that can cause hyponatremia, lowering the threshold of convulsive readiness, with anticoagulants or drugs that affect platelet aggregation, with alcohol, with lithium, St. John's wort, with tryptophan, drugs metabolized with the participation of the CYP2C19 isoenzyme system; with simultaneous use of electroconvulsive therapy (ECT), age 18-24 years (due to the risk of developing suicidal behavior).
Elicea Ku-tab, 28 pcs., 10 mg, tablets dispersible in the oral cavity
Antidepressants should not be prescribed to children and adolescents under 18 years of age due to an increased risk of suicidal behavior (suicide attempts and suicidal thoughts), hostility (with a predominance of aggressive behavior, confrontational behavior and irritation). If a decision is made to initiate antidepressant therapy based on clinical assessment, the patient should be closely monitored.
Use of drugs belonging to the therapeutic group SSRIs, including escitalopram
Some patients with panic disorder may experience increased anxiety when starting antidepressant treatment. This paradoxical reaction usually disappears within the first 2 weeks of treatment. To reduce the likelihood of an anxiogenic effect, low initial doses are recommended.
Escitalopram should be discontinued in the event of the primary development of convulsive seizures or an increase in their frequency (in patients with previously diagnosed epilepsy). SSRIs should not be used in patients with unstable epilepsy; controlled seizures require careful monitoring.
Escitalopram should be used with caution in patients with a history of mania/hypomania. If a manic state develops, escitalopram should be discontinued.
In patients with diabetes mellitus, treatment with escitalopram may alter plasma glucose concentrations. Therefore, dose adjustments of insulin and/or oral hypoglycemic drugs may be required.
Depression is associated with an increased risk of suicidal ideation, self-harm, and suicide (suicidal events). This risk persists until significant remission occurs. Since improvement may not be observed during the first few weeks of therapy or even longer, patients should be closely monitored until their condition improves.
General clinical practice shows that in the early stages of recovery the risk of suicide may increase.
Other psychiatric conditions for which escitalopram is prescribed may also be associated with an increased risk of suicidal events and events. In addition, these conditions may be a comorbidity in relation to a depressive episode. When treating patients with other mental disorders, the same precautions should be taken as when treating patients with a depressive episode.
Patients with a history of suicidal behavior or patients with a significant level of suicidal thoughts before treatment are at greater risk for suicidal ideation or suicide attempts and should be closely monitored during treatment.
A meta-analysis of placebo-controlled clinical trials of antidepressants in adult patients with mental disorders showed that there is an increased risk of suicidal behavior when taking antidepressants in patients under 25 years of age compared with placebo. Drug treatment of these patients, and in particular those at high risk for suicide, should be accompanied by careful monitoring, especially early in treatment and during dose changes.
Patients (and caregivers) should be warned to monitor for any signs of clinical worsening, suicidal behavior or ideation, or unusual changes in behavior and to seek immediate medical advice if these symptoms occur.
The use of SSRIs/SNRIs is associated with the development of akathisia, characterized by the development of subjectively unpleasant or depressing restlessness and the need for constant movement, often combined with an inability to sit or stand quietly. This most often occurs during the first few weeks of treatment. In patients with such symptoms, increasing the dose may lead to worsening.
Hyponatremia, possibly associated with impaired ADH secretion, occurs rarely with SSRIs and usually disappears when therapy is discontinued. Caution should be exercised when using escitalopram and other SSRIs in persons at risk of developing hyponatremia (elderly patients, patients with liver cirrhosis and taking drugs that can cause hyponatremia).
Cases of skin hemorrhages (ecchymosis and purpura) have been reported when taking SSRIs. Escitalopram should be used with caution in patients taking oral anticoagulants and medications that affect blood clotting, as well as in patients with a tendency to bleed.
Because clinical experience with the concomitant use of SSRIs and ECT is limited, caution should be used when escitalopram and ECT are used concomitantly.
The simultaneous use of escitalopram and MAO A inhibitors is not recommended due to the risk of developing serotonin syndrome.
Escitalopram should be used with caution concomitantly with drugs that have serotonergic effects, such as sumatriptan or other triptans, tramadol and tryptophan. Patients taking escitalopram and other SSRIs concomitantly with serotonergic drugs have rarely developed serotonin syndrome. Its development may be indicated by a combination of symptoms such as agitation, tremor, myoclonus and hyperthermia. If this occurs, concomitant treatment with SSRIs and serotonergic drugs should be discontinued immediately and symptomatic treatment initiated.
When stopping treatment, withdrawal syndrome is common, especially if treatment is stopped abruptly. In clinical studies, adverse events at treatment discontinuation occurred in approximately 25% of patients treated with escitalopram and in 15% of patients treated with placebo.
The risk of withdrawal symptoms may depend on several factors, including the duration of therapy and drug dose, and the rate of dose reduction. The most commonly reported reactions were dizziness, sensory disturbances (including paresthesia and electric shock), sleep disturbance (including insomnia and intense dreams), agitation or anxiety, nausea and/or vomiting, tremor, confusion, increased sweating, headache, diarrhea, palpitations, emotional instability, irritability and blurred vision. These symptoms are usually mild to moderate, but may be severe in some patients. Symptoms usually occur within the first few days after stopping treatment, but such symptoms have been extremely rarely reported in patients who accidentally missed taking the drug.
Typically, these symptoms resolve on their own, usually within 2 weeks, although in some patients they may be prolonged (2–3 months or more). Therefore, when stopping treatment, it is recommended to gradually reduce the dose over several weeks or months, according to the patient's condition.
Due to limited experience with use in patients with coronary heart disease, caution is recommended when using the drug.
Escitalopram has been found to cause a dose-dependent prolongation of the QT interval. Cases of QT prolongation and ventricular arrhythmias, including torsade de pointes (TdP), have been reported post-marketing, predominantly in female patients with hypokalemia or pre-existing QT prolongation, or other cardiac disease.
Caution is required when using the drug in patients with severe bradycardia, recent acute myocardial infarction or decompensated heart failure.
Electrolyte imbalances, such as hypokalemia and hypomagnesemia, increase the risk of developing malignant arrhythmias; these disturbances must be corrected before starting treatment with escitalopram.
In patients with stable coronary artery disease, an ECG should be performed before starting treatment.
If signs of cardiac arrhythmia occur during treatment with escitalopram, it is necessary to stop therapy and perform an ECG.
SSRIs, including escitalopram, may affect pupil size, leading to mydriasis. This pupil dilation effect has the potential to narrow the anterior chamber angle, leading to increased IOP and the development of angle-closure glaucoma, especially in predisposed patients. Therefore, in patients with angle-closure glaucoma or a history of glaucoma, caution should be exercised when using escitalopram.
Special information on excipients
Elitseya® Ku-tab® contains lactose, so it should not be used for the following conditions: lactose intolerance, lactase deficiency, glucose-galactose malabsorption syndrome.
Impact on the ability to drive vehicles and other technical devices.
Despite the fact that the drug Elitseya® Qu-tab® does not affect intellectual functions and psychomotor activity, it is not recommended to drive vehicles or machinery during the treatment period.
Precautions and special instructions for use
You should stop using the drug Elitseya if convulsive disorders, epileptic seizures develop, or their frequency increases in case of pharmacologically uncontrolled epilepsy.
If a manic state develops, Elicea® should be discontinued.
Escitalopram may increase blood glucose concentrations in diabetes mellitus, which may require dose adjustments of oral hypoglycemic agents and/or insulin.
Hyponatremia associated with a decrease in the secretion of adrenocorticotropic hormone (ADH) occurs rarely with the use of Elitsey® (more often in older people, patients with cirrhosis of the liver, or constantly taking drugs that can cause hyponatremia) and usually disappears when the drug is discontinued.
If serotonin syndrome develops, the drug should be immediately discontinued and symptomatic treatment prescribed.
Escitalopram should be used with caution in patients with a history of mania/hypomania. If a manic state develops, escitalopram should be discontinued.
Neuroleptic malignant syndrome (NMS) is a rare, potentially dangerous condition associated with the use of antidepressants, including escitalopram. Symptoms of NMS: increased body temperature (hyperpyrexia), muscle rigidity, changes in mental status and instability of the autonomic nervous system (arrhythmia, blood pressure fluctuations, tachycardia, profuse sweating, cardiac arrhythmia). If NMS is detected, you must immediately stop using Elitsey®.
During the first two weeks, akathisia/psychomotor agitation may develop (subjectively unpleasant or irritating restlessness and the need to move, often combined with the inability to sit or stand quietly).
When using the drug Elitsey®, the development of skin hemorrhages (ecchymosis and purpura) is possible. Escitalopram should be used with caution in patients with a tendency to bleeding, as well as those taking indirect anticoagulants and other drugs that affect blood clotting.
The simultaneous use of escialalopram and ethanol is not recommended.
Clinical experience with electroconvulsive therapy (ECT) and escitalopram is limited and caution is advised.
There is limited experience with the use of escitalopram in patients with coronary artery disease, so Elitseya® is recommended to be used with caution in this group of patients.
When escitalopram therapy is quickly discontinued, withdrawal syndrome often occurs: dizziness, sensory disturbances (including paresthesia), sleep disturbances (insomnia, unusual dreams), psychomotor agitation, anxiety, nausea and/or vomiting, tremor, confusion, sweating, headache, diarrhea, palpitations, emotional lability and visual disturbances. The severity of these reactions is usually mild or moderate and the duration is limited. In this regard, it is recommended to discontinue Elicea® gradually, reducing the dose over several weeks or months.
In children, adolescents and young adults (under 24 years of age) with depression and other mental disorders, antidepressants, compared with placebo, increase the risk of suicidal thoughts and suicidal behavior. Therefore, when using escitalopram or any other antidepressants in children, adolescents and young adults (under 24 years of age), the risk of suicide should be weighed against the benefits of their use. In short-term studies, the risk of suicide did not increase in people over 24 years of age, but it decreased slightly in people over 65 years of age. Any depressive disorder itself increases the risk of suicide. Therefore, during treatment with antidepressants, all patients should be monitored for early detection of disturbances or changes in behavior, as well as suicidality.
Interactions with other drugs and other forms of interactions
Concomitant use with MAO-A inhibitors is contraindicated (risk of developing serotonin syndrome).
When used simultaneously with serotonergic drugs (tramadol, sumatriptan and other triptans), caution must be exercised (risk of developing serotonin syndrome). Doses of selegiline up to 10 mg per day have been used safely with racemic citalopram.
The simultaneous use of escitalopram and pimozide is contraindicated.
Concomitant use with drugs that lower the seizure threshold (tricyclic antidepressants, antipsychotics - derivatives of phenothiazine, thioxanthene, butyrophenone; mefloquine, bupropion and tramadol) increases the risk of developing seizures.
Escitalopram enhances the effect of lithium and tryptophan drugs.
Increases the toxicity of St. John's wort (Hypericum perforatum) preparations.
When escitalopram is used simultaneously with indirect anticoagulants and drugs that affect platelet aggregation (atypical antipsychotics and typical antipsychotics - phenothiazine derivatives, most tricyclic antidepressants, acetylsalicylic acid and non-steroidal anti-inflammatory drugs (NSAIDs), ticlopidine and dipyridamiol), it is necessary to monitor blood clotting parameters at the beginning therapy and upon its cessation (risk of bleeding).
The simultaneous use of escitalopram and ethanol is not recommended.
Pharmacokinetic interaction
Escitalopram should be used with caution simultaneously with inhibitors of the CYP2C19 isoenzyme (for example, omeprazole, esomeprazole, fluvoxamine, lansoprazole, ticlopidine) or cimetidine, because The concentration of escitalopram in the blood plasma increases, and therefore a reduction in the dose of escitalopram may be required.
Caution must be exercised when simultaneous use of escitalopram and drugs metabolized by the CYP2C19 isoenzyme and having a low therapeutic index, for example, flecainide, propafenone, metoprolol (for heart failure) or drugs mainly metabolized by the CYP2C19 isoenzyme and acting on the central nervous system (CNS), for example, antidepressants (desipramine, clomipramine, nortriptyline) or antipsychotics (risperidone, thioridazine, haloperidol). In these cases, the dose of these drugs may need to be adjusted.
Concomitant use with metoprolol or desipramine can lead to a twofold increase in the concentrations of the latter two drugs.
Elicea®
When using drugs belonging to the SSRI therapeutic group, including escitalopram, the following should be considered:
Use in children and adolescents under 18 years of age
Antidepressants should not be prescribed to children and adolescents under 18 years of age due to an increased risk of suicidal behavior (suicide attempts and suicidal thoughts), hostility (with a predominance of aggressive behavior, confrontational behavior and irritation). If a decision is made to initiate antidepressant therapy based on clinical assessment, the patient should be closely monitored. In addition, there is insufficient data on long-term safety in children and adolescents regarding growth, maturation, cognitive and behavioral development.
Paradoxical anxiety
Some patients with panic disorder may experience increased anxiety when starting antidepressant treatment. This paradoxical reaction usually disappears within the first two weeks of treatment. To reduce the likelihood of an anxiogenic effect, low initial doses are recommended.
Convulsions
Escitalopram should be discontinued in the event of the primary development of convulsive seizures or in the event of an increase in their frequency (in patients with previously diagnosed epilepsy). SSRIs should not be used in patients with unstable epilepsy; controlled seizures require careful monitoring.
Mania
Escitalopram should be used with caution in patients with a history of mania/hypomania. If a manic state develops, escitalopram should be discontinued. Diabetes
In patients with diabetes mellitus, treatment with escitalopram may alter plasma glucose concentrations. Therefore, dose adjustments of insulin and/or oral hypoglycemic drugs may be required.
Suicide/suicidal ideation or clinical deterioration
Depression is associated with an increased risk of suicidal ideation, self-harm, and suicide (suicidal events). This risk persists until significant remission occurs. Since improvement may not be observed during the first few weeks of therapy or even longer, patients should be closely monitored until their condition improves.
General clinical practice shows that in the early stages of recovery the risk of suicide may increase.
Other psychiatric conditions for which escitalopram is prescribed may also be associated with an increased risk of suicidal events and events. In addition, these conditions may be a comorbidity in relation to a depressive episode. When treating patients with other mental disorders, the same precautions should be taken as when treating patients with a depressive episode.
Patients with a history of suicidal behavior or patients with a significant level of suicidal thoughts before treatment are at greater risk for suicidal ideation or suicide attempts and should be closely monitored during treatment.
A meta-analysis of placebo-controlled clinical trials of antidepressants in adult patients with mental disorders found that there is an increased risk of suicidal behavior in patients under 25 years of age when taking antidepressants compared with placebo. Drug treatment of these patients, and in particular those at high risk for suicide, should be accompanied by careful monitoring, especially early in treatment and during dose changes.
Patients (and caregivers) should be warned to monitor for any signs of clinical worsening, suicidal behavior or ideation, or unusual changes in behavior, and to seek immediate medical advice if these symptoms occur. Akathisia/psychomotor agitation
The use of SSRIs/SNRIs is associated with the development of akathisia, characterized by the development of subjectively unpleasant or depressing restlessness and the need for constant movement, often combined with an inability to sit or stand quietly. This most often occurs during the first few weeks of treatment. In patients with such symptoms, increasing the dose may lead to worsening.
Hyponatremia
Hyponatremia, possibly associated with impaired ADH secretion, occurs rarely with SSRIs and usually disappears when therapy is discontinued. Caution should be exercised when using escitalopram and other SSRIs in persons at risk of developing hyponatremia: elderly patients, patients with cirrhosis of the liver, and those taking drugs that can cause hyponatremia.
Bleeding
Cases of skin hemorrhages (ecchymosis and purpura) have been reported when taking SSRIs. Escitalopram should be used with caution in patients taking oral anticoagulants and drugs that affect blood clotting, as well as in patients with a tendency to bleed.
Electroconvulsive therapy
Because clinical experience with the concomitant use of SSRIs and ECT is limited, caution should be used when escitalopram and ECT are used concomitantly.
The simultaneous use of escitalopram and MAO A inhibitors is not recommended due to the risk of developing serotonin syndrome.
Serotonin syndrome
Escitalopram should be used with caution concomitantly with drugs that have serotonergic effects, such as sumatriptan or other triptans, tramadol and tryptophan. Patients taking escitalopram and other SSRIs concomitantly with serotonergic drugs have rarely developed serotonin syndrome. Its development may be indicated by a combination of symptoms such as agitation, tremor, myoclonus and hyperthermia. If this occurs, concomitant treatment with SSRIs and serotonergic drugs should be discontinued immediately and symptomatic treatment initiated.
QT syndrome, predominantly in female patients with hypokalemia or pre-existing QT prolongation or other cardiac disease.
Caution is required when using the drug in patients with severe bradycardia or in patients with recent acute myocardial infarction or decompensated heart failure.
Electrolyte imbalances, such as hypokalemia and hypomagnesemia, increase the risk of developing malignant arrhythmias; these disturbances must be corrected before starting treatment with escitalopram.
In patients with stable coronary artery disease, an ECG should be performed before starting treatment.
If signs of cardiac arrhythmia occur during treatment with escitalopram, it is necessary to stop therapy and perform an ECG.
Angle-closure glaucoma
SSRIs, including escitalopram, may affect pupil size, leading to mydriasis. This pupil dilation effect has the potential to narrow the anterior chamber angle, leading to increased intraocular pressure and the development of angle-closure glaucoma, especially in patients with a predisposition to this disease. Therefore, in patients with angle-closure glaucoma or a history of glaucoma, caution should be exercised when using escitalopram.
Special information on excipients
Elitsey® contains lactose, so it should not be used for the following conditions: lactose intolerance, lactase deficiency, glucose-galactose malabsorption syndrome.
Overdose
Symptoms: dizziness, tremor, agitation, drowsiness, serotonin syndrome, convulsions, depression of consciousness of varying severity (especially in combination with alcohol and/or other drugs that depress central nervous system function), nausea, vomiting, decreased blood pressure, tachycardia, ECG changes (changes in the ST segment, T wave, widening of the QRS complex, increase in the QT interval), arrhythmias, respiratory depression, metabolic acidosis, rhabdomyolysis, hypokalemia, hyponatremia.
Treatment: symptomatic and supportive: gastric lavage, taking activated charcoal, ensuring airway patency, adequate oxygenation, monitoring the functions of the cardiovascular and respiratory systems. There is no specific antidote.
Pharmacotherapeutic group:
antidepressant
Pharmacological properties
Escitalopram is an antidepressant, a selective serotonin reuptake inhibitor (SSRI), increases the concentration of the neurotransmitter in the synaptic cleft by inhibiting the neuronal reuptake of serotonin, enhances and prolongs the effect of serotonin on postsynaptic receptors. Escitalopram has virtually no or very weak affinity for a number of receptors, incl. serotonin: 5-HT1A, 5-HT2, dopamine: D1 and D2; alpha1 and alpha2 and beta adrenergic receptors, H1-histamine, m-cholinergic receptors, benzodiazepine and opioid receptors, which causes the absence or mild severity of various anticholinergic, sedative, cardiovascular side effects. Escitalopram also does not bind or has very low affinity for various ion channels, including Na+, K+, Cl-, Ca2+ channels.
Pharmacodynamic properties
Suction
Absorption is independent of food intake. The time to reach maximum concentration (TCmax) is about 4 hours after repeated use. Bioavailability - 80%.
Distribution
The apparent volume of distribution (Vd,β/F) after oral administration is approximately 12-26 l/kg. The binding of escitalopram and its main metabolites to plasma proteins is below 80%. The kinetics of escitalopram is linear. The equilibrium concentration (Css) is reached after 1 week, the average Css is 50 nmol/l (from 20 to 125 nmol/l) is achieved with a daily dose of 10 mg.
Metabolism
Metabolized in the liver to pharmacologically active metabolites (demethylated and didemethylated). The main substance and metabolites are partially excreted in the form of glucuronides. After repeated use, the average concentrations of demethylated and didemethylated metabolites are 28-31% and less than 5%, respectively, of the concentration of escitalopram. The metabolism of escitalopram and the demethylated metabolite occurs with the dominant participation of the following cytochrome P450 isoenzymes: CYP2C19, CYP3A4 and CYP2D6.
Removal
The half-life (T1/2) after repeated use is about 30 hours.
Oral clearance is 0.6 l/min, of which 7% is renal. For the main metabolites, T1/2 is significantly higher. Escitalopram and its main metabolites are excreted by the liver and most of them by the kidneys, partially excreted in the form of glucuronides.
T1/2 and AUC increase in elderly patients.
Special patient groups
Old age (over 65 years old)
In elderly patients, escitalopram is eliminated more slowly than in younger patients. The amount of escitalopram in the systemic circulation (AUC - area under the concentration-time curve) in elderly patients is 50% greater than in young patients.
Liver dysfunction
In patients with liver failure of class A and B according to the Child-Pugh classification, T1/2 increases by 2 times.
Polymorphism (in individuals with low activity of the CYP2C19 or CYP2D6 isoenzyme):
in individuals with low activity of the CYP2C19 isoenzyme, the concentration of escitalopram may be 2 times higher than in individuals with high activity of this isoenzyme. There are no significant changes in the concentration of escitalopram with weak activity of the CYP2D6 isoenzyme.
Renal dysfunction
For racemic citalopram, a larger T1/2 was observed in patients with reduced renal function (creatinine clearance 10-53 ml/min).
List of excipients (excipients)
