One of the most “popular” antidepressants among doctors. According to our data, this medicine is one of the ten most frequently prescribed drugs by psychiatrists.
Escitalopram
is produced under many names: cipralex (considered the original, since it was the very first), elicea, esipi, escitalopram, selectra, lenuxin, miracitol, etc.
All of these are analogues, that is, drugs with the same active ingredient, but produced at different factories by different manufacturers.
The drug was obtained as a result of a “modification” of another antidepressant from the group of selective serotonin reuptake inhibitors (SSRIs) - citalopram.
The mechanism of action is associated with a decrease in the flow of the neurotransmitter serotonin back into the neuron after it has entered the intercellular space - the synapse.
The drug promotes the accumulation of serotonin in the synapse (the junction of neurons), and if the painful condition caused the depletion of serotonin, then long-term use of escitalopram leads to the restoration of serotonin metabolism and a decrease in the symptoms of the disease. The main effect is antidepressant and anti-anxiety.
Available in the form of film-coated tablets in a dosage of the active substance of 10 milligrams.
Indications
◊ Recommendations of the Russian Ministry of Health
F32 Depressive episode
F33 Recurrent depressive disorder
F40.0 Agoraphobia
F41.0 Panic disorder (episodic paroxysmal anxiety)
◊ FDA recommendations
- Major depressive disorder (adults and children over 12 years of age)
- GTR
◊ Recommendations from UK Medicines and Healthcare Products Regulatory Agency
- Major depressive episode
- Panic disorder with/without agoraphobia
- Social phobia
- GTR
- OCD
◊ Using Off-label
- Vasomotor symptoms during menopause
- Insomnia
- Dysmorphophobia
- Bulimia [5].
Mechanism of action and pharmacokinetics
Escitalopram is the S-isomer of citalopram. Selectively inhibits the reuptake of serotonin, increasing the concentration of this neurotransmitter in the synaptic cleft. Escitalopram, like other antidepressants from the SSRI group, practically does not bind to dopamine (D1 and D2) receptors, α-adrenergic and m-cholinergic receptors, as well as benzodiazepine and opioid receptors [4]. Long-term use of escitalopram leads to desensitization of somatodendritic 5-HT1A and terminal autoreceptors.
- Bioavailability – 80%.
- Half-life 27-32 hours
- Stable concentration in the blood is maintained for one week
- Metabolized by CYP3A4, CYP2C19; inhibits CYP2D6
Treatment regimen
◊ Dosage and dose selection
- Optimal dose for treating depression, OCD and GAD: 10-20 mg/day
- Start with 10 mg/day, increase to 20 mg if necessary
- Take once daily, morning or evening
- 10 mg escitalopram is comparable to 40 mg citalopram, but without side effects
- A dose of 30-40 mg is suitable for some patients [1]
- To relieve vasomotor symptoms during menopause, 10 mg/day is sufficient, but if ineffective within 4 weeks, the dose may be increased to 20 mg/day
- If anxiety, insomnia, agitation, or akathisia occur at the beginning of treatment or after interruption of treatment, the possibility of bipolar disorder should be considered and switched to a mood stabilizer or an atypical antipsychotic
◊ How quickly it works
- Begins to act after 2-4 weeks
- If there is no effect after 6-8 weeks, you need to increase the dose or switch to another drug
- To prevent relapse, it can be taken for many years.
◊ Expected result
- Complete remission.
- After the symptoms of depression disappear, you should continue taking it for 1 year if this was the treatment of the first episode. If this is to treat a recurrent episode, treatment can be extended indefinitely.
- Use in the treatment of anxiety and chronic pain may be indefinite.
◊ If it doesn't work
- Change the dose, switch to another medicine or add an auxiliary drug;
- Connect psychotherapy;
- Review the diagnosis by identifying comorbid conditions;
- In patients with undiagnosed bipolar affective disorder, the effectiveness of treatment may be low, in which case it is necessary to switch to a mood stabilizer [1].
- In the acute phase of severe depressive disorder, which is accompanied by psychotic or catatonic symptoms, as well as in patients with current suicidal ideation, electroconvulsive therapy should be considered [7].
◊ How to stop taking it
It is usually not necessary to reduce gradually, but to be sure to avoid withdrawal symptoms, you can reduce it gradually. Gradual reduction scheme: dose reduced by 50% - 3 days, again reduced by 50% - 3 days, complete cessation. If withdrawal symptoms appear, increase the dose, wait for withdrawal symptoms to subside, and continue decreasing [1].
◊ Treatment combinations
- For insomnia: trazadone
- For fatigue, drowsiness, loss of concentration: modafinil [3].
- Combinations with other antidepressants may activate bipolar disorder and suicidal ideation
- For bipolar depression, psychotic depression, treatment-resistant depression, treatment-resistant anxiety disorder: mood stabilizers, atypical antipsychotics
- For anxiety disorder: gabapentin, tiagabine
Escitalopram price, where to buy
The price of Escitalopram in pharmacies for 28 pieces is from 300 rubles.
- Online pharmacies in RussiaRussia
- Online pharmacies in UkraineUkraine
ZdravCity
- Escitalopram tablets p.p.o.
10 mg 28 pcs. Berezovsky Pharm. plant ZAO RUR 292 order - Escitalopram tab. p.p.o. 0.01g 30pcsPranafarm LLC
RUB 208 order
- Escitalopram-SZ tablets p.p.o 0.01g 30pcsNAO Northern Star
RUB 252 order
- Escitalopram-Alsi tab. p/o captivity. 10mg 30pcsALSI Pharma ZAO
RUB 284 order
- Escitalopram Canon tab. p/o captivity. 20 mg No. 28 ZAO Kanonpharma Production
605 rub. order
Pharmacy Dialogue
- Escitalopram tablets 10 mg No. 30 Alsi Pharm
RUB 249 order
- Escitalopram-SZ (tab.p.pl.vol.10mg No. 30)Northern Star Nenets Autonomous Okrug
230 rub. order
- Escitalopram (tab. ppl/vol. 10 mg No. 28) Berezovsky plant
RUB 266 order
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Pharmacy24
- Escitalopram Teva 20 mg N28 tablets TOV Teva Operations Poland, Poland
275 UAH order - Escitalopram Teva 10 mg No. 28 tablets TOV Teva Operations Poland, Poland
170 UAH order
Special patient groups
◊ Patients with kidney problems
Use caution if the patient has severe kidney disease [1].
◊ Patients with liver disease
The recommended dose is 10 mg/day [1].
◊ Patients with heart disease
There are no systematic data on the use of escitalopram in people with pathology of the cardiovascular system. Supposedly safe. Useful in recovery after a heart attack [1].
◊ Elderly patients
For elderly patients, a dose of 10 mg is recommended [1].
◊ Children and teenagers
- Recommended for the treatment of depression aged 12-17 years
- It is necessary to regularly and personally check the patient's condition, especially in the first weeks of treatment.
- Use with caution due to the risk of undiagnosed bipolar disorder and suicidality.
- Inform adults about the risks.
◊ Pregnant women
- There have been no adequate studies in pregnant women [1].
- Not recommended for pregnant women, especially in the first trimester
- All risks should be weighed and compared
- Bleeding can be expected during childbirth
◊ Breastfeeding
- The medicine passes into breast milk.
- If the infant shows signs of irritation or sedation, discontinue feeding or escitalopram
- However, treatment after childbirth may be necessary, so the risks should be weighed.
Escitam instructions for use
Composition and release form: Escitam 10 tablets. p/captivity coated 10 mg blister, No. 30, No. 60 Escitalopram 10 mg B Escitam 20 tablets. p/captivity coated 20 mg blister, No. 30, No. 60 Escitalopram 20 mg B
Pharmacodynamics: Escitam is an antidepressant, a selective serotonin reuptake inhibitor (SSRI), which determines the clinical and pharmacological effects of the drug. It has a high affinity for the main binding element and the adjacent allosteric element of the serotonin transporter and has no or very weak ability to bind to a number of receptors, including serotonin 5-HT1A, 5-HT2 receptors, dopamine D1 and D2 receptors, α1-, α2-, β-adrenergic receptors, histamine H1-, M-cholinergic receptors, benzodiazepine and opiate receptors.
Pharmacokinetics: Absorption is almost complete and does not depend on food intake. Cmax in blood plasma is achieved 4 hours after administration. The bioavailability of escitalopram is about 80%. The binding of escitalopram and its main metabolites to blood proteins is not lower than 80%. Metabolism occurs in the liver to the formation of metabolites, which are demethylated and didemethylated. Both are pharmacologically active. Biotransformation of escitalopram to a demethylated metabolite occurs with the help of cytochrome CYP 2C19. There may be a slight participation in the process of isoenzymes CYP 3A4 and CYP 2D6. T½ of the drug is ≈30 hours. Oral clearance is ≈0.6 l/min. The main metabolites have a longer half-life. Escitalopram and its main metabolites are excreted by the liver (metabolic pathway) and kidneys. Most of the dose is excreted as metabolites in the urine. The kinetics of escitalopram is linear. Equilibrium concentration is achieved after ≈1 week. In elderly patients (over 65 years of age), escitalopram is eliminated more slowly than in younger patients.
Indications: Treatment of major depressive episodes, panic disorders with or without agoraphobia, social anxiety disorders (social phobia), generalized anxiety disorders, obsessive-compulsive disorders (OCD).
Application: Escitalopram is used in adults orally 1 time per day, regardless of meals. Major depressive episode. Usually prescribed 10 mg 1 time per day. Depending on the patient's individual response, the daily dose may be increased to 20 mg. The antidepressant effect usually develops within 2–4 weeks. After the symptoms disappear, treatment must be continued for 6 months in order to consolidate the effect. Panic disorders with or without agoraphobia. During the first week, an initial dose of 5 mg/day is recommended, after which the dose can be increased to 10 mg/day. The dose may be further increased to 20 mg/day depending on the individual patient response. The maximum effect in the treatment of panic disorders is achieved after 3 months. The duration of treatment is several months and depends on the severity of the disease. Social anxiety disorders (social phobia). Usually prescribed 10 mg 1 time per day. Depending on the individual sensitivity of the patient, it is recommended to increase the dose to 20 mg/day. A decrease in the severity of symptoms usually occurs after 2–4 weeks of treatment. It is recommended to continue treatment for 3 months. Long-term treatment for 6 months is prescribed to prevent relapse, taking into account the individual manifestations of the disease; The effectiveness of therapy is regularly assessed. Generalized anxiety disorders. Usually prescribed 10 mg 1 time per day. Depending on individual sensitivity, the dose may be increased to a maximum of 20 mg/day. It is recommended to continue treatment for 3 months. Long-term treatment for 6 months is prescribed to prevent relapse, taking into account the individual manifestations of the disease; regularly assessing the effectiveness of treatment. OCD. Usually prescribed 10 mg 1 time per day. Depending on individual sensitivity, the dose may be increased to 20 mg/day. OCD is a chronic disease and treatment must last for a sufficient period to ensure complete resolution of symptoms, which may be several months or even longer. Elderly patients (over 65 years old). The initial dose should be half the usual recommended dose. The recommended daily dose for elderly people is 5 mg. Depending on individual sensitivity and severity of depression, the daily dose can be increased to a maximum of 10 mg/day. Kidney failure. For mild to moderate renal failure there are no restrictions. The drug should be used with caution in patients with severe renal failure (creatinine clearance <30 ml/min). Decreased liver function. The recommended starting dose for the first 2 weeks of treatment is 5 mg/day. Depending on the patient's individual response, the dose may be increased to 10 mg/day. Reduced activity of the cytochrome isoenzyme CYP 2C19. For patients with reduced activity of the CYP 2C19 isoenzyme, the recommended initial dose during the first 2 weeks of treatment is 5 mg/day. Depending on the patient's individual response, the dose may be increased to 10 mg/day. Stopping treatment. When stopping treatment with Escitam, the dose should be reduced gradually over 1–2 weeks to avoid a reaction to drug withdrawal. Contraindications: Hypersensitivity to escitalopram or other components of the drug, simultaneous use with MAO inhibitors or pimozide.
Side effects: Side effects of Escitam are usually transient and minor. They are observed during the 1st–2nd week of treatment and gradually disappear as the patient recovers. Side effects common to all drugs of the SSRI class and escitalopram, which were noted in placebo-controlled studies and in medical use, are listed by organ system and frequency: very often (≥1/10), often (≥1/100, <1/ 10), uncommon (≥1/1000, ≤1/100), rare (≥1/10,000, ≤1/1000), frequency unknown (cannot be determined). Very common: nausea. Often: from the digestive system - decreased or increased appetite, diarrhea, constipation, vomiting, dry mouth; from the central nervous system - anxiety, restlessness, abnormal dreams, decreased libido, anorgasmia in women, insomnia, drowsiness, dizziness, paresthesia, tremor; from the respiratory system - sinusitis, yawning; on the part of the skin and subcutaneous tissue - increased sweating; from the musculoskeletal system - arthralgia, myalgia; from the reproductive system - impaired ejaculation in men, impotence; general disorders - fatigue, pyrexia; established in studies - an increase in body weight. Uncommon: from the cardiovascular system - tachycardia; from the central nervous system - bruxism, agitation, irritability, panic attacks, confusion, taste disturbances, sleep disturbances, fainting; from the respiratory system - nosebleeds; from the digestive system - gastrointestinal bleeding (including rectal); from the skin and subcutaneous tissue - rash, baldness, itching; from the reproductive system - metrorrhagia, menorrhagia; from the organ of vision - pupil dilation, blurred vision; from the organ of hearing - ringing in the ears; general disorders - swelling; established in studies - reduction in body weight. Rarely: from the cardiovascular system - bradycardia; from the central nervous system - aggression, depersonalization, hallucinations, suicide attempts, serotonin syndrome; on the part of the immune system - anaphylactic reactions. Frequency unknown: from the cardiovascular system - orthostatic hypotension; from the central nervous system - mania, dyskinesia, movement disorders, convulsions; from the digestive system - hepatitis; from the kidneys and urinary system - urinary retention; from the blood and lymphatic system - thrombocytopenia; from the endocrine system - impaired secretion of antidiuretic hormone; from the reproductive system - priapism, galactorrhea in men; on the metabolic side - hyponatremia; from the skin and subcutaneous tissue - bruising, swelling; established in studies - abnormal liver function indicators. There are reports of side effects with SSRI drugs such as anorexia and akathisia. Cases of QT interval prolongation have been observed primarily in patients with cardiac disease, but no causal relationship has been established. Withdrawal symptoms usually occur within the first few days after sudden cessation of treatment and resolve in most cases within 2 weeks. In clinical studies, withdrawal symptoms were observed in ≈25% of patients treated with escitalopram and in 15% of patients treated with placebo. Dizziness, headache, sensory disturbances, sleep disturbances, anxiety, nausea and/or vomiting, tremor, confusion, increased sweating, diarrhea, tachycardia, emotional lability, irritability and visual disturbances occurred most frequently. Most of these symptoms are mild and transient, but may be severe and/or prolonged in some patients. In order to avoid withdrawal symptoms, it is recommended to gradually discontinue use of the drug over 1–2 weeks.
Special instructions: Paradoxical anxiety. Some patients with panic disorder may experience an increase in anxiety when starting treatment with an SSRI. This paradoxical reaction usually disappears within 2 weeks of treatment. To reduce the likelihood of anxiogenic effects, low initial doses are recommended. Convulsive attacks. It is necessary to discontinue the drug if convulsive attacks develop. Mania. SSRIs should be used with caution in the treatment of patients with a history of mania/hypomania. If a manic state occurs, the SSRI should be discontinued. Diabetes. In patients with diabetes mellitus, treatment with SSRIs may alter glycemic control (hypoglycemia or hyperglycemia). Dosing of insulin and/or oral hypoglycemic drug may require adjustment. Suicide. Suicidal attempts are typical for people in a state of depression; their threat can exist until stable remission is achieved, both spontaneously and as a result of therapy. Patients taking antidepressants should be carefully monitored, especially early in therapy, for clinical worsening and/or the emergence of suicidal thoughts and behavior. This also applies to the treatment of patients with other mental disorders due to the possible presence of concomitant major depressive disorder. Akathisia. SSRI/SNRI use is associated with the development of akathisia, a condition characterized by an unpleasant, debilitating feeling of restlessness and the need to move, often accompanied by an inability to sit or stand in one place. This condition most likely occurs during the first few weeks of therapy. Increasing the dose may be harmful to patients who experience these symptoms. Hyponatremia. Hyponatremia, likely due to impaired antidiuretic hormone (ADH) secretion, occurs rarely with SSRIs and usually disappears when therapy is discontinued. SSRIs should be prescribed with caution to patients at risk (old age, liver cirrhosis, or concomitant treatment with drugs that cause hyponatremia). Hemorrhages. When taking SSRIs, hemorrhages (ecchymosis and purpura) may develop. SSRIs should be prescribed with caution to patients with a tendency to bleed, as well as to patients taking anticoagulants and drugs that affect blood clotting. ECT (electroconvulsive therapy). Clinical experience with the concomitant use of SSRIs and ECT is limited and caution is recommended. Reversible selective MAO type A inhibitors. Combining escitalopram and MAO type A inhibitors is not recommended due to the risk of serotonin syndrome. Serotonin syndrome. In patients taking SSRIs concomitantly with serotonergic drugs, serotonin syndrome may develop in isolated cases. Escitalopram should be used with caution concomitantly with drugs that have serotonergic effects. A combination of symptoms such as agitation, tremor, myoclonus, and hyperthermia may indicate the development of serotonin syndrome. If such a situation arises, SSRIs and serotonergic drugs must be immediately discontinued and symptomatic therapy prescribed. St. John's wort. The simultaneous use of SSRIs and herbal preparations containing St. John's wort may lead to an increased incidence of adverse reactions. Use during pregnancy and lactation. Clinical data regarding the use of escitalopram in the treatment of pregnant women is limited. Escitam should not be administered to pregnant women. The exception is cases where, after careful consideration of all the disadvantages and advantages, the need to prescribe the drug has been clearly proven. A thorough examination of newborns whose mothers took Escitam during pregnancy, especially in the third trimester, is recommended. Sudden discontinuation of the drug during pregnancy should be avoided. Neonates whose mothers took SSRIs/SNRIs during late pregnancy may experience the following symptoms: respiratory distress, cyanosis, apnea, seizures, temperature fluctuations, difficulty sucking, vomiting, hypoglycemia, hypertension or hypotension, hyperreflexia, tremor, restlessness, irritability, apathy, constant crying, drowsiness and sleep disturbances. Such symptoms can develop due to both serotonergic effects and be signs of withdrawal syndrome. In most cases, complications occur within 24 hours after birth. Since escitalopram passes into breast milk, breastfeeding women are not recommended to take the drug or breastfeeding should be discontinued. Children. Antidepressants should not be used to treat children. Suicidal behavior (suicidal attempts and suicidal ideation) and hostility (primarily aggression, oppositional behavior and anger) were observed more frequently in clinical trials in children and adolescents taking antidepressants compared with those taking placebo. If, for clinical reasons, the decision to prescribe antidepressants is nevertheless made, it is necessary to ensure careful monitoring of the emergence of suicidal ideation in the patient. The ability to influence reaction speed when driving vehicles and working with other mechanisms. In general, escitalopram does not affect intellectual functions or psychomotor reactions, but the possible development of adverse reactions from the nervous system such as dizziness and drowsiness should be taken into account.
Interactions: Contraindicated combinations Non-selective MAO inhibitors. Escytam should not be used when patients are taking non-selective irreversible MAO inhibitors and for 2 weeks after stopping their use. Treatment with MAO inhibitors should be started no earlier than 7 days after stopping Escitam. Pimozide. Due to the interaction of escitalopram with low doses of pimozide and the increased side effects of the latter, simultaneous use is contraindicated. Undesirable combinations Due to the risk of developing serotonin syndrome, the combination of escitalopram with the MAO type A inhibitor moclobemide is not recommended. If the use of this combination is necessary, the minimum recommended doses are initially prescribed under close medical supervision. Combinations to be used with caution Selegiline. Combination with selegiline (irreversible MAO type B inhibitor) requires caution. There is experience in the safe combination of selegiline at a dose of up to 10 mg/day with racemic citalopram. Serotonergic drugs. Concomitant use with serotonergic drugs (for example, tramadol, sumatriptan and other triptans) may cause the development of serotonin syndrome. Drugs that lower the seizure threshold. SSRIs may lower the seizure threshold. Caution is recommended during concomitant use of drugs that lower the seizure threshold, such as antidepressants (tricyclics, SSRIs), antipsychotics (phenothiazines, thioxanthenes, butyrophenones), mefloquine, bupropion and tramadol. Lithium, tryptophan. Since there have been reports of enhanced effects when SSRIs are used concomitantly with lithium or tryptophan, caution is recommended when coadministering these drugs. Anticoagulants. The effects of anticoagulants may change due to simultaneous use with escitalopram. In patients taking oral anticoagulants, it is necessary to monitor the blood coagulation system before and after the use of escitalopram. Alcohol. Escitalopram does not interact pharmacodynamically or pharmacokinetically with alcohol. The combined use of escitalopram and omeprazole (CYP 2C19 inhibitor) increases the concentration of escitalopram in the blood plasma by an average of 50%. The combined use of escitalopram and cimetidine increases the concentration of escitalopram in the blood plasma by an average of 70%. Thus, when using escitalopram concomitantly with CYP2C19 inhibitors (for example, omeprazole, fluoxetine, fluvoxamine, lansoprazole, ticlopidine) and with cimetidine, caution should be exercised when prescribing the maximum permissible dose of escitalopram. A dose reduction of escitalopram may be necessary depending on clinical assessment.
Overdose : Toxicity. Clinical data on escitalopram overdose are limited. Most cases are caused by simultaneous overdose of other drugs. Mostly mild symptoms occurred or the overdose was asymptomatic. Reports of fatal consequences of escitalopram overdose are exceptional, most of them involving concomitant overdose of other drugs. Taking escitalopram in the range of 400–800 mg did not cause any severe symptoms. Symptoms. Signs of escitalopram overdose are mainly manifested by symptoms from the central nervous system (from dizziness, tremor and agitation to rare cases of serotonin syndrome, convulsions and coma), the digestive tract (nausea/vomiting), and the cardiovascular system (hypotension, tachycardia, prolongation of the Q-interval). T, arrhythmia) and electrolyte imbalance (hypokalemia, hyponatremia). Treatment. There is no specific antidote. Proper functioning of the respiratory system should be maintained, adequate oxygenation should be ensured, and gastric lavage should be administered as quickly as possible. It is possible to use activated carbon. Continuous monitoring of vital signs along with symptomatic supportive treatment is necessary.
Storage conditions: In original packaging at a temperature not exceeding 25°C.
Conditions for dispensing from pharmacies: By prescription.
Side effects and other risks
◊ Mechanism of side effects
Side effects are caused by an increase in serotonin. Most side effects occur immediately after starting treatment and go away over time.
◊ Side effects
- Gastroenterological (reduced appetite, nausea, diarrhea, constipation)
- Insomnia, sedation, agitation, tremor
- Sweating
- Urinary dysfunction
- Dry mouth
- Dangerous side effects: seizures, mania, suicidal ideation
- Weight gain: very rare
- Sedation: very rare
- Sexual dysfunction: yes
◊ What to do about side effects
- Wait
- Switch to another antidepressant [1].
◊ Long-term use
Safely
◊Addiction
No.
◊ Overdose
- There are very few reports of overdose.
- Very rare cases of fatal overdoses.
- Vomiting, sedation, cardiac arrhythmia, dizziness, tremor.
Expert advice
- The best antidepressant in terms of tolerability
- Lowest sexual impact compared to other SSRIs
- Lack of response to escitalopram in elderly patients may indicate Alzheimer's disease
- In postmenopausal women, escitalopram works better in combination with estrogen [1]
- Escitalopram and fluoxetine show similar effects in the treatment of depression. The only difference noted is that escitalopram significantly improves microinflammation in the patient’s body [6].
Interaction
Combination with MAO inhibitors, serotonergic drugs, Stramadol and triptans may increase the risk of serotonin syndrome and other complex adverse reactions.
Concomitant use with anticonvulsants may increase the risk of developing seizures.
It is possible to enhance the effects of lithium and tryptophan , increasing the toxicity of St. John's wort and drugs that affect blood clotting.
Escitalopram can significantly increase plasma concentrations of Desipramine and Metoprolol.
