Escitalopram
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2019-09-19
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Clinical Pharmacology
Elycea is an antidepressant, a selective serotonin reuptake inhibitor (SSRI), increases the concentration of a neurotransmitter in the synaptic cleft by inhibiting the reverse neuronal seizure of serotonin, enhances and prolongs the action of serotonin on postsynaptic receptors. Escitalopram has practically no or very weak affinity for a number of receptors, including serotonin: 5-HT1A, 5-NT2, dopamine: D1 and D2; α1- and α2- and β-adrenoreceptors, histamine H1-receptors, m-cholinergic receptors, benzodiazepine and opioid receptors, which causes the absence or weak expression of various anticholinergic, sedative, cardiovascular side effects. Escitalopram also does not bind or has a very low affinity for various ion channels, including Na+To+Cl-Sa2+channels.
Indications
Depression, panic disorders (including with agoraphobia).
Composition
1 tablet contains escitalopram 10 mg
Escitalopram is marketed under different brands and generic names, and comes in different dosage forms:
| Brand name | Manufacturer | Country | Dosage form |
|---|---|---|---|
| Elicea | Krka dd Novo mesto AO | Slovenia | pills |
| Selectra | Abbott | USA | pills |
| Escitalopram | Canonpharma | Russia | pills |
| Asipi | Veropharm | Russia | pills |
| Lenuxin | Gedeon Richter | Hungary | pills |
| Cipralex | Lundbeck AS | Denmark | pills |
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Dosage and Administration
Elycea is taken orally, regardless of the meal. Depressive episodes: 10-20 mg 1 time per day. After the disappearance of the symptoms of depression, it is necessary to continue therapy to consolidate the effect obtained for 6 months. Panic disorders (including with agoraphobia): 5 mg / day for the first week, then 10-20 mg / day. The maximum daily dose is 20 mg. The duration of treatment is several months. When treatment is discontinued, the dose should be gradually reduced over a period of 1-2 weeks in order to avoid the occurrence of the "withdrawal" syndrome. In elderly patients (over 65), the recommended dose is 5 mg / day, the maximum daily dose is 10 mg. With mild to moderate renal failure, dose adjustment is not required. The recommended initial dose with reduced liver function during the first two weeks of treatment is 5 mg / day. Depending on the patient's individual response, the dose may be increased to 10 mg / day. For patients with weak activity of the CYP2C19 isoenzyme, the recommended initial dose for the first two weeks of treatment is 5 mg / day. Depending on the patient's individual response, the dose may be increased to 10 mg / day.
Adverse reactions
1/100 to <1/10), infrequently (from> 1/1000 to <1/100), rarely (from> 1/10 000 to <1/1000), very rarely (from <1/10 000, including individual messages).
Since the cardiovascular system:infrequently - tachycardia; rarely bradycardia; very rarely - orthostatic hypotension.
From the hemopoietic system:very rarely - thrombocytopenia.
From the nervous system:often - insomnia, drowsiness, dizziness, paresthesias, tremor, anxiety, anxiety, nightmares; infrequently - taste disorders, sleep disorders, fainting, gnashing of teeth, psychomotor agitation, akathisia, irritability, panic disorders, confusion; rarely - serotonin syndrome (agitation, tremor, myoclonus, hyperthermia), aggressiveness, depersonalization, hallucinations, suicidal thoughts and behavior; very rarely - dyskinesia, convulsive and manic disorders.
On the part of the respiratory system:often - sinusitis, yawning; infrequently - nosebleeds.
From the digestive system:very often nausea; often - increase or decrease in appetite, diarrhea, constipation, vomiting, dryness of the oral mucosa; infrequently - gastrointestinal bleeding (including rectal bleeding); very rarely - hepatitis.
From the genitourinary system:often - ejaculatory disorders, impotence, decreased libido, anorgasmia (in women); rarely - metrorrhagia, menorrhagia; very rarely - urinary retention, priapism, galactorrhea.
From the senses:infrequently - mydriasis, visual disturbances, tinnitus.
On the part of the skin:often - excessive sweating, alopecia; very rarely - ecchymosis.
From the musculoskeletal system:often - arthralgia, myalgia.
On the part of the endocrine system:very rarely - inadequate secretion of antidiuretic hormone, galactorrhea.
Allergic reactions:often - urticaria, skin rash, pruritus; rarely, anaphylactic reactions; very rarely - angioedema (angioedema).
Other:often - weakness, fever; Infrequently - swelling.
From the laboratory indicators:often - weight gain; infrequently - weight loss; very rarely - hyponatremia, changes in laboratory parameters of liver function.
With the abrupt cancellation of the drug may develop withdrawal syndrome.
Contraindications
Hypersensitivity, simultaneous use of MAO inhibitors, age up to 15 years, pregnancy, lactation.
Drug interactions
When taken simultaneously with MAO inhibitors, the risk of serotonin syndrome and serious adverse reactions increases. Combined use with serotonergic drugs (including tramadol, sumatriptan and other triptans) can lead to the development of serotonin syndrome.Simultaneous reception with drugs that reduce the threshold of convulsive readiness, increases the risk of seizures. Enhances the effect of tryptophan and drugs Li +. Increases the toxicity of drugs Hypericum. Enhances the effect of drugs that affect blood coagulation (requires monitoring of blood coagulation parameters). Drugs metabolized involving CYP2C19 system (including omeprazole), and which are potent inhibitors CYPZA4 and CYP2D6 (including flecainide, propafenone, metoprolol, desipramine, clomipramine, nortriptyline, risperidone, thioridazine, haloperidol), increase concentration of escitalopram. Increases plasma concentration of desipramine and metoprolol by 2 times.
Pregnancy and Lactation
The drug Elicea is not used during pregnancy (safety is not established).
Due to the fact that escitalopram is secreted into breast milk, the use of the drug during breastfeeding is not recommended. If necessary, the use of the drug Elyceum during lactation, breastfeeding should be discontinued.
Special instructions
Escitalopram should be prescribed only 2 weeks after discontinuation of irreversible MAO inhibitors and 24 hours after cessation of therapy with a reversible MAO inhibitor. Non-selective MAO inhibitors can be prescribed no earlier than 7 days after withdrawal of escitalopram. Some patients with panic disorder at the beginning of treatment with escitalopram may experience increased anxiety, which usually disappears within the next 2 weeks of treatment. To reduce the likelihood of anxiety, it is recommended to use low initial doses. The drug should be discontinued in the event of the development of epileptic seizures or their increase in pharmacologically uncontrolled epilepsy. With the development of a manic state, escitalopram should be canceled. Escitalopram may increase blood glucose concentration in patients with diabetes mellitus, which may require correction of doses of hypoglycemic drugs. Clinical experience with the use of escitalopram indicates a possible increase in the risk of suicidal attempts in the first weeks of therapy, and therefore it is very important to carefully monitor patients during this period. Hyponatremia associated with a decrease in the secretion of ADH, while receiving escitalopram, occurs rarely and usually disappears when the drug is withdrawn. With the development of serotonin syndrome, the drug should be immediately canceled and symptomatic treatment prescribed. During the period of treatment, it is necessary to refrain from driving and engaging in potentially hazardous activities that require increased concentration of attention and psychomotor speed.
Overdosage
Symptoms:dizziness, tremor, agitation, drowsiness, serotonin syndrome, convulsions, depression of consciousness of varying severity (especially in combination with alcohol and / or other means of depressing the function of the central nervous system), nausea, vomiting, decrease in blood pressure, tachycardia, changes in ECG (change in segment ST, T wave, expansion of the QRS complex, prolongation of the QT interval), arrhythmias, respiratory depression, metabolic acidosis, rhabdomyolysis, hypokalemia, hyponatremia.
Treatment:Symptomatic and supportive therapy is performed: gastric lavage, Activated charcoal intake, airway obstruction, adequate oxygenation, control of cardiovascular and respiratory system functions. There is no specific antidote.
- Brand name: Elicea
- Active ingredient: Escitalopram
- Dosage form: film coated pills
- Manufacturer: Krka dd Novo mesto AO
Studies and clinical trials of Escitalopram (Click to expand)
- Isolation, characterization, and magnesium-induced self-association kinetics of discrete aggregates of RecA protein from Escherichia coli
- Effect of Vitreoscilla hemoglobin dosage on microaerobic Escherichia coli carbon and energy metabolism
- Intracellular expression of Vitreoscilla hemoglobin modifies microaerobic Escherichia coli metabolism through elevated concentration and specific activity of cytochrome o
- Effect of glucose supply strategy on acetate accumulation, growth, and recombinant protein production by Escherichia coli BL21 (λDE3) and Escherichia coli JM109
- Pharmacokinetic modelling of blood–brain barrier transport of escitalopram in rats
- Homology Modeling of the Serotonin Transporter: Insights into the Primary Escitalopram-binding Site
- Escitalopram in the treatment of generalized anxiety disorder: Double-blind, placebo controlled, flexible-dose study
- Efficacy and tolerability of escitalopram in 12- and 24-week treatment of social anxiety disorder: Randomised, double-blind, placebo-controlled, fixed-dose study
- Escitalopram in the treatment of social anxiety disorder: Analysis of efficacy for different clinical subgroups and symptom dimensions
- Escitalopram in clinical practice: Results of an open-label trial in a naturalistic setting
- Escitalopram in the treatment of anxiety symptoms associated with depression
- A prospective study of escitalopram in the treatment of major depressive episodes in the presence or absence of anxiety
- Escitalopram in major depressive disorder: a multicenter, randomized, double-blind, fixed-dose, parallel trial in a Chinese population
- Randomized placebo-controlled trial of escitalopram and venlafaxine XR in the treatment of generalized anxiety disorder
- Escitalopram in the treatment of major depressive disorder in primary-care settings: an open-label trial
- An open-label study of escitalopram (Lexapro®) for the treatment of ‘Depression of Alzheimer's disease’ (dAD)
- Predicting 6-week treatment response to escitalopram pharmacotherapy in late-life major depressive disorder
- Treating depression to remission in older adults: a controlled evaluation of combined escitalopram with interpersonal psychotherapy versus escitalopram with depression care management
- The antidepressant effects of running and escitalopram are associated with levels of hippocampal NPY and Y1 receptor but not cell proliferation in a rat model of depression
- How long should a trial of escitalopram treatment be in patients with major depressive disorder, generalised anxiety disorder or social anxiety disorder? An exploration of the randomised controlled trial database
- Quality of sleep in escitalopram-treated female patients with panic disorder
- An open, non-randomised comparison of escitalopram and duloxetine for the treatment of subjects with Generalized Anxiety Disorder
- The effect of escitalopram on sleep problems in depressed patients
- Escitalopram in a working population: results from an observational study of 2378 outpatients in Austria
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