Expiration date: 07/2025
Pharmachologic group: antidepressant.
Pharmachologic effect: The antidepressant, selectively inhibits the reuptake of serotonin, a neurotransmitter increases the concentration in the synaptic cleft, amplifies, and prolongs the effect of postsynaptic serotonin receptors.
Escitalopram practically does not bind to serotonin (5-HT), dopamine (D1 and D2), an alpha-adrenergic, histamine, m-cholinergic receptors and benzodiazepine and opiate receptors.
Antidepressant effect usually develops within 2-4 weeks after starting treatment. The maximum therapeutic effect of the treatment of panic disorder is reached after about 3 months after initiation of treatment.
Pharmacokinetics: The absorption is independent of food intake. Bioavailability - 80%. TCmax -. 4 hours Kinetics escitalopram is linear. Css achieved after 1 week. The mean Css of 50 nmol / l (20 to 125 nmol / L) is achieved at a daily dose of 10 mg. The apparent volume of distribution - from 12 to 26 l / kg. Communication with proteins - 80%.
It is metabolized in the liver to active metabolites, demethylated and didemetilirovannogo. After repeated use and the average concentration demethyl didemetilmetabolitov is 28-31% and less than 5% of the concentration of escitalopram respectively. Metabolism in escitalopram desmethyl metabolite occurs mainly via isozymes of cytochrome P450: CYP2C19, and CYPZA4 CYP2D6. In persons with a weak activity of CYP2C19 isozyme escitalopram concentration may be 2 times higher than those with a high activity of this isoenzyme. Significant changes in the concentration of the drug in a weak CYP2D6 isoenzyme activity is not marked.
T1 / 2 after repeated use -. 30 hours At the main metabolites of escitalopram T1 / 2 is longer. Clearance - 0.6 l / min.
Escitalopram and major metabolites are excreted by the liver and most of the - the kidneys, partially displayed in the form of glucuronides. T1 / 2 and AUC increased in elderly patients.
Testimomy: Depression, panic disorder (including with agoraphobia).
Contraindications: Hypersensitivity, simultaneous reception of MAO inhibitors, under the age of 15 years, pregnancy, lactation.
Carefully. Renal insufficiency (creatinine clearance below 30 ml / min), hypomania, mania, pharmacologically uncontrolled epilepsy, depression with suicidal attempts, diabetes, advanced age, liver cirrhosis, a tendency to bleeding, concomitant use with drugs that reduce the seizure threshold, causing hyponatremia, ethanol, drugs metabolized by CYP2C19 with the system.
Dosage and administration: Inside, regardless of meals.
Depressive episodes: 10-20 mg 1 time per day.
After the disappearance of the symptoms of depression, you should continue treatment for fixing the resulting effect within 6 months.
Panic disorder (including with agoraphobia): 5 mg / day for the first week, followed by 10-20 mg / day. The maximum daily dose - 20 mg. Duration of treatment - a few months.
Upon termination of the treatment the dose should be gradually reduced over 1-2 weeks to avoid the syndrome of "cancellation".
In elderly patients (over 65 years), the recommended dose - 5 mg / day, maximum daily dose - 10 mg.
When mild to moderate renal impairment dose adjustment is required.
The recommended initial dose with reduced liver function during the first two weeks of treatment is 5 mg / day. Depending on the individual response of the patient the dose may be increased to 10 mg / day.
For patients with weak activity CYP2C19 isozyme recommended starting dose for the first two weeks of treatment - 5 mg / day. Depending on the individual response of the patient the dose may be increased to 10 mg / day.
Side effects: CNS: dizziness, weakness, insomnia or drowsiness, seizures, tremor, movement disorders, serotonin syndrome (agitation, tremor, myoclonus, hyperthermia), hallucinations, delusions, confusion, agitation, anxiety, depersonalisation, panic attacks, irritability, visual disturbances.
From the digestive system: nausea, vomiting, dryness of the oral mucosa, impaired sense of taste, decreased appetite, diarrhea, constipation.
From the CCC: orthostatic hypotension.
From endocrine system: reduction of ADH secretion, galactorrhea.
With the genitourinary system: loss of libido, impotence, ejaculation disorder, anorgasmia (in women), urinary retention.
For the skin: skin rash, pruritus, ecchymosis, purpura, angioedema.
Allergic reactions: anaphylactic reactions.
Laboratory findings: hyponatremia, changes in laboratory parameters of liver function.
Other: increased sweating, hyperthermia, sinusitis, arthralgia, myalgia, "cancellation" syndrome (dizziness, headaches and nausea).
Symptoms: dizziness, tremor, agitation, somnolence, dizziness, convulsions, tachycardia, ECG changes (change of segment ST, wave T, the expansion of the complex the QRS, QT prolongation), arrhythmias, respiratory depression, vomiting, rhabdomyolysis, metabolic acidosis, hypokalemia.
Treatment: symptomatic and supportive, including gastric lavage, adequate oxygenation, the control function of the cardiovascular and respiratory systems. No specific antidote.
Interaction: When concomitantly with MAO inhibitors increases the risk of serotonin syndrome, and serious adverse reactions.
The combined use of serotonergic drugs (including with tramadol, sumatriptan and other. Triptans) may lead to serotonin syndrome.
Simultaneous treatment with drugs that reduce the seizure threshold, increases the risk of seizures.
It enhances the effect of tryptophan and drugs Li +.
Increases toxicity of St. John's wort preparations.
It enhances the effect of drugs that affect blood clotting (requires monitoring of indicators of blood coagulation).
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 in the plasma concentration of metoprolol and desipramine 2 times.
Cautions: Escitalopram should be administered only after 2 weeks after the cancellation of irreversible MAO inhibitors, and 24 hours after the cessation of therapy, reversible inhibitor of MAO. Non-selective MAO inhibitors may appoint not earlier than 7 days after discontinuation of escitalopram.
Some patients with panic disorder at the beginning of treatment with escitalopram may experience increased anxiety, which disappears typically within the next 2 weeks of treatment. To reduce the risk of anxiety, it is recommended to use a low initial dose.
It is necessary to stop the drug in case of seizures or increased rates pharmacologically uncontrolled epilepsy.
With the development of mania escitalopram should be abolished.
Escitalopram may increase in the blood glucose concentration in diabetes, which may require dose adjustment of hypoglycemic drugs.
Clinical experience with escitalopram indicates a possible increase in the risk of suicide attempts in the realization of the first week of therapy, and therefore it is very important to carry out careful monitoring of the patients during this period.
Hyponatremia, associated with a decrease in the secretion of ADH, while taking escitalopram is rare and usually disappears when you remove the drug.
With the development of serotonin syndrome, the drug should be immediately withdrawn and symptomatic treatment.
During the period of treatment should refrain from driving and activities potentially hazardous activities that require high concentration and psychomotor speed reactions.
