Escitalopram
Escitalopram: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews
- 19. Price in pharmacies
Latin name: Escitalopram
ATX code: N06AB10
Active ingredient: escitalopram (escitalopram)
Producer: Berezovsky pharmaceutical plant (Russia), ALSI Pharma, JSC (Russia)
Description and photo update: 2018-21-11
Prices in pharmacies: from 194 rubles.
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Escitalopram is an antidepressant.
Release form and composition
Escitalopram is available in the form of film-coated tablets: round, biconvex, white, the core of the tablet is almost white or white (10 mg each: 10 pcs. In blisters, in a cardboard box 1, 3 or 6 packages; 7 pcs. And 14 pcs. In blisters, in a cardboard bundle 2 or 4 packs; 28 pcs. In polymer cans, in a cardboard bundle 1 jar; 5 mg and 20 mg each: 10 pcs. In blisters, in a cardboard box 3 or 6 packages).
1 tablet contains:
- active substance: escitalopram oxalate - 6.39 mg, 12.78 mg or 25.56 mg, which is equivalent to 5 mg, 10 mg or 20 mg of escitalopram, respectively;
- auxiliary components: aerosil (colloidal silicon dioxide), microcrystalline cellulose, magnesium stearate, pregelatinized starch;
- shell composition: white opadry - macrogol, titanium dioxide, lactose monohydrate, hypromellose.
Pharmacological properties
Pharmacodynamics
Escitalopram is an antidepressant drug, a selective serotonin reuptake inhibitor. The only possible mechanism of action of escitalopram is the inhibition of the reuptake of 5-HT receptors. It has a high affinity for the primary active center, the affinity for binding to the allosteric center of the serotonin transporter protein is 1000 times lower. Binding of escitalopram at the primary binding site enhances allosteric modulation of the transporter protein, causing a more complete inhibition of serotonin reuptake.
Escitalopram has a very weak ability to bind to alpha 1 -, alpha 2 -, beta-adrenergic receptors, histamine H 1 receptors, dopamine D 1 - and D 2 -receptors, serotonin 5-HT 1A -, 5-HT 2 -receptors, muscarinic cholinergic, opiate, benzodiazepine and a number of other receptors, or does not have it at all.
Escitalopram is the S-enantiomer of racemic citalopram, which has its own therapeutic activity. At the same time, the R-enantiomer is not passive; it opposes the serotonergic properties of the S-enantiomer and its pharmacological effects.
Pharmacokinetics
Regardless of the meal, the absolute bioavailability of escitalopram is 80%. The maximum concentration (C max) in blood plasma is achieved after 4 hours with repeated use.
The volume of distribution (V d) is 12–26 l / kg.
Plasma protein binding averages approximately 56% (no more than 80%).
Escitalopram passes into breast milk.
Metabolized by demethylation, deamination and oxidation with the participation of cytochrome P 450. Biotransformation of escitalopram occurs mainly with the help of the isoenzyme CYP2C19 with the formation of a demethylated metabolite. CYP3A4 and CYP2D6 isoenzymes can take some part, inhibition of one of them is compensated by other enzymes.
In the blood plasma, the content of escitalopram in unchanged form prevails. At steady state, the plasma level of S-DCT (es-demethylcitalopram) is about 33% of the concentration of escitalopram, and the level of S-DCT (es-didemethylcitalopram) is in most cases undetectable. Metabolites are almost not involved in the therapeutic effect of the drug.
After repeated use, T 1/2 (half-life) of escitalopram is from 27 to 32 hours, the total clearance is about 0.6 l / min. T 1/2 of the main metabolites is longer.
Most of the dose taken in the form of metabolites is excreted through the kidneys, the remainder through the liver. In a small amount, escitalopram is excreted unchanged.
For the pharmacokinetics of escitalopram, a linear dose-dependent character is characteristic. After 7 days of therapy, its equilibrium plasma concentration (C ss) is usually established, which averages 50 nmol / l when taking the drug at a dose of 10 mg daily.
In patients over 65 years of age, the T 1/2 is higher, the clearance of escitalopram is lower, and its total concentration in the blood plasma is 50% higher than in younger patients.
With reduced liver function, the excretion of escitalopram slows down, its clearance decreases by about 37%, and T 1/2 doubles. Equilibrium plasma concentrations of escitalopram in the presence of similar doses are almost two times higher than in patients with normal liver function.
Mild to moderate renal impairment causes a slowdown in the excretion of escitalopram and a decrease in clearance by approximately 17%, but this does not significantly affect the pharmacokinetics of the drug. In severe renal failure with creatinine clearance (CC) below 30 ml / min, caution is required.
With a weak activity of CYP2C19, the level of escitalopram concentration in blood plasma is twice as high as compared with patients with high activity of this isoenzyme.
The weak activity of the isoenzyme CYP2D6 does not significantly affect the concentration of the drug.
Indications for use
- episodes of depression of any severity;
- generalized anxiety disorder;
- social phobia (social anxiety disorder);
- panic disorder with and without agoraphobia;
- obsessive-compulsive disorder.
Contraindications
- simultaneous use of reversible non-selective inhibitors of monoamine oxidase (MAO), inhibitors of MAO or MAO-A (monoamine oxidase-A);
- Congenital prolongation of the QT interval or concomitant therapy with drugs that prolong the QT interval on an electrocardiogram (ECG), including pimozide, tricyclic antidepressants, class IA and III antiarrhythmics, macrolides;
- syndrome of glucose-galactose malabsorption, lactase deficiency, lactose intolerance;
- age up to 18 years;
- period of pregnancy;
- breast-feeding;
- hypersensitivity to the components of the drug.
According to the instructions, Escitalopram is prescribed with caution for depression with suicidal attempts, manic disorders (including history), drug-induced uncontrolled epilepsy, simultaneous electroconvulsive therapy, renal failure with a CC less than 30 ml / min, diabetes mellitus, liver cirrhosis, a tendency to bleeding, elderly (over 65) age.
In addition, it is recommended to be careful if it is necessary to simultaneously treat with tryptophan, drugs that are metabolized with the participation of the isoenzyme CYP2C19, reduce the seizure threshold, affect blood clotting (including oral anticoagulants), cause hyponatremia, contain lithium, St. John's wort or ethanol.
Instructions for the use of Escitalopram: method and dosage
Escitalopram tablets are taken orally, 1 time per day, swallowed whole, washed down with a sufficient amount of liquid, regardless of food intake, always at the same time.
During the period of treatment, it is necessary to conduct a regular assessment of therapy.
Recommended daily dosage of Escitalopram:
- depressive episodes: the initial dose is 10 mg. Taking into account the individual tolerance of the drug, to achieve the desired therapeutic effect, the dose can be increased to a maximum daily dose of 20 mg. The effect develops within 14-28 days after the start of the use of the tablets. Long-term treatment, in order to prevent the recurrence of the disease, taking the tablets should be continued for another 180 days in the complete absence of symptoms of depression;
- generalized anxiety disorder: initial dose - 10 mg. The maximum daily dose is 20 mg. The duration of the course is 180 days or longer, including at a dose of 20 mg;
- social phobia: the initial dose is 10 mg. Symptoms usually improve after 14–28 days of treatment. Considering the individual tolerance of the drug and the patient's condition, the daily dose can be reduced to 5 mg or increased to a maximum of 20 mg. The chronic nature of social anxiety disorders requires a minimum duration of therapy - 84 days. For the prevention of relapses of the disease, the use of the drug can last 180 days or longer, taking into account the patient's individual response to the drug;
- panic disorder: the initial dose is 5 mg, after 7 days of therapy, it is increased to 10 mg. The maximum daily dose is 20 mg. Treatment continues until a stable therapeutic effect is achieved, which usually occurs after 90 days of therapy;
- obsessive-compulsive disorder: 10 mg, maximum daily dose 20 mg. The course of treatment is at least 180 days; in order to prevent relapse, it is recommended to continue it for at least 180 days after the symptoms of the disease have completely disappeared.
For the treatment of patients over the age of 65, the daily dose should be ½ the usual dose, the maximum dose is 10 mg per day.
With mild to moderate chronic renal failure, dose adjustment is not required. With severe renal failure (CC less than 30 ml / min), close medical supervision is required.
With hepatic impairment class A or B on the Child-Pugh scale, the initial dose of Escitalopram should be 5 mg per day. After 14 days of therapy, subject to good individual tolerance of the drug, the dose can be increased to 10 mg. In severe form (class C on the Child-Pugh scale) of hepatic insufficiency, the dose should be titrated and accompanied by regular medical supervision.
With a reduced activity of the isoenzyme CYP2C19, the initial dose is prescribed in the amount of 5 mg for 14 days; if it is necessary to increase it, the maximum daily dose should not exceed 10 mg.
Cancellation of Escitalopram should be carried out by gradually reducing (1 time in 7-14 days) the daily dose of the drug. If the condition worsens, it is shown to resume taking the previous dose or to increase the interval between dose reductions. In some cases, it takes 60–90 days or more to stop treatment.
Side effects
- from the central nervous system: very often - dizziness, drowsiness, tremors, headache; often - sleep disorder, migraine, paresthesia; infrequently - extrapyramidal disorders, syncope; rarely - serotonin syndrome (combination of tremor, excitement, hyperthermia and myoclonus); frequency not established - movement disorders, dyskinesia, convulsive disorders;
- from the lymphatic system and blood: frequency not established - thrombocytopenia;
- from the side of the psyche: very often - nervousness, agitation; often - drowsiness, anxiety, confusion, strange dreams, impaired concentration, amnesia, decreased libido, in women - orgasm disturbance; infrequently - hallucinations, euphoria, aggression, depersonalization, bruxism, panic attacks, increased libido; frequency has not been established - mania, suicidal thoughts (including after drug withdrawal), akathisia, psychomotor agitation;
- on the part of the cardiovascular system: very often - a feeling of palpitations; often - arterial hypertension, tachycardia, orthostatic hypotension; rarely - lowering blood pressure (BP), arrhythmia, bradycardia; frequency not established - lengthening of the QT interval on the ECG;
- from the hepatobiliary system: frequency not established - hepatitis;
- from the digestive system: very often - nausea, vomiting; often - dry mouth, diarrhea, constipation, decreased or increased appetite;
- metabolic disorders: often - weight gain; infrequently - decrease in body weight; rarely - lack of secretion of antidiuretic hormone, hypokalemia, hyponatremia; frequency not established - anorexia;
- dermatological reactions: very often - increased sweating; often - itchy skin, rash; infrequently - urticaria, photosensitivity, purpura, alopecia; the frequency has not been established - angioedema, ecchymosis;
- on the part of the hematopoietic organs: rarely - hemorrhages, including gastrointestinal and gynecological bleeding;
- from the senses: very often - violation of accommodation; often - visual impairment, impaired taste; infrequently - ringing in the ears, mydriasis;
- from the urinary system: often - urinary retention, painful urination;
- on the part of the reproductive system: often - impotence, menstrual irregularities, ejaculation disorders; infrequently - menorrhagia, metrorrhagia; frequency not established - priapism, galactorrhea;
- from the respiratory system: often - yawning, rhinitis, sinusitis; infrequently - nosebleeds, cough; rarely - tracheitis, dyspnea;
- on the part of the musculoskeletal system: infrequently - increased risk of injuries and fractures, myalgia, arthralgia;
- allergic reactions: infrequently - hypersensitivity; very rarely - anaphylactic reactions;
- laboratory indicators: often - changes in liver function indicators; infrequently - hyponatremia, increased activity of liver enzymes;
- others: often - weakness; infrequently - edema; rarely - hyperthermia.
The results of post-registration studies indicate cases of prolongation of the QT interval, ventricular arrhythmia, ventricular tachycardia of the "pirouette" type. These undesirable effects more often occur in female patients with cardiovascular diseases.
In the results of epidemiological studies, an increased risk of bone fractures was noted in patients aged 50 years and older, receiving a selective serotonin reuptake inhibitor and tricyclic antidepressants.
Overdose
Symptoms: drowsiness, vomiting, dizziness, confusion, tremor, agitation, tachycardia, arrhythmias, ECG changes (lengthening of the QT interval, changes in the T wave, ST segment, expansion of the QRS complex), metabolic acidosis, rhabdomyolysis, hypokalemia, depression of external respiration, in rare cases - the development of serotonin syndrome, convulsions, coma. Coma and deaths are extremely rare and are usually associated with a simultaneous overdose of other drugs.
Treatment: no specific antidote. Symptomatic and supportive therapy is indicated: immediate gastric lavage, ensuring airway patency, adequate oxygenation and ventilation of the lungs, monitoring the function of the respiratory system. Due to the high risk of developing arrhythmias (including fatal outcomes), the functional state of the cardiovascular system is carefully monitored using an ECG.
special instructions
Adverse events associated with the use of escitalopram can occur during the first two weeks of treatment, usually they do not require discontinuation of the drug and as therapy continues, they significantly weaken.
For insomnia and anxiety, the initial dose of Escitalopram should be reduced.
Abrupt withdrawal of the drug can cause withdrawal symptoms, the most common of which include: dizziness, increased sweating, irritability, insomnia, vivid dreams and other sleep disorders, paresthesias and sensory disorders, agitation, emotional instability, anxiety, tremors, nausea, vomiting, confusion consciousness, headache, heart palpitations, visual disturbances, diarrhea. The severity of these phenomena is individual.
Due to the risk of suicidal attempts at the beginning of the use of the drug, the patient must be carefully monitored and controlled, especially in the treatment of severe depression.
Prescribing escitalopram for the treatment of panic disorder may cause a significant increase in the patient's anxiety or anxiety. If this condition persists for a long period, then the pill should be canceled.
Prolongation of the QT interval on the ECG is dose-dependent and can cause heart rhythm disturbances.
The reason for the development of hyponatremia is a violation of the secretion of antidiuretic hormone. Older women are at greater risk of hyponatremia.
In patients with diabetes mellitus, dose adjustment of oral hypoglycemic agents or insulin is required.
It is not recommended to prescribe escitalopram for unstable epilepsy.
If mania occurs in patients with bipolar disorder or a history of mania, the pill should be discontinued.
The use of alcoholic beverages during the period of drug treatment is contraindicated.
Influence on the ability to drive vehicles and complex mechanisms
It is contraindicated to engage in potentially hazardous activities during the entire period of use of Escitalopram, including driving.
Application during pregnancy and lactation
The appointment of Escitalopram during gestation and breastfeeding is contraindicated.
Animal studies of the drug have found its embryophetotoxicity.
The use of the drug in late pregnancy contributes to the development in newborns of such side effects as respiratory failure, persistent pulmonary hypertension, cyanosis, temperature fluctuations, constant crying, convulsive disorders, muscle hypotension, apnea, vomiting, hypoglycemia, feeding difficulties, hypertension, increased nervous - reflex excitability, hyperreflexia, tremors, irritability, drowsiness, lethargic sleep, insomnia. These symptoms occur within the first 24 hours after birth and may be due to the development of a withdrawal syndrome or serotonergic effect.
If it is necessary to use Escitalopram during lactation, the issue of stopping breastfeeding should be resolved.
Pediatric use
The appointment of Escitalopram to patients under 18 years of age is contraindicated, since there is no information on the efficacy and safety of the drug at this age.
With impaired renal function
With mild to moderate chronic renal failure, dose adjustment is not required. With severe renal failure (CC less than 30 ml / min), the drug is prescribed with caution and under close medical supervision.
For violations of liver function
Escitalopram is prescribed with caution in liver cirrhosis.
For hepatic impairment of class A or B on the Child-Pugh scale, the initial dose should be 5 mg per day. After 14 days of therapy, subject to good individual tolerance of the drug, the dose can be increased to 10 mg. In severe form (class C on the Child-Pugh scale) of hepatic insufficiency, the dose should be titrated and accompanied by regular medical supervision.
Use in the elderly
Escitalopram is prescribed with caution in old age.
For the treatment of patients over the age of 65, the daily dose should be ½ the usual dose, the maximum dose is 10 mg per day.
Drug interactions
With the simultaneous use of Escitalopram:
- irreversible non-selective MAO inhibitors cause the development of serotonin syndrome, therefore this combination is contraindicated. The appointment of escitalopram is possible only 14 days after the cancellation of irreversible nonselective MAO inhibitors, and irreversible nonselective MAO inhibitors - 7 days after the cancellation of escitalopram;
- moclobemide, linezolid and other reversible selective MAO-A inhibitors, selegiline and other irreversible selective MAO-B inhibitors increase the risk of developing serotonin syndrome, so this combination should be avoided;
- drugs that prolong the QT interval, including procainamide, amiodarone and other antiarrhythmics, chlorpromazine, trifluoperazine, thioridazine (phenothiazine derivatives), pimozide and other antipsychotics or antipsychotics, haloperidol, droperidol and other derivatives of butyptyropylinone, imitraplirothyne tetracyclic antidepressants, fluoxetine, venlafaxine and other similar antidepressants, antimicrobial agents of the macrolide group (including erythromycin, clarithromycin), pentamidine, fluoroquinolone and quinolone derivatives (moxifloxacin, sparfloxacin), an azole drug series (protivogucondonetone) cause a pathological lengthening of the QT interval on the ECG and heart rhythm disturbances, including the development of pirouette-type arrhythmias,and be fatal;
- tricyclic antidepressants, selective serotonin reuptake inhibitors, mefloquine, tramadol, neuroleptics - derivatives of thioxanthene, phenothiazine and butyrophenone - can cause a decrease in the seizure threshold;
- tramadol, sumatriptan and other serotonin derivatives increase the risk of developing serotonin syndrome;
- tryptophan, lithium enhance the effect of escitalopram;
- St. John's wort increases the risk of side effects;
- indirect anticoagulants and other drugs that affect blood clotting, can cause a blood clotting disorder;
- warfarin increases prothrombin time by 5%;
- omeprazole (at a dose of 30 mg per day), cimetidine (at a dose of 400 mg 2 times a day) cause a moderate (approximately 50% and 70%, respectively) increase in the concentration of escitalopram in blood plasma, therefore, when the drug is combined with CYP2C19 inhibitors (including esomeprazole, fluvoxamine, ticlopidine, lansoprazole) may require a reduction in the escitalopram dose;
- drugs with a narrow therapeutic range, the metabolism of which occurs under the influence of the CYP2D6 enzyme, including flecainide, metoprolol, propafenone, antidepressants (desipramine, nortriptyline, clomipramine), antipsychotics (haloperidol, risperidone, thioridazine) can increase their plasma levels;
- drugs metabolized by CYP2C19 should be used with caution.
Analogs
The analogues of Escitalopram are: Aktaparoxetine, Elicea, Plizil, Tsipralex, Fluxen, Eisipe, Lenuxin, Miracitol, Sancipam, Selektra, Paroxin, Serlift.
Terms and conditions of storage
Keep out of the reach of children.
Store at temperatures up to 25 ° C in a dark place.
The shelf life is 3 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Escitalopram
Reviews of Escitalopram are mostly positive. Pointing to the drug's efficacy in the treatment of depression and panic disorder, patients report improvements in overall well-being and quality of life. The clinical response to therapy occurs gradually, it is necessary to be prepared for a long course of treatment.
The disadvantages of the drug include the development of undesirable phenomena. Most often, against the background of the drug, dizziness and drowsiness or insomnia occur. This usually occurs at the initial stage of escitalopram application and gradually disappears on its own.
Price for Escitalopram in pharmacies
The price of Escitalopram for a package containing 28 tablets at a dose of 10 mg can range from 274 rubles, 30 tablets at a dose of 20 mg - from 1098 rubles.
Escitalopram: prices in online pharmacies
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Drug name Price Pharmacy |
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Escitalopram 10 mg film-coated tablets 28 pcs. 194 r Buy |
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Escitalopram 10 mg film-coated tablets 30 pcs. 227 r Buy |
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Escitalopram tab. p.p. 10 mg 30 pcs. 243 r Buy |
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Escitalopram 10 mg film-coated tablets 30 pcs. 249 r Buy |
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Escitalopram tablets p.p. 10mg 28 pcs. 263 r Buy |
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Escitalopram 20 mg film-coated tablets 30 pcs. 389 r Buy |
Maria Kulkes Medical journalist About the author
Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
