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Escitalopram

Pharmacodynamics
Escitalopram is an antidepressant, a selective serotonin reuptake inhibitor (SSRI) with high affinity for the primary active center. Escitalopram also binds to the allosteric center of the serotonin transporter protein with an affinity of 1000 times lower. Allosteric modulation of the transporter protein enhances the binding of escitalopram to the primary binding site, which leads to a more complete inhibition of serotonin reuptake. Escitalopram does not have or has a 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, muscarinic cholinergic, benzodiazepine and opiate receptors. 5-HT reuptake inhibition is the only possible mechanism of action that explains the pharmacological and clinical effects of escitalopram. Escitalopram is the S-enantiomer of racemic citalopram with its own therapeutic activity. It is proved that the R-enantiomer is not inert, but counteracts the serotonergic properties and the corresponding pharmacological effects of the S-enantiomer.
Pharmacokinetics
Suction. The absolute bioavailability of escitalopram is 80% and does not depend on food intake. Cmax in plasma is achieved on average 4 hours after repeated use. Distribution. The apparent Vd after oral administration is from 12 to 26 l / kg. The binding of escitalopram to human plasma proteins is not more than 80% (an average of about 56%). Penetrates into breast milk. Metabolism. Escitalopram is metabolized by demethylation, deamination and oxidation with the participation of cytochrome P450. The biotransformation of escitalopram into a demethylated metabolite occurs mainly with the help of the CYP2C19 isoenzyme. Some involvement of CYP3A4 and CYP2D6 isoenzymes is possible. Inhibition of one of these enzymes can be compensated by other enzymes. In human blood plasma, escitalopram predominates unchanged. At equilibrium, the plasma concentration of S-DCT (es-demethylcytalopram) is approximately 33% of the concentration of escitalopram. The level of S-DDTs (es-didemethylcytalopram) was not determined in most subjects. In vitro studies have shown that metabolites do not significantly contribute to the antidepressant effect of escitalopram. Breeding. T1 / 2 escitalopram after repeated use is 27-32 hours. The total oral clearance is about 0.6 l / min. In the main metabolites of escitalopram, T1 / 2 is longer. Escitalopram and its metabolites are excreted both through the liver (metabolic pathway) and through the kidneys, while most of the administered dose is excreted in the form of metabolites in the urine. Pharmacokinetics linearity The pharmacokinetics of escitalopram is linear dose-dependent. The equilibrium plasma concentration (Css) is established after approximately 1 week of therapy. An average equilibrium concentration of 50 nmol / L (in the range from 20 to 125 nmol / L) is achieved with a daily dose of 10 mg. Patients over the age of 65 The elderly (over 65 years) have a longer T1 / 2 and lower clearance values ​​compared to younger patients. The amount of escitalopram in the systemic circulation, calculated using the pharmacokinetic AUC, is 50% higher in the elderly than in healthy young volunteers. Patients with impaired liver function In patients with reduced liver function, escitalopram is excreted more slowly, the clearance of escitalopram is reduced by approximately 37%. T1 / 2 of escitalopram is almost doubled and the equilibrium plasma concentration of escitalopram is almost two times higher compared to patients with normal liver function after taking a similar dose. Patients with impaired renal function In patients with a mild to moderate decrease in renal function, excretion of escitalopram proceeds more slowly (clearance decreases by about 17%) without a significant effect on pharmacokinetics. In patients with severe renal failure (creatinine clearance below 30 ml / min), caution is required. Patients with low CYP2C19 isoenzyme activity In individuals with weak CYP2C19 activity, the concentration of escitalopram is two times higher than in cases with high activity of this isoenzyme. Significant changes in the concentration of the drug in cases with weak activity of the CYP2D6 isoenzyme were not detected.
Contraindications
hypersensitivity to escitalopram or to any of the excipients that make up this drug; escitalopram should not be used in combination with monoamine oxidase (MAO) inhibitors, monoamine oxidase-A (MAO-A) or reversible non-selective MAO inhibitors; escitalopram is contraindicated with simultaneous use with drugs that extend the QT interval on the ECG (in particular, with pimozide, antiarrhythmic drugs of classes IA and III, tricyclic antidepressants, macrolides), as well as with congenital lengthening of the QT interval; children's age under 18 is a contraindication for the use of escitalopram, since the effectiveness and safety of its use at this age have not been established; pregnancy; period of breastfeeding; lactose intolerance; lactase deficiency; glucose-galactose malabsorption. Precautions: renal failure (creatinine clearance less than 30 ml / min), manic disorders (including a history), pharmacologically uncontrolled epilepsy, depression with suicidal attempts, diabetes mellitus, electroconvulsive therapy; advanced age (over 65 years), cirrhosis of the liver, tendency to bleeding; concomitant use with drugs that lower the seizure threshold, tryptophan,drugs containing St. John's wort perforated, lithium; with drugs that cause hyponatremia, oral anticoagulants and other drugs that affect blood coagulation; with drugs metabolized with the participation of the CYP2C19 isoenzyme, ethanol.
Pregnancy and lactation
Escitalopram should not be prescribed to pregnant and breast-feeding women if the potential clinical benefit does not prevail over the theoretical risk, because the safety of the drug during pregnancy and lactation in women is not established. Embryofetotoxicity was observed in rats during studies of the reproductive toxicity of escitalopram in rats, but an increase in the number of congenital malformations was not established. If escitalopram continued in the late stages of pregnancy, especially in the third trimester, then the newborn should be monitored. If the administration of escitalopram continued until the birth or was stopped shortly before the birth, the newborn may develop a "withdrawal" syndrome. If the mother uses selective serotonin reuptake inhibitors or selective serotonin and norepinephrine reuptake inhibitors (SSRIs), the following side effects may develop in the newborn: persistent pulmonary hypertension, respiratory failure, cyanosis, apnea, convulsive disorders,temperature jumps, feeding difficulties, vomiting, hypoglycemia, hypertension, muscle hypotension, hyperreflexia, tremors, increased neuro-reflex irritability, irritability, lethargic sleep, constant crying, drowsiness or insomnia. These symptoms may occur due to the development of the "withdrawal" syndrome or serotonergic action. In most cases, such complications occur within 24 hours after birth. Epidemiological data indicate that the use of SSRIs / SSRIs during pregnancy, especially in the later stages, can increase the risk of developing stable pulmonary hypertension in newborns with a frequency of up to 5 cases per 1000 with a frequency in the general population of 1-2 per 1000. The drug is excreted in small amounts in breast milk, so when taking the drug during lactation, it is recommended to resolve the issue of stopping breastfeeding. Fertility Animal studies have shown that escitalopram can affect sperm quality. Cases from medical practice, including the use of SSRIs, have shown that the effect on sperm quality is reversible. To date, no effect on human fertility has been detected.
Side effects
Adverse reactions associated with the use of escitalopram are observed during the first one to two weeks of treatment and usually significantly weaken as therapy continues and patients improve. Frequency of unwanted adverse reactions (according to the WHO classification): very often - ≥10%; often - ≥1%, but <10%; infrequently - ≥0.1%, but <1%; rarely - ≥0.01%, but <0.1%; very rarely - <0.01%, it is not known - currently there are no data on the prevalence of adverse reactions. The following adverse reactions may occur: From the blood and lymphatic system: unknown - thrombocytopenia. Allergic reactions: infrequently - increased sensitivity; very rarely - anaphylactic reactions. From the mental sphere: very often - agitation, nervousness; often - decreased libido, orgasm disorder (in women), anxiety, confusion, drowsiness, impaired concentration, strange dreams, amnesia; infrequently - aggression, depersonalization, hallucinations, euphoria, increased libido, bruxism, panic attacks; unknown - mania, suicidal thoughts, psychomotor agitation, akathisia. From the digestive system: very often - nausea, vomiting; often - diarrhea, dry mouth, decreased appetite or vice versa its increase, constipation. From the liver and biliary tract: unknown - hepatitis. From the central nervous system: very often - drowsiness, headache, tremor, dizziness; often - migraine, paresthesia, sleep disorder; infrequently - extrapyramidal disorders, syncopal conditions, taste disturbances; rarely - serotonin syndrome (a combination of agitation, tremor, myoclonus and hyperthermia); unknown - dyskinesia, motor disorders, convulsive disorders. From the skin: very often - excessive sweating, often - skin rash, itching; infrequently - photosensitization, urticaria, alopecia, purpura; unknown - angioedema, bruising (ecchymosis). From the cardiovascular system: very often - a feeling of palpitations; often - tachycardia, arterial hypertension, orthostatic hypotension; rarely - bradycardia, lowering blood pressure, arrhythmia; unknown - prolongation of the QT interval on the ECG. From the hemopoietic organs: rarely - hemorrhages (for example, gynecological bleeding, bleeding of the gastrointestinal tract). From the sensory organs: very often - violation of accommodation; often - violation of taste sensations, visual impairment, infrequently - mydriasis, tinnitus (ringing in the ears). From the respiratory system: often - rhinitis, sinusitis, yawning; infrequently - cough, nosebleeds; rarely - dyspnea, tracheitis. From the reproductive system: often - violation of sexual function, namely, violation of ejaculation, decreased libido, impotence, menstrual irregularities; infrequently - metrorrhagia, menorrhagia; unknown - galactorrhea, priapism. From the urinary system: often - painful urination, urinary retention. Metabolic disorders: often - decreased or increased appetite, weight gain; infrequently - weight loss; rarely - insufficient secretion of antidiuretic hormone (ADH), hyponatremia, hypokalemia; unknown - anorexia. From the musculoskeletal system: infrequently - myalgia, arthralgia, increased risk of injuries and fractures. Laboratory indicators: often - a change in laboratory parameters of liver function; infrequently - an increase in the activity of “liver” enzymes, a change in the electrocardiogram (lengthening of the QT interval), hyponatremia. Other: often - weakness; infrequently - swelling; rarely - hyperthermia.
Interaction
Pharmacodynamic interactions Combined use is contraindicated With irreversible non-selective MAO inhibitors Cases of serious adverse reactions have been reported in patients receiving combination therapy with SSRIs and irreversible non-selective MAO inhibitors, as well as in patients who have recently discontinued SSRI therapy and started therapy with such MAO inhibitors. In some cases, patients developed serotonin syndrome. Escitalopram can be prescribed 14 days after discontinuation of treatment with irreversible non-selective MAO inhibitors. At least 7 days should elapse after taking escitalopram before treatment with irreversible, non-selective MAO inhibitors can be prescribed. With reversible selective MAO type A inhibitors (moclobemide) Due to the risk of developing serotonin syndrome, the combined use of escitalopram with reversible selective MAO inhibitors, such as moclobemide, is contraindicated. If there is a reasonable need for the use of such a combination, treatment should begin with the minimum recommended dose under intensive clinical supervision. With reversible non-selective MAO inhibitors (linezolid) The linezolid antibiotic is a reversible non-selective MAO inhibitor and should not be used in patients receiving escitalopram therapy. If there is a reasonable need for the use of such a combination, treatment should start with the lowest doses under close clinical supervision. With irreversible selective MAO inhibitors of type B (selegiline) Caution is necessary in case of combined use of escitalopram and an irreversible selective MAO inhibitor of type B selegiline because of the risk of developing serotonin syndrome. Selegiline in doses up to 10 mg per day was successfully used in conjunction with racemic citalopram. With QT interval extenders It is unacceptable to use with drugs that extend the QT interval, such as antiarrhythmics (procainamide, amiodarone, etc.), antipsychotics / antipsychotics (for example, pimozide, phenothiazine derivatives (chlorpromazine, trifluoperazine, thioridazine, etc.), butyrophenedolone derivatives ( etc.), tricyclic and tetracyclic antidepressants (amitriptyline, imipramine, maprotiline, etc.), SSRIs and similar antidepressants (for example, fluoxetine, venlafaxine, etc.), antimicrobials (macrolide antibiotics and their analogues, for example, erythromycin, clarithromycin; quinolone and fluoroquinolone derivatives: sparfloxacin, moxifloxacin, pentamazone, pentamazole azide) fluconazole), domperidone, ondansetron, since escitalopram in doses exceeding 20 mg per day can cause abnormal changes in the electrical activity of the heart (prolongation of the QT interval on the ECG) and lead to heart rhythm disturbances (including the development of pirouette type arrhythmias) "), which can be fatal. The combined use of escitalopram should be performed with caution when using Drugs that lower the seizure threshold Escitalopram may lower the threshold for convulsive readiness. Caution is required while taking other drugs that lower the threshold of convulsive readiness (tricyclic antidepressants, SSRIs, antipsychotics - derivatives of phenothiazine, thioxanthene and butyrophenone; mefloquine and tramadol). Serotonergic Drugs It is advisable not to combine the administration of the drug Escitalopram with serotonergic drugs such as sumatriptan or other triptans, as well as tramadol, as this can lead to the development of serotonin syndrome. Lithium tryptophan With simultaneous use with tryptophan or with lithium preparations, cases of increased action of escitalopram have been reported. Hypericum perforatum The simultaneous use of escitalopram and preparations containing Hypericum perforatum (Hypericum perforatum) can lead to an increase in side effects. Anticoagulants and blood clotting agents With the simultaneous use of escitalopram with indirect anticoagulants and other agents that affect blood coagulation (for example, atypical antipsychotics and phenothiazine derivatives, most tricyclic antidepressants, acetylsalicylic acid and non-steroidal anti-inflammatory drugs, ticlopidine and dipyridamole) may cause a blood clotting disorder. In such cases, at the beginning or end of escitalopram therapy, regular monitoring of blood coagulation is necessary. With simultaneous administration with warfarin, prothrombin time increases by 5%. There was no interaction of escitalopram with alcohol. However, as is the case with other antidepressants, you should refrain from drinking alcohol during the entire period of treatment with the drug. Pharmacokinetic interactions The effect of other drugs on the pharmacokinetics of escitalopram The metabolism of escitalopram is carried out mainly with the help of the enzyme CYP2C19. CYP3A4 and CYP2D6 may also be involved in metabolism, although to a lesser extent. The metabolism of the main metabolite, S-DCT (demethylated escitalopram), is partially catalyzed by CYP2D6. The simultaneous administration of escitalopram and omeprazole 30 mg once a day (a CYP2C19 inhibitor) led to a moderate (approximately 50%) increase in the concentration of escitalopram in the blood plasma. The simultaneous administration of escitalopram and cimetidine 400 mg 2 times a day (a general inhibitor of medium-strength enzymes) led to a moderate (approximately 70%) increase in the concentration of escitalopram in the blood plasma. Escitalopram should be combined with caution with cimetidine. A dose adjustment is recommended. Therefore, the drug should be combined with caution with CYP2C19 inhibitors (such as omeprazole, esomeprazole, fluvoxamine, lansoprazole, ticlopidine) or cimetidine. After tracking side effects caused by the simultaneous use of other drugs, a dose reduction of escitalopram may be required. The effect of escitalopram on the pharmacokinetics of other drugs Escitalopram is an inhibitor of the enzyme CYP2D6. Caution should be exercised while using escitalopram and drugs with a narrow therapeutic range, which are mainly metabolized by this enzyme, such as flecainide, propafenone and metoprolol (for use in heart failure), or certain drugs that affect the central nervous system, which are mainly metabolized by CYP2D6, for example, antidepressants such as desipramine, clomipramine and nortriptyline or antipsychotics such as risperidone, thioridazine and haloperidol. Dose adjustment may be recommended. Simultaneous administration of the drug with desipramine or metoprolol led to a twofold increase in the concentration of these CYP2D6 substrates in blood plasma. In vitro studies have shown that escitalopram may also be a weak inhibitor of CYP2C19. It is recommended that you use the drug with caution along with drugs metabolized by CYP2C19
Dosage and administration
Escitalopram is taken orally once a day (without chewing, with a small amount of liquid), regardless of the meal. The drug can be used at any time of the day, it is advisable to take the drug at the same time of day. It is recommended to regularly evaluate the treatment. Depressive episodes: Usually start with 10 mg of escitalopram once a day. Depending on the individual response of the patient, the dose may be increased to a maximum of 20 mg per day. The antidepressant effect usually develops 2-4 weeks after the start of treatment. After the symptoms of depression disappear, it is necessary to continue therapy for at least 6 months to consolidate the effect. Panic disorders with / without agoraphobia: For panic disorders during the first week of treatment, the recommended dose is 5 mg per day, then the dose is increased to 10 mg per day. The daily dose, depending on the individual reaction of the patient, can be further increased to 20 mg per day. The maximum therapeutic effect is achieved approximately 3 months after the start of treatment. Therapy lasts several months. Social Anxiety Disorder (social phobia): Usually prescribed 10 mg once daily. Relief of symptoms usually develops 2-4 weeks after the start of treatment. Depending on the individual reaction of the patient, the dose can subsequently be reduced to 5 mg per day or increased to a maximum of 20 mg per day. Since social anxiety disorder is a disease with a chronic course, the minimum recommended duration of a therapeutic course is 12 weeks. To prevent relapse of the disease, the drug can be prescribed for 6 months or longer, depending on the individual patient's response. Generalized Anxiety Disorder: The recommended starting dose is 10 mg once daily. Depending on the individual response of the patient, the dose may be increased to a maximum of 20 mg per day. Long-term administration of the drug (6 months or longer) at a dose of 20 mg per day is allowed. Obsessive-compulsive disorder: Usually prescribed 10 mg 1 time per day. Depending on the individual response of the patient, the dose may subsequently be increased to a maximum of 20 mg per day. Since obsessive-compulsive disorder is a disease with a chronic course, the course of treatment should be long enough to ensure complete relief from the symptoms and last at least 6 months. To prevent relapse, a course of treatment of at least 1 year is recommended. Elderly patients (over 65 years old): It is recommended to use half of the usual recommended dose i.e. 5 mg per day. The maximum dose for elderly patients is 10 mg per day. Patients with renal failure: In chronic renal failure, mild to moderate severity correction of the dosage regimen is not required. In patients with severe renal failure (creatinine clearance below 30 ml / min), the drug should be used with caution under the supervision of a physician. Patients with liver failure: For mild to moderate liver failure (Child-Pugh class A or B), the recommended initial dose for the first two weeks of treatment is 5 mg per day. Depending on the individual response of the patient, the dose may be increased to 10 mg per day. In severe liver failure (class C on the Child-Pugh scale), caution must be exercised during titration, treatment should be carried out under close medical supervision. Decreased CYP2C19 isoenzyme activity: For patients with low CYP2C19 isoenzyme activity, the recommended starting dose for the first two weeks of treatment is 5 mg per day. Depending on the individual response of the patient, the dose may be increased to 10 mg per day. Drug withdrawal: Abrupt withdrawal of the drug should be avoided. When treatment with escitalopram is discontinued, the dose should be reduced gradually with an interval of 1-2 weeks to avoid the occurrence of "withdrawal" syndrome. With intolerance to a dose reduction, it is possible to resume taking the drug in the same dose or reduce the dose with a large interval. The doctor solves this issue individually: for some patients, a period of 2-3 months or more may be required.
Overdose
Overdose symptoms: dizziness, tremor, agitation, drowsiness, dizziness, in rare cases, the development of serotonin syndrome, seizures and coma, tachycardia, ECG changes (ST segment change, T wave, QRS complex expansion, prolongation of the QT interval), arrhythmia, depression respiratory function, vomiting, rhabdomyolysis, metabolic acidosis, hypokalemia. Coma and fatal cases of an overdose of escitalopram are extremely rare, most of them include simultaneous overdose with other drugs. Overdose treatment: there is no specific antidote. Symptomatic and supportive treatment: gastric lavage (as soon as possible after taking the drug inside), to ensure airway patency, adequate oxygenation and ventilation. ECG monitoring of the function of the cardiovascular system is recommended (possible arrhythmias, including fatal ones) and monitoring of the respiratory system
Special instructions
Children's age up to 18 years is a contraindication for the use of escitalopram, since the effectiveness and safety of its use at this age has not been established. Due to the possibility of suicidal attempts, in patients with depression it is necessary to carefully monitor patients at the beginning of treatment and to prescribe the minimum effective doses to reduce the risk of overdose. This precaution should also be observed in the treatment of other mental disorders because of the possibility of a simultaneous illness with a depressive episode. Severe depression is characterized by a risk of suicidal actions, which can persist until significant remission is achieved. In this regard, at the beginning of treatment, constant medical supervision, supervision of patient behavior and the organization of storage and distribution of medicines only by authorized persons are required. In the treatment of panic disorders with the appointment of antidepressants and / or benzodiazepines, in some patients, in response to the treatment started, anxiety or anxiety is significantly increased. This condition, called by specialists “pathological disinhibition” or simply “paradoxical anxiety”, is considered as a rare phenomenon, although this pathological reaction has been repeatedly documented in the scientific literature. This “paradoxical anxiety” usually decreases within the first two weeks after starting treatment. It is recommended that you start with a low dose to reduce the risk of paradoxical anxiety. In this case, drug withdrawal is recommended if such a paradoxical reaction does not disappear for a long time, and if such complications of therapy exceed the benefits of the treatment. In children, adolescents and young people (under 24 years old) with depression and other mental disorders, antidepressants, compared with placebo, increase the risk of suicidal thoughts and suicidal behavior. Therefore, when prescribing the drug Escitalopram or any other antidepressants in this category of patients, the risk of suicide and the benefits of their use should be correlated. In short-term studies in people over 24 years of age, the risk of suicide did not increase, while in people over 65 years of age it decreased slightly. During antidepressant treatment, all patients should be monitored for the early detection of behavioral disorders, as well as suicidal tendencies. Escitalopram can cause a dose-dependent prolongation of the QT interval on the ECG, which can lead to heart rhythm disturbances. Hyponatremia develops due to impaired secretion of antidiuretic hormone, especially a high level of risk in older women. Against the background of taking escitalopram, skin hemorrhages (ecchymosis and purpura) may develop. It is necessary to use the drug with caution in patients with a risk of bleeding, as well as taking oral anticoagulants and drugs that affect blood coagulation. Escitalopram treatment may alter glycemic control in patients with diabetes mellitus. The dose of insulin and / or oral hypoglycemic agents should be adjusted. It is rarely possible to develop akathisia, characterized by a constant or periodically arising feeling of internal motor anxiety and manifested in the inability to sit quietly in one position for a long time or to remain motionless for a long time. Passes during the first weeks of treatment. Patients with bipolar disorder or with mania / hypomania have a history of mania. Then treatment with Escitalopram should be discontinued. It is necessary to use escitalopram with caution in the presence of drug dependence (including a history) and a history of epileptic seizures. In the case of convulsive seizures, as well as in patients with epilepsy with an increase in the frequency of convulsive seizures, the drug Escitalopram, as well as other drugs of the SSRI group, should be discontinued. Use in patients with unstable epilepsy is not recommended. Escitalopram should not be used in combination with monoamine oxidase inhibitors (MAOs). For mild to moderate impaired renal function, dose adjustment is not required; for severe renal impairment, caution is required. In case of impaired liver function, the drug is limited to the minimum recommended doses. In elderly patients, a dose reduction of escitalopram is required. With the development of a manic state, the drug should be discontinued. Clinical experience with the simultaneous use of the drug Escitalopram and electroconvulsive therapy is insufficient, therefore caution is required. At the beginning of treatment, insomnia and feelings of anxiety may occur, which can be solved by adjusting the initial dose. There was no interaction of escitalopram with alcohol. However, as is the case with other antidepressants, you should refrain from drinking alcohol during the entire period of treatment with the drug. Abrupt cessation of escitalopram therapy may lead to withdrawal syndrome. Undesirable reactions such as dizziness, headaches, and nausea may occur. To avoid the occurrence of the "withdrawal" syndrome, a gradual withdrawal of the drug within 1-2 weeks is necessary. The doctor solves this issue individually: for some patients, a period of 2-3 months or more may be required. Influence on the ability to drive vehicles and control mechanisms During the treatment with Escitalopram, patients are not recommended to drive a car or mechanisms. The patient should be informed of the potential dangers of the effects of escitalopram on the ability to drive vehicles and mechanisms.

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