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Lexapro is an antidepressant, a selective serotonin reuptake inhibitor (SSRI) with high affinity to the primary binding site. Lexapro also binds to an allosteric binding site of protein-transporter, with an affinity at a thousand times. Allosteric modulation transporter protein enhances the binding of Lexapro in the primary binding site that results in a more complete inhibition of serotonin reuptake.
Lexapro has no or very 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 receptors , m-cholinergic, benzodiazepine, and opioid receptors.
The absorption is almost complete and independent of food intake. The bioavailability of Lexapro is approximately 80%. The average time to reach Cmax in plasma was 4 hours after repeated use.
The binding of Lexapro and its main metabolites in the plasma proteins below 80%.
Apparent Vd, β / F after oral administration is from 12 to 26 l / kg.
Kinetics of Lexapro is linear.
Css achieved in about 1 week. The mean Css of 50 nmol / l (20 to 125 nmol / L) is achieved at a daily dose of 10 mg.
Lexapro is metabolized in the liver to Dide methylated and methylated metabolites which are pharmacologically active. Nitrogen can be oxidized to N-oxide metabolites. The basic substance and its metabolites in the form of partially allocated glucuronides.
After repeated use of the average concentration and didemetil demethyl metabolite is typically 28-31% and less than 5%, respectively, the concentration of Lexapro. Biotransformation of Lexapro to the demethylated metabolite is mainly with the participation of isoenzyme CYP2C19. Perhaps some part of isozymes CYP3A4 and CYP2D6. In persons with a weak activity of CYP2C19 isozyme Lexapro concentration 2 times higher than in the case of the high activity of this isoenzyme. No significant changes in the concentration of the drug in cases of weak activity of CYP2D6 isoenzyme were detected.
T1 / 2, after repeated use is about 30 hours. The clearance when administered orally is about 0.6 l / min. In the main metabolites of Lexapro T1 / 2 is longer. Lexapro and its main metabolites are excreted by the liver (metabolic pathway) and kidneys. Most metabolites excreted as urine.
Pharmacokinetics in special clinical situations
In the elderly (over 65 years) Lexapro appears slower than in younger patients. The amount of substance in the systemic circulation, calculated by AUC elderly 50% more than in young healthy volunteers.
Tsipraleks administered 1 time / day, regardless of the meal.
During depressive episodes, the drug is usually prescribed at a dose of 10 mg / day. Depending on the individual response of the patient the dose may be increased to a maximum of – 20 mg / day.
The antidepressant effect usually occurs within 2-4 weeks after starting treatment. After the disappearance of the symptoms of depression for at least another 6 months for a need to continue therapy for fixing the resulting effect.
When panic disorder with / without agoraphobia for the first week of treatment recommended dose of 5 mg / day, followed by an increase to 10 mg / day. Depending on the individual response of the patient the dose may be increased to a maximum of – 20 mg / day.
The maximum therapeutic effect is reached after about 3 months after initiation of treatment. The therapy lasts several months.
When social anxiety disorder (social phobia) is prescribed 10 mg 1 time / day. The weakening of symptoms usually occurs within 2-4 weeks after starting treatment. Depending on the individual response of the patient the dose may subsequently be reduced to 5 mg / day and increased to a maximum of – 20 mg / day.
The weakening of symptoms usually occurs within 2-4 weeks after starting treatment.
Since social anxiety disorder is a disease with a chronic course, the minimum recommended duration of the therapeutic course is 3 months. In order to prevent recurrence of the disease the drug may be administered for 6 months or longer, depending on the individual patient response. It is recommended to regularly assess the treatment.
With generalized anxiety disorder usually prescribed 10 mg 1 time / day. Depending on the individual response of the patient the dose may be increased to a maximum of – 20 mg / day.
The minimum recommended duration of the therapeutic course is 3 months. To prevent recurrence of the disease is allowed to use the drug for a long period (6 months and longer). It is recommended to regularly assess the treatment.
With obsessive compulsive disorder is usually prescribed 10 mg 1 time / day. Depending on the individual response of the patient the dose may subsequently be increased to a maximum of – 20 mg / day.
As obsessive-compulsive disorder is a disease with a chronic course of treatment should be long enough to provide complete relief of symptoms, and continued for at least 6 months. To prevent recurrence recommended treatment for at least 1 year.
Elderly patients (over 65 years) is generally recommended to use half the recommended dose (ie, a total of 5 mg / day) and a lower maximum dose (10 mg / day).
Tsipraleks should not be used in children and adolescents younger than 18 years. In addition, there is sufficient data of long-term safety studies of the drug in children and adolescents concerning growth, maturation, cognitive and behavioral development.
In renal insufficiency, mild to moderate dose adjustment is required. Patients with severe renal insufficiency (creatinine clearance By reducing liver function recommended starting dose for the first 2 weeks of treatment was 5 mg / day. Depending on the individual response to the medication dose can be increased to 10 mg / day.
If reduced activity of isoenzyme CYP2C19 recommended starting dose for the first 2 weeks of treatment is 5 mg / day. Depending on the individual response to the medication dose can be increased to 10 mg / day.
Upon termination of treatment Tsipraleksom dose should be reduced gradually over 1-2 weeks to avoid the development of withdrawal syndrome.
The data on Lexapro overdose are limited in many such cases, and there was an overdose of other medications. In most cases, symptoms of an overdose are not shown or are weak. Cases of overdose of Lexapro (without receiving other drugs) fatalities are rare, in most cases, there is also an overdose of drugs and others.
Symptoms: an overdose of Lexapro is mainly arise CNS symptoms (vertigo, tremor, and agitation to rare cases of serotonin syndrome, seizure disorders, and coma), the gastrointestinal tract (nausea / vomiting), cardiovascular system (hypotension, tachycardia, QT prolongation and arrhythmia) and electrolyte imbalance (hypokalemia, hyponatremia).
Treatment: There is no specific antidote. It should ensure the normal airway, oxygenation and ventilation. Gastric lavage should be performed and assign activated carbon. Gastric lavage should be undertaken as soon as possible after taking the drug. It is recommended to monitor the performance of the heart and other vital organs, and symptomatic and supportive therapy.
Non-selective irreversible MAO inhibitors
It reported the occurrence of serious adverse reactions while taking SSRIs and non-selective irreversible MAO inhibitors, and also at the beginning of the patients receiving MAO inhibitors, long before this stop taking SSRIs. In some cases, patients developed serotonin syndrome.
Apply Lexapro together with non-selective irreversible MAO inhibitors is prohibited. Receiving Lexapro may be started 14 days after receiving the cancellation of irreversible MAO inhibitors. Before taking non-selective irreversible MAO inhibitors must be at least 7 days after receiving Lexapro.
Reversible, selective inhibitor of MAO type A (moclobemide)
Due to the risk of serotonin syndrome is not recommended while Lexapro with MAO inhibitors type A moclobemide. If receiving a combination of drugs recognized as clinically necessary, it is recommended to start with the lowest possible dose and to carry out constant monitoring of the clinical condition of the patient. Receiving Lexapro can start at least one day after the cancellation of a reversible inhibitor of MAO-A moclobemide.
Irreversible MAO-B inhibitor (selegiline)
Due to the risk of serotonin syndrome is necessary to be careful when taking Lexapro together with irreversible MAO-B inhibitor selegiline.
The combined use of serotonergic drugs (eg tramadol, sumatriptan and other triptans) may lead to serotonin syndrome.
Drugs that lower the seizure threshold
SSRIs can lower the seizure threshold. It requires careful with Lexapro while using other drugs that reduce the seizure threshold (tricyclic antidepressants, SSRIs, antipsychotic drugs (neuroleptics) – derivatives of phenothiazine, thioxanthene and butyrophenone, mefloquine, bupropion and tramadol).
Since the reported cases enhance the effect, while the use of SSRIs and lithium or tryptophan, caution is advised during concomitant use of these drugs with Lexapro.
St. John’s wort
Concomitant use of SSRIs and products containing St. John’s wort (Hypericum perforatum), may lead to an increase in side effects.
Anticoagulants and drugs affecting blood coagulation
Blood clotting can occur, while the use of Lexapro with oral anticoagulants and drugs that affect blood clotting (eg, atypical antipsychotics and phenothiazines derivatives, by most tricyclic antidepressants, acetylsalicylic acid and non-steroidal anti-inflammatory drugs, ticlopidine and dipyridamole). In such cases, when the beginning or end of Lexapro therapy requires careful monitoring of blood clotting. Simultaneous treatment with NSAIDs may lead to an increase in bleeding.
The influence of other drugs on the pharmacokinetics of Lexapro
The metabolism of Lexapro is mainly carried out with the participation of isoenzyme CYP2C19. To a lesser extent in the metabolism can participate isozymes CYP3A4 and CYP2D6. The metabolism of the major metabolite – demethylated Lexapro – probably partly catalyzed by isoenzyme CYP2D6.
The simultaneous use of Lexapro and omeprazole (CYP2C19 isozyme inhibitor) resulting in a moderate (about 50%) increase in the concentration in the blood plasma of Lexapro.
Simultaneous administration of Lexapro and cimetidine (an inhibitor of isozyme CYP2D6, CYP3A4 and CYP1A2) leads to an increase (approximately 70%) concentration in the blood plasma of Lexapro.
Thus, to apply the maximum possible dose Lexapro simultaneously CYP2C19 isozyme inhibitors (e.g., omeprazole, fluoxetine, fluvoxamine, lansoprazole, ticlopidine) and cimetidine with caution. At the same time taking Lexapro and the aforementioned drugs based on clinical evaluation may be necessary to decrease the dose of Lexapro.
Effect of Lexapro on the pharmacokinetics of other drugs.
Lexapro is an inhibitor of isozyme CYP2D6. Care should be taken while the application of Lexapro and drugs metabolized by this isoenzyme, and having a small therapeutic index, eg flecainide, propafenone and metoprolol (in cases of heart failure), or medicines, mainly metabolized through the CYP2D6 and acting on the central nervous system For example, antidepressants (desipramine, clomipramine, nortriptyline), or antipsychotics (risperidone, thioridazine, haloperidol). These cases may require dose adjustment.
The simultaneous use of Lexapro and desipramine or metoprolol resulting in a twofold increase in the concentration of the latter two drugs.
Lexapro can significantly inhibit isoenzyme CYP2C19. Therefore, caution is advised during concomitant use of Lexapro and drugs metabolized isoenzyme CYP2C19.
Pregnancy and lactation
There are limited data on the admission of Lexapro during pregnancy.
If receiving Lexapro continued late in pregnancy, especially in the III trimester, the newborn should establish surveillance. If receiving Lexapro continued until delivery has been stopped or shortly before birth, the newborn may develop withdrawal symptoms.
In the case of receiving a mother SSRI / SNRI late in pregnancy a newborn may develop the following side effects: respiratory distress, cyanosis, apnea, seizure disorders, temperature jumps, difficulty feeding, vomiting, hypoglycemia, hypertension, hypotonia, hyperreflexia, tremor, increased neuro-reflex excitability, irritability, lethargy, constant crying, sleepiness, poor sleep. These symptoms may occur as a result of withdrawal or serotonergic action. In most cases, such complications occur within 24 hours after birth.
Lexapro during pregnancy should be taken only if absolutely necessary and after careful evaluation of benefit / risk ratio.
Data from epidemiological studies suggest that the use of SSRIs in pregnancy, particularly in late pregnancy, may increase the risk of development of resistant pulmonary hypertension in the newborn.
It is expected that Lexapro will be excreted in breast milk, so during treatment with Lexapro breast-feeding is not recommended.
Side effects most often develop in the first or second week of treatment and then generally become less intense and less likely to occur with continued therapy.
The following are the side effects that occur while taking drugs belonging to the class of SSRIs and marked when taking Lexapro. The information is presented based on data from placebo-controlled clinical studies and spontaneous reports. The frequency is specified as: very common (≥1 / 10), common (of ≥1 / 100 to <1/10), uncommon (from ≥1 / 1,000 to <1/100), rarely (of ≥1 / 000 to 10 <1/1000), very rare (<1/10 000), or unknown (the frequency of occurrence can not be estimated from the available data).
From the hematopoietic system: unknown – thrombocytopenia.
Immune system: rarely – anaphylactic reactions.
From endocrine system: unknown – inadequate secretion of antidiuretic hormone (ADH).
Metabolic and Nutritional: common – decreased appetite, increased appetite, weight gain; rarely – weight loss; unknown – hyponatremia, anorexia.
On the part of the psyche: often – anxiety, restlessness, abnormal dreams, decreased libido, anorgasmia (female); infrequently – Bruxism, agitation, nervousness, panic attacks, confusion; rare – aggression, depersonalization, hallucinations; unknown – mania, suicidal ideation, suicidal behavior. The incidence of suicidal thoughts and behavior have been noted when taking Lexapro and immediately after discontinuation.
From the nervous system: often – insomnia, drowsiness, dizziness, paraesthesia, tremor; infrequently – taste disturbance, sleep disturbance, syncope; rarely – serotonin syndrome; unknown – dyskinesia, movement disorders, seizure disorders, psychomotor agitation / akathisia.
For part of the vision: rarely – mydriasis (pupil dilation), blurred vision.
On the part of the ear and labyrinth disorders: rarely – tinnitus (ringing in the ears).
Since the cardiovascular system: rarely – tachycardia; rarely – bradycardia; unknown – QT prolongation on the ECG, orthostatic hypotension.
The respiratory system: often – sinusitis, yawning; rarely – nosebleeds.
From the digestive tract: often – nausea; often – diarrhea, constipation, vomiting, dry mouth; rarely – gastrointestinal bleeding (including rectal bleeding).
Liver and Biliary: Unknown – hepatitis, disorders of the liver function.
Skin and subcutaneous tissue disorders: often – increased sweating; rarely – urticaria, alopecia, rash, itching; unknown – ecchymosis, angioedema.
From the musculoskeletal system: often – arthralgia, myalgia.
On the part of the kidney and urinary tract: Unknown – urinary retention.
Reproductive system and breast cancer: often – impotence, abnormal ejaculation; infrequently – metrorrhagia (uterine bleeding), menorrhagia; unknown – Galactorrhea, priapism.
On the part of the body as a whole and at the injection site disorders: often – fatigue, pyrexia; Infrequent – edema.
The Post-registration period, there were cases of lengthening the interval QT, primarily in patients with pre-existing heart disease. In double-blind, placebo-controlled studies in healthy volunteers ECG change from baseline QTc (correction formula Friederici) was 4.3 ms at a dose of 10 mg / day and 10.7 ms – at 30 mg / day.
Epidemiological studies involving patients aged 50 years and older showed the existence of an increased risk of bone fractures in patients receiving SSRIs and tricyclic antidepressants. The mechanism of this risk is not installed.
Cancel SSRIs / SNRIs (selective noradrenaline reuptake inhibitors and serotonin) (especially sharp) often leads to withdrawal symptoms. Most often there are dizziness, sensitivity disturbances (including paraesthesia and sensations of current flow), sleep disturbances (including insomnia and intense dreams), agitation or anxiety, nausea and / or vomiting, tremor, confusion, increased sweating, headache, diarrhea, palpitations, emotional instability, irritability and visual disturbances. Usually, these effects are mild or moderate and pass quickly, however, in some patients they may be manifested in a more acute form, and / or longer. It is recommended that the gradual abolition of the drug by reducing the dose.
Conditions and terms
The drug should be stored out of reach of children at or above 25 ° C. Shelf life – 3 years.
– Depressive episodes of any severity;
– Panic disorder with / without agoraphobia;
– Social anxiety disorder (social phobia);
– Generalized anxiety disorder;
– Obsessive-compulsive disorder.
– Concomitant use of non-selective irreversible MAO inhibitors;
– Concomitant use of pimozide;
– Children and teens under 18 years of age (efficacy and safety have not been confirmed);
– Hypersensitivity to Lexapro and other ingredients.
Precautions: severe renal insufficiency (creatinine clearance below 30 ml / min), mania and hypomania, pharmacologically uncontrolled epilepsy, expressed suicidal behavior, diabetes, cirrhosis, bleeding tendency; simultaneous reception of MAO A inhibitor (moclobemide) and MAO inhibitors (selegiline); with serotonergic drugs; with drugs that reduce the seizure threshold; lithium, tryptophan pharmaceutical preparations containing St. John’s wort; with oral anticoagulants and drugs that affect blood clotting; with drugs that can cause hyponatremia; with drugs metabolized with isoenzyme CYP2C19; ethanol; Electroconvulsive therapy; old age, pregnancy, breastfeeding.
Lexapro does not come with ethanol in pharmacodynamic or pharmacokinetic interaction. However, as is the case with other psychotropic drugs, the simultaneous use of Lexapro and alcohol is not recommended.
Effects on ability to drive vehicles and management mechanisms
Despite the fact that Tsipraleks does not affect intelligence and psychomotor activity, in patients during treatment is not recommended to drive or mechanisms.
If the kidney function
In renal insufficiency, mild to moderate dose adjustment is required. Patients with severe renal insufficiency (creatinine clearance If abnormal liver function
Patients with impaired hepatic function The recommended starting dose for the first 2 weeks of treatment is 5 mg / day. Depending on the individual response to the medication dose can be increased to 10 mg / day.
The use in the elderly
With care to elderly patients
Application in childhood
Is contraindicated in children under the age of 18
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