Instructions for use CIPRALEX
When using drugs belonging to the SSRI therapeutic group, the following should be considered.
Use in children and adolescents under 18 years of age
Cipralex should not be prescribed to children and adolescents under 18 years of age due to an increased risk of suicidal behavior (suicide attempts and suicidal ideation) and hostility (with a predominance of aggressive behavior, confrontational behavior and irritation). If a decision is made to initiate antidepressant therapy based on clinical assessment, the patient should be closely monitored. In addition, there is insufficient data from long-term studies on the safety of the drug in children and adolescents regarding growth, maturation, cognitive and behavioral development.
Paradoxical anxiety
Some patients with panic disorder may experience increased anxiety when starting antidepressant treatment. This paradoxical reaction usually disappears within the first two weeks of treatment. To reduce the likelihood of an anxiogenic effect, it is recommended to use low initial doses.
Seizures
Escitalopram should be discontinued in the event of the primary development of convulsive seizures or in the event of an increase in their frequency (in patients with previously diagnosed epilepsy). SSRIs should not be used in patients with unstable epilepsy; Controlled seizures require careful monitoring.
Mania
SSRIs should be used with caution in patients with a history of mania/hypomania. If a manic state develops, SSRIs should be discontinued.
Diabetes
In patients with diabetes, treatment with SSRIs may alter blood glucose concentrations. Therefore, dose adjustments of insulin and/or oral hypoglycemic drugs may be required.
Suicide/suicidal ideation or clinical worsening
Depression is associated with an increased risk of suicidal ideation, self-harm, and suicide (suicidal events). This risk persists until significant remission occurs. Since improvement may not be observed during the first few weeks of therapy or even longer, patients should be closely monitored until their condition improves. General clinical practice shows that in the early stages of recovery the risk of suicide may increase.
Other psychiatric conditions for which escitalopram is prescribed may also be associated with an increased risk of suicidal events and events. In addition, these conditions may be a comorbidity in relation to a depressive episode. When treating patients with other mental disorders, the same precautions should be taken as when treating patients with a depressive episode.
Patients with a history of suicidal behavior or patients with a significant level of suicidal thoughts before treatment are at greater risk for suicidal ideation or suicide attempts and should be closely monitored during treatment. A meta-analysis of placebo-controlled clinical trials of antidepressants in adult patients with mental disorders found that there is an increased risk of suicidal behavior in patients under 25 years of age when taking antidepressants compared with placebo.
Drug treatment of these patients, and in particular those at high risk for suicide, should be accompanied by careful monitoring, especially early in treatment and during dose changes. Patients (and caregivers) should be warned to monitor for any signs of clinical worsening, suicidal behavior or ideation, or unusual changes in behavior, and to seek immediate medical advice if these symptoms occur.
Akathisia/psychomotor agitation
SSRI/SNRI use is associated with the development of akathisia, characterized by the development of subjectively unpleasant or distressing restlessness and a need for constant movement, often combined with an inability to sit or stand quietly. This most often occurs during the first few weeks of treatment. In patients with such symptoms, increasing the dose may lead to worsening.
Hyponatremia
Hyponatremia, possibly associated with impaired antidiuretic hormone (ADH) secretion, occurs rarely with SSRIs and usually disappears when therapy is discontinued. Caution should be exercised when prescribing escitalopram and other SSRIs to persons at risk of developing hyponatremia:
- elderly, patients with liver cirrhosis and taking drugs that can cause hyponatremia.
Bleeding
Cases of skin hemorrhages (ecchymosis and purpura) have been reported when taking SSRIs. SSRIs should be used with caution in patients taking oral anticoagulants and drugs that affect blood clotting (for example, atypical antipsychotics and phenothiazines, most tricyclic antidepressants, acetylsalicylic acid and nonsteroidal anti-inflammatory drugs (NSAIDs), ticlopidine and dipyridamole), as well as in patients with a tendency to bleed.
Electroconvulsive therapy (ECT)
Because clinical experience with the concomitant use of SSRIs and electroconvulsive therapy (ECT) is limited, caution should be used when escitalopram and ECT are used concomitantly.
Serotonin syndrome
Escitalopram should be used with caution concomitantly with drugs that have serotonergic effects, such as sumatriptan or other triptans, tramadol and tryptophan.
In rare cases, patients taking SSRIs concomitantly with serotonergic drugs have developed serotonin syndrome. Its development may be indicated by a combination of symptoms such as agitation, tremor, myoclonus and hyperthermia. If this occurs, concomitant treatment with SSRIs and serotonergic drugs should be immediately discontinued and symptomatic therapy initiated.
St. John's wort
Concomitant use of SSRIs and herbal medicines containing St. John's wort (Hypericum perforatum) may lead to an increased incidence of adverse reactions.
Withdrawal syndrome when stopping treatment
When you stop taking the drug, especially abruptly, a “withdrawal” syndrome often occurs. In clinical studies, side effects at discontinuation of treatment were observed in approximately 25% of patients taking escitalopram and in 15% of patients taking placebo. The development of withdrawal syndrome may depend on several factors, including duration of therapy and dosage, as well as the rate of dose reduction. The most commonly reported symptoms were dizziness, sensory disturbance (including paresthesia and sensations of current passing), sleep disturbance (including insomnia and intense dreams), agitation or anxiety, nausea and/or vomiting, tremor, confusion, increased sweating, headache pain, diarrhea, palpitations, emotional instability, irritability, visual disturbances. Typically, these effects are mild or moderate, but in some patients they may be more severe.
Symptoms usually appear within the first few days after stopping the drug, but rare cases of such symptoms have been reported in patients who have missed a dose.
In most cases, symptoms go away on their own within 2 weeks, although in some patients they may persist for 2-3 months or more. It is therefore recommended that the dose of escitalopram be gradually reduced upon discontinuation of therapy over several weeks or months according to the patient's needs.
IHD
Due to limited experience with clinical use, patients with coronary heart disease should take this drug with caution.
QT prolongation
Escitalopram causes a dose-dependent prolongation of the QT interval.
During the post-marketing period, cases of QT prolongation and the development of ventricular arrhythmias, including torsade de pointes (TdP), have been reported, primarily in women with hypokalemia, a history of QT prolongation, or other heart disease.
Use with caution in patients with severe bradycardia, or recent myocardial infarction or uncompensated heart failure.
Electrolyte imbalances, such as hypokalemia or hypomagnesemia, increase the risk of malignant arrhythmias and should be corrected before starting escitalopram. Before starting treatment, patients with stable heart disease should have an ECG checked.
If signs of cardiac arrhythmia appear while taking escitalopram, treatment should be stopped and an ECG performed.
Effect on the ability to drive a car or use machinery
Although escitalopram does not affect intellectual function or psychomotor performance, any drug that affects the psyche may affect judgment and skills. Patients should be informed of the potential risk of effects on their ability to drive or operate machinery.
Indications for taking escitalopram
- Endogenous depression of mild to moderate severity.
- Panic attacks, panic disorder, generalized anxiety disorder, phobias.
- Organic anxiety and depressive disorders.
- Neuroses, neurasthenia, mixed anxiety and depressive disorder, somatoform disorders, psychosomatic diseases, prolonged reactive states (mental trauma, adaptation disorders).
- Alcohol and drug addiction, substance abuse.
The convenience of taking ecitalopram is that you do not need to adjust the dose (recommended - 10 mg / 1 tablet once a day
), rarely have side effects, according to psychiatrists it gives a positive effect in the vast majority of cases of use.
The disadvantages include the slow onset of the therapeutic effect over the course of a month, and a slight increase in anxiety in the first days of use (which is very inconvenient when treating panic attacks, phobias and anxiety disorders).
Overdose
In clinical practice, cases of overdose of Cipralex are known, which usually manifest themselves as follows:
- darkened consciousness, soporosity ;
- tremor of the limbs , impaired fine motor skills;
- seizures;
- agitation (strong emotional arousal, which is accompanied by a feeling of anxiety and an unreasonable need to move);
- significant changes in the electrocardiogram (expansion of the ventricular complex, depolarization of the depolarization segment);
- arrhythmias of the tachycardia ;
- metabolic acidosis , hypokalemia ;
- depression of the respiratory function of the respiratory system.
There is no specific antidote or antagonist for Cipralex, so treatment of overdose is based on symptomatic and palliative care for the patient. First of all, you should rinse the stomach in order to evacuate unabsorbed remnants of the pharmaceutical drug from the body. Next, it is necessary to ensure sufficient oxygenation and constant monitoring of the vital systems of the human body.
Side effects
Cipralex is a strong drug, therefore its action can be characterized by a large number of unwanted reactions from the body. For example, it is noted:
- dyspeptic disorders ( nausea , vomiting , diarrhea , abdominal pain);
- asthenic syndrome ( insomnia or drowsiness , headache, constant fatigue, dizziness );
- metabolic disorders in the form of sweating , hyperthermia and hyponatremia ;
- thrombocytopenia and, as a consequence, insufficiency of the blood coagulation system;
- orthostatic collapse or hypotension ;
- decreased reproductive function ( decreased libido and potency in both men and women);
- allergic reactions (the range of undesirable effects includes manifestations from angioedema, angioedema , up to anaphylactic shock );
- arthralgia and myalgia of idiopathic origin , which are not associated with stress on the joints or muscles;
- skin rash , purpura , ecchymosis .
It should be noted that the adverse effects of treatment usually occur in the first or second week of a conservative therapeutic course and significantly reduce their manifestations if the rehabilitation is continued according to a given plan.
Since the drug belongs to list B of pharmacological products, if you abruptly stop taking Cipralex after long-term treatment with the drug, withdrawal syndrome . That is, the body does not have enough active substance. This manifests itself in the form of severe headaches, irritability, nausea and frequent dizziness.
Compound
The composition of the drug is given equivalent to the three main forms of release (see the next paragraph) based on the mass calculation per one tablet of the active substance escitalopram oxalate - 6.39/12.77/25.54 mg:
- fine crystalline cellulose (MCC) – 72.49/97.49/195 mg;
- ordinary talc 5.04/7/14 mg;
- croscarmellose sodium – 3.24/4.5/9 mg;
- Magnesium stearate – 0.9/1.25/2.5 mg.
The film coating of the tablets is an important component of the drug Cipralex. It consists of:
- hypromellose 5cP – 1.58/2.19/3.51 mg;
- titanium dioxide (E171) – 0.526/0.73/1.17 mg;
- macrogol 400 – 0.146/0.2/0.325 mg.
Contraindications
Pharmacological treatment with Cipralex should be abandoned if:
- hypersensitivity or intolerance to the constituent components of the drug;
- childhood and adolescence (the therapeutic course is not recommended for those under 18 years of age);
- simultaneous treatment with monoamine oxidase (antidepressants) or p imozide (antipsychotic medications);
- acute or chronic renal failure with creatine clearance below 30 ml/min;
- epilepsy , which is not controlled by pharmacological agents.
Cipralex should only be taken under the supervision of qualified medical personnel in one of the following situations:
- non-insulin-dependent diabetes mellitus (for type I, consultation with an endocrinologist is required);
- elderly age;
- cirrhosis , acute or chronic liver failure ;
- tendency to frequent hemorrhages due to insufficiency of the blood coagulation system;
- hereditary and acquired metabolic diseases .
Release form
The drug is available in the form of round or oval biconvex white film-coated tablets with different dosages:
- 5 mg of active substance (marked “EK”) – 14 tablets in a blister pack (usually made of aluminum foil or PVC), 2 packs in a cardboard box.
- Cipralex 10 mg (symmetrical o and “L” relative marks on one of the surfaces) – 14 tablets in a blister, 1, 2 or 4 contours in a box.
- 20 mg of biologically active component (marked “E” and “N” on both sides of the line on one side of the tablet) - in a box there are 2 blisters with 14 filled cells.
Pharmacodynamics and pharmacokinetics
The absorption of the active ingredients does not depend on food intake, since the drug is an extremely strong pharmaceutical drug. Absolute bioavailability is about 80 percent, and the average half-life is 4 hours (however, this parameter may vary depending on the individual parameters of the body and environmental conditions).
Cipralex is metabolized in the liver . The constituent elements of the drug, even after oxidation, remain biologically active and, undergoing some changes in metabolic processes, are released in the form of glucuronides . Next, the metabolites are sent to the kidneys, which excrete waste drug residues through urine. Clearance after oral administration of the drug is 0.6 l/min.
The kinetics of escitalopram oxalate is described linearly. Equilibrium concentration in the systemic circulation, with a daily dose of 10 mg (the optimal amount of the active ingredient for an adult), is achieved after just one week of a conservative course of treatment with Cipralex.
In elderly patients (over 65 years of age), the pharmacological drug is eliminated somewhat more slowly. Clinical trials have shown that during a therapeutic dose, after a single dose of Cipralex, the amount of the active component in the systemic bloodstream of elderly people is 50 percent greater than in young volunteers.
Pharmacological action
Cipralex belongs to the pharmacological group of potent antidepressants . serotonin transporter enzyme , the drug inhibits the reuptake of the neurotransmitter in synaptic structures (the drug has a greater effect on the metabolic pathways of serotonin than on any other messengers). Accordingly, the physiological transmitter of the impulse is located in the synaptic cleft of the neuronal contact for a longer period of time, which causes an enhanced, prolonged effect on the postsynaptic membrane .
It should be noted that the drug is strong and long-acting, as it binds in two places to the serotonin transport enzyme. First of all, the main active component has high affinity for the primary amino acid sequence of the transporter protein. Also, the components of Cipralex bind to the allosteric center of this molecule, which secondarily enhances the effect of the drug, that is, leads to a more complete inhibition of neurotransmitter reuptake.
Cipralex exhibits weak activity to receptors as:
- serotonin 5-HT1A and 5-HT2;
- dopamine D1 and D2;
- alpha and beta adrenergic synapses;
- histamine H1 receptor cells;
- opioids and benzodiazepines;
- m-cholinergic receptors.
