Cipralex

Antidepressants 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 thoughts), 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.

When using drugs belonging to the SSRI therapeutic group, including escitalopram, the following should be considered.

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.

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.

Escitalopram should be used with caution in patients with a history of mania/hypomania. If a manic state develops, escitalopram should be discontinued.

In patients with diabetes mellitus, treatment with escitalopram may change blood glucose concentrations. Therefore, dose adjustments of insulin and/or oral hypoglycemic drugs may be required.

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.

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, possibly related to impaired antidiuretic hormone (ADH) secretion caused by SSRIs, is rare and usually resolves when therapy is discontinued. Caution should be exercised when prescribing escitalopram and other SSRIs to persons at risk of developing hyponatremia: the elderly, patients with cirrhosis, and those taking drugs that can cause hyponatremia.

Cases of skin hemorrhages (ecchymosis and purpura) have been reported when taking SSRIs. Escitalopram should be used with caution in patients taking oral anticoagulants and medications that affect blood clotting, as well as in patients with a tendency to bleed.

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.

Combining escitalopram and MAO A inhibitors is not recommended due to the risk of developing 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 escitalopram and other 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 discontinued immediately and symptomatic treatment initiated.

Alcohol
Escitalopram does not interact pharmacodynamically or pharmacokinetically with alcohol. However, as with other psychotropic drugs, the simultaneous use of escitalopram and alcohol is not recommended.

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.

Indications for use

It is recommended to include Cipralex in a conservative treatment regimen if neurological pathologies such as:

prolonged periods of depression of any severity;
panic disorders (which may be explained by agoraphobia - fear of open spaces);
depressive stage of manic-depressive psychosis ;
various types of social phobias or simply anxiety among people;
obsessive-compulsive disorder (the medical explanation for “obsession”);
neurosis ;
generalized anxiety syndrome.

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.

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.

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.

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 .

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.

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.