Expiration date: 01/2025

The composition and form of issue: 

Tablets, film-coated. 1 tablet contains:

ESCITALOPRAM (oxalate) 5 mg

component composition amount 

excipients: croscarmellose sodium talc microcrystalline silica colloidal anhydrous magnesium stearate 

shell: hypromellose macrogol 400 titanium dioxide (E171) 

in a contour acheikova packing 14 PCs. in cardboard pack 2 packs (5 mg, 20 mg) or in cardboard pack 1, 2 or 4 packs (10 mg).

Description pharmaceutical form:

Tablets 5 mg: white color, convex, round, with a diameter of 6 mm, marked with "EK" on a break — core and shell white.

Tablets 10 mg: white color, convex, oval (8 mm × 5 5 mm), with valium, marked "E" and "L" symmetrically about the risks on a break — core and shell white.

Tablets 20 mg: white color, convex, oval (11, 5 mm × 7 mm), with valium, marked "E" and "N" symmetrically about the risks on a break — core and shell white.

Feature:

Antidepressant, SSRI.

Pharmacokinetics:

Suction

Absorption not dependent on food intake. Bioavailability of ESCITALOPRAM is about 80%. The average time to achieve Cmax in plasma about 4 hours after repeated use.

Distribution

The binding of ESCITALOPRAM and its main metabolites with the proteins of blood plasma below 80%.

The apparent volume of distribution after oral administration is about 12 to 26 l/kg.

The kinetics of ESCITALOPRAM is linear.

CSS achieved after approximately 1 week. Average CSS 50 nmol/l (20 to 125 nmol/l) is achieved at a daily dose of 10 mg.

Metabolism

ESCITALOPRAM is metabolized in the liver to the demethylated and didemetilirovannogo metabolites, which are pharmacologically active. The basic substance and its metabolites are partially allocated in the form of glucuronides.

After repeated use of the average concentration of demethyl - and didemethyl-metabolites is typically 28-31% and less 5% accordingly, the concentration of ESCITALOPRAM. Biotransformation of ESCITALOPRAM in demetilirovaniu metabolite occurs mainly with the participation of isoenzyme CYP2C19. Perhaps some part isoenzymes CYP3A4 and CYP2D6. In individuals with poor CYP2C19 activity concentration of ESCITALOPRAM may be 2 times higher than in cases with high activity of this isoenzyme. Significant changes in the concentration of the drug in cases with weak activity isoenzyme CYP2D6 was found.

Excretion

T1/2 after multiple dosing is about 30 h Cl oral application is of about 0, 6 l/min. the major metabolites of ESCITALOPRAM T1/2 more long lasting. ESCITALOPRAM and its main metabolites are excreted by the liver (metabolic pathway) and kidneys. A large part is excreted as metabolites in the urine.

Pharmacokinetics in special clinical cases

In elderly age (over 65 years) ESCITALOPRAM appears slower than in younger patients. The number of substances in the systemic circulation, calculated using AUC in the elderly is 50% more than in young healthy volunteers.

Description pharmacological action:

The inhibition of serotonin reuptake leads to increased concentration of this neurotransmitter in the synaptic cleft, strengthens and prolongs its action on postsynaptic receptor sites.

ESCITALOPRAM has no or has very weak ability to bind to several receptors, including serotonin 5-HT1A-, 5-HT2-receptors, dopamine D1 - and D2-receptors, &alpha1-, &alpha2-, &beta-adrenergic receptors, histamine H1-receptors, m-cholinergic receptors, benzodiazepine and opioid receptors.

Indications:

• depressive episodes of any severity
  
• panic disorder with or without agoraphobia.
  

Contraindications:

• hypersensitivity to ESCITALOPRAM and other components of the drug
  
• simultaneous reception of MAO inhibitors
  
• pregnancy
  
• lactation (breast-feeding)
  
• children up to age 15 years.
  

Application of pregnancy and breast-feeding:

Cipralex contraindicated during pregnancy and lactation (breastfeeding).

The use of SSRIs in the third trimester of pregnancy may have a negative impact on psychophysical development of a newborn. Was the following disorders in newborns whose mothers took SSRIs until delivery: irritability, tremor, hypertension, increased muscle tone, constant crying, difficulty sucking, a bad dream. Violations may indicate serotonergic effects or the occurrence of the syndrome. In the case of SSRI-use during pregnancy taking them should not abruptly interrupted.

Side effects:

From the digestive system: frequently — nausea, loss of appetite, diarrhea, possible constipation — vomiting, dry mouth, changes in laboratory parameters of liver function.

CNS and peripheral nervous system: frequently — insomnia or drowsiness, dizziness, weakness, possible visual disturbances, seizures, tremor, movement disorders, breach of taste sensations, serotonin syndrome, hallucinations, mania, confusion, agitation, anxiety, depersonalization, panic attacks, irritability.

From the metabolic: the most often — increased sweating, hyperthermia possibly hyponatremia.

From the reproductive system: most often — decreased libido, impotence, violation of ejaculation, anorgasmia (in women).

Of the cardiovascular system: possible orthostatic hypotension.

From the endocrine system: possible — insufficient secretion of ADH, galactorrhea.

From the side of musculoskeletal system: possible — arthralgia, myalgia.

Allergic reactions: possible anaphylactic reaction, angioedema.

Dermatological reactions: possible skin rash, itching, ekhimozy, purpura.

Other: most often a sinus infection can urinary retention.

With a sharp lifting of the drug after prolonged use, the possible withdrawal reactions — dizziness, headache and nausea. The severity of these reactions is low, but the duration is limited.

Side effects most often develop on the 1st or 2nd week of treatment and then usually become less intense and occur less frequently with continued therapy.

Drug interactions:

Pharmacodynamic interaction

While the use of Sipralexa with MAO inhibitors, and also at the beginning of MAO inhibitors sick shortly before it ceased accepting Sipralexa, it may cause serious adverse reactions. In such cases, you may develop serotonin syndrome.

Cipralex the combined use of serotonergic drugs (e.g. tramadol, sumatriptan and other Triplane) can lead to the development of serotonin syndrome.

Cipralex can reduce the seizure threshold. Care should be taken while appointing Sipralexa and other drugs that reduce the seizure threshold.

As cases enhance the action with a joint appointment Cipralex and lithium or tryptophan, are advised to exercise caution when concomitant administration of these drugs.

The simultaneous appointment Cipralex and preparations containing St. John's wort (Hypericum perforatum) may lead to an increase in the number of side effects.

When concomitant administration of ESCITALOPRAM with oral anticoagulants and drugs that affect blood clotting (e.g. atypical antipsychotics and phenothiazine, most tricyclic antidepressants, acetylsalicylic acid and NSAIDs, ticlopidine and dipyridamole), it can cause a bleeding disorder. In such cases, at the beginning or at the end of therapy with ESCITALOPRAM careful monitoring of blood clotting.

While taking ESCITALOPRAM alcohol does not enter into pharmacodynamic or pharmacokinetic interaction. However, as in the case of other psychotropic drugs, the simultaneous use of ESCITALOPRAM and alcohol is not recommended.

Pharmacokinetic interaction

Concomitant use with drugs that inhibit the CYP2C19 isoenzyme, may increase the concentration of ESCITALOPRAM in plasma. With caution you should apply at the same time ESCITALOPRAM similar drugs (e.g. omeprazole) may require dose reduction of ESCITALOPRAM.

With caution should designate Cipralex in high doses simultaneously with cimetidine in high doses, which is a potent inhibitor of the isoenzyme CYP2D6, CYP3A4 and CYP1A2.

ESCITALOPRAM is an inhibitor of the isoenzyme CYP2D6. Caution should be exercised with concomitant administration of ESCITALOPRAM and drugs metabolized by this isoenzyme, and having a small therapeutic index, for example, flecainide, propafenon and metoprolol (when used in heart failure) or drugs that are mainly metabolized by CYP2D6 isoenzyme and acting on the CNS, such as antidepressants (desipramine, clomipramine, although) or antipsychotics (risperidone, thioridazine, haloperidol). In these cases, you may need dose correction.

Co-administration of ESCITALOPRAM and desipramine or metoprolol leads to a twofold increase in the concentration of the latter two drugs.

ESCITALOPRAM may slightly inhibit isoenzyme CYP2C19. Therefore, it is recommended to exercise caution with concomitant use of ESCITALOPRAM and drugs metabolized with participation of this isoenzyme.

Method of application and dose:

Inside, regardless of meals, 1 time per day.

In depressive episodes, usually in a dose of 10 mg/day. Depending on individual patient response, the dose may be increased to a maximum of 20 mg/day.

Antidepressant effect usually develops within 2-4 weeks after the start of treatment. After the disappearance of symptoms of depression at least for another 6 months you must continue therapy to consolidate the obtained effect.

Panic disorder with/without agoraphobia in the first week of treatment recommended dose is 5 mg/day with subsequent increase up to 10 mg/day. Depending on individual patient response, the dose may be increased to a maximum of 20 mg/day.

The maximum therapeutic effect is achieved after about 3 months after starting treatment. Therapy lasts for several months.

At patients of elderly age (over 65 years) it is recommended to use half of the usual recommended dose (i.e. 5 mg/day) and a lower maximum dose (10 mg/day).

In renal insufficiency, mild and moderate severity dose adjustment is not required. Patients with renal insufficiency, severe (creatinine Cl <30 ml/min) the drug should be administered with caution.

Patients with impaired liver function recommended starting dose for the first 2 weeks of treatment is 5 mg/day. Depending on the individual response to treatment dose can be increased to 10 mg/day.

With decreased activity of isoenzyme CYP2C19 the recommended starting dose for the first 2 weeks of treatment is 5 mg/day. Depending on the individual response to treatment dose can be increased to 10 mg/day.

When discontinuing treatment with Cipralex dose should be reduced gradually over 1-2 weeks to prevent development of the syndrome.

Overdose:

Symptoms: dizziness, tremor, agitation, drowsiness, dizziness, seizures, tachycardia, ECG changes (ST segment changes and tooth T, the expansion of the complex QRS, prolongation of the interval QT), arrhythmias, depression of respiratory activity, vomiting, rhabdomyolysis, metabolic acidosis, hypokalemia.

Treatment: specific antidote exists. Treatment is symptomatic and supportive: gastric lavage, adequate oxygenation. The monitoring function of the cardiovascular and respiratory systems.

Special instructions:

ESCITALOPRAM cannot be administered concurrently with MAO inhibitors. ESCITALOPRAM can be appointed within 14 days after cessation of treatment irreversible MAO inhibitors and at least 1 day after cessation of treatment reversible inhibitor of MAO type A, including moclobemide. At least 7 days should pass after taking ESCITALOPRAM before you begin treatment non-selective MAO inhibitors.

Some patients with panic disorders at the beginning of treatment with SSRIs (including ESCITALOPRAM) may experience increased anxiety. Such a paradoxical reaction usually disappears within 2 weeks of treatment. To reduce the likelihood of anxiogenic effect, it is recommended to use the drug in low initial doses.

ESCITALOPRAM should be repealed in the case of seizures. Not recommended the use of the drug in patients with unstable epilepsy with controlled seizures should be carefully monitored. If you increase the frequency of seizures SSRIs, including ESCITALOPRAM, you must cancel.

Caution should be applied to ESCITALOPRAM in patients with the history of mania/hypomania. With the development of mania ESCITALOPRAM should be abolished.

In the treatment with ESCITALOPRAM in patients with diabetes mellitus may change the level of glucose in the blood. Therefore, you may need to adjust doses of insulin and/or oral hypoglycemic drugs.

The risk of suicide inherent in depression and may persist until significant improvement of the condition occurred spontaneously or due to therapy. Careful monitoring of patients being treated with antidepressants especially in early treatment due to clinical deterioration and/or the emergence of suicidal manifestations (thoughts and behavior). This precaution should be observed when treating other psychiatric disorders because of the possibility of the simultaneous development of a depressive episode.

Hyponatremia, possibly associated with impaired secretion of ADH, while taking ESCITALOPRAM is rare and usually disappears when the abolition of therapy. With caution should designate ESCITALOPRAM and other SSRIs to patients at risk for the development of hyponatremia: the elderly, patients with liver cirrhosis and receiving drugs that can cause hyponatremia.

When receiving ESCITALOPRAM may develop skin hemorrhages (purpura and ekhimozy). You must be wary of ESCITALOPRAM in patients with bleeding tendency, as well as oral anticoagulants and drugs that affect blood clotting.

Clinical experience with use of ESCITALOPRAM in combination with electroconvulsive therapy is limited, therefore, in this case care should be taken.

Avoid concomitant use of ESCITALOPRAM and MAO inhibitors type A because of the risk of serotonine syndrome.

An patients taking ESCITALOPRAM and other SSRIs at the same time with serotonergic medications, and in rare cases may develop serotonin syndrome. Must be used with caution ESCITALOPRAM simultaneously with drugs having serotonergic activity. A combination of symptoms such as agitation, tremor, myoclonus, hyperthermia, may indicate the development of serotonin syndrome. If this happens, SSRIs and serotonergic drugs should be lifted immediately and appoint a simptomaticescuu therapy.

The simultaneous use of ESCITALOPRAM and alcohol is not recommended.

Effects on ability to drive vehicles and management mechanisms

Although ESCITALOPRAM no effect on psychomotor activity, during treatment is not recommended to drive or mechanisms.