ESIIPI - instructions for use, doses, side effects, contraindications

Active substance:
Escitalopram oxalate	6.39 mg	12.77 mg	25.54 mg
in terms of escitalopram	5 mg	10 mg	20 mg
Excipients:	for the preparation of a core tablet weighing:
	90 mg	125 mg	250 mg
Croscarmellose sodium (vivasol)	3.24 mg	4.5 mg	9.0 mg
ProSolve SMCC 90 [Microcrystalline cellulose Silicon dioxide colloid]	77.67 mg	103.98 mg	207.96 mg
Magnesium stearate	0.9 mg	1.25 mg	2.5 mg
Talc	1.8 mg	2.5 mg	5.0 mg
Excipients:	to obtain a tablet coated with a film coating, a mass
	92.25 mg	128.12 mg	255.02 mg
Opadrai II white [Hypromellose	2.25 mg	3.12 mg	5.02 mg
(hydroxypropylmethylcellulose)	0.63 mg	0.87 mg	1.41 mg
Lactose Monohydrate	0.81 mg	1.12 mg	1.81 mg
Macrogol (polyethylene glycol 4000)	0.225 mg	0.312 mg	0.5 mg
Titanium dioxide (E 171)]	0.585 mg	0.818 mg	1.3 mg

Description:

The tablets covered with a film cover of white color, round, biconcave without risks (a dosage of 5 mg) and with a risk (dosages of 10 mg and 20 mg).

Pharmacotherapeutic group:antidepressant

ATX: & nbsp

N.06.A.B.10 Escitalopram

Pharmacodynamics:

Antidepressant, selectively inhibits serotonin reuptake (SSRIs); to raisewThe concentration of this neurotransmitter in the synaptic cleft increases and prolongs the action of serotonin on postsynaptic receptors. Escitalopram has no or very little ability to bind to a number of receptors, including: serotonin 5-HT_1A, 5-HT₂ receptors, dopamine D₁ and D₂ receptors, α₁, α₂-, β-adrenergic receptors, histamine H₁, muscarinic cholinergic, benzodiazepine and opioid receptors.

The antidepressant effect usually develops in 2-4 weeks after the start of treatment. The maximum therapeutic effect of treatment of panic disorders is reached approximately 3 months after the start of treatment.

Pharmacokinetics:

Absorption is not dependent on food intake. Bioavailability - 80%. Time to reach the maximum concentration in the blood plasma (TC_mOh) - 4 hours. The kinetics of escitalopram is linear. The equilibrium concentration (C_ss) is achieved after 1 week. Average Css 50 nmol / l (20 to 125 nmol / l) is achieved with a daily dose of 10 mg. The apparent volume of distribution is from 12 to 26 l / kg. The connection with proteins is below 80%.

Metabolized in the liver to active demethylated and demodetylated metabolites. After repeated use, the average concentration of demethyl- and didemetilmetabolites is 28-31% and less than 5%, respectively, of the concentration of escitalopram. Metabolism of escitalopram in the demethylated metabolite occurs mainly with the help of cytochrome P isoenzymes450: CYP2C19, CYP3A4 and CYP2D6. In persons with a weak isoenzyme activity CYP2C19 the concentration of escitalopram can be in 2 times higher than in individuals with high activity of this isoenzyme. Significant changes in drug concentration with a weak isoenzyme activity CYP2D6 is not observed. The half-life (T_1/2) after multiple application - 30 hours. The main metabolites of escitalopram T_1/2more prolonged. Clearance - 0,6 l / min.

Escitalopram and its major metabolites are excreted by the liver and a large part - by the kidneys, partially excreted in the form of glucuronides. T_1/2and the area under the "concentration-time" curve (AUC) increases in elderly (over 65 years) patients.

Indications:

- Depressive episodes of any severity;

- panic disorder with / without agoraphobia;

- obsessive-compulsive disorder.

Contraindications:

- Hypersensitivity to escitalopram and auxiliary components of the drug;

- Lactase deficiency, lactose intolerance, glucose-galactose malabsorption;

- children's, youthful age (up to 18 years);

- simultaneous reception with monoamine oxidase inhibitors (MAO);

- pregnancy, the period of breastfeeding.

Pregnancy and lactation:

Escitalopram is contraindicated in pregnancy and lactation (breastfeeding).

The use of SSRI in the third trimester of pregnancy can adversely affect the psychophysical development of the newborn. The following disorders were registered in newborns whose mothers took SSRIs up to the birth: irritability, tremor, hypertension, increased muscle tone, constant crying, difficulty sucking,a bad dream. Violations may indicate serotonergic effects or the onset of withdrawal syndrome.

If SSRIs are used during pregnancy, their intake should not be severely interrupted.

Dosing and Administration:

ESIIPI is administered orally once a day, regardless of food intake.

Depressive episodes

Usually prescribe 10 mg once a day. Depending on the individual reaction of the patient, the dose may be increased to a maximum of 20 mg / day. The antidepressant effect usually develops in 2-4 weeks after the start of treatment. After the disappearance of the symptoms of depression, at least for another 6 months, it is necessary to continue therapy to fix the effect.

Panic disorder with or without agoraphobia

During the first week of treatment, a dose of 5 mg / day is recommended, which is then increased to 10 mg / day. Depending on the individual reaction of the patient, the dose may be increased to a maximum of 20 mg / day. The maximum therapeutic effect is achieved approximately 3 months after the start of treatment. The therapy lasts for several months.

Obsessive-compulsive disorder

Usually prescribe 10 mg once a day.Depending on the individual reaction of the patient, the dose can subsequently be increased to a maximum of 20 mg / day. Because obsessive-compulsive disorder is a disease with chronic course, treatment should be long enough to ensure complete relief from symptoms and last at least 6 months. To prevent relapse, treatment is recommended for at least 1 year.

Elderly patients (over 65 years of age)

It is recommended to use half of the usually recommended dose (ie, only 5 mg / day) and a lower maximum dose (10 mg / day).

Children and teenagers under the age of 18

Antidepressants should not be given to children and adolescents under the age of 18 because of the increased risk of suicidal behavior (suicidal attempts and thoughts), hostility (with a predominance of aggressive behavior, a tendency to confrontation and irritation). If a decision is made to initiate antidepressant therapy, the patient should be carefully monitored.

Decreased kidney function

With mild and moderate renal failure, dose adjustments are not required.Patients with severe renal failure (creatinine clearance CL_cr below 30 ml / min), the preparation of AICIPI should be administered with caution.

Decreased liver function

The recommended initial dose for the first two weeks of treatment is 5 mg / day. Depending on the individual reaction of the patient, the dose may be increased to 10 mg / day. With severe hepatic insufficiency, care must be taken when titrating.

Reduced activity of cytochrome P₄₅₀2S19

For patients with a weak isoenzyme activity, P₄₅₀2S19 the recommended initial dose for the first two weeks of treatment is 5 mg / day. Depending on the individual reaction of the patient, the dose may be increased to 10 mg / day.

Discontinuation of treatment

At the termination of treatment with the drug AICIPI, the dose should gradually decrease within 1-2 weeks in order to avoid the occurrence of withdrawal syndrome.

Side effects:

From the central nervous system: dizziness, weakness, insomnia or drowsiness, convulsions, tremor, motor disorders, serotonin syndrome (agitation, tremor, myoclonus, hyperthermia), visual disturbances.

From the side of the psyche: hallucinations, mania, confusion, agitation, anxiety, depersonalization, panic attacks, increased irritability,

From the respiratory system: sinusitis, yawning.

From the digestive system: nausea, vomiting, dry mouth, taste disorders, decreased appetite, diarrhea, constipation.

From the side of the cardiovascular system: orthostatic hypotension.

From the endocrine system: decrease in the secretion of antidiuretic hormone (ADH).

From the genitourinary system: retention of urine.

From the side of the organs of sight: visual impairment.

On the part of the reproductive system: galactorrhea, decreased libido, impotence, impaired ejaculation, anorgasmia (in women).

From the skin: skin rash, itching, ecchymosis, purpura, angioedema, increased sweating.

From the musculoskeletal system: arthralgia, myalgia.

Laboratory indicators: hyponatremia, changes in laboratory parameters of liver function.

Other: hyperthermia, anaphylactic reactions.

With a sharp discontinuation of the drug, there may be a "cancellation" syndrome (dizziness, headaches and nausea).To avoid the occurrence of withdrawal syndrome, a gradual withdrawal of the drug within 1-2 weeks is recommended.

Overdose:

Symptoms

Dizziness, tremor, agitation, drowsiness, confusion, convulsive seizures, tachycardia, changes in the electrocardiogram (ECG) (change ST-T, expansion of the complex QRS, lengthening the interval QT), arrhythmias, respiratory depression, vomiting, rhabdomyolysis, metabolic acidosis, hypokalemia.

Treatment

There is no specific antidote. Treatment is symptomatic and supportive: gastric lavage, adequate oxygenation. Monitoring the function of the cardiovascular and respiratory systems.

Interaction:

With simultaneous administration with MAO inhibitors, as well as at the start of MAO inhibitors in patients who had recently taken escitalopram, the risk of developing serotonin syndrome increases.

Joint application with serotonergic drugs (including tramadol, sumatriptan, etc. triptans) can lead to the development of serotonin syndrome.

Simultaneous reception with drugs that reduce the threshold of convulsive readiness (tricyclic antidepressants,SSRIs, antipsychotics - phenothiazines, thioxanthenes, butyrophenones) increases the risk of seizures.

Enhances the effect of tryptophan and lithium preparations (Li+).

Increases the toxicity of St. John's Wort preparations.

With simultaneous use with oral anticoagulants and drugs that affect blood clotting (for example, atypical antipsychotics and phenothiazines, most tricyclic antidepressants, acetylsalicylic acid, nonsteroidal anti-inflammatory drugs, ticlopidine, dipyridamole), blood coagulability is possible, careful monitoring of the relevant parameters is necessary.

Escitalopram does not enter with pharmacodynamic or pharmacokinetic interaction with alcohol. However, as with other psychotropic drugs, simultaneous use of escitalopram and alcohol is not recommended.

Drugs metabolized with the participation of the system CYP2C19 (incl. omeprazole, esomeprazole, fluvoxamine, lansoprazole, ticlopidine), cimetidine as well as drugs that are inhibitors CYP3A4 and CYP2D6 (including flecainide, propafenone, metoprolol, desipramine, clomipramine, nortriptyline, risperidone, thioridazine, haloperidol), increase the concentration of escitalopram in the blood plasma of patients. Escitalopram increases concentration in plasma of desipramine and metoprolol by 2 times.

Special instructions:

Escitalopram should be administered only 2 weeks after the discontinuation of irreversible monoamine oxidase inhibitors (MAO) and 24 hours after discontinuation of therapy with a reversible MAO inhibitor. Non-selective MAO inhibitors can be prescribed no earlier than 7 days after the withdrawal of escitalopram.

Some patients with panic disorder at the beginning of SSRI treatment may experience an increase in anxiety, which usually disappears during the next 2 weeks of treatment. To reduce the likelihood of an alarm, it is recommended to use low initial doses.

It is necessary to cancel the drug in case of convulsive seizures. It is not recommended to use in patients with unstable epilepsy; in controlled seizures

careful monitoring is necessary. With increasing frequency of convulsive seizures, the drug should be canceled.

Escitalopram should be used with caution in patients with a history of mania / hypomania. With the development of the manic state escitalopram should be canceled.

Escitalopram can increase the concentration of glucose in the blood in diabetes mellitus, which may require correction of doses of hypoglycemic drugs.

The risk of committing suicide is inherent in depression and may persist until a significant improvement in the condition occurs spontaneously or as a result of ongoing therapy. Careful observation of patients on antidepressant medication is necessary, especially at the beginning of treatment because of the possibility of clinical deterioration and / or the appearance of suicidal manifestations (thoughts and behavior). This precaution should be followed in the treatment of other mental disorders due to the possibility of concurrent depressive episode.

Hyponatremia associated with a decrease in the secretion of the antidiuretic hormone ADH, while taking escitalopram occurs rarely and usually disappears when the drug is withdrawn.

When taking escitalopram, it is possible to develop skin manifestations: ecchymosis, purpura. Care should be taken when prescribing the drug to patients prone to bleeding or taking anticoagulants.

It is not recommended simultaneous administration of escitalopram and MAO type A inhibitors because of the risk of developing serotonin syndrome. It is necessary to exercise caution when used simultaneously with drugs that have a serotonergic effect. The combination of such symptoms as agitation, tremor, myoclonus, hyperthermia, may indicate the development of serotonin syndrome. In this case, simultaneous reception of SSRIs and serotonergic drugs should be stopped and symptomatic treatment should begin.

Effect on the ability to drive transp. cf. and fur:Although escitalopram does not affect the psychomotor activity, during the period of treatment it is not recommended to operate the car and the mechanisms.

Form release / dosage:

Tablets, film-coated, 5 mg, 10 mg and 20 mg.

Packaging:

For 7 or 14 tablets in a contour mesh package.

For 14 or 28 tablets in a jar of polymer materials.

Each can, 1 or 2 contourcell packs of 14 tablets, or 2 or 4 contour packs of 7 tablets together with the instructions for use are placed in a pack of cardboard.

Storage conditions:

At a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

2 years.

Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LP-002063

Date of registration:25.04.2013

Date of cancellation:2018-04-25

The owner of the registration certificate:VEROPHARM SA VEROPHARM SA Russia

Manufacturer: & nbsp

VEROPHARM SA Russia

Representation: & nbspVEROPHARM, AO VEROPHARM, AO Russia

Information update date: & nbsp03.10.2015

Illustrated instructions

Instructions

AYSIIP (ACP)