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

CORE:
Active substance:	5 mg	10 mg	20 mg
Escitalopram oxalate	6.39 mg	12.78 mg	25.56 mg
(which corresponds to escitalopram	5 mg	10 mg	20 mg)
Excipients:
Lactose Monohydrate	53.610 mg	107.220 mg	214.440 mg
Crospovidone	3.750 mg	7,500 mg	15,000 mg
Povidone K30	0.375 mg	0.750 mg	1,500 mg
Cellulose
microcrystalline	7,500 mg	15,000 mg	30,000 mg
Starch pregelatinized	1.875 mg	3.750 mg	7,500 mg
Magnesium stearate	1,500 mg	3,000 mg	6,000 mg
SHELL:
* Drop off white 33G28707	1.875 mg	3.750 mg	7,500 mg

* White Foam 33G28707 consists of a mixture of hypromellose 6cP (40%), titanium dioxide (24%), lactose monohydrate (22%), macrogol 3000 (8%) and triacetin (6%).

Description:

Tablets 5 mg: round, biconvex tablets, covered with a film shell of white color with a bevel.

Type of tablet on a cross-section: white rough mass with a shell of white color.

Tablets 10 mg and 20 mg: oval, biconvex tablets, covered with a film shell of white color with a risk on one side.

Type of tablet on a cross-section: white rough mass with a shell of white color.

Pharmacotherapeutic group:antidepressant

ATX: & nbsp

N.06.A.B.10 Escitalopram

Pharmacodynamics:

Escitalopram is an antidepressant, a selective serotonin reuptake inhibitor (SSRI), increases the concentration of the neurotransmitter in the synaptic cleft by inhibiting the reverse neuronal capture of serotonin, enhances and prolongs the action of serotonin on postsynaptic receptors. Escitalopram practically does not possess or possesses a very weak affinity for a number of receptors, incl. serotonin: 5-HT_1A, 5-HT₂, dopamine: D₁ and D₂; alpha₁ and alpha₂ and beta-adrenoreceptors, H₁, histamine, m-holinoretseptora, benzodiazepine and opioid receptors, which causes the absence or weak expression of various anticholinergic, sedative, cardiovascular side effects. Escitalopram also does not bind or has very low affinity for various ion channels, including Na⁺, K⁺, Cl^-, Ca²⁺channels.

Pharmacokinetics:

Suction

Absorption does not depend on food intake. Time to reach the maximum concentration (TC_mOh), is about 4 hours after repeated use. Bioavailability - 80%.

Distribution

Apparent volume of distribution (V_{d, β}/ F) after ingestion is approximately 12-26 l / kg. The association of escitalopram and its major metabolites with plasma proteins below 80%. The kinetics of escitalopram are linear. The equilibrium concentration (Css) is achieved after 1 week, the average Css - 50 nmol / l (20 to 125 nmol / l) is achieved with a daily dose of 10 mg.

Metabolism

Metabolized in the liver to pharmacologically active metabolites (demethylated and didemethyl). The main substance and metabolites are partially deduced in the form of glucuronides. After repeated use, the average concentrations of demethylated and didemethylated metabolites are 28-31% and less than 5%, respectively,of the concentration of escitalopram. Metabolism of escitalopram and demethylated metabolite occurs with the dominant participation of the following cytochrome P450 isoenzymes: CYP2C19, CYP3A4 and CYP2D6.

Excretion

The half-life (T_1/2) after repeated use is about 30 hours. The clearance for oral administration is 0.6 l / min, of which 7% - Renal. The main metabolites of T_1/2considerably higher. 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_1/2 and AUC increases in elderly patients.

Special patient groups

Elderly age (over 65 years)

In elderly patients escitalopram is slower than in younger patients. The amount of escitalopram in the systemic circulation (AUC - area under the curve "concentration-time") in elderly patients is 50% more than in young people.

Dysfunction of the liver

In patients with hepatic insufficiency of Class A and B according to the Child-Pugh T classification_1/2 increases by 2 times.

Polymorphism (in individuals with low isoenzyme activity CYP2C19 or CYP2D6): in persons with low isoenzyme activity CYP2C19 the concentration of escitalopram can be 2 times higher than in persons with high activity of this isoenzyme.Significant changes in the concentration of escitalopram with a weak isoenzyme activity CYP2D6 is not observed.

Renal impairment

For racemic citalopram, a larger T_1/2 in patients with decreased renal function (KK 10-53 ml / min).

Indications:

Depression, panic disorder (including with agoraphobia).

Contraindications:

- Hypersensitivity to escitalopram and other components of the drug;

- simultaneous use with monoamine oxidase inhibitors (MAO);

- age under 18 years (effectiveness and safety not studied);

- pregnancy and the period of breastfeeding;

- simultaneous application with pimozide;

- galactosemia, lactase deficiency, glucose-galactose malabsorption syndrome.

Carefully:

Pharmacologically uncontrolled epilepsy, mania / hypomania history, diabetes, depression with suicidal attempts, advanced age, liver cirrhosis, chronic renal failure (creatinine clearance (CC) of less than 30 ml / min) and coronary heart disease (CHD), bleeding tendency ; simultaneous use of drugs that can cause hyponatremia, reducing the threshold of convulsive readiness, with anticoagulants or drugs,affecting platelet aggregation, with alcohol, with lithium, St. John's wort, with tryptophan, drugs metabolized with the participation of the isoenzyme system CYP2C19; with the simultaneous use of electroconvulsive therapy (ECT), age 18-24 years (due to the risk of developing suicidal behavior).

Pregnancy and lactation:

Elytseya® is not used in pregnancy (safety not established).

Due to escitalopram is secreted into breast milk, the use of the drug in the period of breastfeeding is not recommended. If it is necessary to use Elitsa® during lactation, breastfeeding should be discontinued.

Dosing and Administration:

Inside, 1 time per day, regardless of food intake.

Depressive episodes

The recommended dose is 10 mg per day.

Depending on the individual reaction of the patient, the dose can be increased to a maximum of 20 mg per day.

The antidepressant effect develops 2-4 weeks after the start of treatment. After the disappearance of the symptoms of depression should continue therapy for at least 6 months. to fix the effect obtained.

To stop therapy with escitalopram, it is necessary to gradually reduce the dose within 1-2 weeks in order to reduce the risk of developing the "withdrawal" syndrome.

Panic disorders (including with agoraphobia)

At 5 mg / day for the first week, then 10-20 mg / day.

The maximum daily dose is 20 mg.

The maximum therapeutic effect is achieved approximately 3 months after the start of treatment.

Elderly patients (over 65 years of age)

The recommended dose is 5 mg per day, the maximum daily dose is 10 mg per day.

Renal impairment

With a mild or moderate degree of renal failure (creatinine clearance (CK) of more than 30 ml / min), dose adjustment is not required;

With severe renal failure (QC less than 30 ml / min) - the drug should be administered with caution.

Impaired liver function

If the liver function is disturbed, the initial dose is 5 mg per day for 2 weeks. Depending on the individual reaction of the patient, the dose may be increased to 10 mg per day.

In severe violations of liver function, slower titration of doses is recommended.

Reduced isoenzyme activity CYP2C19

The recommended initial dose for the first 2 weeks is 5 mg per day, depending on the individual response of the patient, the dose can be increased to 10 mg per day.

Side effects:

Classification of the incidence of adverse events (WHO):

very often> 1/10

often from> 1/100 to <1/10

infrequently from> 1/1000 to <1/100

rarely from> 1/10000 to <1/1000

very rarely from <1/10000, including individual messages.

From the cardiovascular system: infrequently - tachycardia; rarely - bradycardia; very rarely - orthostatic hypotension.

On the part of the hematopoiesis system: very rarely - thrombocytopenia.

From the nervous system: often - insomnia, drowsiness, dizziness, paresthesia, tremor, anxiety, anxiety, nightmarish dreams; infrequently - a violation of taste, sleep disorders, fainting, gnashing of teeth, psychomotor agitation, akathisia, increased irritability, panic disorder, confusion; rarely - serotonin syndrome (agitation, tremor, myoclonus, hyperthermia), aggressiveness, depersonalization, hallucinations, suicidal thoughts and behavior; very rarely - dyskinesia, convulsive and manic disorders.

On the part of the respiratory system: often - sinusitis, yawning; infrequently - nosebleeds.

From the digestive system: very often - nausea; often - increased or decreased appetite, diarrhea, constipation,vomiting, dryness of the oral mucosa; infrequently - gastrointestinal bleeding (including rectal); very rarely - hepatitis;

From the genitourinary system: often - violations of ejaculation, impotence, decreased libido, anorgasmia (in women); rarely - metrorrhagia, menorrhagia; very rarely - urinary retention, priapism, galactorrhea.

From the sense organs: infrequently - mydriasis, vision disorders, tinnitus.

From the skin: often - increased sweating, alopecia; very rarely - ecchymosis.

From the side of the musculoskeletal system: often - arthralgia, myalgia.

From the endocrine system: very rarely - inadequate secretion of antidiuretic hormone (ADH), galactorrhea.

Allergic reactions: often - hives, skin rashes, skin itching; rarely - anaphylactic reactions, very rarely - angioedema (Quincke's edema).

Other: often - weakness, fever; rarely - swelling.

Laboratory indicators: often - weight gain; infrequently - weight loss; very rarely - hyponatremia, changes in laboratory parameters of liver function.

With a sharp withdrawal of the drug may develop a syndrome of "cancellation."

Overdose:

Symptoms: dizziness, tremor, agitation, drowsiness, serotonin syndrome, seizures, depression of consciousness of varying severity (especially in combination with alcohol and / or other CNS depressant drugs), nausea, vomiting, lowering blood pressure, tachycardia, ECG changes (change segment ST, T wave, expansion of the complex QRS, increasing the interval QT), arrhythmias, respiratory depression, metabolic acidosis, rhabdomyolysis, hypokalemia, hyponatremia.

Treatment: symptomatic and supportive: gastric lavage, reception of activated charcoal, provision of airway patency, adequate oxygenation, control of cardiovascular and respiratory systems. There is no specific antidote.

Interaction:

Simultaneous use with MAO-A inhibitors is contraindicated (risk of developing serotonin syndrome).

With simultaneous application from serotonergic drugs (tramadol, sumatriptan and other triptans), caution (risk of developing serotonin syndrome) should be observed. Doses of selegiline up to 10 mg per day were safely applied with racemic citalopram.

Contraindicated simultaneous use of escitalopram and pimozide.

Simultaneous use with drugs that reduce the threshold of convulsive readiness (tricyclic antidepressants, antipsychotics - derivatives of phenothiazine, thioxanthene, butyrophenone; mefloquine, bupropion and tramadol) increases the risk of seizures.

Escitalopram enhances the effect of drugs lithium, tryptophan.

Increases the toxicity of drugs St. John's wort perforated (Hypericum perforatum).

With the simultaneous use of escitalopram from indirect anticoagulants and drugs that affect platelet aggregation (atypical antipsychotics and typical antipsychotics - phenothiazine derivatives, most tricyclic antidepressants, acetylsalicylic acid and non-steroidal anti-inflammatory drugs (NSAIDs), ticlopidine and dipyridamiol) it is necessary to monitor the coagulation rates at the beginning of therapy and when it stops (the risk of bleeding).

It is not recommended simultaneous application of escitalopram and ethanol.

Pharmacokinetic interaction

Caution should be applied escitalopram simultaneously with inhibitors of the isoenzyme CYP2C19 (for example, omeprazole, esomeprazole, fluvoxamine, lansoprazole, ticlopidine) or cimetidine, t. the concentration of escitalopram in the blood plasma increases, in connection with which, it may be necessary to reduce the dose of escitalopram.

Caution should be exercised when concomitant use of escitalopram and drugs metabolized by the isoenzyme CYP2C19 and having a small therapeutic index, for example, flecainide, propafenone, metoprolol (with heart failure) or drugs, mainly metabolized by the isoenzyme CYP2C19 and acting on the central nervous system (CNS), for example antidepressants (desipramine, clomipramia, nortriptyline) or antipsychotics (risperidone, thioridazine, haloperidol). In these cases, a dose adjustment of these drugs may be required.

Simultaneous application from metoprolol or desipramine can lead to a twofold increase in the concentrations of the last two drugs.

Special instructions:

It is necessary to stop the use of Elitseya ® in case of development of convulsive disorders,epileptic seizures or their increase in pharmacologically uncontrolled epilepsy.

With the development of the manic state the drug Elitsea® should be canceled. Escitalopram can increase the concentration of glucose in the blood in diabetes mellitus, which may require correction of doses of oral hypoglycemic drugs and / or insulin.

Hyponatremia, associated with a decrease in secretion of adrenocorticotropic hormone (ADH), with the use of the drug Elytseya appears rarely (usually in elderly people, patients with cirrhosis of the liver, or constantly taking drugs that can cause hyponatremia) and usually disappears when the drug is withdrawn.

When developing serotonin syndrome the drug should be immediately withdrawn and symptomatic treatment is prescribed.

Caution should be applied escitalopram in patients with a history of mania / hypomania. With the development of the manic state escitalopram necessary cancel.

Malignant neuroleptic syndrome (CNS) - a rare, potentially dangerous condition associated with the use of antidepressants, including escitalopram.Symptoms of the ZNS: increased body temperature (hyperpyrexia), muscle rigidity, changes in mental status and instability of the autonomic nervous system (arrhythmia, fluctuations in blood pressure, tachycardia, profuse sweating, heart rhythm disturbance). When identifying the NSA, it is necessary to immediately stop the use of Elitsea®.

During the first two weeks, development is possible akathisia / psychomotor agitation (subjectively unpleasant or irritating anxiety and the need for movement, often in combination with the inability to sit or stand still).

When using Elitsea®, development is possible skin hemorrhages (ecchymosis and purpura). It is necessary to use caution escitalopram in patients with a tendency to bleeding, and also taking indirect anticoagulants and other drugs that affect blood coagulability.

Simultaneous use of escitaloprama and ethanol is not recommended.

Clinical experience electroconvulsive therapy (ECT) and escitalopram is limited, so caution is recommended.

The experience of using escitalopram is limited in patients with ischemic heart disease, therefore the preparation Elitseya® is recommended to be used with caution in this group of patients.

With the rapid withdrawal of escitalopram therapy, withdrawal syndrome: dizziness, sensory disturbances (including paresthesia), sleep disturbances (insomnia, unusual dreams), psychomotor agitation, anxiety, nausea and / or vomiting, tremor, confusion, sweating, headache, diarrhea, palpitations, emotional lability and visual impairment. The severity of these reactions is usually mild or moderate and duration is limited. In this regard, the preparation Elitsea ® is recommended to cancel gradually, reducing the dose for several weeks or months.

In children, adolescents and young people (under 24 years) with depression, other mental disorders, antidepressants, compared with placebo, increase the risk of suicidal thoughts and suicidal behavior. Therefore, when using escitalopram or any other antidepressants in children, adolescents and young people (younger than 24 years), the risk of suicide and the benefits of their use should be correlated. In short-term studies in people over 24 years of age, the risk of suicide did not increase, but in people older than 65 years, it declined slightly. Any depressive disorder in itself increases the risk of suicide.Therefore, during treatment with antidepressants, all patients should be monitored for early detection of abnormalities or behavioral changes, as well as suicidal tendencies.

Effect on the ability to drive transp. cf. and fur:

During the period of treatment, it is necessary to refrain from managing motor vehicles and engaging in potentially dangerous activities requiring an increased concentration of attention and speed of psychomotor reactions, in connection with the possibility of developing dizziness, hallucinations, confusion, depersonalization, and other side effects.

Form release / dosage:

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

Packaging:

When packing in Krka, dd, Novo mesto, Slovenia:

7 tablets per blister (contour mesh package) from the combined material OPA / Al / PVC and aluminum foil.

4 or 8 blisters (contour mesh packages) are placed in a cardboard pack together with instructions for use.

When packing on LLC "KRKA-RUS", Russia:

7 tablets in a contour mesh package from a combined material OPA/A1/PVC (polyamide / aluminum foil / polyvinyl chloride) and aluminum foil.

4 contour mesh packages together with instructions for use are placed in a pack of cardboard.

Storage conditions:

At temperatures not higher than 30 ° C, in the original packaging.

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:PL-000615

Date of registration:21.09.2011

Date of cancellation:2016-09-21

The owner of the registration certificate:KRKA-RUS, LLC KRKA-RUS, LLC Russia

Manufacturer: & nbsp

KRKA-RUS, LLC Russia

KRKA, d.d. Slovenia

Representation: & nbspKRKA KRKA Slovenia

Information update date: & nbsp04.10.2015

Illustrated instructions

Instructions

Elicea® (Elicea® )