ELICEA Q-TAB PILLS 10MG

Tradename

Elicea® Q-Tab®

International non-proprietary name

Escitalopram

Dosage Form

Tablets, dispersible in the mouth, 5 mg, 10 mg, 20 mg

Composition

One pill contains

active substance - escitalopram oxalate 6.3875 mg or 12.775 mg or 25.55 mg (equivalent to escitalopram 5 mg or 10 mg or 20 mg, respectively),

Excipients: potassium polacrilin, hydrochloric acid, concentrated, lactose monohydrate (dried spray), microcrystalline cellulose, sodium croscarmellose, potassium acesulfame, negesperidin-dihydrochalcone, peppermint flavoring, Magnesium stearate

Pharmacotherapeutic group

Psychoanaleptics. Antidepressants. Serotonin reuptake inhibitors are selective to escitalopram.

Pharmacological properties

Pharmacokinetics

Absorption

The drug is absorbed almost completely, regardless of the meal. With repeated ingestion, the time to reach the maximum plasma concentration (T max) is, on average, 4 hours. The absolute bioavailability of escitalopram after oral administration is comparable to racemic citalopram and reaches about 80%.

The apparent approximate volume of distribution after oral administration is about 12–26 L / kg.The binding of escitalopram and its major metabolites to plasma proteins is less than 80%.

Biotransformation

The biotransformation of escitalopram is carried out mainly in the liver, to active demethylated and dimethylated metabolites. In addition, nitrogen can be oxidized to form the N-oxide metabolite. Both the parent substance and the metabolites are partially excreted as glucuronides. After repeated use, the average concentration of demethyl and dimethylmetabolites is 28-31% and less than 5%, respectively, of the concentration of escitalopram. The biotransformation of escitalopram into the demethylated metabolite occurs mainly with the help of CYP2C19 isoenzymes. The participation of the enzymes CYP3A4 and CYP2D6 is also possible.

Removal

The half-life (T1 / 2) after taking a multiple dose is about 30 hours, the oral plasma clearance is 0.6 l / min. The half-life of the major metabolites is significantly long. ESCITALOPRAM and its main metabolites are excreted by the liver (metabolite) and most of it by the kidneys. Pharmacokinetics of the drug is linear and dose dependent. Stable plasma concentration is achieved after 1 week. Average stable concentrations of 50 nmol / l (from 20 to 125 nmol / l) are achieved when taking a daily dose of 10 mg.

Reduced kidney function

In patients with reduced renal function (creatinine clearance (CK) 10-53 ml / min) - a longer T1 / 2 and a weak increase in the concentration of racemic citalopram. Plasma concentrations of metabolites have not been studied, but they may be elevated.

Reduced liver function

In patients with mild to moderate hepatic insufficiency (in patients with cirrhosis of the liver with syndrome of portal hypertension, criteria A and B), T1 / 2 of escitalopram is twice as long and the concentration is 60% higher than in patients with normal liver function.

Elderly patients (over 65)

In elderly patients, escitalopram is more slowly excreted compared with young patients. Systemic exposure (AUC) is approximately 50% higher in elderly patients compared with younger patients.

Polymorphism

It is noted that relative to the CYP2C19 enzyme, the slow metabolisers have a two-fold higher concentration of escitalopram in blood plasma than in fast-metabolisers. With respect to the CYP2D6 enzyme, there were no significant changes in the concentration of slow metabolizers.

Pharmacodynamics

Mechanism of action

Escitalopram is a selective serotonin reuptake inhibitor (5-HT) with a high ability to bind to the primary binding site. It also binds to the allosteric site, while having a binding capacity of 1000 times less.

Escitalopram has no or very little ability to bind to a number of receptors, including: serotonin 5-HT1A, 5-HT2 receptors, dopamine DA D1 and D2 receptors, α1, α2, β-adrenergic receptors, histamine H1 receptors, muscarinic cholinergic receptors, benzodiazepine and opioid receptors.

Inhibition of serotonin 5-HT reuptake is a typical mechanism of action explaining the pharmacological and clinical action of escitalopram.

Indications for use

- depressive episodes of any degree

- panic disorder with or without agoraphobia

- social anxiety disorders (social phobia)

- generalized anxiety disorders

- obsessive compulsive disorders

Dosage and administration

Safety of daily doses above 20 mg has not been established. Elicea® Q-Tab® pills are taken once a day, regardless of the meal.

Depressive episodes of severe

The usual dosage is 10 mg once daily. Depending on the patient's individual response, the dose may be increased to a maximum of 20 mg per day.

An antidepressant effect usually takes 2 to 4 weeks to obtain. After the disappearance of the symptoms of depression, it is necessary to continue treatment for at least 6 months to consolidate the effect obtained.

Panic disorders with or without agoraphobia

During the first week of treatment, a dose of 5 mg per day is recommended, followed by an increase to 10 mg per day. Depending on the patient's individual response, the dose may be increased to a maximum of 20 mg / day.

The maximum therapeutic effect is achieved 3 months after the start of treatment. Therapy lasts for several months.

Social anxiety disorders

The usual dosage is 10 mg per day. It usually takes 2 to 4 weeks to alleviate the symptoms of the disease. Subsequently, depending on the individual response of the patient, the dose may be reduced to 5 mg or increased to a maximum of 20 mg per day.

Socio-anxiety disorder is a disease with a chronic course, therefore, in order to consolidate the result, it is recommended to continue therapy for 12 weeks. Prolonged treatment of respondents was investigated within 6 months, treatment can be administered individually to prevent relapse; Periodically, the benefits of therapy should be re-evaluated.

Anxiety disorder is a well-defined diagnostic terminology for an individual disorder, which should not be confused with excessive shyness. Pharmacotherapy is indicated only when this disorder has a significant impact on professional and social activities.

The place of this therapy in comparison with cognitive-behavioral therapy is not defined.

Pharmacotherapy is part of an overall therapeutic strategy.

Generalized anxiety disorders

The initial dose is 10 mg per day. Depending on the individual response of the patient, the dose may be increased by the domaximal - 20 mg per day.

Long-term therapy of respondents was investigated for at least 6 months in patients receiving 20 mg per day. Periodically, the benefits of therapy and dosage should be re-evaluated.

Obsessive compulsive disorder (OCD)

The initial dose is 10 mg per day. Depending on the individual response of the patient, the dose may be increased to a maximum of 20 mg per day.

Since OCD is a chronic disease, patients should receive treatment for a sufficient period of time to ensure elimination of the symptom. Periodically, the benefits of therapy and dosage should be re-evaluated.

Elderly patients (over 65)

The initial dose is 5 mg per day. Depending on the individual response of the patient, the dose may be increased to 10 mg per day. The efficacy of Elicea® Cu-Tab® for the treatment of social anxiety disorders in the elderly has not been studied.

Use in patients with renal failure

In patients with mild to moderate renal insufficiency, individual dose selection is not required. Care should be taken when prescribing in patients with severe renal failure (CC below 30 ml / min).

Use in patients with liver failure

In patients with mild or moderate liver failure in the first two weeks of treatment, the recommended initial daily dose is 5 mg per day. Depending on the individual response of the patient, the dose may be increased to 10 mg per day. Caution should be exercised when prescribing in patients with severe liver failure.

Slow cytochrome CYP2C19 metabolizers

In patients characterized by a low metabolic rate towards CYP2C19 cytochrome, the initial recommended dose in the first two weeks of therapy is 5 mg per day.

Depending on the individual response of the patient, the dose may be increased to 10 mg per day.

Withdrawal symptom when discontinuing therapy

It is necessary to avoid abrupt discontinuation of therapy with Elicea® K-Tab®. When discontinuing therapy, the dose should be reduced gradually over a period of one to two weeks in order to avoid the risk of a symptom of termination. In the event of intolerable symptoms after reducing the dose or discontinuing therapy, it is possible to resume treatment with prescribed doses of the drug. Therefore, the attending physician may continue to reduce the dosage, but with a less dramatic reduction.

Mode of application

The pills Elycea® KU-TAB® is prescribed as a single daily dose and should be taken without food. The pill should be placed on the tongue, where it dissolves quickly and is swallowed with saliva. The resorption pill is quite fragile, so care should be taken to handle it. The pill does not have a fracture line and cannot be divided into equal halves.

A resorption pill is the preferred dosage form for patients who have difficulty swallowing conventional pills or in situations where there is no liquid.

The drug Elyceya® Ku-Tab® in pills for resorption is bioequivalent to escitalopram in coated pills with the same speed and extent of absorption. It has the same dose and frequency of use as escitalopram in coated tablets.Escitalopram lozenges can be used as an alternative to Escitalopram in coated tablets.

Side effects

Adverse reactions often occur in the first or second week of treatment and then become less intense, and their frequency decreases with further treatment.

Very often (≥ 1/10):

- headache

- nausea

Often (≥ 1/100, <1/10):

• decrease in appetite, increase in appetite, increase in body weight
• fear, anxiety, abnormal dreams, women and men: decreased libido, women: anorgasmia
• insomnia, drowsiness, dizziness, paresthesias, tremor
• sinusitis, yawning
• diarrhea, constipation, vomiting, dry mouth
• increased sweating
• arthralgia, myalgia
• men: ejaculatory disorders, impotence
• fatigue, fever

Not often (≥ 1/1000, ≤ 1/100):

• weight loss
• bruxism, agitation, nervousness, panic attacks, confusion
• taste disturbance, sleep disturbance, syncope
• mydriasis, visual impairment
• tinnitus
• tachycardia
• nosebleeds
• Gastrointestinal bleeding (including rectal bleeding)
• urticaria, alopecia, rash, itching
• women: uterine bleeding, menorrhagia
• edema