Escitam Asino (escitalopram) coated tablets 10 mg. №60

Description

Escitam Asino Composition
active substance: escitalopram;

1 tablet contains escitalopram oxalate (12.775 mg 25.55 mg) in terms of escitalopram 10 mg;

excipients: microcrystalline cellulose, croscarmellose sodium, hydroxypropyl methylcellulose (hypromellose), colloidal silicon dioxide, talc, magnesium stearate

casing Opadry II White: polyvinyl alcohol, titanium dioxide (E 171), polyethylene glycol (macrogol), talc.

Escitam Asino Dosage form
Film-coated tablets.

Basic physical and chemical properties:

tablets 10 mg tablets of a round shape with a biconvex surface, film-coated white, with a notch.

Pharmacotherapeutic group
Antidepressants. Selective serotonin reuptake inhibitors (SSRIs). ATX code N06A B10.

Pharmacodynamics
Escitalopram is an antidepressant, selective serotonin reuptake inhibitor, which leads to the clinical and pharmacological effects of the drug. It has a high affinity for the main binder and the adjacent allosteric serotonin transporter element and has no or very weak ability to bind to a number of receptors, including serotonin 5-HT1A-, 5-HT2-receptors, dopamine D1- and D2-receptors , α1-, α2-, β-adrenergic receptors, histamine H1-, M-cholinergic receptors, benzodiazepine and opiate receptors.

Escitalopram is the S-enantiomer of racemic citalopram with its own therapeutic activity. It has been proven that the R-enantiomer is not inert, but counteracts the serotonergic properties and the corresponding pharmacological effects of the S-enantiomer.

Pharmacokinetics
Absorption is almost complete and does not depend on food intake. The maximum concentration in blood plasma is reached 4 hours after administration. The bioavailability of escitalopram is approximately 80%. The apparent volume of distribution (Vd, β / F) after oral administration is 12 to 26 l / kg.

The binding of escitalopram and its main metabolites with blood proteins is less than 80%.

In the liver, metabolites are formed, demethylated and didemethylated and are pharmacologically active. Nitrogen can also be oxidized to an N-oxide metabolite.

Both the metabolites and the parent compound are partially excreted in the form of glucuronides.

After repeated use, the average concentration of demethyl- and didemethylmetabolite is usually 28-31% and <5% of the escitalopram concentration, respectively. The metabolism of escitalopram to the demethylated metabolite occurs primarily via cytochrome CYP2C19. Possible insignificant participation in the process of isoenzymes CYP3A4 and CYP2D6. The half-life (T1 / 2) of the drug is approximately 30 hours. Clearance (Cloral) for oral administration is approximately 0.6 L / min. In major metabolites, the elimination half-life is longer. Escitalopram and its major metabolites are excreted by the liver (metabolic pathway) and kidneys. Most of the dose is excreted in the urine as metabolites. The kinetics of escitalopram is linear. Equilibrium concentration is reached after 1 week. The average equilibrium concentration of 50 nmol / L (from 20 to 125 nmol / L) is achieved with a daily dose of 10 mg.

In elderly patients (from 65 years), escitalopram is excreted more slowly than in young patients. Systemic exposure (AUC) in the elderly is 50% higher than in young healthy volunteers.

In patients with mild to moderate hepatic impairment (Child-Pugh grades A and B), the elimination half-life was twice as long and the exposure was 60% higher than in those with normal liver function.

In patients with impaired renal function (CLcr 10-53 ml / min), when using racemic citalopram, a long half-life and slightly higher exposure were observed. The concentration of metabolites in plasma has not been studied, but may be elevated.

Patients with weak metabolic CYP2C19 function had twice the plasma concentration of escitalopram than patients with normal CYP2C19 function. There were no significant changes in exposure with reduced CYP2D6 function.

Escitam Asino Indications
Treatment of major depressive episodes, panic disorders with or without agoraphobia, social anxiety disorders (social phobia), generalized anxiety disorders, obsessive-compulsive disorder.

Contraindications
Hypersensitivity to escitalopram or other components of the drug, simultaneous treatment with non-selective irreversible MAO inhibitors (MAO inhibitors) or pimozide.