$51.20
Manufacturer: Ukraine
Treatment of major depressive episodes, panic disorders with or without agoraphobia, social anxiety disorders (social phobia), generalized anxiety disorders, obsessive-compulsive disorders.
Description
Escitam Storage
active substance: escitalopram;
1 tablet contains escitalopram hydrogen oxalate 12,775 mg or 25,550 mg in terms of 10 mg or 20 mg of escitalopram;
excipients: microcrystalline cellulose, croscarmellose sodium, talc, magnesium stearate, colloidal anhydrous silica;
mixture for film coating: hypromellose, titanium dioxide (E 171), polyethylene glycol 400 (macrogol 400).
Escitam Dosage form
Film-coated tablets.
Basic physical and chemical properties:
oval tablets, coated with a white film, with engraving “E9CM” on one side, a dash and engraving “10” on the other side (figure on both sides of the dash);
oval tablets, coated with a white film, with engraving “E9CM” on one side, a dash and engraving “20” on the other side (figure on both sides of the dash).
Pharmacotherapeutic group
Antidepressants. ATX code N06A B10.
Pharmacological properties
Pharmacodynamics.
Escitalopram is an antidepressant, a selective serotonin reuptake inhibitor, which determines the clinical and pharmacological effects of the drug. It has a high affinity for the main binding element and the adjacent allosteric element of the serotonin transporter 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-cholinoreceptors, benzodiazepines and opiate receptors. Escitalopram is the S-enantiomer of racemic citalopram with its own therapeutic activity. It is proved 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 in 4 hours after reception. 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 major metabolites to blood proteins is at least 80%.
Metabolism occurs in the liver to form demethylated and didemethylated metabolites. Both are pharmacologically active. Nitrogen can also be oxidized to the N-oxide metabolite. Both the metabolites and the parent compound are partially excreted as glucuronides. After repeated administration, the mean concentration of demethyl and didemethyl metabolites is usually 28–31% and <5% of the escitalopram concentration, respectively.
The biotransformation of escitalopram to the demethylated metabolite is via cytochrome CYP2C19. Insignificant participation in the process of isoenzymes CYP3A4 and CYP2D6 is possible. The half-life (T1 / 2) of the drug is approximately 30 hours. Clearance (Cloral) when taken orally is approximately 0.6 l / min
In major metabolites, the half-life is longer. Escitalopram and its major metabolites are excreted through the liver (metabolic pathway) and kidneys.
Most of the dose is excreted as metabolites in the urine. The kinetics of escitalopram are linear. Equilibrium concentration is reached in about 1 week. The average equilibrium concentration of 50 nmol / l (from 20 to 125 nmol / l) is reached at a daily dose of 10 mg. In elderly patients (over 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. Patients with mild or moderate hepatic impairment (Child-Pugh classes A and B) had twice the half-life and 60% longer exposures than those with normal hepatic function.
Patients with renal impairment (CLcr 10-53 ml / min) had a longer half-life and slightly higher exposure with racemic citalopram.
Plasma metabolites have not been studied but may be elevated.
Patients with poor CYP2C19 metabolic function had twice the plasma concentrations of escitalopram than patients with normal CYP2C19 function.
No significant changes in exposure with reduced CYP2D6 function were observed.
Escitam Indication
Treatment of major depressive episodes, panic disorders with or without agoraphobia, social anxiety disorders (social phobia), generalized anxiety disorders, obsessive-compulsive disorders.
Contraindication
Hypersensitivity to escitalopram or to other components of the drug; concomitant treatment with non-selective irreversible monoamine oxidase inhibitors (MAO inhibitors) is contraindicated due to the risk of developing serotonin syndrome with agitation, tremor, hyperthermia, etc. (see section “Interaction with other medicinal products and other forms of interaction”); combination of escitalopram with reversible MAO-A inhibitors (eg moclobemide) or reversible non-selective MAO inhibitor linezolid is contraindicated due to the risk of serotonin syndrome (see section “Interaction with other medicinal products”).
Recent Reviews