Fevarin (fluvoxamine) coated tablets 100 mg. №15

Description

Fevarin Storage
active substance: fluvoxamine;

1 tablet contains fluvoxamine maleate 50 mg or 100 mg;

Excipients: mannitol (E 421), corn starch, pregelatinized starch, sodium stearyl fumarate, colloidal anhydrous silica, hypromellose, macrogol 6000, talc, titanium dioxide (E 171).

Fevarin Dosage form
Film-coated tablets.

Fevarin Basic physical and chemical properties:

film-coated tablets, 50 mg: round, convex on both sides, white or almost white, film-coated, on one side – with a notch and marked “291” on both sides of it; diameter – about 9 mm; the tablet can be divided into two equal parts.

film-coated tablets, 100 mg: oval, convex on both sides, white or almost white, film-coated, on the one hand – with a notch and marked “313” on both sides of it; length – about 15 mm, width – about 8 mm; the tablet can be divided into two equal parts.

Pharmacotherapeutic group
Antidepressants. Selective serotonin reuptake inhibitors. ATX code N06A B08.

Pharmacological properties

Pharmacodynamics.

Receptor binding studies have shown that fluvoxamine is a potent serotonin reuptake inhibitor in both vitro and in vivo and has minimal affinity for serotonin receptor subtypes. The drug has little ability to bind to α-adrenergic, ß-adrenergic, histaminergic, muscarinic, cholinergic or dopaminergic receptors.

Fluvoxamine has a high affinity for sigma-1 receptors, for which it acts as an agonist at therapeutic doses.

Pharmacokinetics.

Absorption.

Fluvoxamine is completely absorbed after oral administration. The maximum concentration in plasma is reached in 3 – 8 hours after reception. Due to the first-pass mechanism, the average absolute bioavailability is 53%.

The pharmacokinetics of Fevarin® are not affected by concomitant meals.

Distribution.

In vitro, 80% of fluvoxamine is bound to plasma proteins. The volume of distribution in humans is 25 l / kg.

Metabolism.

Fluvoxamine is extensively metabolized in the liver. Although in vitro the major isoenzyme involved in fluvoxamine metabolism is CYP2D6, plasma concentrations in individuals with reduced CYP2D6 activity are not much higher than in those with good metabolism.

The mean plasma half-life is approximately 13 to 15 hours after a single dose and is slightly prolonged (17 to 22 hours) with multiple doses. Equilibrium plasma concentrations are usually reached within 10 to 14 days.

Fluvoxamine is extensively transformed in the liver, mainly by oxidative dimethylation, resulting in the formation of at least nine metabolites that are excreted by the kidneys. The two main metabolites show little pharmacological activity. Other metabolites are pharmacologically inactive. Fluvoxamine is a potent inhibitor of CYP1A2 and CYP2C19, moderately inhibiting CYP2C9, CYP2D6 and CYP3A4.

Fluvoxamine demonstrates linear pharmacokinetics at a single dose. Equilibrium plasma concentrations are higher than those calculated for a single dose, and this disproportionate increase is most pronounced at higher daily doses.

Special groups of patients.

The pharmacokinetics of fluvoxamine are the same in healthy adults, the elderly and patients with renal insufficiency. Fluvoxamine metabolism is impaired in patients with liver disease.

Equilibrium plasma concentrations of fluvoxamine are twice as high in children aged 6 to 11 years as in children aged 12 to 17 years. Plasma concentrations in children aged 12 to 17 years are the same as in adults.

Indication

Depression
Obsessive-compulsive disorder (OCD).

Contraindication
The drug is contraindicated in patients with hypersensitivity to fluvoxamine maleate or to any of the other components of the drug.

Do not prescribe concomitantly with tizanidine, monoamine oxidase inhibitors (MAOIs) (see sections “Interaction with other medicinal products and other forms of interaction” and “Features of use”). Fevarin® treatment can be started no earlier than two weeks after discontinuation of reversible MAOIs or the day after discontinuation of reversible MAOIs (eg moclobemide, linezolid).

Treatment with any of the MAOIs can be started no earlier than one week after stopping Fevarin®.

Fevarin® should not be used concomitantly with pimozide and ramelteon (see sections “Interaction with other medicinal products and other forms of interaction”).