Influcein, capsules 75 mg 10 pcs

Antiviral agent. It is a prodrug, the active metabolite (oseltamivir carboxylate) of which selectively inhibits neuraminidase of influenza virus types A and B.

The neuraminidase is a glycoprotein which catalyzes the cleavage of the bond between the terminal sialic acid and sugar, thus contributing to the spread of the virus in the respiratory tract (virions exit from the infected cell and penetrate into the cells of the respiratory epithelium, preventing inactivation of the virus by the epithelial mucus).

Oseltamivir carboxylate acts outside the cells and competitively inhibits neuraminidase of the virus.

Inhibits influenza virus growth in vitro and suppresses viral replication and pathogenicity in vivo.

Reduces excretion of influenza A and B viruses from the body.

It does not affect the production of antibodies in response to the administration of inactivated influenza vaccine.

The resistance rate of clinical virus isolates is 2%.

Indications

Active ingredient

Composition

Associates:

calcium hydrophosphate – 25 mg,

corn starch pregelatinized – 46.3 mg,

croscarmellose sodium – 7.2 mg,

sodium stearyl fumarate – 1.5 mg,

talc – 1.5 mg.

Capsule body composition:

gelatin – 45.2956 mg, titanium dioxide – 0.9244 mg;

Capsule cap composition:

gelatin – 29.1077 mg, titanium dioxide – 0.3971 mg, quinoline yellow dye – 0.2739 mg, sunset yellow dye – 0.0013 mg.

Interaction

Directions for use

Special Instructions

Use with caution in children.

The safety and efficacy of oseltamivir have not been established in patients with hepatic impairment.

There are no data on the safety of oseltamivir in patients with a CK of less than 10 ml/min.

Synopsis

Features

After oral administration it is almost completely absorbed from the gastrointestinal tract, absorption does not depend on food intake. It has a “first pass” effect through the liver. Under the action of intestinal and hepatic esterases it is converted to the active metabolite. 75% of the dose taken orally enters systemic bloodstream as an active metabolite, less than 5% – as the parent substance. Plasma concentrations of both prodrug and active metabolite are proportional to dose.

The average Vd of the active metabolite is 23 l. Binding to plasma proteins is 3%.

Extracted as an active metabolite mainly by the kidneys by glomerular filtration and tubular secretion. T1/2 oseltamivir is 1-3 hours. Oseltamivir carboxylate is not further metabolized and excreted by the kidneys, its T1/2 is 6-10 h. Renal clearance is 18.8 l/h. Excreted through the intestine is less than 20%.

In elderly patients (65-78 years) the concentration of the active metabolite in equilibrium is 25-35% higher than in younger patients. In patients with renal insufficiency the excretion rate of oseltamivir carboxylate is inversely proportional to the CK value.

Contraindications

Side effects

Digestive system disorders: nausea, vomiting (usually when taken in high doses, or in the first days of treatment); rarely – diarrhea, abdominal pain.

CNS disorders: insomnia, dizziness, headache.

Respiratory system disorders: nasal congestion, sore throat, cough.

Others: feeling of fatigue, weakness.

Similarities