Ingavirin, capsules 60 mg 10 pcs

An antiviral agent. Anti-inflammatory agent.

TAC code: [J05AX].

Pharmacological properties

Pharmacodynamics

Antiviral drug.

In preclinical and clinical studies showed the effectiveness of Ingavirin^® against influenza viruses of type A (A(H1N1), including pandemic A(H1N1)pdm09 (“swine”), A(H3N2), A(H5N1)) and type B, adenovirus, parainfluenza virus, respiratory syncytial virus; in preclinical studies: coronavirus, metapneumovirus, enteroviruses, including coxsackievirus and rhinovirus.

Ingavirin^® reduces the viral load, accelerates viral elimination, reduces the duration of the disease and reduces the risk of complications.

The mechanism of action is realized at the level of infected cells through activation of innate immunity factors that are suppressed by viral proteins. In particular it was shown in experimental studies that Ingavirin ^® increases expression of the interferon receptor of the first type IFNAR on the surface of epithelial and immunocompetent cells. Increased density of interferon receptors leads to increased sensitivity of cells to signals of endogenous interferon.

The process is accompanied by activation (phosphorylation) of protein-transmitter STAT1, transmitting a signal to the cell nucleus for induction of synthesis of antiviral genes. It was shown that under the conditions of infection the preparation activates synthesis of antiviral effector protein MxA (early antiviral response factor inhibiting intracellular transport of ribonucleoprotein complexes of various viruses) and phosphorylated form of PKR inhibiting translation of viral proteins, thus slowing down and stopping the process of viral reproduction.

The action of the preparation Ingavirin^® consists in significant decrease of symptoms of cytopathic and cytodestructive action of the virus, decrease of number of infected cells, restriction of pathological process, normalization of composition and structure of cells and morphological pattern of tissues in the zone of infection both at early and late stages of the process.

The anti-inflammatory activity is caused by suppression of production of key pro-inflammatory cytokines (tumor necrosis factor (TNF-α), interleukins (IL-1β and IL-6) and decrease of myeloperoxidase activity.

In experimental studies it is shown that combined use of Ingavirin^® with antibiotics improves the effectiveness of therapy in models of bacterial sepsis including that caused by penicillin-resistant strains of Staphylococcus aureus.

The experimental toxicological studies conducted indicate a low level of toxicity and a high safety profile of the drug.

According to the parameters of acute toxicity the drug Ingavirin^® belongs to the 4th class of toxicity – “Low-toxic substances” (when determining LD₅₀ in acute toxicity experiments lethal doses of the drug could not be determined).

The drug has no mutagenic, immunotoxic, allergic and carcinogenic properties, it has no local irritant effect. The drug Ingavirin^® has no effect on reproductive function, does not have embryotoxic and teratogenic effects.

There is no effect of the drug Ingavirin^® on the hematopoietic system when the age-appropriate dose is taken with the recommended regimen and course.

Pharmacokinetics

Intake and distribution.

In an experiment using radioactive labeling it was found that the drug quickly enters the blood from the gastrointestinal tract, distributing to internal organs. Maximal concentrations in blood, plasma and most organs are reached 30 minutes after drug administration. The AUC values (area under the pharmacokinetic curve “concentration – time”) of kidney, liver and lung are slightly higher than AUC in blood (43.77 µg.h/g). The AUC values for the spleen, adrenal glands, lymph nodes and thymus are lower than the blood AUC. MRT (mean drug retention time) in blood is 37.2 hours.

When taking the drug once a day, it accumulates in the internal organs and tissues. At that qualitative characteristics of pharmacokinetic curves after each administration of the drug are identical: rapid increase of the drug concentration after each administration 0.5-1 hour after administration and then slow decrease by 24 hours.

Metabolism.

The drug is not metabolized in the body and is excreted unchanged.

Extracted.

The main process of excretion occurs within 24 hours. During this period, 80% of the dose taken is eliminated: 34.8% is eliminated in the time interval from 0 to 5 hours, and 45.2% in the time interval from 5 to 24 hours. Of these, 77% are excreted through the intestines and 23% through the kidneys.

Indications

Treatment of influenza A and B and other acute respiratory viral infections (adenoviral infection, parainfluenza, respiratory syncytial infection, rhinovirus infection) in children from 7 to 17 years old.

Prevention of influenza A and B and other acute respiratory viral infections in children from 7 to 17 years old.

Pharmacological effect

Antiviral agent. Anti-inflammatory agent.

ATX code: [J05AX].

Pharmacological properties

Pharmacodynamics

Antiviral drug.

Preclinical and clinical studies have shown the effectiveness of the drug Ingavirin® against influenza viruses type A (A(H1N1), including pandemic strain A(H1N1)pdm09 (“swine”), A(H3N2), A(H5N1)) and type B, adenovirus, parainfluenza virus, respiratory syncytial virus; in preclinical studies: coronavirus, metapneumovirus, enteroviruses, including Coxsackie virus and rhinovirus.

Ingavirin® reduces the viral load, accelerates the elimination of viruses, shortens the duration of the disease, and reduces the risk of complications.

The mechanism of action is realized at the level of infected cells due to the activation of innate immune factors suppressed by viral proteins. In experimental studies, in particular, it was shown that the drug Ingavirin® increases the expression of the first type interferon receptor IFNAR on the surface of epithelial and immunocompetent cells. An increase in the density of interferon receptors leads to an increase in the sensitivity of cells to endogenous interferon signals.

The process is accompanied by activation (phosphorylation) of the transmitter protein STAT1, which transmits a signal to the cell nucleus to induce the synthesis of antiviral genes. It has been shown that under conditions of infection, the drug activates the synthesis of the antiviral effector protein MxA (an early factor of the antiviral response that inhibits the intracellular transport of ribonucleoprotein complexes of various viruses) and the phosphorylated form of PKR, which suppresses the translation of viral proteins, thus slowing down and stopping the process of viral reproduction.

The effect of the drug Ingavirin® is to significantly reduce the signs of the cytopathic and cytodestructive effects of the virus, reduce the number of infected cells, limit the pathological process, normalize the composition and structure of cells and the morphological picture of tissues in the area of ​​the infectious process, both in its early and late stages.

The anti-inflammatory effect is due to the suppression of the production of key pro-inflammatory cytokines (tumor necrosis factor (TNF-α), interleukins (IL-1β and IL-6)), and a decrease in the activity of myeloperoxidase.

Experimental studies have shown that the combined use of the drug Ingavirin® with antibiotics increases the effectiveness of therapy in a model of bacterial sepsis, including that caused by penicillin-resistant strains of staphylococcus.

Experimental toxicological studies conducted indicate a low level of toxicity and a high safety profile of the drug.

According to the parameters of acute toxicity, the drug Ingavirin® belongs to toxicity class 4 – “Low toxic substances” (when determining LD50 in acute toxicity experiments, lethal doses of the drug could not be determined).

The drug does not have mutagenic, immunotoxic, allergenic or carcinogenic properties, and does not have a local irritant effect. The drug Ingavirin® does not affect reproductive function and does not have embryotoxic or teratogenic effects.

There is no effect of the drug Ingavirin® on the hematopoietic system when taking an age-appropriate dose in the recommended regimen and course.

Pharmacokinetics

Absorption and distribution.

An experiment using a radioactive label established that the drug quickly enters the blood from the gastrointestinal tract, distributing throughout the internal organs. Maximum concentrations in the blood, blood plasma and most organs are reached 30 minutes after administration of the drug. The AUC values ​​(area under the pharmacokinetic concentration-time curve) of the kidneys, liver and lungs are slightly higher than the AUC of blood (43.77 mcg.h/g). AUC values ​​for the spleen, adrenal glands, lymph nodes and thymus are lower than blood AUC. MRT (mean drug retention time) in the blood is 37.2 hours.

When taking a course of the drug once a day, it accumulates in internal organs and tissues. At the same time, the qualitative characteristics of the pharmacokinetic curves after each administration of the drug are identical: a rapid increase in the concentration of the drug after each administration 0.5-1 hour after administration and then a slow decrease by 24 hours.

Metabolism.

The drug is not metabolized in the body and is excreted unchanged.

Excretion.

The main elimination process occurs within 24 hours. During this period, 80% of the dose taken is excreted: 34.8% is excreted in the time interval from 0 to 5 hours and 45.2% in the time interval from 5 to 24 hours. Of these, 77% is excreted through the intestines and 23% through the kidneys.

Special instructions

It is not recommended to take other antiviral drugs at the same time without first consulting a doctor.

Save the instructions. It may be needed again. If you have any questions, consult your doctor.

Active ingredient

Pentanedioic acid imidazolylethanamide

Composition

One capsule contains:

active substance:

Pentanedioic acid imidazolylethanamide (vitaglutam) calculated as 100% substance – 60.00 mg;

excipients: lactose monohydrate, potato starch, colloidal silicon dioxide (aerosil), magnesium stearate;

hard gelatin capsules: titanium dioxide E 171, iron dye yellow oxide E 172, gelatin;

ink composition for the logo: shellac, propylene glycol E 1520, titanium dioxide E 171.

Pregnancy

The use of the drug during pregnancy has not been studied. The use of the drug during lactation has not been studied, therefore, if it is necessary to use the drug during lactation, breastfeeding should be stopped.

Contraindications

Hypersensitivity to the active substance or any other component of the drug.

Lactase deficiency, lactose intolerance, glucose-galactose malabsorption.

Pregnancy.

Breastfeeding period.

Children’s age up to 7 years.

This dosage form is not intended for use in persons 18 years of age and older (it is necessary to use dosage forms that provide the possibility of taking the drug Ingavirin® at a dose of 90 mg).

Side Effects

Allergic reactions (rare).

Interaction

Medicinal
the interaction of the drug Ingavirin® has not been described.

Overdose

About cases
an overdose of the drug Ingavirin® has not been reported to date.

Storage conditions

In a dry place, protected from light and out of reach of children, at a temperature not exceeding 25°C.

Shelf life

3 years. Do not use after the expiration date stated on the package.

Manufacturer

Valenta Pharm JSC, Russia