Imidazoliletanamid pentandiovoy acid
When ATH: J05AX
Pharmacological action
Viricide. It is active against influenza A and influenza B, adenoviral infection.
In experiments in vitro and in vivo effectively suppresses reproduction and cytopathic effect of the virus of influenza A and influenza B, Adenovirus. The antiviral mechanism of action caused by the suppression of viral reproduction at step Nuclear phase, delayed migration of newly synthesized NP virus from the cytoplasm to the nucleus.
It has a modulating effect on the functional activity of interferon: It causes an increase in the content of interferon in the blood to physiological norms, It stimulates and normalizes the reduced α-interferonprodutsiruyuschuyu ability of white blood cells, It stimulates γ-interferonprodutsiruyuschuyu ability of white blood cells.
It causes the generation of cytotoxic lymphocytes, and increases the content of NK T-lymphocytes, possessing high killer activity against virus-transformed cells and a pronounced antiviral activity.
The anti-inflammatory effect is due to inhibition of the production of key proinflammatory cytokines (FNOα, ИЛ-1b и ИЛ-6), reduction of myeloperoxidase activity.
The therapeutic efficacy of the flu is manifested in shortening the period of fever, reduction intoxication (headache, weakness, dizziness), catarrhal symptoms, reducing the number of complications and duration of the disease.
Pharmacokinetics
Absorption and distribution
When used in the recommended doses definition plasma drug available methods it is not possible.
In experimental studies using radioactive label was established, that the drug rapidly enters the blood from the gastrointestinal tract and is distributed evenly over the internal organs.
Cmax in blood, blood plasma and most organs are achieved through 30 minutes after administration. AUC values kidney, liver and lungs slightly higher than AUC blood (43.77 g × h / g). AUC values spleen, adrenal, lymph nodes and thymus enlarge blood AUC. The average retention time of the drug in the blood – 37.2 no.
At 5-day course of oral administration 1 time / day is its accumulation in internal organs and tissues. Moreover the qualitative characteristics of pharmacokinetic curves after each injection were identical: a rapid increase of drug concentration following each administration and then slowly fall to 24 sometimes.
Metabolism and excretion
Do not metabolized in the body and is excreted unchanged in.
The basic process excretion occurs within 24 no. During this time the output 80% dose. For the first 5 h output 34.8%, in the following hours – 45.2%. Of those displayed in the feces 77%, urine – 23%.
Testimony
It has antiviral effects, effective against influenza viruses A and B, adenoviral infection. In the experiment, in vitro and live effectively suppresses reproduction and cytopathic effect of influenza viruses A and B, Adenovirus. The antiviral mechanism of action - inhibition of viral replication at the stage of nuclear phase, delay migration of newly synthesized viral NP from the cytoplasm to the nucleus.
It has a modulating effect on the functional activity of interferon: It causes an increase in the content of interferon in the blood to physiological norms, It stimulates and normalizes the reduced α-interferonprodutsiruyuschuyu ability of white blood cells, стимулирует c- interferonprodutsiruyuschuyu ability of white blood cells.
It causes the generation of cytotoxic lymphocytes, and increases the content of NK-T-cells, possessing high killer activity against virus-transformed cells and a pronounced antiviral activity.
The anti-inflammatory effect is due to inhibition of the production of key proinflammatory cytokines (TNF-a, IL-1β and IL-6), reduction of myeloperoxidase activity.
The therapeutic efficacy of the flu is manifested in shortening the period of fever, reduction intoxication (headache, weakness, dizziness), catarrhal symptoms, reducing the number of complications and duration of the disease in general.
Toxicological studies indicate low toxicity and high safety profile of the drug (LD50 exceeds the therapeutic dose is more than 3000 time). Established, that the preparation has no mutagenic and carcinogenic, It did not affect reproductive function, It does not have immunotoxic and allergenic properties, does not have any irritant action.
Dosage regimen
The drug is taken orally by 90 mg 1 times / day for 5 days, regardless of the meal.
The drug should be started with the appearance of the first symptoms of the disease, not later 36 h From the onset of illness.
Side effect
Allergic reactions (rarely).
Contraindications
Hypersensitivity of the components of the drug.
Pregnancy.
Children up to age 18 years.
Pregnancy and lactation
Use of the drug during pregnancy and lactation has not been studied. If necessary, use during lactation should stop breastfeeding.
Cautions
Not recommended simultaneous reception of other antivirals.
Drug Interactions
The data is not provided.
