riamilovir and Disease-Models--Animal

Prophylactic efficacy of Triazavirin against experimental Forest-Spring encephalitis was studied on albino mice. vs. the active drug Ribavirin. A significant increase of the animal lifespan in the test groups (from 4 to 5 days) and a statistically (p < or = 0.05) valid decrease of the virus accumulation level in the target organ (the brain) were observed.

Topics: Animals; Azoles; Brain; Cell Line; Disease Models, Animal; Encephalitis, Tick-Borne; Mice; Swine; Triazines; Triazoles

Therapeutic activity of Triazavirin against experimental influenza A was studied on albino mice intranazally infected with influenza virus A/Chicken/Kurgan/Russia/02/05 (H5N1) vs. reference drugs (Oseltamivir, Remantadin and Arbidol). The study showed that in a therapeutic dose of 1 mg/kg Triazavirin was efficient in protection of the animals from death. Its protective therapeutic efficacy (36.7+/-1.7%) was close to that of Oseltamivir (50.0+/-0.0%), comparable with that of Remantadin (38.3+/-1.7%) and higher than that of Arbidol (11.7+/-1.7%). During the whole observation period (up to the terminal phase) Triazavirin inhibited the influenza virus A accumulation in the lungs of the infected albino mice by more than 3 lg.

Topics: Animals; Antiviral Agents; Azoles; Disease Models, Animal; Dose-Response Relationship, Drug; Drug Evaluation, Preclinical; Humans; Influenza A Virus, H5N1 Subtype; Influenza, Human; Lung; Mice; Russia; Triazines; Triazoles

Influenza viruses of types A and B cause periodic pandemics in the human population. The antiviral drugs approved to combat influenza virus infections are currently limited. We have investigated an effective novel inhibitor of human influenza A and B viruses, triazavirine [2-methylthio-6-nitro-1,2,4-triazolo[5,1-c]-1,2,4-triazine-7(4I)-one] (TZV). TZV suppressed the replication of influenza virus in cell culture and in chicken chorioallantoic membranes, and it protected mice from death caused by type A and B influenza viruses. TZV was also effective against a rimantadine-resistant influenza virus strain and against avian influenza A virus H5N1 strains. The pharmacokinetic parameters and bioavailability of TZV were calculated after the administration of TZV to rabbits. The TZV metabolite AMTZV [2-methylthio-6-amino-1,2,4-triazolo[5,1-s]-1,2,4-triazin(e)-7(4I)-one] was discovered in IAK 293T and Huh7 cell cultures, a liver homogenate, and rabbit blood after intragastric administration of TZV. AMTZV was nontoxic and inactive as an inhibitor of influenza virus in cell culture. Most likely, this metabolite is a product of TZV elimination.

Topics: Animals; Antiviral Agents; Azoles; Disease Models, Animal; Dogs; Drug Design; Hepatocytes; Humans; Influenza A virus; Influenza B virus; Injections, Intravenous; Kidney; Mice; Mice, Inbred CBA; Orthomyxoviridae Infections; Rabbits; Stomach; Triazines; Triazoles; Virus Replication

The authors present materials on experimental basis of approximate safe level of exposure to new anti-flu medication Triazavirin in air of workplace. The article covers acute toxicity parameters for various intake routes, results of irritating and sensitizing effects evaluation, determination of threshold concentration for single inhalation effect, value of recommended approximate safe level of exposure.

Topics: Air Pollutants, Occupational; Animals; Azoles; Disease Models, Animal; Maximum Tolerated Dose; Mice; Occupational Diseases; Prognosis; Rats; Risk Factors; Triazines; Triazoles