[Experimental comparative pharmacokinetics of levofloxacin, triazavirin, and related conjugate].

A comparative study of the pharmacokinetics of levofloxacin and triazavirine as well as 2-methylthio-6-nitro-1,2,4-triazolo[5,1-ñ]-1,2,4-triazine-7(4Í)-ide (3S)-(-)-9-fluoro-2,3-dihydro-3-methyl-10-(4-methylpiperazin-1-yl)-7-oxo-7H-pyrido[1,2,3-d,e]-1,4-benzoxazine-6-carboxylic acid (conjugate 2) obtained by conjugation of triazavirine and levofloxacin, representing a new class of pharmacological agents, was carried out in experiments on rats. It is established that conjugate 2 in comparison to individual levofloxacin and triazavirine has a higher relative bioavailability and lower rate of elimination, which can lead to improved effectiveness of therapy at reduced dose and frequency of drug administration.

[Influence of new thiazole and tetrazole derivatives on the antioxidant status of natural mouse populations having elevated 90Sr].

The studies on Apodemus (S.) uralensis captured on the control, not contaminated, territories and within the East Ural Radioactive Trace (EURT) area with soil pollution by 90Sr up to 16.7 MBq/m2 (451 Ci/km2), an average concentration of 90Sr up to 160 Bq/g of wet bone were performed. Thiazole or tetrazole derivatives, fluoroquinolone (antibacterial medication pefloxacin) were administered intraperitoneally or orally for ten days. The biochemical parameters of lipid peroxidation and antioxidant system in the peripheral blood plas- ma, erythrocytes, liver and spleen were studied. The effect of the preparations on the reduction of the con- centration of TBA-reactive substances (TBARS), the degree of osmotic hemolysis of cells, as well as the RNA/DNA ratio on the increase of the catalase activity, ceruloplasmin content was reflected. It characterizes the orientation on the normalization of the redox balance of homeostasis, the level of destructive processes in cells and tissues and the functional activity of the genome. It helps to increase the radioresistance and non- specific resistance of the organism under conditions of radioactive contamination of the environment.

[Therapeutic efficacy of Triazavirin, a novel Russian chemotherapeutic, against influenza virus A (H5N1)].

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.

[Triazavirin prophylactic efficacy against influenza virus A (H5N1)].

The experimental study of the prophylactic efficacy of Triazaverin against the experimental form of the influenza virus A (H5N1) on albino mice intranasally infected with the influenza virus A/Chicken/Kurgan/Russia/02/05 vs. the reference drugs Tamiflu, Remantadin and Arbidol showed that in doses of 1 to 100 mg/kg it was efficient in the animal protection from death. The drug was also efficient in the urgent prophylaxis. Triazaverin effectively inhibited the influenza A virus multiplication in the lungs of the albino mice.

[Investigation of triazavirin antiviral activity against influenza A virus (H5N1) in cell culture].

Analysis of triazavirin efficacy with respect to influenza A virus (H5N1) in sensitive cell culture MDSK vs. effective antigrippe drugs, such as tamiflu, remantadin and arbidol showed that triazavirin in a wide range of the concentrations was efficient in inhibition of the virus cytopathic activity and formation of the specific hemagglutinin.