1. [Experimental comparative pharmacokinetics of levofloxacin, triazavirin, and related conjugate].
- Author
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Blazhennikova IV, Kurliakova AF, Bykov VN, Geĭbo DS, Nikiforov AS, Stepanov AV, Charushin VN, Chupakhin ON, Kotovskaia SK, and Rusinov VL
- Subjects
- Animals, Anti-Infective Agents blood, Anti-Infective Agents chemistry, Azoles blood, Azoles chemistry, Biological Availability, Carboxylic Acids blood, Carboxylic Acids chemistry, Half-Life, Injections, Intramuscular, Levofloxacin blood, Levofloxacin chemistry, Male, Rats, Triazines blood, Triazines chemistry, Triazoles, Anti-Infective Agents pharmacokinetics, Azoles pharmacokinetics, Carboxylic Acids pharmacokinetics, Levofloxacin pharmacokinetics, Triazines pharmacokinetics
- Abstract
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.
- Published
- 2015