[Significance of cellular pharmacokinetic data in predicting antibiotic activity in body cells: comparative research on preparations acting on Pseudomonas aeruginosa].
Penetration of carbenicillin, cefotaxime, gentamicin and sisomicin into leukocytes of peripheral blood in man and their intracellular distribution were studied. By its capacity for penetration into leukocytes cefotaxime was superior to the other antibiotics. The levels of sisomicin and carbenicillin absorption by the cells were equal. The level of gentamicin penetration into the cells was the lowest. After penetration into the cells the main part of carbenicillin was preserved in its active form in the cytoplasm. Absorption of the antibiotic by the nuclei, granules, mitochondria and microsomes was insignificant. Cefotaxime was bound to the organoids and not more than 20 per cent of the antibiotic were preserved in its active form. The aminoglycosides were mainly absorbed by the cell granule fraction and the level of the active form of sisomicin in the cytoplasm was twice as higher as that of gentamicin. On the basis of the data on the cell pharmacokinetics of the above antibiotics, their mean therapeutic serum levels and mean geometric values of their MICs for P. aeruginosa it was suggested that in case of intracellular localization of P. aeruginosa the increase in the antibiotic efficacy was of the following order: gentamicin less than cefotaxime less than or equal to sisomicin less than carbenicillin.
D000042:Absorption; D000900:Anti-Bacterial Agents / Q000097:blood* / Q000494:pharmacology; D002462:Cell Membrane / Q000378:metabolism; D006801:Humans; D066298:In Vitro Techniques; D007700:Kinetics; D007962:Leukocytes / Q000378:metabolism*; D011379:Prognosis; D011485:Protein Binding / Q000187:drug effects; D011550:Pseudomonas aeruginosa / Q000187:drug effects*; D013997:Time Factors
D000900:Anti-Bacterial Agents
Znachenie dannykh kletochnoĭ farmakokinetiki v prognoze aktivnosti antibiotikov v kletkakh organizma: sravnitel'noe issledovanie preparatov, deĭstvuiushchikh na sinegnoĭnuiu palochku.