Аннотация
С целью сравнения фармакодинамики антистафилококкового эффекта даптомицина и ванкомицина с помощью динамической системы моделировали in vitro их фармакокинетику в широком диапазоне концентраций, включающем терапевтические значения. Для фармакодинамических исследований были выбраны два клинических штамма — Staphylococcus aureus 866 и S.aureus 10, различающихся степенью чувствительности к обоим антибиотикам. Значения МПК составляли в случае даптомицина 0,35 мкг/мл (в отношении S.aureus 866) и 1,1 мкг/мл (S.aureus 10), а в случае ванкомицина — 0,7 и 1,3 мкг/мл соответственно. Моноэкспоненциальные фармакокинетические профили даптомицина и ванкомицина, реализуемые у человека, воспроизводили с периодом полувыведения, равным 9 ч и 6 ч соответственно. Даптомицин вводили однократно, ванкомицин — два раза с интервалом в 12 ч. Значения моделируемого отношения площади под фармакокинетической кривой к МПК (ПФК/МПК) для даптомицина варьировали в пределах 43-970 ч, для ванкомицина — в пределах 33–1150 ч. Антистафилококковый эффект антибиотиков оценивали при помощи интегрального параметра АВВС, т.е. площади между кривыми контрольного роста и роста (или гибели) бактерий в присутствии антибиотика. Полученные зависимости АВВС от ПФК/МПК были специфичны для каждого штамма и антибиотика. При одном и том же значении ПФК/МПК антистафилококковый эффект у даптомицина был выше, чем у ванкомицина, в том числе и при терапевтических значениях ПФК/МПК, соответствующих клиническим дозам (4 мг/кг для даптомицина и 2×1 г для ванкомицина).
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