Chemotherapy · 2009 · 16 citations · 0 references
MedicinePharmacologyAntimicrobial PharmacologyDrug DeliveryPharmacodynamicsCellular Drug UptakeDrug DispositionDrug DistributionCellular ChemotaxisCellular Drug AccumulationChemotaxisConcentrationConcentration-dependent ActivityDrug Uptake KineticsPhagocyte Antimicrobial Activity
The cellular/extracellular (C/E) concentration ratio of teicoplanin in polymorphonuclear leukocytes (PMNs) increased rapidly with time (C/E 60 +/- 13 at 20 min). The C/E ratio was time- and concentration-dependent. At 20 min and an initial concentration of 75 +/- 16 micrograms/ml the cellular drug concentration was 4,700 +/- 1,300 micrograms/ml. The mechanism of drug uptake was by an active process and transported (cellular) drug retained its antimicrobial activity. Washing removed 42% of cellular drug. Teicoplanin inhibited PMN chemotaxis at very high concentrations and PMN microbicidal activity at lower concentrations.