title: High teicoplanin uptake by human neutrophils.
abstract: 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.
authors.affiliation: Department of Medicine, Hartford Hospital, Conn.
authors.forename: E G
authors.initials: EG
authors.lastname: Maderazo
authors.forename: S P
authors.initials: SP
authors.lastname: Breaux
authors.forename: C L
authors.initials: CL
authors.lastname: Woronick
authors.forename: R
authors.initials: R
authors.lastname: Quintiliani
authors.forename: C H
authors.initials: CH
authors.lastname: Nightingale
mesh_terms: D001693:Biological Transport, Active; D002634:Chemotaxis, Leukocyte / Q000187:drug effects; D002981:Clindamycin / Q000493:pharmacokinetics; D005260:Female; D006020:Glycopeptides / Q000493:pharmacokinetics / Q000494:pharmacology; D006801:Humans; D008297:Male; D009504:Neutrophils / Q000187:drug effects / Q000378:metabolism*; D017334:Teicoplanin
chemical_list: D006020:Glycopeptides; D002981:Clindamycin; D017334:Teicoplanin