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Evaluation of the extracellular and intracellular activities (human THP-1 macrophages) of telavancin versus vancomycin against methicillin-susceptible, methicillin-resistant, vancomycin-intermediate and vancomycin-resistant Staphylococcus aureus.
J Antimicrob Chemother. 2006 Dec; 58(6):1177-84.JA

Abstract

OBJECTIVES

To compare extracellular and intracellular activities of telavancin (versus vancomycin) against Staphylococcus aureus (MSSA, MRSA, VISA and VRSA).

METHODS

Determination of cfu changes (3-24 h) in culture medium and in macrophages at concentrations ranging from 0.01 to 1000x MIC.

RESULTS

Extracellularly, telavancin displayed a fast, concentration-dependent bactericidal activity against all strains. The concentration-effect relationship was bimodal for MSSA and MRSA [two successive sharp drops in bacterial counts (0.3-1x MIC and 100-1000x MIC) separated by a zone of low concentration dependency]. When compared at human total drug Cmax (vancomycin, 50 mg/L; telavancin, 90 mg/L) towards MSSA, MRSA and VISA, telavancin caused both a faster and more marked decrease of cfu, with the limit of detection (>5 log decrease) reached already at 6 versus 24 h for vancomycin. Intracellularly, the bactericidal activity of telavancin was less intense [-3 log (MSSA) to -1.5 log (VRSA) at Cmax and at 24 h]. A bimodal relationship with respect to concentration (at 24 h) was observed for both MSSA and MRSA. In contrast, vancomycin exhibited only marginal intracellular activity towards intraphagocytic MSSA, MRSA and VISA (max. -0.5 log decrease at 24 h and at Cmax).

CONCLUSIONS

Telavancin showed time- and concentration-dependent bactericidal activity against both extracellular and intracellular S. aureus with various resistance phenotypes. The data support the use of telavancin in infections where intracellular and extracellular S. aureus are present. Bimodality of dose responses (MSSA and MRSA) could indicate multiple mechanisms of action for telavancin.

Authors+Show Affiliations

Unité de Pharmacologie cellulaire et moléculaire, Université catholique de Louvain, B-1200 Brussels, Belgium.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Comparative Study
Journal Article
Research Support, N.I.H., Extramural
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

17062609

Citation

Barcia-Macay, Maritza, et al. "Evaluation of the Extracellular and Intracellular Activities (human THP-1 Macrophages) of Telavancin Versus Vancomycin Against Methicillin-susceptible, Methicillin-resistant, Vancomycin-intermediate and Vancomycin-resistant Staphylococcus Aureus." The Journal of Antimicrobial Chemotherapy, vol. 58, no. 6, 2006, pp. 1177-84.
Barcia-Macay M, Lemaire S, Mingeot-Leclercq MP, et al. Evaluation of the extracellular and intracellular activities (human THP-1 macrophages) of telavancin versus vancomycin against methicillin-susceptible, methicillin-resistant, vancomycin-intermediate and vancomycin-resistant Staphylococcus aureus. J Antimicrob Chemother. 2006;58(6):1177-84.
Barcia-Macay, M., Lemaire, S., Mingeot-Leclercq, M. P., Tulkens, P. M., & Van Bambeke, F. (2006). Evaluation of the extracellular and intracellular activities (human THP-1 macrophages) of telavancin versus vancomycin against methicillin-susceptible, methicillin-resistant, vancomycin-intermediate and vancomycin-resistant Staphylococcus aureus. The Journal of Antimicrobial Chemotherapy, 58(6), 1177-84.
Barcia-Macay M, et al. Evaluation of the Extracellular and Intracellular Activities (human THP-1 Macrophages) of Telavancin Versus Vancomycin Against Methicillin-susceptible, Methicillin-resistant, Vancomycin-intermediate and Vancomycin-resistant Staphylococcus Aureus. J Antimicrob Chemother. 2006;58(6):1177-84. PubMed PMID: 17062609.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Evaluation of the extracellular and intracellular activities (human THP-1 macrophages) of telavancin versus vancomycin against methicillin-susceptible, methicillin-resistant, vancomycin-intermediate and vancomycin-resistant Staphylococcus aureus. AU - Barcia-Macay,Maritza, AU - Lemaire,Sandrine, AU - Mingeot-Leclercq,Marie-Paule, AU - Tulkens,Paul M, AU - Van Bambeke,Françoise, Y1 - 2006/10/24/ PY - 2006/10/26/pubmed PY - 2007/3/23/medline PY - 2006/10/26/entrez SP - 1177 EP - 84 JF - The Journal of antimicrobial chemotherapy JO - J Antimicrob Chemother VL - 58 IS - 6 N2 - OBJECTIVES: To compare extracellular and intracellular activities of telavancin (versus vancomycin) against Staphylococcus aureus (MSSA, MRSA, VISA and VRSA). METHODS: Determination of cfu changes (3-24 h) in culture medium and in macrophages at concentrations ranging from 0.01 to 1000x MIC. RESULTS: Extracellularly, telavancin displayed a fast, concentration-dependent bactericidal activity against all strains. The concentration-effect relationship was bimodal for MSSA and MRSA [two successive sharp drops in bacterial counts (0.3-1x MIC and 100-1000x MIC) separated by a zone of low concentration dependency]. When compared at human total drug Cmax (vancomycin, 50 mg/L; telavancin, 90 mg/L) towards MSSA, MRSA and VISA, telavancin caused both a faster and more marked decrease of cfu, with the limit of detection (>5 log decrease) reached already at 6 versus 24 h for vancomycin. Intracellularly, the bactericidal activity of telavancin was less intense [-3 log (MSSA) to -1.5 log (VRSA) at Cmax and at 24 h]. A bimodal relationship with respect to concentration (at 24 h) was observed for both MSSA and MRSA. In contrast, vancomycin exhibited only marginal intracellular activity towards intraphagocytic MSSA, MRSA and VISA (max. -0.5 log decrease at 24 h and at Cmax). CONCLUSIONS: Telavancin showed time- and concentration-dependent bactericidal activity against both extracellular and intracellular S. aureus with various resistance phenotypes. The data support the use of telavancin in infections where intracellular and extracellular S. aureus are present. Bimodality of dose responses (MSSA and MRSA) could indicate multiple mechanisms of action for telavancin. SN - 0305-7453 UR - https://www.unboundmedicine.com/medline/citation/17062609/Evaluation_of_the_extracellular_and_intracellular_activities__human_THP_1_macrophages__of_telavancin_versus_vancomycin_against_methicillin_susceptible_methicillin_resistant_vancomycin_intermediate_and_vancomycin_resistant_Staphylococcus_aureus_ L2 - https://academic.oup.com/jac/article-lookup/doi/10.1093/jac/dkl424 DB - PRIME DP - Unbound Medicine ER -