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Macrolides and Ketolides

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Book cover Fundamentals of Antimicrobial Pharmacokinetics and Pharmacodynamics

Abstract

Macrolides and ketolides are characterized by a very wide tissular distribution, which is related to their capacity to accumulate in the acidic compartments of the cells. This property is considered an advantage, because it concentrates the drug at the site of infection. Yet, the low serum levels consecutive to this tissular distribution may favor the selection of resistance. Macrolides are essentially bacteriostatic and ketolides are slowly bactericidal. The pharmacodynamic indice that best predicts efficacy is the free 24 h-AUC/MIC ratio for both subclasses. Despite their high concentration inside the cells, macrolides and ketolides remain bacteriostatic against intracellular bacteria, with a potency similar to that observed extracellularly. New formulations have been developed to optimize patient’s adherence (extended release tablets) or to further increase antibiotic concentration at the site of infection (powders for inhalation).

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Authors and Affiliations

  1. Louvain Drug Research Institute, Université catholique de Louvain, Pharmacologie cellulaire et moléculaire, Avenue Mounier 73 B1.73.05, 1200, Brussels, Belgium

    Françoise Van Bambeke Pharm.D., Ph.D.

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  1. Françoise Van Bambeke Pharm.D., Ph.D.
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Correspondence to Françoise Van Bambeke Pharm.D., Ph.D. .

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  1. Division of Clinical Pharmacology, Cincinnati Children's Hospital Medical Center, Cincinnati, Ohio, USA

    Alexander A. Vinks

  2. Dept. Pharmaceutics, University of Florida, Gainesville College of Pharmacy, Gainesville, Florida, USA

    Hartmut Derendorf

  3. Dept. of Medical Microbiology, Radboudumc, Radboud University Nijmegen, Nijmegen, The Netherlands

    Johan W. Mouton

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Van Bambeke, F. (2014). Macrolides and Ketolides. In: Vinks, A., Derendorf, H., Mouton, J. (eds) Fundamentals of Antimicrobial Pharmacokinetics and Pharmacodynamics. Springer, New York, NY. https://doi.org/10.1007/978-0-387-75613-4_11

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