The macrolide antibiotics: a pharmacokinetic and pharmacodynamic overview

Curr Pharm Des. 2004;10(25):3045-53. doi: 10.2174/1381612043383322.


The macrolide antimicrobial family is comprised of 14, 15 and 16 member-ringed compounds that are characterized by similar chemical structures, mechanisms of action and resistance, but vary in the different pharmacokinetic parameters, and spectrum of activity. The macrolides accumulate in many tissues such as the epithelial lining fluid and easily enter the host defense cells, predominantly macrophages and polymorphonuclear leukocytes (PMNs). Concentrations of the macrolides in respiratory tract tissues and extracellular fluids are in almost all cases higher than simultaneously measured serum concentrations, making them useful for respiratory tract infections. This review will focus on pharmacokinetic and pharmacodynamic aspects of the clinical relevant macrolides including azithromycin, clarithromycin, dirithromycin, erythromycin and roxithromycin.

Publication types

  • Comparative Study
  • Review

MeSH terms

  • Anti-Bacterial Agents / pharmacokinetics*
  • Anti-Bacterial Agents / pharmacology
  • Area Under Curve
  • Bacteria / drug effects
  • Bacteria / growth & development
  • Gastrointestinal Tract / drug effects
  • Gastrointestinal Tract / microbiology
  • Gastrointestinal Tract / pathology
  • Humans
  • Macrolides / chemistry
  • Macrolides / pharmacokinetics*
  • Macrolides / pharmacology
  • Macrophages / metabolism
  • Neutrophils / metabolism
  • Respiratory Mucosa / drug effects
  • Respiratory Mucosa / microbiology
  • Respiratory Mucosa / pathology
  • Tissue Distribution


  • Anti-Bacterial Agents
  • Macrolides