Macrolide Antibiotics

Description

The current state of research, development, and use of macrolides as a treatment option for bacterial infections is the subject of this monograph. Macrolides, whose first representative (erythromycin) was introduced into the market in the 1950s, have been optimised by various companies into effective, safe, and convenient treatments with overwhelming success. Various compounds, such as azithromycin, clarithromycin, erythromycin, and roxithromycin, are in current effective use for treatment of infections mainly of the respiratory, gastrointestinal, and urogenital tracts and skin and soft tissues. A highly competitive research environment and critical medical need for improved macrolides have led to various new scaffolds and derivatives such as the ketolides ABT-773 and telithromycin, which are in development or in the regulatory process for market approval. The individual chapters cover aspects of microbiology, clinical use and experience, pharmacokinetics, pharmacodynamics, biochemistry, and chemistry. They are written by leading experts in their respective fields. Thus, readers - whether they are professionals in the pharmaceutical industry, physicians treating infections, or biochemists, chemists, pharmacologists or microbiologists at hospitals, health institutes, or universities - will find a detailed and up-to-date knowledge base about current research activities and a sound, stimulating overview of the compound class. Front Matter....Pages I-X Introduction to the macrolide antibiotics....Pages 1-13 Macrolides: a clinical overview....Pages 15-24 Pharmacokinetics/pharmacodynamics of macrolides....Pages 25-36 Cellular accumulation of macrolide antibiotics. Intracellular bioactivity....Pages 37-52 Clarithromycin and new derivatives of erythromycin....Pages 53-72 Azithromycin and novel azalides....Pages 73-95 Ketolides: novel antibacterial agents designed to overcome resistance to erythromycin A within gram-positive cocci....Pages 97-140 Novel macrolide derivatives active against resistant pathogens....Pages 141-155 Polyketide diversity....Pages 157-175 Biosynthesis of the macrolide antibiotic, tylosin....Pages 177-184 In vitro activity of macrolides against traditional susceptible bacteria....Pages 185-200 Activity of macrolides against mycobacteria....Pages 201-213 Chlamydia pneumoniae and asthma and atherosclerosis: role of macrolides....Pages 215-228 Activity of macrolides in sexually transmitted diseases....Pages 229-241 Helicobacter pylori and macrolides....Pages 243-260 Effects of macrolide antibiotics on ribosome function....Pages 261-280 Mechanisms of resistance to macrolides, lincosamides, and ketolides....Pages 281-317 Back Matter....Pages 319-323