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Produktbild: Quinolone Antibacterials
Band 127

Quinolone Antibacterials

Aus der Reihe Handbook of Experimental Pharmacology

Fr. 137.00

inkl. gesetzl. MwSt., Versandkostenfrei

Beschreibung

Produktdetails

Einband

Taschenbuch

Erscheinungsdatum

12.02.2012

Herausgeber

Jochen Kuhlmann + weitere

Verlag

Springer Berlin

Seitenzahl

491

Maße (L/B/H)

23.5/15.5/2.8 cm

Gewicht

767 g

Auflage

Softcover reprint of the original 1st ed. 1998

Sprache

Englisch

ISBN

978-3-642-80366-6

Beschreibung

Produktdetails

Einband

Taschenbuch

Erscheinungsdatum

12.02.2012

Herausgeber

Verlag

Springer Berlin

Seitenzahl

491

Maße (L/B/H)

23.5/15.5/2.8 cm

Gewicht

767 g

Auflage

Softcover reprint of the original 1st ed. 1998

Sprache

Englisch

ISBN

978-3-642-80366-6

Herstelleradresse

Springer-Verlag KG
Sachsenplatz 4-6
1201 Wien
AT

Email: ProductSafety@springernature.com

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  • Produktbild: Quinolone Antibacterials
  • 1 History and Introduction.- A. Chemistry.- B. Antibacterial Activity.- C. Oxygen and 4-Quinolones.- D. 4-Quinolone Kinetics and Distribution in Humans.- E. Outlook.- References.- 2 The Chemistry of the Quinolones: Methods of Synthesizing the Quinolone Ring System.- A. Introduction.- B. Methods of Synthesizing the Quinolone Ring System.- I. Gould-Jacobs Reaction.- II. Dieckmann Cyclization of Diesthers.- III. Cycloaracylation Procedure.- IV. Biere and Seelen Approach.- V. Isatoic Anhydride Procedure.- VI. Camps Quinolone Synthesis.- VII. Meth-Cohn Quinolone Synthesis.- VIII. Synthesis of Quinolone Analogues.- IX. Synthesis of 4-Cinnolone-3-carboxylic Acids.- X. Synthesis of 4-Pyridone-3-carboxylic Acids.- References.- 3 The Chemistry of the Quinolones: Chemistry in the Periphery of the Quinolones.- A. Introduction.- B. 1-Position.- C. 2-Position.- D. 3-Position.- E. 4-Position.- F. 5-Position.- G. 6-Position.- H. 7-Position.- I. Synthesis of Specific Amines.- 1. Bicyclic Piperazine Derivatives.- 2. Aminopyrrolidine and Aminomethylpyrrolidine Derivatives.- 3. 3,4-Bridged Pyrrolidine Derivatives.- 4. Mixed Derivatives.- II. C-N Linkage.- III. C-S Linkage.- IV. C-O Linkage.- V. C-C Linkage.- I. 8-Position.- References.- 4 Mode of Action.- A. Introduction.- B. Effects on Bacteria.- C. Effects on DNA Gyrase.- I. Reactions of Gyrase.- II. Mechanistic Steps.- 1. DNA Binding.- 2. DNA Cleavage.- 3. ATPase.- III. Illegitimate Recombination.- IV. Summary.- D. Mode of Binding.- I. Binding of Quinolones to DNA.- II. Effect of DNA Gyrase on Quinolone Binding.- III. Cooperative Quinolone-DNA Binding Model.- IV. DNA Cleavage is not an Absolute Requirement for Quinolone Binding to a Gyrase-DNA Complex.- V. A Role for Magnesium Ions in the Binding of Quinolones to DNA.- VI. Binding of Quinobenzoxazines to DNA.- VII. Quinolone Binding to Quinolone-Resistant Mutants of DNA Gyrase.- VIII. Mode of Binding of Topoisomerase II-Targeting Drugs.- IX. Problems with Current Models.- X. Conclusions.- E. Mechanism of Cell Killing.- I. Paradoxical Effects of Quinolones.- II. Poison Hypothesis.- III. Polymerase Blocking.- F. Conclusions and Future Prospects.- References.- 5 The In Vitro Antibacterial Activity of Quinolones: A Review.- A. Introduction.- B. In Vitro Activity.- C. The Future.- References.- 6 Pharmacokinetics of Fluoroquinolones in Experimental Animals.- A. Introduction.- B. Norfloxacin.- C. Pefloxacin.- D. Enoxacin.- E. Ofloxacin.- F. Ciprofloxacin.- G. Temafloxacin.- H. Tosufloxacin.- I. Fleroxacin.- J. Lomefloxacin.- K. Sparfloxacin.- L. Penetration of Quinolones at Sites of Infection.- References.- 7 Pharmacodynamics of Fluoroquinolones in Experimental Animals.- A. Introduction.- B. Bacterial Killing In Vivo.- C. In Vivo Postantibiotic Effects.- D. Pharmacodynamic Parameters Determining Efficacy.- E. Emergence of Resistance to Fluoroquinolones.- I. P. aeruginosa Experimental Infections.- II. Staphylococcal Infections in Experimental Animals.- III. Miscellaneous Infection Models.- IV. Factors Contributing to the Emergence of Resistance In Vivo.- References.- 8 Interaction of Quinolones with Host-Parasite Relationship.- A. Introduction.- B. Effect on Adherence.- C. Effect Against Slowly Growing Bacteria.- D. Effect on Exoenzyme Production.- I. E. coli.- II. P. aeruginosa.- E. Quinolone-Induced Endotoxin Release.- F. Summary.- References.- 9 Mechanisms of Resistance to Fluoroquinolones.- A. Introduction.- B. Target Site Modification.- I. Mutations in gyrA.- II. Mutations in gyrB.- III. Mutations in Other Topoisomerase Genes.- C. Reduced Intracellular Accumulation.- I. Decreased Uptake.- II. Increased Efflux.- III. The mar Operon.- D. Reduced Killing.- E. Prevalence of Fluoroquinolone Resistance.- I. Community Acquired Pathogens.- II. Nosocomial Pathogens.- III. Impact of Fluoroquinolone Use in Agriculture.- F. Distribution of Resistance Mechanisms.- G. Summary.- References.- 10 Toxicology and Safety Pharmacology of Quinolones.- A. Introduction.- B. Arthropathy.- C. Achilles Tendinitis and Rupture.- D. Nephropathy.- E. Effects on Central Nervous System.- F. Ocular Toxicity.- G. Impairment of Spermatogenesis.- H. Cardiovascular Effects.- I. Possible Mutagenic and Carcinogenic Effects.- J. Phototoxicity.- K. Photocarcinogenicity and Photomutagenicity.- L. Drug Interactions.- M. Metabolic and Nutritional Effects.- N. Conclusion.- References.- 11 Clinical Pharmacology.- A. Introduction.- B. Pharmacokinetics of Fluoroquinolone Antibiotics.- I. Healthy Subjects.- 1. Absorption.- 2. Intravenous Administration.- 3. Bioavailability.- 4. Distribution.- 5. Disposition.- II. The Elderly.- III. Patients with Various Degrees of Renal Failure.- 1. Ciprofloxacin.- 2. Norfloxacin.- 3. Ofloxacin.- 4. Enoxacin.- 5. Fleroxacin.- 6. Pefloxacin.- 7. Lomefloxacin.- 8. Summary.- IV. Patients with Hepatic Failure.- V. Fluoroquinolones in Pediatric Patients.- C. Interactions of Fluoroquinolone Antibiotics with Other Drugs.- I. Interactions During the Absorption Process.- 1. Food and Dairy Products.- 2. Al3+-, Ca2+- and Mg2+-Containing Antacids.- 3. Sucralfate.- 4. Didanosine.- 5. Other Metal Cations.- 6. Chemotherapy Treatment.- 7. Activated Charcoal.- II. Interactions of Fluoroquinolones Due to Alterations in Metabolism.- 1. Theophylline, Caffeine and Structurally Closely Related Substances.- 2. Antipyrine.- 3. Phenytoin.- 4. H2-Receptor Antagonists.- 5. K+/Na+-ATPase Inhibitors.- 6. Warfarin.- 7. Cyclosporine.- 8. Rifampin.- 9. Oral Contraceptive Steroids.- 10. Benzodiazepines (Diazepam, Temazepam).- III. Alterations in Renal Excretion.- 1. Probenecid.- 2. ?-Lactam Antibiotics.- IV. Pharmacodynamic Interactions.- 1. Nonsteroidal Anti-inflammatory Drugs.- 2. Metronidazole.- V. Conclusions.- D. Adverse Reactions of Fluoroquinolones.- I. Gastrointestinal Tract.- II. Central Nervous System.- III. Skin and Allergic Reactions.- 1. Photosensitivity.- 2. Photoallergy.- IV. Nephropathy and Crystalluria.- V. Arthropathy and Musculoskeletal Disorders.- VI. Body Systems.- VII. Others.- References.- 12 Concentration-Effect Relationship of the Fluoroquinolones.- A. Introduction.- B. Pharmacodynamic Data of Antimicrobials as a Basis for Clinical Use.- I. ?-Lactams: Concentration-Independent Killing Rate.- II. Aminoglycosides: Concentration-Dependent Killing Rate.- III. Fluoroquinolones.- 1. In Vitro Models.- 2. Animal Models.- 3. Clinical Data.- 4. Overall Evaluation of Pharmacodynamics.- C. Pharmacokinetic Aspects.- I. Protein Binding.- II. Tissue Concentrations and Volume of Distribution.- D. Summary and Conclusion.- References.- 13 Clinical Use of Quinolones.- A. Introduction.- B. Urinary Tract Infections and Prostatitis.- I. Acute Uncomplicated Urinary Tract Infection.- II. Complicated Urinary Tract Infection.- III. Prostatitis.- C. Gastrointestinal Infections and Traveller’s Diarrhea.- I. Salmonella typhi — Enteric Fever.- II. Salmonella typhi Carriers.- III. Salmonella Gastroenteritis Outbreaks.- IV. Shigellosis.- V. Cholera.- VI. Traveller’s Diarrhea — Prevention.- VII. Traveller’s Diarrhea — Therapy.- D. Respiratory Tract Infections.- I. Acute Exacerbation of Chronic Bronchitis.- II. Pneumonia.- III. Recurrent Respiratory Tract Infections in Patients with Cystic Fibrosis.- IV. Sinusitis.- V. Bacterial Otitis (Chronic Suppurative Otitis Media).- VI. Malignant External Otitis.- E. Osteomyelitis.- F. Skin and Skin Structure Infection.- G. Sexually Transmitted Diseases.- I. Gonorrhea.- II. Chancroid.- III. Nongonococcal Urethritis.- H. Intra-abdominal Infections.- I. Anaerobic Intra-abdominal Infections.- II. Cholangitis.- III. Peritonitis in Chronic Ambulatory Dialysis Patients.- IV. Gynecological Infections.- I. Bacteremia and Sepsis.- J. Surgical Prophylaxis.- I. Transurethral Prostatic Surgery.- II. Endoscopic Retrograde Cholangiopancreatography.- III. Abdominal Surgery.- K. Infections in Neutropenic Patients.- I. Empirical Treatment of Febrile Neutropenic Patients.- II. Prophylaxis in Neutropenic Cancer Patients.- L. Use of Quinolones in Pediatrics.- M. Remarks.- References.- 14 Future Aspects.- A. Introduction.- B. Molecular Structure and Mechanism of Action.- C. Antimicrobial Activity.- I. Gram-Positive Bacteria.- 1. Staphylococci.- 2. Streptococci.- 3. Enterococci.- II. Anaerobic Bacteria.- III. Mycobacterium tuberculosis.- D. Bacterial Resistance.- E. Future Use of Quinolones in Pediatrics.- F. Antitumor Potential.- G. New Attitudes.- H. Directions of Future Research on the Quinolones.- References.