The Quinolones - 1st Edition - ISBN: 9780120595150, 9781483216034

The Quinolones

1st Edition

Editors: Vincent T. Andriole
eBook ISBN: 9781483216034
Imprint: Academic Press
Published Date: 1st November 1988
Page Count: 274
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The Quinolones covers reviews on the history, chemistry and mechanism of action, in vitro properties, pharmacokinetics, clinical overview, toxicity, adverse effects and drug interactions, and future prospects of the 4-quinolones. The book discusses the microbiology of quinolones, particularly with consideration of the development of resistance, pharmacology, toxicology, and clinical uses. Chemists, microbiologists, pharmacologists and clinicians will find the book useful.

Table of Contents



1 The Quinolones: History and Overview

1.1 Mechanism of Action

1.2 Activity In Vitro

1.3 Bacterial Resistance

1.4 Clinical Pharmacology

1.5 Clinical Uses

1.5.1 Genitourinary and Gastrointestinal Infections

1.5.2 Respiratory Tract Infections

1.5.3 Skin and Bone Infections

1.5.4 Other Infections

1.6 Adverse Effects

1.7 Summary


2 Chemistry and Mechanisms of Action of the Quinolone Antibacterials 23

2.1 Chemistry

2.2 Target Site

2.3 Selectivity

2.4 Antibacterial Activities

2.5 4-Quinolone Interactions with Ions

2.6 4-Quinolone Interactions with Oxygen

2.7 4-Quinolone Interactions with Other Antibacterials

2.8 Resistance


3 In Vitro Properties of the Quinolones

3.1 Gram-Negative Aerobes

3.1.1 Enterobacteriaceae

3.1.2 Other Gram-Negative Aerobes

3.2 Gram-Positive Aerobes

3.3 Anaerobes

3.4 Miscellaneous Organisms

3.5 Development of Resistance

3.6 Conclusion


4 Pharmacokinetics of Fluorinated Quinolones


4.1 Serum Concentrations

4.2 Urine Concentrations

4.3 Steady State

4.4 Pharmacokinetics

4.5 Elimination

4.6 Bioavailability

4.7 Impaired Renal Function

4.8 Impaired Liver Function

4.9 Impact of Food

4.10 Interactions

4.11 Influence of Disease

4.12 Extravascular Penetration


5 Clinical Overview of the Newer 4-Quinolone Antibacterial Agents


5.1 Urinary Tract Infections

5.1.1 Pharmacology

5.1.2 Microbiology

5.1.3 Clinical Studies

5.2 Respiratory Tract Infections

5.2.1 Pharmacology

5.2.2 Microbiology

5.2.3 Clinical Studies

5.3 Gastrointestinal Infections

5.3.1 Pharmacology

5.3.2 Microbiology

5.3.3 Clinical Studies

5.4 Skin and Soft-Tissue Infections

5.4.1 Pharmacology

5.4.2 Microbiology

5.4.3 Clinical Studies

5.5 Osteomyelitis

5.5.1 Pharmacology

5.5.2 Microbiology

5.5.3 Clinical Studies

5.6 Sexually Transmitted Diseases

5.6.1 Pharmacology

5.6.2 Microbiology

5.6.3 Clinical Studies

5.7 Immunocomprised Patients

5.8 Central Nervous System Infections

5.8.1 Neisseria Meningitidis Nasopharyngeal Carriers

5.9 Other Potential Uses

5.9.1 Endocarditis

5.9.2 Mycobacteria

5.9.3 Brucellosis

5.10 Summary


6 Safety Overview: Toxicity, Adverse Effects and Drug Interactions

6.1 Introduction

6.2 Toxicity of Quinolones

6.2.1 General Remarks

6.2.2 Arthropathy in Laboratory Animals

6.2.3 Renal Tolerability

6.2.4 Testicular Toxicity

6.2.5 Ocular Toxicity

6.2.6 Mutagenicity

6.2.7 Prenatal Toxicity

6.3 Adverse Effects of Fluoroquinolones in Clinical Studies

6.3.1 General Considerations

6.3.2 Gastrointestinal Side-Effects

6.3.3 Side-Effects on the Central Nervous System

6.3.4 Hypersensitivity Reactions

6.3.5 Phototoxicity

6.3.6 Case Reports of Arthralgia During Quinolone Therapy

6.3.7 Other Rarely Registered Side-Effects

6.3.8 Side-Effects Observed in Clinical Trials with Individual Fluoroquinolones

6.3.9 Side-Effects Observed in Comparative Double Blind Studies

6.4 Drug Interactions

6.4.1 General Remarks

6.4.2 Influence of pH and Magnesium on Antibacterial Activity of Quinolones

6.4.3 Interactions Between Quinolones and Antacids

6.4.4 Influence of Antiulcer Drugs and Breakfast on the Bioavailability of Quinolones

6.4.5 Interactions in Renal Elimination

6.4.6 Interactions Between Quinolones and Theophylline

6.4.7 Interactions Between Quinolones and Caffeine

6.4.8 Interactions Between Quinolones and Warfarin


7 The Quinolones: Prospects

7.1 Microbiology

7.2 Resistance of Bacteria to Quinolones

7.3 Pharmacology

7.4 Toxicological Issues

7.5 Clinical Considerations for Future Use of Quinolones

7.5.1 Urinary Tract Infections

7.5.2 Sexually Transmitted Diseases

7.5.3 Respiratory Infections

7.5.4 Gastrointestinal Infections

7.5.5 Osteomyelitis

7.5.6 Mycobacterial Infections

7.6 Prophylactic Use of Quinolones

7.7 Summary




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© Academic Press 1988
Academic Press
eBook ISBN:

About the Editor

Vincent T. Andriole

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