The Quinolones
, by Andriole, Vincent T.Note: Supplemental materials are not guaranteed with Rental or Used book purchases.
- ISBN: 9780120595150 | 012059515X
- Cover: Hardcover
- Copyright: 1/1/1989
The Quinolones, Second Edition provides the most current review of quinolone antibacterial agents available & a look into new quinolone development. The book provides comprehensive & updated coverage of thehistory, chemistry, pharmacology, efficacy & safety aspects of quinolones. New chapters describe the use of quinolones in treating specific infections, including sexually transmitted diseases, respiratory infections, gastrointestinal infections, & bacterial meningitis. This text is a valuable reference for primary care physicians & infectious disease specialists as well as researchers & industry personnel involved in the development of new antimicroagents.
Contributors | p. xv |
Preface | p. xix |
The Quinolones: History and Overview | |
Introduction | p. 2 |
Structure-Activity Relationships (SARs) | p. 3 |
Antibacterial Activity | p. 6 |
Mode of Action | p. 6 |
Spectrum of Activity | p. 6 |
Bacterial Resistance to Fluoroquinolones | p. 8 |
Clinical Pharmacology | p. 9 |
Penetration into Respiratory Tissues | p. 10 |
Elimination Pathways | p. 11 |
Pharmacodynamics of Quinolones | p. 12 |
Clinical Uses | p. 12 |
Urinary Tract Infections | p. 12 |
Sexually Transmitted Diseases | p. 13 |
Respiratory Infections | p. 13 |
Gastrointestinal Infections | p. 14 |
Skin and Soft Tissue Infections | p. 15 |
Bone Infections | p. 15 |
Neutropenic Cancer Patients | p. 16 |
Prophylaxis | p. 16 |
Pharmacoeconomic Aspects of Fluoroquinolone Usage | p. 16 |
Use of Fluoroquinolones in Pediatrics | p. 17 |
Adverse Drug Reactions | p. 19 |
Interactions with Other Drugs | p. 22 |
Interactions Reducing Absorption | p. 22 |
Metabolic and Inhibitory Interactions | p. 23 |
Conclusion | p. 23 |
References | p. 24 |
Chemistry and Mechanism of Action of the Quinolone Antibacterials | |
Introduction | p. 34 |
Structural and Historical Background | p. 34 |
General Structural Features of the Quinolones | p. 35 |
First-Generation Quinolones | p. 36 |
Second-Generation Quinolones | p. 38 |
Third- and Fourth-Generation Quinolones | p. 42 |
In Vitro Potency | p. 43 |
In Vivo Activity | p. 51 |
Selectivity: Activity against Mammalian Topoisomerase II and Genetic Toxicity | p. 53 |
Chemical Properties | p. 55 |
Future Directions | p. 57 |
Compounds Lacking the C-6 Fluorine | p. 57 |
2-Pyridones | p. 59 |
Alteration of Primary Enzymatic Target | p. 60 |
Mechanism of Action | p. 61 |
Replication of DNA | p. 61 |
Bacterial Topoisomerases | p. 63 |
Topoisomerase Sensitivity to Fluoroquinolones | p. 71 |
Killing of Bacterial Cells by Fluoroquinolones | p. 75 |
Conclusion | p. 81 |
References | p. 82 |
Comparative In-Vitro Properties of the Quinolones | |
Introduction | p. 99 |
Gram-Negative Aerobes | p. 102 |
Enterobacteriaceae | p. 102 |
Other Gram-Negative Aerobes | p. 107 |
Gram-Positive Aerobes | p. 117 |
Anaerobes | p. 125 |
Miscellaneous Organisms | p. 130 |
Conclusion | p. 132 |
References | p. 132 |
Bacterial Resistance to Quinolones: Mechanisms and Clinical Implications | |
Introduction | p. 140 |
Mechanisms of Quinolone Resistance | p. 140 |
Gram-Negative Bacteria | p. 140 |
Escherichia coli | p. 140 |
Salmonella spp. | p. 142 |
Klebsiella spp. | p. 143 |
Pseudomonas aeruginosa | p. 143 |
Neisseria gonorrhoeae | p. 145 |
Campylobacter spp. | p. 145 |
Helicobacter pylori | p. 145 |
Miscellaneous | p. 146 |
Gram-Positive Bacteria | p. 146 |
Staphylococcus aureus | p. 146 |
Streptococcus pneumoniae | p. 147 |
Enterococcus faecalis | p. 148 |
Mycobacteria | p. 148 |
Clinical Impact of Bacterial Resistance to Quinolones | p. 149 |
Prevalence of Quinolone Resistance | p. 149 |
Fluoroquinolone Resistance in Hospital Practice | p. 149 |
Fluoroquinolone Resistance in Community-Acquired Infections | p. 151 |
Quinolone Use and Emergence of Resistance | p. 155 |
References | p. 156 |
Pharmacokinetics and Pharmacodynamics of the Fluoroquinolones | |
Introduction | p. 170 |
Basic Concepts of Pharmacokinetics and Pharmacodynamics | p. 170 |
Pharmacokinetics | p. 171 |
Absorption | p. 172 |
Distribution | p. 174 |
Elimination | p. 179 |
Special Population | p. 181 |
Drug Interactions | p. 182 |
Pharmacodynamics | p. 185 |
Bactericidal Activity: Time-Kill Curves | p. 185 |
Pharmacodynamic Surrogate Markers and Clinical Outcome | p. 186 |
Post-Antibiotic Effects | p. 188 |
Conclusion | p. 191 |
References | p. 191 |
Use of Quinolones in Urinary Tract Infection and Prostatitis | |
Introduction | p. 203 |
Urinary Tract Infection | p. 204 |
Pharmacology | p. 207 |
Microbiology | p. 207 |
Clinical Studies | p. 209 |
Limitations of Available Studies | p. 209 |
Acute Uncomplicated Urinary Infection | p. 209 |
Acute Nonobstructive Pyelonephritis | p. 213 |
Complicated Urinary Infection | p. 214 |
Bacterial Prostatitis | p. 215 |
Conclusion | p. 218 |
References | p. 218 |
Use of the Quinolones in Sexually Transmitted Diseases | |
Introduction | p. 228 |
Gonococcal Infections | p. 229 |
Background | p. 229 |
In-Vitro Activity of Quinolones against Neisseria gonorrhoeae | p. 230 |
Clinical Studies | p. 230 |
Resistance of N. gonorrhoeae to the Quinolones | p. 233 |
Chlamydia trachomatis | p. 235 |
Background | p. 235 |
In-Vitro Activity of Quinolones against C. trachomatis | p. 235 |
Clinical Studies | p. 235 |
Pelvic Inflammatory Disease | p. 238 |
Chancroid | p. 239 |
Background | p. 239 |
In-Vitro Activity of Quinolones against Haemophilus ducreyi | p. 239 |
Clinical Studies | p. 240 |
Donovanosis | p. 241 |
Bacterial Vaginosis | p. 241 |
Special Toxicity Considerations When Quinolones Are Used for Treating Sexually Transmitted Diseases | p. 242 |
Conclusion | p. 243 |
References | p. 243 |
Treatment of Respiratory Infections with Quinolones | |
Introduction | p. 255 |
Clinical Issues in the Therapy of Respiratory Infection | p. 257 |
Community-Acquired Pneumonia | p. 257 |
Hospital-Acquired Pneumonia | p. 260 |
Acute Exacerbations of Chronic Bronchitis | p. 261 |
Pharmacological Advantages for the Use of Quinolones in Respiratory Infection | p. 262 |
Penetration into Lung Tissue | p. 262 |
Mechanism of Killing | p. 265 |
Microbiologic Advantages of Quinolones for Respiratory Infection | p. 267 |
Activity against Common Respiratory Pathogens | p. 268 |
Clinical Efficacy of Quinolones for the Therapy of Respiratory Tract Infections | p. 271 |
Community-Acquired Pneumonia | p. 271 |
Hospital-Acquired Pneumonia | p. 274 |
Acute Exacerbations of Chronic Bronchitis | p. 275 |
Conclusion | p. 276 |
References | p. 277 |
Use of Quinolones in Surgery and Obstetrics and Gynecology | |
Introduction | p. 285 |
Surgical Wound Prophylaxis | p. 286 |
Soft Tissue Infection | p. 288 |
Intraabdominal Infection | p. 289 |
Gynecologic Infections | p. 291 |
Postoperative Pelvic Infections | p. 293 |
Pelvic Inflammatory Disease | p. 294 |
Upper Genital Tract Infection | p. 295 |
Pregnancy | p. 296 |
Conclusion | p. 297 |
References | p. 297 |
Use of the Quinolones for Treatment and Prophylaxis of Bacterial Gastrointestinal Infections | |
Introduction | p. 304 |
Pharmacology | p. 304 |
Microbiology | p. 304 |
Effects on Human Intestinal Microflora | p. 305 |
Clinical Studies | p. 305 |
Empirical Therapy of Acute Diarrhea | p. 305 |
Traveler's Diarrhea | p. 308 |
Nontyphoidal Salmonellosis | p. 309 |
Typhoid Fever | p. 310 |
Shigellosis | p. 312 |
Cholera and Other Vibrios | p. 314 |
Campylobacter | p. 315 |
Antimicrobial Resistance to Quinolones | p. 316 |
Conclusion | p. 317 |
References | p. 318 |
Use of the Quinolones in Treatment of Bacterial Meningitis | |
Introduction | p. 325 |
Pharmacology | p. 326 |
In-Vitro Activity of Quinolones against Meningeal Pathogens | p. 326 |
CSF Penetration of the Quinolones in Vivo | p. 328 |
Microbiology | p. 335 |
Studies of Clinical Efficacy | p. 336 |
Case Reports | p. 336 |
Chemoprophylaxis of Meningococcal Meningitis | p. 336 |
Clinical Trial of Trovafloxacin | p. 338 |
Conclusion | p. 339 |
References | p. 339 |
Use of the Quinolones in Immunocompromised Patients | |
Introduction | p. 343 |
Risk Factors and Associated Infections | p. 344 |
Rationale for Fluoroquinolone Use | p. 346 |
Effect of Fluoroquinolones on Endogenous Microflora | p. 347 |
Infection Prevention in Afebrile Neutropenic Patients | p. 348 |
Empiric Therapy in Febrile Neutropenic Patients | p. 350 |
Risk-Based Therapy for Febrile Neutropenia | p. 352 |
Treatment of Specific Infections | p. 354 |
Legionellosis | p. 354 |
Mycobacterial Infections | p. 356 |
Miscellaneous Infections | p. 358 |
Conclusion | p. 359 |
References | p. 360 |
Use of the Quinolones in Skin and Skin Structure (Osteomyelitis) and Other Infections | |
Introduction | p. 371 |
Skin and Soft Tissue Infection | p. 372 |
Pharmacology | p. 373 |
Microbiology | p. 373 |
Clinical Studies | p. 374 |
Bone and Joint Infection | p. 378 |
Osteomyelitis | p. 378 |
Pharmacology | p. 379 |
Microbiology | p. 380 |
Clinical Studies | p. 382 |
Septic Arthritis | p. 388 |
Conclusion | p. 389 |
References | p. 390 |
Safety Overview: Toxicity, Adverse Effects, and Drug Interactions | |
Introduction | p. 398 |
Toxicity of Quinolones (Studies in Animals) | p. 399 |
General Remarks | p. 399 |
Effects on Connective Tissue Structures (Cartilage, Tendon) | p. 400 |
Neurotoxicity | p. 404 |
Phototoxicity, Photomutagenicity, and Photocarcinogenicity | p. 405 |
Nephrotoxicity | p. 406 |
Ocular Toxicity | p. 407 |
Cardiotoxicity | p. 408 |
Reproductive and Developmental Toxicity | p. 408 |
Mutagenicity and Carcinogenicity | p. 411 |
Adverse Effects of Fluoroquinolones in Clinical Studies | p. 413 |
Adverse Effects of Fluoroquinolones | p. 413 |
Adverse Effects Observed in Preregistration Clinical Trials | p. 420 |
Adverse Effects Observed in Comparative Double-Blind Studies | p. 429 |
Drug Interactions | p. 433 |
Influence of pH and Magnesium on Antibacterial Activity of Quinolones in Vitro | p. 434 |
Interactions between Quinolones and Antacids | p. 434 |
Influence of Breakfast or Dairy Products on the Bioavailability of Quinolones | p. 436 |
Interactions in Renal Elimination | p. 438 |
Interactions between Quinolones and Theophylline | p. 438 |
Interactions between Quinolones and Caffeine | p. 440 |
Interactions with Digoxin | p. 440 |
Interactions between Quinolones and Other Drugs | p. 441 |
References | p. 442 |
Use of the Quinolones in Pediatrics | |
Introduction | p. 455 |
Animal Data | p. 456 |
Quinolone Arthropathy | p. 456 |
Histopathology | p. 457 |
Possible Mechanisms | p. 458 |
Tendopathy | p. 458 |
Pharmacokinetics | p. 460 |
Clinical Experiences | p. 460 |
Tolerability | p. 460 |
Development of Resistance | p. 461 |
Quinolone-Associated Arthralgia | p. 462 |
Studied Indications | p. 463 |
Newest Compounds | p. 467 |
Recommendations | p. 468 |
Conclusion | p. 468 |
References | p. 469 |
The Quinolones: Prospects | |
Introduction | p. 477 |
Molecular Mechanisms of the Quinolones: Key Discoveries | p. 478 |
Microbiology | p. 480 |
Pharmacokinetics | p. 481 |
Clinical Uses | p. 482 |
Adverse Events | p. 483 |
Quinolones: Future Developments | p. 486 |
Current Quinolone Status and Classification | p. 487 |
Conclusion | p. 490 |
References | p. 491 |
Index | p. 497 |
Table of Contents provided by Syndetics. All Rights Reserved. |
What is included with this book?
The New copy of this book will include any supplemental materials advertised. Please check the title of the book to determine if it should include any access cards, study guides, lab manuals, CDs, etc.
The Used, Rental and eBook copies of this book are not guaranteed to include any supplemental materials. Typically, only the book itself is included. This is true even if the title states it includes any access cards, study guides, lab manuals, CDs, etc.