The quinolones:
Saved in:
| Format: | Book |
|---|---|
| Language: | English |
| Published: |
San Diego [u.a.]
Academic Press
1998
|
| Edition: | 2. ed. |
| Subjects: | |
| Online Access: | Inhaltsverzeichnis |
| Item Description: | Literaturangaben |
| Physical Description: | XX, 441 S. graph. Darst. |
| ISBN: | 0120595141 |
Staff View
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| 245 | 1 | 0 | |a The quinolones |c ed. by Vincent T. Andriole |
| 250 | |a 2. ed. | ||
| 264 | 1 | |a San Diego [u.a.] |b Academic Press |c 1998 | |
| 300 | |a XX, 441 S. |b graph. Darst. | ||
| 336 | |b txt |2 rdacontent | ||
| 337 | |b n |2 rdamedia | ||
| 338 | |b nc |2 rdacarrier | ||
| 500 | |a Literaturangaben | ||
| 650 | 7 | |a Antibacteriële activiteit |2 gtt | |
| 650 | 7 | |a Biologische activiteit |2 gtt | |
| 650 | 7 | |a Chinolonen |2 gtt | |
| 650 | 7 | |a Dynamica |2 gtt | |
| 650 | 7 | |a Farmacochemie |2 gtt | |
| 650 | 4 | |a Quinolone antibacterial agents | |
| 650 | 4 | |a Quinolones | |
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CONTENTS
Contributors xv
Preface xix
1 The Quinolones: History and Overview
Peter Ball
Introduction 2
Structure Activity Relationships 3
Antibacterial Activity 3
Mode of Action 3
Spectrum of Activity 6
Bacterial Resistance to Fluoroquinolones 8
Clinical Pharmacology 9
Penetration into Respiratory Tissues 9
Elimination Pathways 9
Clinical Uses 11
Urinary Tract Infections 11
Sexually Transmitted Diseases 12
Respiratory Infections 12
Gastrointestinal Infections 14
Skin and Soft Tissue Infections 14
Bone Infections 15
Neutropenic Cancer Patients 15
Prophylaxis 16
Pharmacoeconomic Aspects of Fluoroquinolone Usage 16
Use of Fluoroquinolones in Pediatrics 17
Adverse Drug Reactions 18
V
VI Contents
Interactions with Other Drugs 20
Interactions Reducing Absorption 20
Metabolic and Inhibitory Interactions 21
Conclusion 21
References 22
2 Chemistry and Mechanism of Action of the
Quinolone Antibacterials
Thomas D. Gootz and Katherine E. Brighty
Introduction 29
Structural and Historical Background 30
General Structural Features of the Quinolones 31
First Generation Quinolones 32
Second Generation Quinolones 34
Third Generation Quinolones 38
In Vitro Potency 39
Overall Potency 39
Activity against Representative Gram Positive Pathogens 40
Activity against Mycobacterium Tuberculosis 43
Activity against Mycoplasma Pneumoniae 43
Activity against Gram Negative Pathogens 44
Activity against Anaerobes 45
Activity against Quinolone Resistant Organisms 45
In Vivo Activity 46
Pharmacokinetics 46
Phototoxicity 47
Theophylline Interactions 48
Selectivity: Activity against Mammalian Topoisomerase II and
Genetic Toxicity 48
Chemical Properties 49
Aqueous Solubility 49
Chelation of Divalent and Trivafent Metal Cations 50
Stereochemistry 51
Future Directions 52
C 6 Amino Derivatives 52
2 Pyridones 52
Modification of the C 3 Carboxylic Acid 53
Mechanism of Action 54
Replication of DNA 54
Bacterial Topoisomerases 56
Classi/ication 56
DNA Gyrase 57
Topoisomerase IV 59
Contents Vii
Topoisomerase Sensitivity to Fluoroquinolones 60
DNA Gyrase versus Topoisomerase IV 60
Models of Fluoroquinolone Interactions with the Topoisomerases 61
Killing of Bacterial Cells by Fluoroquinolones 62
Stabilization oj the Cleavable Complex and Subsequent Events 62
The SOS Response 65
Factors That Affect the Bactericidal Activity of Quinolones 66
Conclusion 68
References 68
3 In Vitro Properties of the Quinolones
Ian Phillips, Anna King, and Kevin Shannon
Introduction 81
Gram Negative Aerobes 84
Enterobacteriaceae 84
Other Gram Negative Aerobes 88
Gram Positive Aerobes 95
Anaerobes 104
Miscellaneous Organisms 110
Miscellaneous Compounds 111
Conclusion 112
References 112
4 Bacterial Resistance to Quinolones: Mechanisms and
Clinical Implications
Thilo Kohler and Jean Claude Pechere
Introduction 117
Mechanisms of Quinolone Resistance 117
Gram Negative Bacteria 118
Escherichia coli 118
Salmonella spp. 119
Klebsiella spp. 120
Pseudomonas aeruginosa 120
Neisseria gonorrhoeae 122
Campylobacter spp. 122
Helicobacter pylori 122
Miscellaneous 123
Gram Positive Bacteria 123
Staphylococcus aureus 123
Streptococcus pneumoniae 124
Enterococcus faecalis 124
Mycobacteria 125
viii Contents
Clinical Impact of Bacterial Resistance to Quinolones 125
Prevalence of Quinolone Resistance 125
Fluoroquinolone Resistance in Hospital Practice 125
Gram Positive Cocci 126
Enterobacteriaceae 126
Other Cram Negative Rods 126
Fluoroquinolone Resistance in 128
Community Acquired Infections
Respiratory Pathogens 128
Genital Pathogens 128
Urinary Pathogens 129
Digestive Pathogens 129
Quinolone Use and Emergence of Resistance 129
References 133
5 Pharmacokinetics of the Fluoroquinolones
Tom Bergan
Basic Pharmacokinetics 144
Bioavailability 144
Serum Concentrations 146
Serum Half Life 151
Volume of Distribution 152
Elimination 152
Extravascular Penetration 157
Fluid Penetration 158
Cellular Penetration 161
Tissue Penetration 162
Effect of Gender 164
Effect of Age 164
Effect of Impaired Renal Function 165
Effect of Impaired Hepatic Function 166
Effect of Food 167
Drug Interactions 168
Influence of Disease 169
References 170
6 Use of Quinolones in Urinary Tract Infection
and Prostatitis
Lindsay E. Nicolle
Urinary Tract Infection 183
Pharmacology 186
Microbiology 187
Contents ix
Clinical Studies 188
Limitations of Available Studies 188
Acute Uncomplicated Urinary Infection 188
Acute Nonobstructive Pyelonephritis 191
Complicated Urinary Infection 192
Bacterial Prostatitis 193
Conclusion 196
References 197
7 Use of the Quinolones in Sexually Transmitted Diseases
Richard P. DiCarlo and David H. Martin
Introduction 203
Gonococcal Infections 205
Background 205
In Vitro Activity of Quinolones against Neisseria gonorrhoeae 206
Clinical Studies 207
Resistance of N. gonorrhoeae to the Quinolones 208
Chlamydia trachomatis 210
Background 210
In Vitro Activity of Quinolones against C. trachomatis 210
Clinical Studies 210
Pelvic Inflammatory Disease 213
Chancroid 214
Background 214
In Vitro Activity of Quinolones against Haemophilus ducreyi 214
Clinical Studies 215
Donovanosis 216
Bacterial Vaginosis 216
Special Toxicity Considerations When Quinolones Are
Used for Treating Sexually Transmitted Diseases 217
Conclusion 218
References 218
8 Treatment of Respiratory Infections with Quinolones
Michael S. Niederman
Introduction 229
Clinical Issues in the Therapy of Respiratory Infection 231
Community Acquired Pneumonia 231
Hospital Acquired Pneumonia 233
Acute Exacerbations of Chronic Bronchitis 234
Pharmacologic Advantages for the Use of Quinolones in
Respiratory Infection 235
X Contents
Penetration into Lung Tissue 235
Mechanism of Killing 237
Microbiologic Advantages of Quinolones for
Respiratory Infection 238
Activity against Common Respiratory Pathogens 239
Pneumococcus 239
Atypical Pathogens 240
Haemophilus influenzae 240
Anaerobes 240
Enteric Gram Negatives, Including Pseudomonas aeruginosa 241
Clinical Efficacy of Quinolones for the Therapy of Respiratory
Tract Infections 242
Community Acquired Pneumonia 242
Hospital Acquired Pneumonia 244
Acute Exacerbations of Chronic Bronchitis 245
Conclusion 246
References 246
9 Use of Quinolones in Surgery and Obstetrics
and Gynecology
Sebastian Faro and John Weigelt
Introduction 251
Surgical Wound Prophylaxis 252
Soft Tissue Infection 254
Intra abdominal Infection 255
Gynecologic Infections 256
Postoperative Pelvic Infections 258
Pelvic Inflammatory Disease 259
Upper Genital Tract Infection 260
Pregnancy 261
Conclusion 262
References 263
10 Use of the Quinolones for the Treatment and Prophylaxis
of Bacterial Gastrointestinal Infections
Davidson H. Hamer and Sherwood L. Gorbach
Introduction 267
Pharmacology 268
Microbiology 268
Effects on Human Intestinal Microflora 269
Contents xi
Clinical Studies 269
Empirical Therapy of Acute Diarrhea 269
Traveler's Diarrhea 271
Nontyphoidal Salmonellosis 272
Typhoid Fever 274
Shigellosis 276
Cholera and Other Vibrios 278
Campylobacter 279
Antimicrobial Resistance to Quinolones 279
Conclusion 280
References 281
11 Use of the Quinolones in Treatment of
Bacterial Meningitis
Rodrigo Hasbun and Vincent J. Quagliarello
Introduction 287
Pharmacology 288
In Vitro Activity of Quinolones against Meningeal Pathogens 288
Cerebrospinal Fluid Penetration of the Quinolones in Vivo 289
Animal Models 289
Humans 293
Microbiology 295
Studies of Clinical Efficacy 295
Case Reports 295
Chemoprophylaxis of Meningococcal Meningitis 296
Clinical Trial of Trovafloxacin 297
Summary 298
References 299
12 Use of the Quinolones in Immunocompromised Patients
Kenneth V. I. Rolston
Introduction 303
Risk Factors and Associated Infections 304
Rationale for Fluoroquinolone Use 306
Effect of Fluoroquinolones on Endogenous Microflora 307
Infection Prevention in Afebrile Neutropenic Patients 307
Empiric Therapy in Febrile Neutropenic Patients 309
Risk Based Therapy for Febrile Neutropenia 311
Treatment of Specific Infections 314
Legionellosis 314
Mycobacterial Infections 315
Miscellaneous Infections 316
xii Contents
Summary 317
References 318
13 Use of the Quinolones in Skin and Skin Structure
(Osteomyelitis) and Other Infections
Adolf W. Karchmer
Introduction 327
Skin and Soft Tissue Infection 328
Pharmacology 328
Microbiology 328
Clinical Studies 330
Bone and Joint Infection 333
Osteomyelitis 333
Pharmacology 334
Microbiology 334
Clinical Studies 336
Septic Arthritis 343
Conclusion 344
References 345
14 Use of the Quinolones in Pediatrics
Urs B. Schaad
Introduction 351
Animal Data 352
Quinolone Arthropathy 352
Histopathology 353
Possible Mechanisms 353
Pharmacokinetics 355
Clinical Experiences 355
Tolerability 355
Quinolone Associated Arthralgia 356
Studied Indications 357
Cystic Fibrosis 359
Complicated Urinary Tract Infection 359
Enteric Infections 359
Chronic Ear Infections 360
Neutropenia in Cancer Patients 360
Central Nervous System Infections 361
Recommendations 361
Conclusion 361
References 362
Contents Xtii
15 Safety Overview: Toxicity, Adverse Effects, and
Drug Interactions
Ralf Stahlmann and Hartmut Lode
Introduction 370
Toxicity of Quinolones (Preclinical Data) 371
General Remarks 371
Chondrotoxicity 371
Neurotoxicity 374
Phototoxicity 375
Nephrotoxicity 376
Ocular Toxicity 376
Cardiotoxicity 377
Reproductive and Developmental Toxicity 378
Male Fertility 378
Teratogenicity 378
Postnatal Studies 379
Mutagenicity and Carcinogenicity 380
Adverse Effects of Fluoroquinolones in Clinical Studies 382
Adverse Effects of Fluoroquinolones 382
Gastrointestinal Reactions 383
Central Nervous System Reactions 383
Skin Reactions (Hypersensiti\ity, Phototoxicity) 384
Musculoskeletal Reactions (Arthralgia, Tendinitis) 385
Cardiovascular Reactions 387
Renal Reactions 387
Other Rarely Registered Adverse Effects 387
Adverse Effects Observed in Preregistration Clinical Trials 387
Norfloxacin 388
Ciprofloxacin 389
Ofloxacin (Levofloxacin) 390
Enoxacin 391
Pefloxacin 392
Fleroxacin 392
Sparfloxacin 393
Grepajloxacin 394
Trovafloxacin 396
Adverse Effects Observed in Comparative Double Blind Studies 396
Drug Interactions 399
Influence of pH and Magnesium on Antibacterial Activity
of Quinolones in Vitro 400
Interactions Between Quinolones and Antacids 400
Influence of a Breakfast or Dairy Products on the
Bioavailability of Quinolones 403
Interactions in Renal Elimination 403
xiv Contents
Interactions between Quinolones and Theophylline 403
Interactions between Quinolones and Caffeine 405
Interactions between Quinolones and Other Drugs 406
References 407
16 The Quinolones: Prospects
Vincent T. Andriole
Introduction 417
Historical Perspectives 418
Molecular Mechanisms of the Quinolones 418
Microbiology 419
Pharmacokinetics 420
Clinical Uses 421
Adverse Events 421
Quinolones: Future Developments 422
Current Quinolone Status and Classification 424
Summary 426
References 426
Index 431 |
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| spelling | The quinolones ed. by Vincent T. Andriole 2. ed. San Diego [u.a.] Academic Press 1998 XX, 441 S. graph. Darst. txt rdacontent n rdamedia nc rdacarrier Literaturangaben Antibacteriële activiteit gtt Biologische activiteit gtt Chinolonen gtt Dynamica gtt Farmacochemie gtt Quinolone antibacterial agents Quinolones Gyrasehemmer (DE-588)4217839-3 gnd rswk-swf (DE-588)4143413-4 Aufsatzsammlung gnd-content Gyrasehemmer (DE-588)4217839-3 s DE-604 Andriole, Vincent T. Sonstige oth HBZ Datenaustausch application/pdf http://bvbr.bib-bvb.de:8991/F?func=service&doc_library=BVB01&local_base=BVB01&doc_number=008273433&sequence=000002&line_number=0001&func_code=DB_RECORDS&service_type=MEDIA Inhaltsverzeichnis |
| spellingShingle | The quinolones Antibacteriële activiteit gtt Biologische activiteit gtt Chinolonen gtt Dynamica gtt Farmacochemie gtt Quinolone antibacterial agents Quinolones Gyrasehemmer (DE-588)4217839-3 gnd |
| subject_GND | (DE-588)4217839-3 (DE-588)4143413-4 |
| title | The quinolones |
| title_auth | The quinolones |
| title_exact_search | The quinolones |
| title_full | The quinolones ed. by Vincent T. Andriole |
| title_fullStr | The quinolones ed. by Vincent T. Andriole |
| title_full_unstemmed | The quinolones ed. by Vincent T. Andriole |
| title_short | The quinolones |
| title_sort | the quinolones |
| topic | Antibacteriële activiteit gtt Biologische activiteit gtt Chinolonen gtt Dynamica gtt Farmacochemie gtt Quinolone antibacterial agents Quinolones Gyrasehemmer (DE-588)4217839-3 gnd |
| topic_facet | Antibacteriële activiteit Biologische activiteit Chinolonen Dynamica Farmacochemie Quinolone antibacterial agents Quinolones Gyrasehemmer Aufsatzsammlung |
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