Antibiotics and Antibiotic Resistance

215 Pages·2011·3.73 MB·English

by  Ola Skold(auth.)

ANTIBIOTICS AND
ANTIBIOTIC RESISTANCE
ANTIBIOTICS AND
ANTIBIOTIC RESISTANCE
Ola Sko¨ld, M.D., Ph.D.
ProfessorofMicrobiology
UppsalaUniversity
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LibraryofCongressCataloging-in-PublicationData:
Sko¨ld,Ola.
[Antibiotikaochantibiotikaresistens.English]
Antibioticsandantibioticresistance/OlaSko¨ld.
p.;cm.
Translationof:Antibiotikaochantibiotikaresistens/OlaSko¨ld.c2006.
Includesindex.
ISBN978-0-470-43850-3(cloth)
1. Antibiotics.2. Drugresistanceinmicroorganisms. I.Title.
[DNLM:1. Anti-BacterialAgents.2. DrugResistance,Microbial. QV350]
RM267.S555132011
615(cid:2).329–dc22
2011002200
PrintedintheUnitedStatesofAmerica
ePDFISBN:978-1-118-07556-2
oBookISBN:978-1-118-07560-9
ePubISBN:978-1-118-07558-6
10987654321
TothememoryofJ.B.Neilands,ProfessorofBiochemistry,
UniversityofCalifornia,Berkeley
‘‘ThefinestGentlemanofScienceIevermet’’
CONTENTS
Preface xiii
1 ANTIBIOTICS:THEGREATESTTRIUMPH
OF SCIENTIFICMEDICINE 1
Selectivity 3
DevelopmentofResistance 4
Sulfonamide:TheFirstAntibacterialAgentActing
Selectively 5
ChemotherapeuticsandAntibiotics 9
Penicillin:TheFirstAntibiotic 9
TheFirstTherapeuticTrial 12
RediscoveryofPenicillinbyaBasicScientific
Approach 13
Betalactams 14
Streptomycin:TheSecondAntibioticintheHistory
ofAntibacterialAgents 16
TheFirstRemedyforTuberculosis 18
Conclusion 19
vii
viii CONTENTS
2 DISTRIBUTIONOF ANTIBIOTICS 21
QuantitativeEvaluationofAntibioticsConsumption 22
DefinedDailyDoses 22
InternationalDistributionofAntibiotics:
AScandinavianExample 22
ControlofAntibioticsOveruse 25
3 SULFONAMIDES AND TRIMETHOPRIM 29
GeneralAspectsRegardingtheDevelopment
ofResistance 30
Sulfonamides 32
SulfonamidesasRemedies 32
ResistancetoSulfonamide 34
ResistancetoSulfonamidesinNeisseriameningitidis 35
CharacterizationoftheSulfonamide-Resistant
DihydropteroateSynthaseinN.meningitidis 40
CharacterizationoftheOtherSulfonamide-Resistant
DihydropteroateSynthaseinN.meningitidis 42
ResistancetoSulfonamidesinStreptococcus
pyogenes 44
ResistancetoSulfonamidesinCampylobacterjejuni 46
ResistancetoSulfonamidesinStreptococcus
pneumoniae 46
ResistancetoSulfonamidesinPneumocystisjiroveci
(carinii) 47
ResistancetoSulfonamidesinStaphylococcusaureus
andS.haemolyticus 48
ResistancetoSulfonamidesinMycobacteriumleprae 49
Plasmid-BorneResistancetoSulfonamides 49
Trimethoprim 51
CONTENTS ix
InnateResistancetoTrimethoprim 55
ChromosomalResistancetoTrimethoprim 56
Plasmid-BorneResistancetoTrimethoprim 59
PossiblePathogenicityChangeinC.jejuniby
AcquiringTrimethoprimResistanceGenes 65
ExperimentalTestoftheReversibilityof
TrimethoprimResistance 66
Conclusion 67
4 PENICILLINSAND OTHER BETALACTAMS 69
TheBetalactamRing:TheCharacteristic
ofallBetalactams 70
TheAntibacterialMechanismofBetalactams 73
Penicillins 74
PenicillinswithanEnlargedSpectrum 75
PenicillinsStabletoPenicillinases 77
CounteractingResistancebytheInhibition
ofBetalactamases 80
OtherAntibacterialBetalactams 81
Cephalosporins 81
Monobactams 84
Thienamycins 85
Betalactamases 87
HorizontalSpreadofBetalactamases 87
Penicillin-BindingProteins 90
ResistancetoBetalactamsbyChangesinthePBPs 91
AVeryOldProphecyCameTrue 94
5 GLYCOPEPTIDES 95
MechanismofAntibacterialAction 96
x CONTENTS
Resistance 98
AvoparcinandClinicalResistancetoGlycopeptides 100
VancomycinasanAntibioticofLastResort 101
6 AMINOGLYCOSIDES 103
TheAntibacterialMechanismofStreptomycin 104
BactericidalEffect 106
ClinicalSideEffects 106
BacterialResistancetoAminoglycosides 109
HorizontalSpreadofAminoglycosideResistance 110
Conclusion 113
7 OTHER ANTIBIOTICSINTERFERING
WITH BACTERIALPROTEINSYNTHESIS 115
Chloramphenicol 115
ClinicalSideEffects 117
BacterialResistancetoChloramphenicol 117
Tetracyclines 119
MechanismofAction 120
ClinicalSideEffects 121
BacterialResistancetoTetracyclines 121
ErythromycinandRelatedAntibiotics 123
Macrolides 123
ResistancetoErythromycin 124
ClinicalUseofMacrolides 125
Lincosamides 125
Streptogramins 126
FusidicAcid 128
CONTENTS xi
Linezolid 129
Conclusion 131
8 QUINOLONES 133
TheEffectofQuinolonesonBacteria 134
ClinicalUseofQuinolones 136
BacterialResistancetoQuinolones 139
MutationalResistance 139
ResistancebyQuinoloneEfflux 140
TransferablePlasmid-BorneResistance 140
Conclusion 145
9 ANTIBACTERIALAGENTSNOT RELATED
TOTHE LARGE ANTIBIOTICFAMILIES 147
RemediesforTuberculosis 147
Rifampicin 149
MechanismofAction 150
Resistance 151
Plasmid-BorneResistance 151
OtherAgentsAgainstTuberculosis 152
IsoniazidorIsonicotinicAcidHydrazide 153
Pyrazinamide 154
Ethambutol 155
Cycloserine 156
para-AminosalicylicAcid 157
TuberculostaticDrugsRecruitedfromEarlier
KnownGroupsofAntibioticsFoundOriginally
withOtherAntibacterialSpectra 158
xii CONTENTS
Diarylquinolines 159
TheBattleAgainstTuberculosis 159
Nitrofurantoin 161
Nitroimidazoles 161
Phosphomycin 163
Conclusion 165
10 MECHANISMS FOR THE HORIZONTALSPREAD
OF ANTIBIOTICRESISTANCEAMONG BACTERIA 167
TransferableResistance:Conjugation 167
MutationalResistance 170
Plasmid-BorneResistanceAgainstAntibacterial
Agents 171
Plasmids 173
TheOriginofRPlasmids 176
Transposons 178
Integrons 182
11 HOW TOMANAGE ANTIBIOTICRESISTANCE 187
CrossResistanceBetweenRelatedAntibiotics 188
TheEvolutionofAntibacterialResistance 188
HowtoCounteractResistanceDevelopment 190
CurtailingtheUseofAntibiotics 191
IntroductionofTrulyNewAntibacterialAgents 193
AntibacterialPeptides 193
InhibitionofPathogenicity 197
InhibitionofBacterialFattyAcidSynthesis 198
ResistanceDevelopmentAccelerates 200
Index 203