Helicobacter pylori and Antibacterial Agents

André. Bryskier; John Lowther; Catherine Couturier

doi:10.1128/9781555815929.ch40

Chapter 40 : Helicobacter pylori and Antibacterial Agents

Authors: André. Bryskier, John Lowther, Catherine Couturier

Content Type: Reference

Publication Year: 2005

Category: Bacterial Pathogenesis

Book DOI: 10.1128/9781555815929

Chapter DOI: 10.1128/9781555815929.ch40

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Abstract:

The recognition of Helicobacter pylori as an etiological agent of gastric peptic ulcer, gastric adenocarcinoma, and mucosaassociated lymphoid tissue lymphoma is one of the most important advances made in gastroenterology in the past 50 years. Eradication therapy is recommended for infected persons who develop peptic ulcer disease or gastric lymphoma or who are beginning long-term treatment with nonsteroidal anti-inflammatory drugs. Among the few conserved families of efflux systems associated with bacterial resistance to antibacterial agents, one is widespread among gram-negative bacilli: the RND family. In Tartu, Estonia, 56 patients suffering from H. pylori infections were enrolled for testing of the susceptibility of H. pylori clinical isolates to antibacterial agents. There are few data regarding the H. pyloriresistance rate in the United States. The frequency of primary clarithromycin and metronidazole resistance among patients enrolled in different geographical areas in the U.S.-based clinical trials between 1993 and 1999 was assessed by MIC determinations using E-test. The rate of resistance to amoxicillin and tetracycline in this study among H. pylori isolates was low. The marked decrease of metronidazole in gastric juice after repeated administration of omeprazole is explained by the elevation of gastric pH induced by omeprazole. Ciprofloxacin was administered as a single dose of 500mg in 15 patients undergoing biopsies. Ciprofloxacin levels ranged from 1.5 to 1,762 mg/kg. Optimal concentrations were obtained after 1 h of dosing and reached 500 mg/kg. The in vitro activities of various antibacterial agents against H. pylori were assessed, including linezolid, dalfopristin-quinupristin, mupirocin, aminoglycosides, and fosfomycin.

Citation: Bryskier A, Lowther J, Couturier C. 2005. Helicobacter pylori and Antibacterial Agents, p 1011-1054. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch40

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Helicobacter pylori and Antibacterial Agents

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Figure 1

Proton pump inhibitors

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Figure 1

Proton pump inhibitors

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Figure 2

Ebrotidine

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Figure 2

Ebrotidine

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Figure 3

5-Hydroxyquinoline

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Figure 3

5-Hydroxyquinoline

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Figure 4

FR-180102

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Figure 4

FR-180102

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Figure 5

Piperidyl derivatives

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Figure 5

Piperidyl derivatives

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Figure 6

Guanidine analogs

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Figure 6

Guanidine analogs

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Figure 7

FR-145175

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Figure 7

FR-145175

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Figure 8

Triazolyl cephems

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Figure 8

Triazolyl cephems

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Figure 9

Anti-H. pylori action of cephems

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Figure 9

Anti-H. pylori action of cephems

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Figure 10

Thiazolyl cephems

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Figure 10

Thiazolyl cephems

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Figure 11

FR-182024

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Figure 11

FR-182024

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Figure 12

Macrolides with anti-H. pylori activity

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Figure 12

Macrolides with anti-H. pylori activity

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Figure 13

Telithromycin

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Figure 13

Telithromycin

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Figure 14

Cethromycin

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Figure 14

Cethromycin

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Figure 15

NADH oxidase in metronidazole-resistant H. pylori

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Figure 15

NADH oxidase in metronidazole-resistant H. pylori

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Figure 16

Bicyclic fluoroquinolone with anti-H. pylori activity

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Figure 16

Bicyclic fluoroquinolone with anti-H. pylori activity

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Figure 17

Y-26611

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Figure 17

Y-26611

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Figure 18

Y-34867

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Figure 18

Y-34867

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Figure 19

Structure and activity of natural quinolones against H. pylori

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Figure 19

Structure and activity of natural quinolones against H. pylori

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Figure 20

Rotenoids

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Figure 20

Rotenoids

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Figure 21

TAK-083

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Figure 21

TAK-083

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Figure 22

BAS-118

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Figure 22

BAS-118

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Figure 23

Catechin derivatives

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Figure 23

Catechin derivatives

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Figure 24

Pyloricidin derivatives

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Figure 24

Pyloricidin derivatives

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Figure 25

Nitazoxanide

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Figure 25

Nitazoxanide

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Figure 26

Pyrrazolyl derivatives: inhibition of DHODase of H. pylori

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Figure 26

Pyrrazolyl derivatives: inhibition of DHODase of H. pylori

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Figure 27

Plautonol

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Figure 27

Plautonol

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Figure 28

Thiourea analogs of plautonol with H. pylori activity

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Figure 28

Thiourea analogs of plautonol with H. pylori activity

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Figure 29

Diol plaunotol analogs

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Figure 29

Diol plaunotol analogs

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Figure 30

Cabreuvin

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Figure 30

Cabreuvin

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Figure 31

Calvatic acid

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Figure 31

Calvatic acid

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Figure 32

Sulforaphane

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Figure 32

Sulforaphane

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Tables

Helicobacter pylori and Antibacterial Agents

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Table 1

Main Helicobacter species and their hosts a

Table 1

Main Helicobacter species and their hosts a

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Table 2

Virulence factors of H. pylori

Table 2

Virulence factors of H. pylori

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Table 3

E-test methods for H. pylori

Table 3

E-test methods for H. pylori

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Table 4

Influence of pH on anti-H. pylori activities of various antibacterials a

Table 4

Influence of pH on anti-H. pylori activities of various antibacterials a

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Table 5

Zone size for metronidazole against H. pylori

Table 5

Zone size for metronidazole against H. pylori

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Table 6

Table 6 Prevalence of H. pylori resistance in Lisbon, Portugal

Table 6

Table 6 Prevalence of H. pylori resistance in Lisbon, Portugal

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Table 7

Prevalence of H. pylori isolates resistant to antibacterials in the United Kingdom

Table 7

Prevalence of H. pylori isolates resistant to antibacterials in the United Kingdom

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Table 8

Prevalence of H. pylori isolates resistant to antibacterials in England

Table 8

Prevalence of H. pylori isolates resistant to antibacterials in England

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Table 9

H. pylori resistance in children in Belgium

Table 9

H. pylori resistance in children in Belgium

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Table 10

Epidemiological survey in Spain for H. pylori susceptibility in children

Table 10

Epidemiological survey in Spain for H. pylori susceptibility in children

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Table 11

Prevalence (secondary) of H. pylori resistant strains in two geographical areas in Germany

Table 11

Prevalence (secondary) of H. pylori resistant strains in two geographical areas in Germany

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Table 12

Prevalence of H. pylori resistance to metronidazole in Europe from 1990 to 1991

Table 12

Prevalence of H. pylori resistance to metronidazole in Europe from 1990 to 1991

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Table 13

Prevalence of H. pylori resistance to antibacterials in Europe in 1998

Table 13

Prevalence of H. pylori resistance to antibacterials in Europe in 1998

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Table 14

Rate of resistance of H. pylori to clarithromycin (MIC, >1.0 μg/ml) in the United States

Table 14

Rate of resistance of H. pylori to clarithromycin (MIC, >1.0 μg/ml) in the United States

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Table 15

Prevalence of metronidazole and clarithromycin resistance of H. pylori in two areas in Japan

Table 15

Prevalence of metronidazole and clarithromycin resistance of H. pylori in two areas in Japan

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Table 16

Prevalence of H. pylori isolates resistant to antibacterials in Korea

Table 16

Prevalence of H. pylori isolates resistant to antibacterials in Korea

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Table 17

Clarithromycin resistance of H. pylori in Brazil

Table 17

Clarithromycin resistance of H. pylori in Brazil

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Table 18

Prevalence of H. pylori resistance in Lebanon

Table 18

Prevalence of H. pylori resistance in Lebanon

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Table 19

Prevalence of H. pylori resistance in Saudi Arabia

Table 19

Prevalence of H. pylori resistance in Saudi Arabia

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Table 20

In vitro anti-H. pylori activity of bismuth salts (n = 16) a

Table 20

In vitro anti-H. pylori activity of bismuth salts (n = 16) a

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Table 21

Anti-Helicobacter activities of proton pump inhibitors

Table 21

Anti-Helicobacter activities of proton pump inhibitors

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Table 22

Activity against urease (measured by the indophenol method)

Table 22

Activity against urease (measured by the indophenol method)

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Table 23

In vitro activities of H2-antagonists against H. pylori

Table 23

In vitro activities of H2-antagonists against H. pylori

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Table 24

Comparative anti-H. pylori activity of ebrotidine

Table 24

Comparative anti-H. pylori activity of ebrotidine

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Table 25

Comparative anti-H. pylori activity of FR-180102

Table 25

Comparative anti-H. pylori activity of FR-180102

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Table 26

Anti-H. pylori activity of piperidyl derivative a

Table 26

Anti-H. pylori activity of piperidyl derivative a

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Table 27

Anti-H2 activities of guanidino derivatives

Table 27

Anti-H2 activities of guanidino derivatives

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Table 28

Anti-H. pylori activities and anti-H2-receptors of furothiazolyl derivatives

Table 28

Anti-H. pylori activities and anti-H2-receptors of furothiazolyl derivatives

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Table 29

Anti-H2 activity of a pyridyl derivative

Table 29

Anti-H2 activity of a pyridyl derivative

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Table 30

Anti-H. pylori activity of FR-145715

Table 30

Anti-H. pylori activity of FR-145715

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Table 31

Eradication of H. pylori in gnobiotic piglets with FR-145715

Table 31

Eradication of H. pylori in gnobiotic piglets with FR-145715

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Table 32

Amino acid changes in strain 69A (amoxicillin resistant)

Table 32

Amino acid changes in strain 69A (amoxicillin resistant)

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Table 33

Concentrations of amoxicillin and ampicillin in gastric tissue

Table 33

Concentrations of amoxicillin and ampicillin in gastric tissue

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Table 34

Half-lives of degradation of antibacterials at pH 2.0

Table 34

Half-lives of degradation of antibacterials at pH 2.0

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Table 35

Intragastric pH gradient in humans a

Table 35

Intragastric pH gradient in humans a

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Table 36

Amoxicillin concentrations in serum and gastric tissues a

Table 36

Amoxicillin concentrations in serum and gastric tissues a

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Table 37

In vitro activity of FR-182024 against H. pylori isolates

Table 37

In vitro activity of FR-182024 against H. pylori isolates

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Table 38

In vitro activities of β-lactam antibiotics against H. pylori

Table 38

In vitro activities of β-lactam antibiotics against H. pylori

/content/10.1128/9781555815929.ch40.ch40tab39

Table 39

In vitro comparative activities of fropenem and other antibacterials against H. pylori (n = 100)

Table 39

In vitro comparative activities of fropenem and other antibacterials against H. pylori (n = 100)

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Table 40

In vitro activities of macrolides against H. pylori

Table 40

In vitro activities of macrolides against H. pylori

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Table 41

Kinetics of macrolide interaction with H. pylori 70S ribosomes

Table 41

Kinetics of macrolide interaction with H. pylori 70S ribosomes

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Table 42

Frequency of spontaneous mutation in H. pylori

Table 42

Frequency of spontaneous mutation in H. pylori

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Table 43

Correlation between E. coli and H. pylori numeration

Table 43

Correlation between E. coli and H. pylori numeration

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Table 44

Gastric mucosa tissue concentration of roxithromycin

Table 44

Gastric mucosa tissue concentration of roxithromycin

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Table 45

Gastric tissue level of clarithromycin and the main metabolite

Table 45

Gastric tissue level of clarithromycin and the main metabolite

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Table 46

Azithromycin concentrations in gastric juice and tissue

Table 46

Azithromycin concentrations in gastric juice and tissue

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Table 47

Gastric tissue concentration of erythromycin

Table 47

Gastric tissue concentration of erythromycin

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Table 48

In vitro activities of A-69334 and A-70310 against H. pylori

Table 48

In vitro activities of A-69334 and A-70310 against H. pylori

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Table 49

In vitro activity of telithromycin against H. pylori

Table 49

In vitro activity of telithromycin against H. pylori

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Table 50

In vitro activity of telithromycin against clarithromycin-resistant H. pylori

Table 50

In vitro activity of telithromycin against clarithromycin-resistant H. pylori

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Table 51

Influence of pH on determination of MICs for H. pylori

Table 51

Influence of pH on determination of MICs for H. pylori

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Table 52

In vitro activity of ABT-773 against H. pylori

Table 52

In vitro activity of ABT-773 against H. pylori

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Table 53

In vitro activity of ABT-773 against H. pylori isolates resistant to clarithromycin (n = 15)

Table 53

In vitro activity of ABT-773 against H. pylori isolates resistant to clarithromycin (n = 15)

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Table 54

In vitro activities of cyclines against H. pylori

Table 54

In vitro activities of cyclines against H. pylori

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Table 55

In vitro activity of metronidazole against H. pylori

Table 55

In vitro activity of metronidazole against H. pylori

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Table 56

In vitro activity of metronidazole against competent and noncompetent H. pylori strainsa

Table 56

In vitro activity of metronidazole against competent and noncompetent H. pylori strainsa

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Table 57

In vitro activities of nitroimidazole analogs against H. pyloria

Table 57

In vitro activities of nitroimidazole analogs against H. pyloria

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Table 58

Pharmacokinetics of metronidazole in gastric juice with and without omeprazole

Table 58

Pharmacokinetics of metronidazole in gastric juice with and without omeprazole

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Table 59

In vitro activities of quinolones against H. pylori

Table 59

In vitro activities of quinolones against H. pylori

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Table 60

Anti-H. pylori activities of 7-morpholinoquinolones

Table 60

Anti-H. pylori activities of 7-morpholinoquinolones

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Table 61

In vitro activities of ansamycin derivatives

Table 61

In vitro activities of ansamycin derivatives

/content/10.1128/9781555815929.ch40.ch40tab62

Table 62

In vitro activities of rifalazil and KRM-1657

Table 62

In vitro activities of rifalazil and KRM-1657

/content/10.1128/9781555815929.ch40.ch40tab63

Table 63

Bactericidal activities of ansamycins against H. pylori

Table 63

Bactericidal activities of ansamycins against H. pylori

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Table 64

Frequency of mutation induced with ansamycins against H. pylori

Table 64

Frequency of mutation induced with ansamycins against H. pylori

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Table 65

H. pylori: rpoB mutations a

Table 65

H. pylori: rpoB mutations a

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Table 66

In vitro activities of various antibacterials against H. pylori

Table 66

In vitro activities of various antibacterials against H. pylori

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Table 67

In vitro activity of TAK-083 against H. pylori (n = 54)

Table 67

In vitro activity of TAK-083 against H. pylori (n = 54)

/content/10.1128/9781555815929.ch40.ch40tab68

Table 68

In vitro activity of BAS-118 against H. pylori (n = 100)

Table 68

In vitro activity of BAS-118 against H. pylori (n = 100)

/content/10.1128/9781555815929.ch40.ch40tab69

Table 69

In vitro activity of pyloricidin B against H. pylori (n = 50)

Table 69

In vitro activity of pyloricidin B against H. pylori (n = 50)

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Table 70

In vivo activity of pyloricidin B against H. pylori

Table 70

In vivo activity of pyloricidin B against H. pylori

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Table 71

In vitro activities of azole antifungals against H. pylori

Table 71

In vitro activities of azole antifungals against H. pylori

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Table 72

Genes of pyrimidine biosynthesis and salvage pathways a

Table 72

Genes of pyrimidine biosynthesis and salvage pathways a

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Table 73

Anti-H. pylori activities of cytoprotective antiulcer agents (n = 14)

Table 73

Anti-H. pylori activities of cytoprotective antiulcer agents (n = 14)

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Table 74

In vitro activity of sucralfate

Table 74

In vitro activity of sucralfate

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Table 75

In vitro activity of calvatic acid against H. pylori

Table 75

In vitro activity of calvatic acid against H. pylori