Inhibitory antimicrobial concentrations against Campylobacter pylori in gastric mucosa.
Gastric mucosal concentrations of erythromycin, amoxycillin, ampicillin and ciprofloxacin were determined in patients at upper gastrointestinal endoscopy 38-480 min after a 500 mg dose of erythromycin ethyl succinate, erythromycin stearate, amoxycillin, pivampicillin or ciprofloxacin. All the agents attained concentrations greater than the MIC 90 for Campylobacter pylori. The macrolides attained the lowest concentrations. There was no significant difference between concentrations attained with erythromycin ethyl succinate and stearate. High concentrations were attained by amoxycillin (range 14.6-322 mg/kg) and pivampicillin (range 47.5-209 mg/kg). Ciprofloxacin attained very high concentrations (range 35-1762 mg/kg); inhibitory concentrations 35 mg/kg) were still present at 6 h after the dose. Ciprofloxacin and erythromycin are ineffective in vivo despite these high gastric mucosal concentrations. Penetration into the gastric mucus and crypts where C. pylori is found will be determined by physicochemical properties of the antimicrobials, such as pKa, stability, activity over a wide range of pH, and lipid solubility.
McNulty
C A
CA
Public Health Laboratory, Gloucestershire Royal Hospital, UK.
Dent
J C
JC
Ford
G A
GA
Wilkinson
S P
SP
D000328:Adult; D000368:Aged; D000369:Aged, 80 and over; D000658:Amoxicillin / Q000493:pharmacokinetics; D000900:Anti-Bacterial Agents / Q000493:pharmacokinetics*; D002167:Campylobacter / Q000187:drug effects*; D002851:Chromatography, High Pressure Liquid; D002939:Ciprofloxacin / Q000493:pharmacokinetics; D004917:Erythromycin / Q000493:pharmacokinetics; D005753:Gastric Mucosa / Q000378:metabolism* / Q000382:microbiology; D006801:Humans; D008826:Microbial Sensitivity Tests; D008875:Middle Aged; D010917:Pivampicillin / Q000493:pharmacokinetics
D000900:Anti-Bacterial Agents; D010917:Pivampicillin; D002939:Ciprofloxacin; D004917:Erythromycin; D000658:Amoxicillin