amoxicillin-potassium-clavulanate-combination and bacampicillin

Oral treatment of groups of four mice with different daily dosages of three related antibiotics, amoxycillin, augmentin and bacampicillin, has indicated the influence of the amount of the dose that reaches the intestine in a biologically active form. Augmentin (amoxycillin plus clavulanic acid to protect it against enzymatic hydrolysis) appeared to have a suppressive effect on the indigenous colonization-resistance-associated microflora. Dose-effect curves of amoxycillin alone, showed the same shape but at a lower level. Bacampicillin treatment practically did not have an effect on the faecal flora. Only at doses of bacampicillin of well above 1.5 mg per day, an indication was seen of CR-flora disturbance. At a dose level of 2 mg and more per day, a low concentration of beta-aspartylglycine was found in the faeces. A normal undisturbed intestinal flora normally produces in mice sufficient enzyme to degrade completely this dipeptide released by the host organism into the intestinal tract.

Topics: Administration, Oral; Amoxicillin; Amoxicillin-Potassium Clavulanate Combination; Ampicillin; Animals; Clavulanic Acids; Dose-Response Relationship, Drug; Drug Therapy, Combination; Enterobacteriaceae; Escherichia coli; Feces; Female; Mice; Streptococcus

During the three years 1981-3, 134 (9.1%) of 1473 patients presenting at our clinics were found to be infected with penicillinase producing strains of Neisseria gonorrhoeae (PPNG). Minimum inhibitory concentrations (MICs) of benzylpenicillin and ampicillin against these PPNG strains were 8 mg/l or more, whereas against non-PPNG strains they were consistently 4 mg/l or less. In contrast, the MIC of BRL25000 (two parts amoxycillin and one part clavulanic acid, the beta lactamase inhibitor) was 4 mg/l or less even against PPNG strains. MICs of a number of other drugs commonly used to treat gonorrhoea, such as cephaloridine, cefoxitin, tetracycline, doxycycline, minocycline, kanamycin, and spectinomycin, showed no appreciable differences between non-PPNG and PPNG strains and the MIC of cephaloridine in particular was relatively high. BRL25000 proved to be very effective in the treatment of PPNG infection and cured all of 121 patients treated. A daily dose of 2.25g, cured 105 patients in two days, 11 patients in three days, four patients in four days, and one patient in five days. A new rapid diagnostic method for detecting PPNG strains, capable of application at an outpatient clinic and providing a result on the following day, is described.

Topics: Amoxicillin; Amoxicillin-Potassium Clavulanate Combination; Ampicillin; Clavulanic Acids; Drug Combinations; Female; Gonorrhea; Humans; Japan; Male; Neisseria gonorrhoeae; Penicillinase