Les nouvelles quinolones

A model of ascending urinary tract infection due to an isolate of Escherichia coli was developed in normal and streptozotocin-induced mice to compare the efficacy of norfloxacin and trimethoprim-sulphamethoxazole. Norfloxacin and trimethoprim-sulphamethoxazole both were effective in reducing the number of colony forming units of E. coli from the kidneys of normal experimentally-infected mice, although norfloxacin yielded a greater quantitative reduction of colony forming units. Norfloxacin was substantially more effective than trimethoprim-sulphamethoxazole in reducing the number of colony forming units from kidney homogenates when the test animals were diabetic. This study supports the initiation of clinical trials to evaluate norfloxacin in diabetic patients.

Norfloxacin versus trimethoprim-sulphamethoxazole: efficacy in a model of ascending urinary tract infection in normal and streptozotocin-induced diabetic mice

https://www.bmj.com/content/bmj/3/5722/585.2.full.pdf

Treatment of typhoid.

Norfloxacin (NFLX) a synthetic oral antibacterial agent of quinolone carboxylic acid, was given to 6 healthy men aged 23 to 29 years and weighing 57 to 88 kg (average 64.7 kg) at a dose of 200 mg (two 100 mg tablets) once after breakfast and its fecal and urinary recoveries were determined for 5 days after the administration. Fecal and urinary recoveries of NFLX or ciprofloxacin (CPFX) were examined under various experimental conditions where the drugs were added to the urine or feces. Effects of the drug on the clinical laboratory test parameters and side effects were also examined. The following results were obtained. 1. NFLX reached the highest level in the feces in 5 cases in 24 hours and in 1 case in 48 hours; average peak fecal level was 137.1 micrograms/g in 24 hours. Fecal recoveries were 2.32 to 36.90% in 5 days after dosing with an average of 13.83%. 2. Urinary levels of the drug reached their peaks within 24 hours (average 51.46 micrograms/ml) in all cases and then decreased. Urinary recoveries were 11.15 to 46.44% in 5 days after dosing. Both fecal and urinary levels of the drug varied greatly among the subjects. 3. The sum of the fecal and the urinary recoveries in each case varied from 13.47 to 76.88% (average 42.24%).(ABSTRACT TRUNCATED AT 250 WORDS)

Fecal and urinary excretion of norfloxacin in adults

Perspectives des nouvelles molécules antibiotiques: leur place en médecine praticiennne

Cette mise au point sur les quinolones de troisieme generation permet de degager plusieurs points importants sur cette nouvelle classe d'antibiotiques systemiques. Dans la premiere partie, concernant la pharmacie chimique, sont detailles la relation structure-activite a savoir qu'un halogene, le fluor, augmente fortement leur activite, ainsi que le mecanisme d'action, par inhibition enzymatique de l'A.D.N. gyrase bacterienne. Dans la deuxieme partie, s'interessant a la pharmacologie, sont a retenir les qualites pharmacocinetiques telles que la longue demi-vie d'elimination, la bonne diffusion dans la plupart des tissus et des milieux extra-vasculaires, un large spectre antimicrobien et une bonne tolerance. Enfin, ce travail souligne l'importance d'une bonne prescription lors d'une anti-biotherapie par ces quinolones.

Vincent Viel

Papers

Mise au point sur les quinolones de troisième génération