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PubMed1997

[Penetration of azithromycin into human neutrophils: effect of hydrogen peroxide production].

BACKGROUND: The aim of this study was to evaluate the uptake of azythromycin at therapeutic concentrations by human polymorphonuclear leukocytes (PMN), as well as the effect of environmental temperature, pH, and cell viability on this uptake. The effect of azythromycin and other macrolides on hydrogen peroxide production by PMN was also assessed. METHODS: Uptake of radiolabeled azythromycin by PMN was determined by a radiometric technique. Hydrogen peroxide production by PMN was measured by the phenol red method. RESULTS: The intracellular concentrations achieved by azythromycin in PMN were 20 to 60 fold the extracellular ones, even at extracellular concentration of 0.125 mg/l. The uptake was significantly affected by low temperature, acid pH, and cell viability. Hydrogen peroxide production was not affected by the macrolides studied. CONCLUSIONS: Azythromycin at therapeutical concentrations achieves high intracellular accumulation in human PMN. The effect of environmental temperature, pH and cell viability on uptake points out that a passive diffusion, with lysosome trapping, is the essential mechanism of azythromycin uptake by phagocytic cells. In spite of the high intracellular concentrations achieved by macrolides, hydrogen peroxide production by PMN is not affected by these compounds.

Anti-Bacterial Agents↗
PubMed1998

[Comparative trial of 3-day azithromycin versus 10-day coamoxilav course efficacy in acute sinusitis].

AIM: To investigate the validity of a short-term course of azitromycin in acute sinusitis (AS). Comparison of clinical and bacteriological effects, tolerance of azitromycin and co-amoxiclav. MATERIALS AND METHODS: 50 AS patients were given a single 500 mg daily dose of axitromycin for 3 days and 50 such patients received co-amoxiclav 625 mg 3 times a day for 10 days. The examination performed before the treatment, 72 hours, 10-12 and 26-30 days after its beginning assessed the presence of fever, head ache, pain at palpation at the site of the sinuses projection, nasal breathing and discharge. X-ray examination and microbiological analysis of the puncture biopsy from the nasal sinuses were conducted before treatment and on its day 10-12. RESULTS: On the treatment hour 72 and day 10-12 azitromycin efficiency was significantly higher than that of co-amoxiclav. Recovery on the treatment day 10-12 was registered in 41(82%) and 26(52%) patients, improvement--in 6(12%) and 21(42%), no effect--in 3(6%) and 2(4%) patients, respectively, for azitromycin and co-amoxiklav. On the treatment days 26-30, 45 and 43 patients recovered, respectively. The causative agents were mainly S.aureus and Str.pyogenes. Eradication of the pathogens in response to azitromycin occurred in 29, to co-amoxiclav in 18 patients. The latter caused side effects more frequently. CONCLUSION: Azitromycin vs. co-amoxiclav provides cure in acute sinusitis for a shorter time, is better tolerated and less toxic.

Acute Disease↗