Temafloxacin hydrochloride, a new fluoroquinolone, was given orally in doses of 300 or 600 mg twice daily for ten days to 36 patients, all hospitalized because of severe acute purulent exacerbations of chronic bronchitis. Sputum cultures before, during and after treatment showed that the infection was eliminated in 12/18 evaluable patients given 300 mg and in 13/16 receiving the 600 mg doses. Haemophilus influenzae, Branhamella catarrhalis and Streptococcus pneumoniae were effectively eliminated, but only half the Pseudomonas aeruginosa infections were eradicated. MICs for most pathogens were 1 mg/l or less (including the majority of the pneumococci) but the MICs for Ps. aeruginosa ranged from 0.5 to greater than 16 mg/l, those for 10 of the 22 strains being greater than 2 mg/l. Pharmacokinetic studies on serum and sputum specimens showed serum Cmax values of 3.5 and 6.0 mg/l, the sputum Cmax being 2.35 and 4.17 mg/l after the different doses. No interaction with concomitant theophylline could be found. Two patients complained of moderate nausea or water-brash. Temafloxacin can be considered safe and effective at these dosages, but for Ps. aeruginosa infections higher dosages need to be investigated.
In a double-blind prospective study, 180 patients admitted to hospital with acute purulent exacerbations of chronic bronchitis were treated for seven days with twice daily 1 g intramuscular injections of either cefodizime or cefotaxime. Sputum cultures performed before, during and immediately after treatment showed complete eradication of the infection in 89/90 given cefodizime and 86/90 receiving cefotaxime. Some symptomatic Pseudomonas aeruginosa superinfections occurred with each agent. During the follow-up week, recurrences or reinfections after apparent clearance occurred in 15 patients given cefodizime and in 21 receiving cefotaxime. Pharmacokinetic studies in blood showed mean Cmax values of 50.8 mg/l for cefodizime and 36.5 mg/l for cefotaxime, corresponding values in the sputum being 1.61 and 0.62 mg/l. Mean AUC values in both blood and sputum were 2 1/2- to 3-fold higher for cefodizime. Some features suggested better performance by cefodizime than by cefotaxime, but the clinical results were not statistically significantly different.
In normal human lungs, neuroendocrine (NE) cells can be found as solitary NE cells and in corpuscular aggregates, the neuroepithelial bodies. By means of a quantitative morphometric method, we compared the number and distribution of chromogranin-reactive NE cells in anthracosilicotic and control lungs. After death, 14 pairs of control and 12 pairs of anthracosilicotic lungs were sampled. The extents of anthracosilicosis and emphysema were described for the right lung. The left upper lobe was used for quantitative determination of the number and distribution of NE cells, visualized by immunohistochemical staining for chromogranin. In contrast to expectations, we found no statistical difference in the numbers of chromogranin-reactive NE cells per 10 cm of epithelium between control (11.0) and anthracosilicotic (2.4) lungs. In both groups, there was a much greater number of chromogranin-reactive cells in the more peripheral compared to the central airways. Most peripheral NE cells were arranged in neuroepithelial bodies, which were not found in the central airways.
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