摘要:

SummaryA series of experiments was carried out in vitro to investigate the activity of erythromycin, used alone or in combination with penicillin, against staphylococci, pneumococci and Group A streptococci at various stages of their growth. The results showed that at concentrations of 1.0μg/ml, 3.0μg/ml and even at the minimum inhibitory concentration of 0.6μg/ml against Staphylococcus aureus SG511, erythromycin produced a marked reduction in bacterial counts. It is suggested that erythromycin and other antibiotics that inhibit protein synthesis may induce anabolic andcatabolic insufficiency inmicro-organisms. When 3.0 fig erythromycin/ml'was combined with 1 unit penicillin/ml, the effect of erythromycin on bacteria previously exposed to penicillin was found to be more satisfactory than that of the opposite sequence. The effect of 0.1μg erythromycin/ml on pneumococci (MIC:0.031μg/ml) was to induce a similar reduction in bacterial counts, as did the combination with 1 unit penicillinjml {MIC: 0.031μg/ml). The effect of 0.2μg erythromycin/ml on the streptococcal counts was weaker, as also was that of 0.2 units penicillin/ml (MICs: 0.031μg/ml, and 0.031 units/ml). When the antibiotics were combined, the results were similar to those obtained with the other bacterial species.

ISSN:0300-7995    

DOI:10.1185/03007997809110242

出版商:Taylor&Francis    

年代:1978

数据来源: Taylor

摘要:

SummaryA study was carried out in 15 healthy volunteers to investigate the absorption of erythromycin after oral administration when given on an empty stomach or together with food. Plasma concentrations were measured from capillary blood samples collected at various times after administration of a single 500 mg tablet dose of erythromycin stearate to subjects who had fasted overnight and received no food for a further 3 hours. The measurements were repeated, 1 week later, when the subjects took the test dose immediately before a standardized breakfast. In a third series, measurements were taken at steady state. The volunteers had taken their first tablet on Day 7 with food, having received 1 tablet (500 mg) 8 hourly from Day 1. The results showed that the single dose taken on an empty stomach produced the lowest peak plasma concentration. Peak plasma concentration was not only significantly higher but was reached 1 hour earlier when the test dose was taken immediately before a meal, and the findings were not significantly different in the steady state series. It is recommended, therefore, that patients being treated with erythromycin stearate should be instructed to take their tablets just before a meal and not, as previously advised, 1 hour before or 2 hours afterwards.

ISSN:0300-7995    

DOI:10.1185/03007997809110243

出版商:Taylor&Francis    

年代:1978

数据来源: Taylor

摘要:

SummarySputum and serum levels of erythromycin were investigated in 20 adult patients with bronchial disease after oral administration of 500 mg erythromycin stearate and in 20 healthy volunteers after an intravenous infusion of 500 mg erythromycin lactobionate. For comparison, saliva and serum levels were also investigated in 6 healthy volunteers after an intravenous infusion, and after an oral liquid dose of 500 mg erythromycin ethylsuccinate. In the 6 hours after the first dose of erythromycin stearate, sputum concentrations of between 0.2 and 0.6μg/ml were achieved, sufficient for the elimination of most pathogenic bacteria in acute or chronic bronchitis, and were maintained with 500 mg doses 3-times daily. Intravenous infusion resulted in sputum levels approximately 2 to 3 times higher. In healthy volunteers, peak concentrations in saliva and serum after oral administration were only about 15 % of the peak concentrations after intravenous infusion. The ratio between saliva and serum levels was constant and lower (3:1) inpatients. Similar differences between saliva/serum and sputum/serum ratios were also found in patients with bronchial disease.

ISSN:0300-7995    

DOI:10.1185/03007997809110244

出版商:Taylor&Francis    

年代:1978

数据来源: Taylor

摘要:

SummarySerum and sputum levels of erythromycin and ampicillin were measured over a 24-hour period after single oral 500 mg doses in 30 patients with chronic bronchial disease. Although the serum level curves were similar for both antibiotics, sputum levels were considerably higher and more prolonged with erythromycin. Three groups of 10 patients were each given a different dosage regimen of erythromycin to see which was the most effective in maintaining high serum and sputum levels. Patients received either 250 mg 5-times at 4-hourly intervals, 250 mg 4-times at 6-hourly intervals, or 500 mg 4-times at 6-hourly intervals, and serum and sputum levels were measured over a 24-hour period. The results showed that similar, significantly higher sputum levels were achieved and maintained with the 500 mg 4-times and the 250 mg 5-times dosage regimens than with the 250 mg 4-times dosage regimen.

ISSN:0300-7995    

DOI:10.1185/03007997809110245

出版商:Taylor&Francis    

年代:1978

数据来源: Taylor

摘要:

SummaryConcentrations of erythromycin in middle ear effusions and in plasma were measured at various periods of time in a total of 65 patients, with secretory otitis media requiring myringotomy, who had been treated with a standard dosage for up to 10 days. After an initial slow penetration into the effusion, the mean concentrations of erythromycin were equal in plasma and secretion at the steady state level, although higher concentrations in secretion than in plasma were measured in more than half the patients. Erythromycin remained at higher concentrations and for a longer time in middle ear secretions than in plasma when administration was stopped.

ISSN:0300-7995    

DOI:10.1185/03007997809110246

出版商:Taylor&Francis    

年代:1978

数据来源: Taylor

摘要:

SummaryConcentrations of erythromycin in seminal plasma and in blood plasma were investigated in 11 healthy volunteers after a 1 g oral dose, and in 15 patients with sub-clinical prostatitis treated with 500 mg 8-hourly for 3 to 5 days. In the volunteers, peak concentrations of the antibiotic in blood plasma were noted 3 to 4 hours after drug intake and 4 to 6 hours after in seminal plasma. In the patients, similar mean values and ranges to those in the volunteers were found in seminal plasma. Analysis of the various fractions of split ejaculates from the volunteers revealed similar secretory patterns for zinc and for erythromycin, indicating that the antibiotic was mainly secreted in the seminal plasma by the prostate.

ISSN:0300-7995    

DOI:10.1185/03007997809110247

出版商:Taylor&Francis    

年代:1978

数据来源: Taylor

摘要:

SummaryA clinical and pharmacological evaluation of erythromycin ethylsuccinate was carried out in 20 patients with acute exacerbations of chronic bronchitis. Administration of a 1 g dose after a meal on Day 1 produced serum concentrations of 3.36μg/ml after 60 min and 3.12μg/ml after 90 min. Serum levels on Day 4 of treatment with 1 g 4-times daily showed an accumulation of erythromycin, concentrations of over 4μg/ml being found at 1 to 2 hours after the first dose. Twelve of the 15 patients with microscopic evidence of pus in the sputum and positive for H. influenzae (12) and/or pneumococci (5) showed a satisfactory response to treatment, as did the other 5 patients with negative cultures. In the 3 patients who failed to respond clinically, H. influenzae was still present on culture and the sputum remained purulent. In 2 patients regarded as clinically cured, the sputum was mucoid but H. influenzae persisted. There was no evidence of patient intolerance of treatment with erythromycin ethylsuccinate.

ISSN:0300-7995    

DOI:10.1185/03007997809110248

出版商:Taylor&Francis    

年代:1978

数据来源: Taylor

摘要:

SummaryA study was carried out in 45 patients with non-inflammatory lung disease requiring resection of lung and/or bronchial tissue to investigate the effects of bromhexine on the concentrations of erythromycin in serum and in these tissues. The patients, randomly divided into three groups, were treated for 4 days before surgery with either erythromycin alone (1 g, 12-hourly) or given simultaneously with 16 mg or with 32 mg bromhexine 12-hourly. A final dose was given 2 to 3 hours before operation on Day 4. The results showed that there was no significant difference in the changes with time in serum concentrations of erythromycin after the final dose, nor with respect to the levels of the antibiotic in lung tissue, expressed as a percentage of serum concentrations. In bronchial tissue, however, the results suggested a dual dose-dependent effect of bromhexine, the lower doses appearing to increase and the higher doses to depress the concentrations of erythromycin.

ISSN:0300-7995    

DOI:10.1185/03007997809110249

出版商:Taylor&Francis    

年代:1978

数据来源: Taylor

摘要:

SummaryThe mechanism by which Propionibacterium acnes induces inflammatory lesions in acne vulgaris is still unknown. To investigate the effect of erythromycin stearate in acne vulgaris, the composition of the skin surface lipids was analyzed before, during and after treatment in 17 patients given 500 mg daily for 1 week and 250 mg daily for 2 months. The clinical anti-inflammatory effect was also evaluated. Quantitative thin-layer chromatography showed that the fatty acid fraction of the skin surface lipids decreased significantly in all patients during treatment. The clinical anti-inflammatory effect was good in 14 of the 17 patients. ATR-infrared spectroscopy showed that the clinical effect precedes the detectable reduction in fatty acids in the skin surface lipids. Even if a toxic effect of the fatty acids is responsible for the inflammation in most patients, an allergy to the fatty acids in some cases cannot be excluded. Sensitization tests on guinea-pigs showed that short-chained and middle-chained fatty acids, especially, are highly allergenic. The effect of erythromycin stearate on the lipase activity was also studied in a model system (purified pancreatic lipase). The enzyme activity was not affected by exposure to the drug. Consequently, the effect of erythromycin stearate on P. acnes was evaluated in acne patients, the bacteria being identified by aid of gas-chromatography. All the strains isolated were highly sensitive to erythromycin stearate before and after treatment. Semi-quantitative screening of P. acnes isolates on Tween 80 and tributyrine agar dishes after erythromycin stearate therapy indicated that P. acnes strains lacked lipolytic activity. However, in none of the patients' pustules or cysts was P. acnes completely inhibited. Sub-culturing demonstrated no significant quantitative decrease in the numbers of P. acnes after 1 week of therapy but did so after 4 weeks. Erythromycin stearate, therefore, may decrease the viability and numbers of P. acnes.

ISSN:0300-7995    

DOI:10.1185/03007997809110250

出版商:Taylor&Francis    

年代:1978

数据来源: Taylor

摘要:

SummaryPresent methods for in vitro sensitivity testing of non-sporing anaerobic bacteria to antibiotics have been found to be unreliable and inconsistent. Studies have been carried out, therefore, to identify the variable factors involved. The results showed that in addition to the pH of the medium, variations in a number of other factors relating both to the methodology and to the reagents used could result in major changes in disc sensitivity testing and MIC determinations for erythromycin. Procedures for standardization of method and reagents are briefly discussed.

ISSN:0300-7995    

DOI:10.1185/03007997809110251

出版商:Taylor&Francis    

年代:1978

数据来源: Taylor