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PubMed1998

[Phenotypic characterization of erythromycin resistance in strains of the genus Streptococcus isolated from clinical specimens].

There are presently two recognized mechanisms of resistance to macrolide antibiotics in species of the genus Streptococcus: target modification and efflux. Target modification occurs in the ribosomes through the production of a ribosomal methylase codified for the erm genes and it is phenotypically known as MLSB resistance. Expression of MLSB resistance can be inducible or constitutive. Active efflux has been recently described in S. pyogenes and S. pneumoniae, and its expression is known as M phenotype. We studied the susceptibility, by determining the MIC using agar dilution, to penicillin, erythromycin and clindamycin, of 295 strains of the genus Streptococcus clinically isolated from 1993 to 1996 (70 S. pyogenes, 81 S. pneumoniae, 37 viridans group, and 107 S. milleri). We also studied the phenotype pattern of erythromycin-clindamycin resistance in the strains resistant to erythromycin by using the double-disc test. We found a 17.2% resistance to erythromycin and a 12.5% resistance to clindamycin. The M phenotype, initially described in S. pyogenes, was also observed in 6.6% of our S. pneumoniae strains, 25% of S. viridans spp., and 4.8% in the S. milleri group.

Anti-Bacterial Agents↗
PubMed1987

High-performance liquid chromatographic assay of erythromycin and its esters using electrochemical detection.

A high-performance liquid chromatographic analysis of erythromycin and its esters in plasma, urine and saliva is presented. A diethyl ether extract of sample was chromatographed on a reversed-phase column and components of the column effluent were monitored by electrochemical detection at +0.9 V (vs. Ag/AgCl). The method sensitivity limit was 10 ng with inter-day coefficients of variation from 3.2 to 10.3%. In order to assess precisely the relative concentrations of erythromycin esters (ethylsuccinate or estolate) and their active by-product erythromycin base, it is necessary to adopt measures preventing their continuous hydrolysis in biological fluids and during sample preparation.

Chromatography, High Pressure Liquid↗
PubMed1981

Pharmacokinetics of erythromycin ethylsuccinate and estolate in infants under 4 months of age.

We studied the pharmacokinetics of erythromycin estolate and ethylsuccinate suspensions in infants under 4 months of age who were being treated for chlamydial infections or pertussis. We conducted our studies after the initial dose of 10 mg/kg and subsequently during steady-state treatment. The estolate preparation resulted in higher peak concentrations in sera, and its absorption and elimination half-lives were longer. Peak concentrations occurred 3 h after a dose with the estolate preparation and 1 h after a dose with the ethylsuccinate preparation. The area under the curve for the estolate preparation was about three times greater than that for the ethylsuccinate preparation. Based on these findings, we recommend that erythromycin estolate suspensions be given to young infants at 8- or 12-h intervals (30 mg/kg per day in three divided doses or 20 mg/kg per day in two divided doses) and that erythromycin ethylsuccinate is best given at 6-h intervals (40 mg/kg per day in four divided doses).

Chlamydia Infections↗
PubMed1988

The determination of water in erythromycin by Karl Fischer titration.

Important interlaboratory variation was obtained for the water content of erythromycin samples as determined by the Karl Fischer method. It is demonstrated that the variation is related to the type of reagents used. In poorly buffered systems erythromycin enol ether and water are formed by acid degradation of erythromycin. However, when an appropriate solvent is used, accurate titration of water in erythromycin is possible. A 10% m/v solution of imidazole in methanol is preferred to pyridine or a mixture of pyridine and methanol for it has a good buffer capacity, it lacks the unpleasant odour of pyridine and it allows a high titration speed.

Journal Article↗
PubMed1998

In-vitro susceptibility of group A beta-haemolytic streptococci (GABHS) to penicillin, erythromycin, clarithromycin and azithromycin in Styria, Austria.

248 Strains of group A beta-haemolytic streptococci (GABHS) were tested against penicillin and the macrolide antibiotics, erythromycin, clarithromycin and azithromycin. 213 (85.9%) GABHS isolates were taken from throat swabs from patients with pharyngotonsillitis, 35 isolates (14.1%) were from other body sites or from invasive infections. The age of the patients ranged from 9 months to 89 years, 155 of the patients (62.5%) were below 10 years of age. The results of the E-test method and a disk diffusion assay were compared; to classify the phenotype of the erythromycin-resistant strains, a disk induction test was carried out. None of the 248 GABHS strains showed resistance to penicillin, whereas 53 GABHS isolates (21.4%) were resistant to the macrolide antibiotics included in the test. There were only minor discrepancies between the two testing methods. The MIC data obtained with the E-test method suggested that among the macrolides, erythromycin and clarithromycin had slightly higher antistreptococcal activity than azithromycin in vitro. 50 (94.3%) of the erythromycin-resistant GABHS showed the pattern of novel resistance (M phenotype), 2 (3.8%) strains showed inducible resistance (IR) and 1 (1.9%) strain exhibited consecutive resistance (CR).

Adolescent↗
PubMed1979

In vitro comparison of rosamicin and erythromycin against urinary tract pathogens.

The in vitro activity of rosamicin and erythromycin was compared at various pH values against 311 strains of bacteria representing common urinary tract pathogens. Alkalinization of the media consistently and significantly increased the antibacterial activity of rosamicin against all of the organisms tested. This was also true for erythromycin except when tested against strains of Proteus. At pH 8, rosamicin was two- to sixfold more active than erythromycin against Enterobacteriaceae. The activity of both antibiotics against Pseudomonas aeruginosa was very similar when tested at pH 8. Erythromycin was twice as active as rosamicin at pH 8 against group D streptococci. The activity of both antibiotics was bacteriostatic and inoculum size dependent, regardless of the organism tested or the pH of the test media. The greater activity of rosamicin against Enterobacteriaceae warrants clinical investigation.

Anti-Bacterial Agents↗
PubMed2003

Clinical and molecular epidemiology of erythromycin-resistant beta-hemolytic lancefield group G streptococci causing bacteremia.

Among 100 patients with group G beta-hemolytic streptococcal bacteremia in a 6-year period (1997 to 2002), seven had bacteremia caused by erythromycin-resistant strains. Five of the seven patients had cellulitis and/or abscesses. The two isolates resistant to erythromycin and clindamycin possessed erm genes, one ermTR and the other ermB. The five isolates resistant to erythromycin but sensitive to clindamycin and one of those resistant to both erythromycin and clindamycin possessed mef genes.

Bacteremia↗
PubMed2000

[Clinical evaluation of the paste of erythromycin ethylsuccinate-metronidazole CP for root canal sterilization].

OBJECTIVE: The infected root canal was sterilized by anti-bacteria compound paste and the efficacy was compared with FC. METHODS: According to the mixed infection in infected root canal of anaerobic bacteria and obligate anaerobe, the paste made of erythromycin ethylsuccinate, metronidazole and CP was selected to seal and sterilize the root canal. RESULTS: The clinical observation of 180 patients with entirely developed root apex of acute and chronic apical periodontitis shown that there was no significant difference comparing erythromycin ethylsuccinate metronidazole-CP with FC in root canal sterilization, therefore, the irritability and poisonousness of the paste can be reduced by using erythromycin ethylsuccinate metronidazole CP instead of FC. CONCLUSION: The root canal sterilization drug of erythromycin ethylsuccinate metronidazole-CP was a safe and effective method to promote the restoration of root apex diseases.

English Abstract↗
PubMed1987

Quantitative determination of erythromycin 2'-ethylsuccinate in human plasma by fast atom bombardment mass spectrometry.

A method for simultaneous quantitative determination of erythromycin 2'-ethylsuccinate and erythromycin in human plasma is described. After extracting the deuterium-labelled internal standards and analytes from alkalinized plasma to diethyl ether the extracts were analysed by fast atom bombardment mass spectrometry. The quantification limit for 2'-ethylsuccinate ester was 50 ng ml-1 and for erythromycin 100 ng ml-1. The calibration curves were linear up to 5 micrograms ml-1 for both. The precision of the method at higher concentration was less than 2% and at the quantification limit approximately 6% for both analytes.

Deuterium↗
PubMedDate not supplied

Erythromycin-sulfisoxazole for persistent acute otitis media due to ampicillin-resistant Haemophilus influenzae.

In patients with acute otitis media who had failed to improve with ampicillin therapy, 35% of Haemophilus strains isolated from the middle ear were ampicillin-resistant. Twenty-nine children (24 of whom had failed to respond to ampicillin) were treated with 40 mg erythromycin ethylsuccinate per kg per day and 100 to 150 mg sulfisoxazole per kg per day. Middle ear exudate was cultured on chocolate and 5% sheep blood agar. Twenty-three of 29 Haemophilus isolates were nontypable, 10% (3 children) were type b, 2 were Haemophilus parainfluenzae and one was not typed. All strains were resistant to ampicillin by disc susceptibility testing, and 28 of 29 strains produced beta-lactamase. The minimal inhibitory concentration of ampicillin for 15 strains ranged from 3.12 to 100 micrograms/ml (median, 6.25 micrograms/ml). The erythromycin ethylsuccinate and acetyl sulfisoxazole combination was effective in treatment of acute otitis media secondary to ampicillin-resistant Haemophilus influenzae. After 10 days of erythromycin ethylsuccinate-sulfisoxazole therapy, 18 patients had normal tympanic membranes. Of 11 with middle ear effusion, 7 cleared, 3 had recurrent otitis media within 1 month and 1 had persistent otitis media with effusion. Our experience suggests the efficacy of this combination in otitis media caused by ampicillin-resistant H. influenzae.

Acute Disease↗
PubMed1983

Interaction between warfarin and erythromycin.

In the patient described, marked exacerbation of the hypoprothrombinemic response to warfarin coincided with the addition of erythromycin to the drug regimen. A subsequent study in rats provided evidence that erythromycin is capable of increasing the anticoagulant response to single doses of warfarin. On the basis of case findings, preliminary laboratory data, and related clinical data we conclude that the interaction between warfarin and erythromycin is one of potential significance.

Animals↗
PubMed1980

Influence of food on absorption of erythromycin ethyl succinate.

Erythromycin plasma concentrations were determined in 18 subjects after a single dose (800 mg) of a new formulation of erythromycin ethyl succinate taken immediately before, immediately after, and 1 h after food. Adequate absorption occurred with all treatments, although bioavailability was best when the drug was taken before food. Absorption was delayed by food, with the highest and earliest peak plasma erythromycin levels occurring under fasting conditions.

Adult↗
PubMed1963

ALTERATION IN TRANSFORMABILITY OF DIPLOCOCCUS PNEUMONIAE AFTER THE ACQUISITION OF GENETIC DETERMINANTS INDUCING RESISTANCE TO ERYTHROMYCIN.

Sirotnak, Francis M. (Sloan-Kettering Institute for Cancer Research, New York, N.Y.), Ramona B. Lunt, and Dorris J. Hutchison. Alteration in transformability of Diplococcus pneumoniae after the acquisition of genetic determinants inducing resistance to erythromycin. J. Bacteriol. 86:735-739. 1963.-The genetic alteration of a highly transformable (competent) recipient strain of Diplococcus pneumoniae by the transformation of at least two of three identified erythromycin-resistance determinants (Ery(a), Ery(b), Ery(c)) results in a marked decrease (Ery(a-b) recombinant) or complete loss (Ery(a-c) recombinant) in the ability to be transformed. The occurrence of transformable cells in cultures of the R6 Ery(a-b) recombinant strains, although greatly diminished, still varies during growth in a manner characteristic of the fully competent parent strain. Both Ery(b) and Ery(c) determinants appear to be linked to Ery(a). In experiments using P(32)-labeled deoxyribonucleic acid (DNA), data correlating DNA uptake with transformation show a decrease or loss in uptake capacity of the erythromycin-resistant strains.

DNA↗
PubMed1983

Erythromycin estolate and jaundice.

Using prescription-event monitoring to determine whether erythromycin estolate was a more frequent cause of jaundice than erythromycin stearate or tetracycline 12 208 patients, for whom 5343 doctors had prescribed one of the three drugs, were identified by the Prescription Pricing Authority. Of the questionnaires sent to general practitioners about the possible occurrence of jaundice, 76% were returned. There were 16 reports of jaundice, of which four were attributable to gall stones, three to cancer, six to viral hepatitis, and only three were possibly related to an antibiotic. All three patients, in whom the antibiotic was a possible cause, had been treated with erythromycin stearate. No case was attributable to the estolate which had previously been suspected of being a more frequent cause of jaundice. Although the incidence is unknown, it is very unlikely to be more than one in 100.

Adolescent↗
PubMed1989

Roxithromycin compared with erythromycin against genitourinary chlamydial infections.

The efficacy and safety of roxithromycin 300 mg once a day was compared with that of erythromycin 500 mg twice a day, both for seven days, in a double blind study of 281 patients (188 men, 93 women) with genitourinary chlamydial infections. At the end of the treatment 251 (89%) patients were evaluable, and at follow up two weeks later 227 (81%) were evaluable. The bacteriological cure rate was close to 100% at the end of both treatment regimens. At follow up 55/75 (73%) evaluable men and 38/39 (97%) evaluable women treated with roxithromycin were chlamydia negative compared with 50/71 (70%) evaluable men and 37/42 (88%) evaluable women treated with erythromycin. Of the 47 who were still chlamydia positive, reinfection could not be excluded in half the men and all the women. Side effects were mainly gastrointestinal and were found in about 15% of patients receiving each treatment, but did not necessitate discontinuing treatment in any case. Roxithromycin seems to be as safe and efficacious as erythromycin in treating chlamydial infections in men and women, and it has the advantage that treatment is by a single daily dose.

Chlamydia Infections↗
PubMedDate not supplied

Erythromycin toxicity in primary cultures of rat hepatocytes.

Cultured rat hepatocytes were used to study the toxicity of erythromycin base (EB), erythromycin estolate (EE) and a new fluorinated derivative, (8S)-8-fluoroerythromycin A (EF). EF was not cytotoxic after 18 h incubation at concentrations up to 8 X 10(-4) M and EE was much more toxic than EB at all concentrations studied. EE toxicity was greater in a serum-free medium and was not increased by induction of cytochrome P-450 with phenobarbitone. In hepatocytes co-cultured with rat-liver epithelial cells EE, but not EF, raised the cytochrome P-450 content and formed stable cytochrome P-450 complexes with about 40% of the haemoprotein. The lack of correlation between cytochrome P-450 content and cytotoxicity suggests that some of the parent erythromycin drugs and not their metabolites are the toxic entities.

Animals↗
PubMedDate not supplied

Metabolism of propionyl erythromycin lauryl sulfate. II. Fate of the lauryl sulfate moiety in the rat and man.

The absorption, excretion, and metabolism of [1-14C]lauryl sulfate as either the sodium or propionyl erythromycin salt has been studied in the rat and man. In the rat 88% of the radiolabel from propionyl erythromycin [1-14C]lauryl sulfate was excreted in the urine in the 24-hr period following a single oral dose. More than 95% of the radiolabel was excreted as the metabolite butyric acid 4-sulfate. This metabolite was shown to be derived from carbons 1-4 of the lauryl sulfate moiety. There was no evidence of sulfate cleavage in the rat. In man 51-59% of the administered ratioactivity was recovered in the urine. The major excretion product was butyric acid 4-sulfate accounting for approximately 95% of urinary radioactivity. The remainder was unchanged lauryl sulfate. A significant portion of the radiolabeled propionyl erythromycin lauryl sulfate was converted to 14CO2 indicating that the sulfate linkage was cleaved. A minimum value of 9-16% of the dose was metabolized in this manner.

Animals↗
PubMed1988

[Multicenter study of the clinical efficacy and tolerance of roxithromycin compared to erythromycin ethylsuccinate in lower respiratory tract infections].

In a double blind, randomised investigation in 193 hospitalized patients, with low respiratory infections, roxithromycin (150 mg bd) and erythromycin ethylsuccinate (1 g bd) were compared. Assessment of safety was made in 183 patients and clinical response in 155 patients. The mean duration of treatment was 11 days in both groups. Clinical effectiveness was 82% (67/82) for roxithromycin and 77% (56/73) for erythromycin ethylsuccinate. Roxithromycin appears to have a good effectiveness and to be effective as erythromycin ethylsuccinate. The safety profile is satisfactory in both groups.

Adolescent↗