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PubMed1982

Hepatotoxicity to both erythromycin estolate and erythromycin ethylsuccinate.

Two patients experienced hepatotoxicity associated with erythromycin estolate (Ilosone) usage, followed 13 and 15 years later by an hepatotoxic reaction with administration of erythromycin ethylsuccinate (E.E.S.). These cases provide further evidence for erythromycin ethylsuccinate-associated hepatotoxicity and demonstrate erythromycin cross-sensitivity after previous erythromycin estolate liver injury. Hepatotoxicity to both sensitivity after previous erythromycin estolate liver injury. Hepatotoxicity to both estolate and ethylsuccinate preparations of erythromycin stimulates speculation regarding the potentially hepatotoxic moiety of the erythromycin molecule. Furthermore, these cases suggest that all erythromycin preparations should be avoided or used only with careful monitoring in patients with previous erythromycin-associated liver injury.

Adult↗
PubMed1984

The pharmacokinetics and tolerance of oral erythromycin stearate compared with erythromycin ethylsuccinate: implications for preventing endocarditis.

Serum concentrations of erythromycin were monitored in 11 healthy adult volunteers following single dose oral administration of erythromycin stearate, 1.5 g, and erythromycin ethylsuccinate 3.0 g. Peak serum concentrations occurred at 30 min to 2 h after the dose, usually at 1 h. Mean serum peak erythromycin concentrations (standard deviation) were 4.8 mg/l (+/- 2.0) following 1.5 g erythromycin stearate and 2.8 mg/l (+/- 1.4) after 3.0 g erythromycin ethylsuccinate. Both types of erythromycin frequently caused mild gastrointestinal side-effects but there were fewer side-effects associated with erythromycin ethylsuccinate. However, because of the increased serum erythromycin concentrations between 1 and 6 h after the dose of the stearate preparation compared to ethylsuccinate we recommend erythromycin stearate, 1.5 g, as the preferred loading dose, given 1 h before the dental procedure, for preventing endocarditis in susceptible patients allergic to penicillin.

Administration, Oral↗
PubMed1994

Inhibition of erythromycin-resistant propionibacteria on the skin of acne patients by topical erythromycin with and without zinc.

Propionibacteria resistant to high concentrations of erythromycin [minimal inhibitory concentration (MIC) > or = 0.5 mg/ml] are now commonly isolated from the skin of antibiotic-treated acne patients. This double-blind study was carried out to assess the ability of 4% w/v erythromycin with and without 1.2% w/v zinc acetate to reduce the numbers of erythromycin-resistant propionibacteria in vivo, and also to monitor the acquisition of resistant strains de novo during therapy. Under laboratory conditions, erythromycin-resistant propionibacteria were shown to be as sensitive to zinc acetate as fully sensitive strains. In vivo, the erythromycin/zinc complex and erythromycin alone produced highly significant reductions in total propionibacteria (P < 0.001) and in the number of erythromycin-resistant strains (P < 0.001 at 8 weeks). After 12 weeks, resistant propionibacteria were reacquired, or acquired de novo, by three patients treated with erythromycin alone and four patients treated with the erythromycin/zinc complex. In contrast, changes in numbers of Micrococcaceae were slight and, after 12 weeks, erythromycin-resistant strains were predominant in both treatment groups. In vitro MIC determinations suggested that this finding might be explained by the exceptionally high degree of erythromycin resistance displayed by some staphylococcal strains (MIC > 4 mg/ml) and by the relative insensitivity of all staphylococcal strains to zinc acetate. Erythromycin with and without zinc was clinically effective, and both preparations produced significant reductions in acne grade, and inflamed and non-inflamed lesion counts (P < 0.001).(ABSTRACT TRUNCATED AT 250 WORDS)

Acetates↗
PubMed1992

Double-blind study comparing erythromycin and mupirocin for treatment of impetigo in children: implications of a high prevalence of erythromycin-resistant Staphylococcus aureus strains.

Staphylococcus aureus has been consistently isolated from a high proportion of impetiginous lesions, and in several recent studies, it was present in the majority of the cases. Since recently a large proportion of S. aureus strains in our community showed erythromycin resistance, we undertook a prospective double-blind controlled study comparing topical mupirocin with oral erythromycin to determine (i) the prevalence of erythromycin-resistant S. aureus strains in impetigo and (ii) whether an increased rate of failure of erythromycin treatment was associated with such resistance. A total of 102 patients 3 to 185 months old (median = 49 months) were enrolled. Culture was positive for 97 of 102 (95%) patients, and S. aureus was present in 93% of the patients for whom cultures were positive. S. aureus was the single pathogen in 64% of these patients. Erythromycin-resistant S. aureus strains were present in 27 of 91 (28%) patients for whom cultures were positive. In all cases but one, S. aureus was resistant to penicillin, and in all cases it was sensitive to mupirocin. A marked difference was observed in favor of mupirocin in the clinical courses of the disease. However, only patients with erythromycin-resistant S. aureus strains had unfavorable courses compared with those treated with mupirocin (failure rate, 47 versus 2%, respectively). Patients with erythromycin-susceptible S. aureus strains who received erythromycin had a failure rate of 8%. In four patients, S. aureus strains initially susceptible to erythromycin became resistant during treatment. We conclude that erythromycin-resistant S. aureus strains are commonly isolated from impetigo in our region.(ABSTRACT TRUNCATED AT 250 WORDS)

Bacteria↗
PubMed1988

Plasma bactericidal activity after administration of erythromycin estolate and erythromycin ethylsuccinate to healthy volunteers.

In a crossover design study, we compared the plasma bactericidal activities of erythromycin estolate (500 mg) and erythromycin ethylsuccinate (600 mg) after administration of a single oral dose to 12 healthy volunteers. Both erythromycin esters displayed very good plasma bactericidal activities against Streptococcus pneumoniae. The median bactericidal titers produced in plasma against Streptococcus pyogenes and Streptococcus pneumoniae were significantly higher with erythromycin estolate than with the ethylsuccinate ester at both 2 and 8 h after dosing (P less than 0.05 by Student's t test). Both erythromycin esters showed rather weak bactericidal activity against Branhamella catarrhalis; a further look at these results indicated that erythromycin estolate presented 50% of the plasma samples at 2 h with bactericidal titers superior or equal to 1:8, versus 11% for the ethylsuccinate ester. Of the 60 plasma bactericidal activity tests performed against Staphylococcus aureus, only 6 (10%) and 3 (5%) exhibited titers of 1:8 or greater for erythromycin estolate and erythromycin ethylsuccinate, respectively. Clinical trials are warranted in which these products are compared in infections other than Streptococcus pyogenes pharyngitis, for which the clinical superiority of erythromycin estolate has been demonstrated.

Adult↗
PubMed1991

Evolution of Staphylococcus aureus resistance to erythromycin in Denmark, 1959 to 1988: correlations between characteristics of erythromycin-resistant bacteraemia strains.

In an attempt to characterize erythromycin-resistant Staphylococcus aureus we present the intricate relationships between the following factors: phage type, period of isolation, antibiogram, minimum inhibitory concentration (MIC) to erythromycin, inducible or constitutive resistance, spectinomycin susceptibility, hospital- or community-acquired infection, and mortality rate. We studied 718 cases of bacteraemia with erythromycin-resistant S. aureus, occurring between 1959 and 1988. Central factors were phage type pattern, period of isolation, and antibiogram. Between 1959 and 1973 the majority of the erythromycin-resistant strains were multiresistant and belonged to the 83A complex and the related group III. They were mainly inducibly resistant, spectinomycin resistant, and had intermediate MICs (1-4 mg l-1) to erythromycin. The majority of these strains came from hospital-acquired infections and still exist today, although in decreased numbers. By contrast, erythromycin-resistant S. aureus isolated in recent years are usually co-resistant only to penicillin and more rarely also to tetracycline. These strains have inducible resistance, are spectinomycin susceptible, and have a high erythromycin MIC. They are isolated both from hospital- and community-acquired infections. Strains with constitutive resistance to macrolides occurred at a stable low level (13%) during the whole observation period and always had high MICs to erythromycin. The mortality rate among patients with S. aureus bacteraemia due to an erythromycin-resistant strain was only associated with the year of infection and decreased from 61% in the first 15-year period to 40% in the subsequent 15 years.

Bacteriophage Typing↗
PubMed1979

Plasma levels following single and repeated doses of erythromycin estolate and erythromycin stearate.

The pharmacokinetics of erythromycin and erythromycin 2'-propanoate were studied in healthy male volunteers following single and repeated doses of erythromycin stearate tablets, erythromycin estolate capsules, and a suspension. Estolate dosages gave rise to higher plasma levels of total drug than the stearate. However, the stearate yielded higher plasma levels of erythromycin base. Absorption of all dosage forms, except the suspension, was delayed, and pharmacokinetic interpretation of both single- and multiple-dose data required incorporation of an absorption lag time. The absorption of erythromycin stearate was inhibited by food and also by low fluid volumes in fasted subjects. Absorption of erythromycin estolate was increased in the presence of food and was not greatly affected by fluid volume. Although single-dose data poorly predicted circulating levels of erythromycin following repeated doses, trends observed after single doses were maintained during chronic treatment.

Adult↗
PubMed1991

Evolution of Staphylococcus aureus resistance to erythromycin in Denmark, 1959 to 1988: comparison with erythromycin-susceptible strains.

Between 1959 and 1988, all Staphylococcus aureus strains (15 168 patients) isolated from blood in Denmark have been collected, investigated and stored, and clinical data has been obtained. Erythromycin resistance was found in 4.9% of these strains. The frequency of erythromycin resistance peaked at 25% in 1966, due to the spread in hospitals of multiresistant strains of the 83A complex. When these strains dominated, an increased mortality rate was seen in patients infected with erythromycin-resistant S. aureus. In contrast to most countries, erythromycin resistance in S. aureus declined to less than 5% in 1971, continued to fall to 1.3% in 1983, and has increased slowly to 2.4% in 1988. The decline was only due to a decrease of multiresistant strains. Erythromycin-resistant strains isolated in recent years are predominantly resistant only to penicillin and erythromycin and belong to many different phage type patterns. In Denmark, inducible resistance has occurred at a stable high frequency of approximately 90% of the erythromycin-resistant strains during the last 30 years. Erythromycin-resistant strains isolated today, however, have higher minimum inhibitory concentrations, and are rarely resistant to spectinomycin, in contrast to the strains isolated in the first half of the observation period.

Denmark↗
PubMedDate not supplied

Bioinequivalence of erythromycin ethylsuccinate and enteric-coated erythromycin pellets following multiple oral doses.

Bioequivalence comparisons between erythromycin ethylsuccinate and an enteric-coated erythromycin base pellet product were made following multiple-dose, oral administration. Twenty-four volunteers participated in a ten-dose protocol (one dosage unit every six hours) using a complete crossover design. Plasma samples were assayed using a microbiological method specific for erythromycin base in the presence of the ester. Without correcting for the differences in doses administered, the amount of active erythromycin base absorbed from the enteric-coated pellet (250 mg base) was five to seven times that absorbed from the erythromycin ethylsuccinate product (400 mg base equivalent) at steady state. Erythromycin ethylsuccinate is not bioequivalent to an enteric-coated erythromycin base pellet product. The lower bioavailability of the ethylsuccinate may be due to instability in the acidic medium of the stomach.

Administration, Oral↗
PubMed1999

Cholestasis and liver cell damage due to hypersensitivity to erythromycin stearate--recurrence following therapy with erythromycin succinate.

Erythromycin is a frequently used antibiotic in patients with atypical respiratory infection and/or an allergy to penicillin. We report the case of a young woman who developed severe cholestasis and jaundice following treatment with erythromycin stearate. Two years later her general practitioner prescribed erythromycin succinate for pharyngitis. She experienced a severe second episode of jaundice and malaise. Different esters of erythromycin have been introduced to reduce side effects such as allergic reactions to erythromycin. The findings in our patient underline the fact that hypersensitivity is caused by the erythromycin molecule, independent from the type of esterification. Because of these side effects newer makrolides should be given preference over erythromycin.

Adult↗
PubMed1995

Evaluation of the intestinal absorption of erythromycin in man: absolute bioavailability and comparison with enteric coated erythromycin.

To determine the role of acid hydrolysis on the gastrointestinal absorption of erythromycin, six healthy subjects received erythromycin as a 240 mg intravenous dose, a 250 mg oral solution administered via endoscope directly into the duodenum and bypassing the stomach, and an enteric-coated 250 mg capsule. Blood samples were collected for 6 hours and serum erythromycin quantified by a microbiological method. The time to achieve maximum serum concentrations for the solution was 0.25 +/- 0.08 (mean +/- SD) hours and for the capsule was 2.92 +/- 0.55 hours. The absolute bioavailability of erythromycin from the capsule was 32 +/- 7% and for the duodenal solution 43 +/- 14%. The ratio of the areas under the serum erythromycin concentration-time curve of capsule to solution was 80 +/- 28% (range 38 to 110%). There is substantial loss of erythromycin apart from gastric acid hydrolysis, which cannot be accounted for by hepatic first-pass metabolism. Attempts to further improve the oral bioavailability of erythromycin beyond 50% by manipulation of formulation are likely to be futile.

Administration, Oral↗
PubMed1988

Time course of the antibacterial activity of erythromycin stearate and erythromycin acistrate against two Staphylococcus aureus strains in vitro.

The antibacterial efficacy of erythromycin stearate (ES) and a new erythromycin prodrug, erythromycin acistrate (EA, 2'-acetyl erythromycin stearate), was compared in two Staphylococcus aureus strains, one sensitive and the other resistant to erythromycin. The growth was continuously monitored turbidometrically for 24 h. With the sensitive S. aureus, the inhibitory effects of both ES and EA were visible within 1-2 h when the antibiotics were added at 0 or 1.5 h after the beginning of the incubation. When they were added at 3 h, their action was immediate at 0.5 and 1 mg/l, and 5 mg/l caused a complete inhibition of the growth. At 0.5 and 1 mg/l, however, ES was much more effective than EA. When EA and ES (1, 5 or 10 mg/l) were added at 0 or 1.5 h to the resistant staphylococcal culture, the lag phases (no detectable growth) were prolonged as a function of drug concentration but eventually the growth was restored. The action of EA was weaker and the lag phases were 2-5 h shorter than those after ES. When the compounds were added at 3 h, the antibacterial effect was visible immediately. The increase of absorbance was slowed down even by 1 mg/l of ES and almost prevented by 5 mg/l. At these concentrations EA was less effective than ES, but the two erythromycins were equally active at 10 mg/l. These results show that addition of EA acts on both staphylococci as rapidly as addition of ES but to a lesser extent. Evidently EA is antibacterially weaker than ES, or rapidly hydrolyzed to erythromycin after it has been added to the test system.

Drug Resistance, Microbial↗
PubMed1989

Effect of erythromycin acistrate and erythromycin stearate on human colonic microflora.

The effects of erythromycin acistrate (2'-acetyl erythromycin stearate), a new erythromycin derivative, and erythromycin stearate on the faecal microflora were compared in a randomized cross-over study. 12 healthy volunteers were given either drug 500 mg t.i.d. for 1 week. Their faeces were studied before, immediately after, and 1 week after the drug administration period. After a wash-out period of 4 weeks, the drugs were interchanged. Both erythromycin acistrate and erythromycin stearate induced changes in the normal colonic microflora to about the same extent. The most marked effect was the suppression of gram-negative anaerobic and aerobic rods. Clostridium difficile appeared in 1 subject on both drugs. Also the counts of aerobic gram-positive cocci were altered; enterococci increased in number. An increased resistance to erythromycin was noted among staphylococci and enterococci after both drugs.

Adolescent↗
PubMed1976

L-aspartate of erythromycin A cyclic 11,12-carbonate, a new semisynthetic erythromycin derivative.

Erythromycin A cyclic 11,12-carbonate, a compound with high antibacterial activity, forms with L-aspartic acid a salt possessing valuable properties as a potential chemotherapeutic agent. The L-aspartate of erythromycin A cyclic 11,12-carbonate exhibits strong anti-bacterial activity, especially against Gram-positive bacteria and shows low toxicity. The serum and the lung tissue levels of the discussed salt after a single dose administration to a rat were measured in comparison with those of erythromycin, its L-aspartate, erythromycin cyclic 11,12-carbonate and its L-glutamate. The new erythromycin derivative showed definitely superior characteristics to those of the other substances tested. The activity of the L-aspartate of erythromycin A cyclic 11,12-carbonate in chemotherapy of experimental staphylococcal infection and experimental pneumococcal bronchopneumonia in mice is superior to that of the parent carbonate and erythromycin itself.

Animals↗