Efficacy and tolerability of erythromycin acistrate and erythromycin stearate in acute skin infections of patients with atopic eczema

Op, Salo; Gordin, A.; Brand, H. Kim; Antikaínen, Riitta

doi:10.1093/jac/21.suppl_d.101

Cited by 11 publications

(5 citation statements)

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“…In spite of growing concern about rising resistance rates, erythromycin is still one of the mainstays of therapy for this indication (4, 14, 15). Recent reports from worldwide antimicrobial surveillance programmes indicated that between 49 (USA, 16), 38 (Europe, 17) and 24% (Asia, 18) of all S. aureus strains are now resistant to erythromycin.…”

Section: Discussionmentioning

confidence: 99%

Antimicrobial susceptibility of skin‐colonizing S. aureus strains in children with atopic dermatitis

Hoeger

2004

Pediatric Allergy Immunology

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Children with atopic dermatitis (AD) are prone to recurrent cutaneous and occasional systemic infections caused by Staphylococcus aureus. Antibiotic therapy represents an important component of the overall management of AD, especially during exacerbations of disease. Erythromycin is still widely used as a first-line antibiotic for this indication. We studied 115 consecutive children (mean age: 2.7 yr, range: 0.2-15) with moderate to severe AD (mean SCORAD: 43.2, range: 16-77) presenting to our outpatient department. Staphylococcus aureus was isolated from 100 of 115 (87%). Antimicrobial susceptibility testing revealed resistance against erythromycin in 18 and against roxithromycin in 19%, respectively. Six percentage of the strains were resistant or only intermediately susceptible to fusidic acid, 13% to amoxicillin and 1% to clindamycin. All strains isolated were susceptible to oxacillin, amoxicillin/clavulanic acid, cefadroxil and cefuroxim. The high rate of primary resistance to macrolides should be born in mind when starting antibiotic therapy in children with AD. Since Gram-positive cocci represent the only relevant microbial agents in AD, first generation cephalosporins such as cefadroxil, whose antimicrobial spectrum is basically restricted to Gram-positive bacteria, would appear to be the ideal first-line antibiotics for the treatment of bacterial superinfections.

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Section: Discussionmentioning

confidence: 99%

Antimicrobial susceptibility of skin‐colonizing S. aureus strains in children with atopic dermatitis

Hoeger

2004

Pediatric Allergy Immunology

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“…For instance, erythromycin-A 2′-ethylsuccinate is used as an oral suspension in children to reduce the unpleasant taste of the drug. Topical therapy of acute skin infections in patients with atopic eczema, with both ERY acistrate and ERY stearate, was able to eradicate the infection due to S. aureus in more than 60% of cases (7).…”

Section: Introductionmentioning

confidence: 99%

Amphiphilic Erythromycin-Lipoamino Acid Ion Pairs: Characterization and In Vitro Microbiological Evaluation

et al. 2011

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A series of amphiphilic ion pairs of erythromycin (ERY) with lipoamino acids (LAAs) were produced. The ion pairs were prepared by evaporation of a water/ethanol co-solution of the drug and LAA bearing an alkyl side chain of 10-16 carbon atoms. For the sake of comparison, equimolar physical mixtures were prepared by triturating ERY and the LAA in the absence of any solvent. FTIR spectroscopy confirmed the structure of ion pairs, while differential scanning calorimetry and powder X-ray diffractometry were used to assess the formation of new saline species. The solubility pattern of the coevaporates in different aqueous and organic solvents confirmed their amphiphilic properties. ERY-LAA ion pairs were submitted to an in vitro microbiological assay against different bacterial strains, both susceptible and resistant to macrolides. The presence of the LAA moiety was shown not altering the antibacterial spectrum of activity of the drug. These results can be the basis for a further evaluation of ERY-LAA ion pairs as a mean to improve the penetration of the drug inside bacterial cells and to optimize the loading of ERY in lipid-based nanocarriers.

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“…Although its half-life in plasma is short and the pharmacokinetic (PK) profile intraindividually heterogeneous, it is very well distributed throughout body tissues and accumulates in leukocytes (11). While clinical studies have shown the effectiveness of erythromycin in skin and soft tissue infections (33,39), the in vivo penetration and the resulting free concentrations in interstitial space of soft tissues, i.e., the most important site of bacterial infections, have not been reported until now. High cellular uptake, relatively short retention, and fast back release from white blood cells (WBCs) are considered important properties of the PK of erythromycin (1).…”

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confidence: 99%

Blood, Tissue, and Intracellular Concentrations of Erythromycin and Its Metabolite Anhydroerythromycin during and after Therapy

Krasniqi

Matzneller

Kinzig

et al. 2012

Antimicrob Agents Chemother

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For macrolides, clinical activity but also the development of bacterial resistance has been attributed to prolonged therapeutic and subtherapeutic concentrations. Although erythromycin is a long-established antimicrobial, concomitant determination of the pharmacokinetics of erythromycin and its metabolites in different compartments is limited. To better characterize the pharmacokinetics of erythromycin and its anhydrometabolite (anhydroerythromycin [AHE]) in different compartments during and after the end of treatment with 500 mg of erythromycin four times daily, concentration-time profiles were determined in plasma, interstitial space of muscle and subcutaneous adipose tissue, and white blood cells (WBCs) at days 1 and 3 of treatment and 2 and 7 days after end of therapy. In WBCs, concentrations of erythromycin exceeded those in plasma approximately 40-fold, while free concentrations in plasma and tissue were comparable. The observed delay of peak concentrations in tissue might be caused by fast initial cellular uptake. Two days after the end of treatment, subinhibitory concentrations were observed in plasma and interstitial space of both soft tissues, while 7 days after the end of treatment, erythromycin was not detectable in any compartment. This relatively short period of subinhibitory concentrations may be advantageous compared to other macrolides. The ratio of erythromycin over AHE on day 1 was highest in plasma (2.81 ؎ 3.45) and lowest in WBCs (0.27 ؎ 0.22). While the ratio remained constant between single dose and steady state, after the end of treatment the concentration of AHE declined more slowly than that of the parent compound, indicating the importance of the metabolite for the prolonged drug interaction of erythromycin. Macrolides account for 10 to 15% of the worldwide consumption of antibiotics (25,31). Although in many countries erythromycin has been replaced by newer relatives like azithromycin and clarithromycin, prescription of erythromycin still has a substantial place in less developed countries but also certain regions within Europe (15, 40). However, bacterial resistance against macrolides dramatically escalated in many countries during the last decades (14,23,35). Total consumption of antimicrobials on the one hand and the presence of long periods of exposure of bacterial populations to subinhibitory concentrations of antibiotics on the other hand are considered critical factors for selecting bacterial resistance (2, 3, 16).Erythromycin is known for its highly variable bioavailability after oral ingestion and its susceptibility toward degradation under acidic conditions. Although its half-life in plasma is short and the pharmacokinetic (PK) profile intraindividually heterogeneous, it is very well distributed throughout body tissues and accumulates in leukocytes (11). While clinical studies have shown the effectiveness of erythromycin in skin and soft tissue infections (33, 39), the in vivo penetration and the resulting free concentrations in interstitial space of soft tissues, i.e., the ...

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Efficacy and tolerability of erythromycin acistrate and erythromycin stearate in acute skin infections of patients with atopic eczema

Cited by 11 publications

References 0 publications

Antimicrobial susceptibility of skin‐colonizing S. aureus strains in children with atopic dermatitis

Antimicrobial susceptibility of skin‐colonizing S. aureus strains in children with atopic dermatitis

Amphiphilic Erythromycin-Lipoamino Acid Ion Pairs: Characterization and In Vitro Microbiological Evaluation

Blood, Tissue, and Intracellular Concentrations of Erythromycin and Its Metabolite Anhydroerythromycin during and after Therapy

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