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PubMed1989

Reversal of drug resistance by erythromycin: erythromycin increases the accumulation of actinomycin D and doxorubicin in multidrug-resistant cells.

Development of resistance to one type of lipophilic chemotherapeutic drug often leads to resistance to other, structurally unrelated, lipophilic drugs. This suggests that non-toxic lipophilic agents may interfere with and reverse drug resistance by saturating the pathway through which multidrug-resistant (MDR) cells protect themselves against cytotoxic drugs. The lipophilic antibiotic, erythromycin, can significantly reverse the resistance of MDR WEHI 164 murine fibrosarcoma cells to the chemotherapeutic drugs, doxorubicin and actinomycin-D. The MDR cells showed an approximately 10-fold higher expression of the P-glycoprotein than the drug-sensitive parental cells from which the resistant cells were derived. The accumulation of actinomycin-D and doxorubicin was much lower in the drug-resistant cells than in the sensitive parental cells. The concentrations of erythromycin which reversed the drug resistance of the MDR cells increased the accumulation of actinomycin-D and doxorubicin in these cells to a level comparable to that observed in the sensitive parental cells. Our data suggest that erythromycin reverses drug resistance by saturating the drug-binding sites on the P-glycoprotein, thereby reducing the capacity of this protein to pump drugs out of resistant cells. Some of our MDR cells have also become more resistant to tumour necrosis factor (TNF). However, erythromycin did not reverse TNF resistance, suggesting that the mechanisms of multi-drug and TNF resistance are different. TNF did not influence drug accumulation in MDR cells.

ATP Binding Cassette Transporter, Subfamily B, Mem↗

PubMed1989

Development of erythromycin-resistance in Staphylococcus aureus as a consequence of high erythromycin consumption.

In a mixed ward for skin and venereology patients the erythromycin consumption was 6-8 fold higher than in other wards at the same hospital. Erythromycin-resistance occurred in 15.5% of the infecting Staphylococcus aureus strains isolated from this ward, compared with 3.5% in other wards of the hospital and 2.3% in Denmark as a whole. The resistant strains belonged to different phage-type patterns, but 18 out of 19 strains contained a 1.5 MDa plasmid and had an erythromycin-inducible resistance mechanism. Erythromycin resistance was frequent (approximately 10%) among Danish S. aureus strains in the years 1963 to 1969, mainly due to the spread of multiply-resistant strains of the 83A complex. During the last ten years, however, only 1-2% of the strains have been resistant, but a slow increase in resistance has taken place during the last three years among strains of all phage patterns including strains of group II, the 94, 96 complex and type 95.

Bacteriophage Typing↗

PubMed2002

Increased prevalence of erythromycin resistance in streptococci: substantial upsurge in erythromycin-resistant M phenotype in Streptococcus pyogenes (1979-1998) but not in Streptococcus pneumoniae (1985-1999) in Taiwan.

A total of 394 nonduplicate isolates of Streptococcus pyogenes collected from 1979 to 1998 and 267 nonduplicate isolates of Streptococcus pneumoniae collected from October, 1998, to May, 1999, in Taiwan were evaluated. Among the 220 erythromycin-resistant (MIC, > or =1 microg/ml) S. pyogenes isolates, 35% had an M phenotype and 65% had an ML phenotype (inducible resistance [iML], 0.5%, and constitutive resistance [cML], 64.5%). Among the 243 erythromycin-resistant S. pneumoniae isolates, the majority (65.4%) had an ML phenotype (iML, 0.4%, and cML, 65%) and 34.6% had an M phenotype. A substantial upsurge in the incidence of M-phenotype erythromycin-resistant isolates was found with time for S. pyogenes (0% in 1979-1984 and 100% in 1997-1998), and an increasing incidence of M-phenotype among erythromycin-resistant S. pneumoniae was also noted (<20% before 1994 and 45.4% in 1999). All S. pyogenes and all but four S. pneumoniae isolates exhibiting a cML or iML phenotype had harbored the ermAM gene. The presence of the mefA gene was demonstrated in all isolates of S. pyogenes and the mefE gene in all but four S. pneumoniae isolates exhibiting the M phenotype. Due to the increasing susceptibility of S. pyogenes and S. pneumoniae isolates to clindamycin, susceptibility tests of these two organisms to macrolides and clindamycin should be performed simultaneously in the clinical microbiology laboratory, particularly in areas with high rates of macrolide resistance.

Anti-Bacterial Agents↗

PubMed1988

Absorption of erythromycin acistrate and erythromycin base in the fasting and non-fasting state.

Absorption of erythromycin acistrate (EA) and two erythromycin base (EB) preparations (enterotablet A and B) taken after an overnight fast or immediately before a standard breakfast was studied in 29 healthy volunteers in three separate studies, in a cross-over, randomized design. In Study I, the absorption of a single dose (400 mg) of EA was similar in the fasting and non-fasting state. There was, however, more interindividual variation and in two subjects absorption was markedly impaired in the presence of food. Cimetidine given at two doses (400 + 800 mg) had no effect on the pharmacokinetics of erythromycin acistrate. In Study II, the effect of food on the bioavailability of the two EB preparations was studied after a single dose of 500 mg (2 x 250 mg enterocoated tablets) and after multiple dosing (2 x 250 mg tid). When given with a standard breakfast, erythromycin base was significantly better absorbed from enterotablet A than from enterotablet B, whether given as a single dose or in repeated doses. Study III followed the same design as Study II except that the tablet size of both enterotablets A and B was now 500 mg. Even in this study the absorption of enterotablet A was significantly better than that of enterotablet B. EA is adequately absorbed when taken before a meal. Cimetidine does not interfere with its elimination. Concomitant food intake produced considerably dissimilar absorption of two commercially available enterocoated EB preparations. Although at steady-state this was less prominent than after a single dose, it may have some clinical significance.

Adult↗

PubMed1988

Effects of erythromycin base and erythromycin esters on protein synthesis in vivo in Escherichia coli.

The inhibitory effects on protein synthesis in vivo of erythromycin base and several erythromycin esters have been determined. An experimental method was used, especially suited for studies on short-lived antibiotics causing low levels of inhibition. Most of the tested derivatives were 2-3% as active as erythromycin base while a split product of erythromycin, anhydroerythromycin, was 4% as effective.

Bacterial Proteins↗

PubMed1993

Distribution of genes encoding erythromycin ribosomal methylases and an erythromycin efflux pump in epidemiologically distinct groups of staphylococci.

Erythromycin-resistant staphylococci can be divided into two phenotypic classes based on their pattern of cross-resistance to other macrolides, lincosamides and type B streptogramins. Strains inducibly or constitutively resistant to all MLS antibiotics possess erythromycin ribosomal methylase (erm) genes, whereas strains inducibly resistant to only 14 and 15-membered ring macrolides and type B streptogramins harbour msrA, which encodes an ATP-dependent efflux pump. Dot-blot hybridization was used to study the distribution of ermA, ermB, ermC and msrA in five epidemiologically distinct groups of staphylococci. The most widely-distributed resistance determinant was ermC, which was detected in 112 (50.6%) of 221 isolates, alone in 106 isolates and in combination with a second erythromycin resistance determinant in six strains. MsrA was detected in 73 (33%) of isolates, alone in 65 and in combination with a methylase gene in eight strains. This determinant was responsible for erythromycin resistance in over one-third (36.4%) of clinical isolates of coagulase-negative staphylococci. ErmA and ermB were present in only a minority of isolates (5.9 and 7.2% of strains, respectively). The resistance determinants present in ten strains did not hybridize to any of the four probes although, in all cases, their resistance phenotype was consistent with the possession of a methylase gene. Interestingly, ermB was found exclusively in animal isolates of Staphylococcus intermedius, Staphylococcus xylosus and Staphylococcus hyicus, but not in coagulase-negative staphylococci of human origin. This determinant has previously only been found in a small number of epidemiologically related strains of Staphylococcus aureus.

Animals↗

PubMed1989

A 4% erythromycin and zinc combination (Zineryt) versus 2% erythromycin (Eryderm) in acne vulgaris: a randomized, double-blind comparative study.

A double-blind, randomized multi-centre study was performed to evaluate the efficacy of a 4% erythromycin and zinc combination (Zineryt) versus 2% erythromycin (Eryderm). One-hundred and twenty-two patients suffering from acne vulgaris were treated with either Zineryt lotion or 2% erythromycin lotion. Acne grading and lesion counts for comedones, papules, pustules, nodules and macules were performed at each visit at 0, 1, 2, 4, 8 and 12 weeks. Treatment with Zineryt lotion was found to be more effective than with 2% erythromycin as regards the reduction in number of the acne lesions and the severity grade of the acne.

Acetates↗

PubMed1984

Effects of erythromycin-inactivating Lactobacillus crop flora on blood levels of erythromycin given orally to chicks.

Germ-free, day-old chickens were colonized with a Lactobacillus fermentum strain isolated from poultry which was able to inactivate in vitro erythromycin and other macrolide and lincosamide antibiotics. Similar control chickens were colonized with a non-degrading L. fermentum strain. Only in chickens colonized with the non-degrading strain were blood levels considered to be therapeutically active achieved with erythromycin in the drinking water. Five groups of broiler chickens of different age originating from three farms all possessed an erythromycin-degrading crop flora. In none of these were therapeutic blood levels attained when erythromycin was given in the drinking water.

Administration, Oral↗

PubMed1987

Distribution of erythromycin esterase and rRNA methylase genes in members of the family Enterobacteriaceae highly resistant to erythromycin.

The distribution of nucleotide sequences related to ereA, ereB, and ermAM was studied by colony hybridization in 112 strains of members of the family Enterobacteriaceae that are highly resistant to erythromycin. The ereA and ereB genes encoding erythromycin esterases type I and II, respectively, were detected in strains inactivating the 14-membered macrolides erythromycin and oleandomycin. Because all 52 strains resisting these antibiotics by inactivation were detected by ereA (n = 23), ereB (n = 23), or both probes (n = 6), only two classes of genes accounted for this resistance phenotype. The ermAM gene encoding a streptococcal rRNA methylase was detected in 21 strains of Escherichia coli and two strains of Klebsiella spp. Determination of the MICs of macrolide, lincosamide, and streptogramin (MLS) antibiotics demonstrated a correlation between hybridization with ermAM and the so-called MLS resistance phenotype. The presence of 11 strains coresistant to MLS antibiotics that did not hybridize to the ermAM probe suggests that, as in gram-positive organisms, MLS resistance in members of the family Enterobacteriaceae involves more than one class of rRNA methylase. Numerous strains (n = 18) were found to produce both an erythromycin esterase type II and an rRNA methylase. Physical linkage between ereB and ermAM may be responsible for the codissemination of the genes. Despite their exogenous origin, ereB and ermAM are already disseminated in various genera of the Enterobacteriaceae.

Carboxylic Ester Hydrolases↗

PubMed1988

Serum, sputum and bronchial concentrations of erythromycin in chronic bronchitis after single and multiple treatments with either propionate-N-acetylcysteinate or stearate erythromycin.

Serum and bronchial concentrations of erythromycin were determined in 30 chronic bronchitic patients during an exacerbation phase of bacterial infections. The levels were measured after single and multiple oral treatments with erythromycin-propionate-N-acetylcysteinate (EPAC) or erythromycin stearate (ES) in a double-blind design. EPAC showed higher and longer-lasting erythromycin levels in serum, sputum and pure bronchial mucus than ES. It is believed that EPAC is better absorbed because of its greater stability in the gastrointestinal juices. Higher concentrations in bronchial secretions not always depend on the blood levels. It seems to be possible that the N-acetylcysteine moiety in the molecule of EPAC drug can facilitate antibiotic penetration because of its mucolytic activity. The clinical response (disappearance of fever, clearance of bacterial pathogens from sputum, reduction of quantity and viscosity of sputum) also occurred faster in the EPAC than in the ES group.

Acetylcysteine↗

PubMed1983

Tolerance and efficacy of erythromycin stearate tablets versus enteric-coated erythromycin base capsules in the treatment of patients with acne vulgaris.

In a randomized, and for the investigator, blind study side-effects and efficacy of two oral erythromycin preparations have been compared. Twenty patients with acne vulgaris, predominantly of the face, received erythromycin stearate tablets and another twenty patients received erythromycin enteric-coated base capsules. All patients were given 500 mg twice a day for 2 weeks. An improvement was seen in both groups, most pronounced in patients treated with the stearate tablets. Twenty per cent of the patients given the base preparation withdrew from therapy due to gastro-intestinal side-effects, as compared to 10% in the erythromycin stearate group.

Acne Vulgaris↗

PubMed1989

[Comparative studies of cyclic 11, 12 erythromycin carbonate (davercin) and erythromycin a levels in lung tissue, serum and bronchial secretions].

A comparison of serum, pulmonary tissue and bronchial secretory levels of erythromycin and cyclic--11,12 carbonate of erythromycin (Davercin--Polfa) was carried out in 55 patients with lung cancer. All patients received erythromycin and Davercin 80 hours prior surgery, during which a small fragment of pulmonary tissue was removed for further evaluation. Concentration of both antibiotics was determined microbiologically. Better penetration of Davercin to the pulmonary tissue was found, as well as higher tissue concentration. The study demonstrates the advantage of Davercin over erythromycin in treating bacterial infections of the respiratory system.

Body Fluids↗

PubMed1988

Human pharmacokinetics of erythromycin propionate-N-acetylcysteinate: comparative evaluation with erythromycin stearate and N-acetylcysteine.

The pharmacokinetic pattern of erythromycin propionate-N-acetylcysteinate (EPAC) (erythromycin stinoprate I.N.N.), a new derivative, was studied on 12 healthy volunteers after single and multiple oral treatments. Microbiological and/or HPLC analytical methods were used to titer either erythromycin as base, propionate and total or N-acetylcysteine (NAC). In the acute experiment, a comparative evaluation was performed with erythromycin stearate (ES) and with N-acetylcysteine, according to a randomized-multi-crossover design. EPAC showed a better bioavailability than ES with longer-lasting serum levels of active antibiotic. NAC concentrations in the serum after EPAC were practically identical to those found after an oral administration of NAC alone. The multiple treatment study, performed in the same 12 volunteers with only EPAC, indicated that the pharmacokinetic pattern is somewhat different from that observed after a single dose, since higher concentrations were present at the steady state conditions.

Acetylcysteine↗

PubMed1979

Erythromycin levels in serum during treatment with erythromycin stearate and base.

The serum concentrations of erythromycin during treatment with erythromycin stearate and erythromycin base were compared in a randomised cross-over study with 21 hospital patients. No statistically significant differences between the brands were found in the serum erythromycin levels at any time or in the areas under the serum level-time curve.

Administration, Oral↗

PubMed1980

Erythromycin estolate vs. erythromycin base, surface excess properties and surface scanning changes in isolated liver cell systems.

Chang liver cells and isolated rat hepatocytes were exposed to medium containing different concentrations of erythromycin estolate or erythromycin base for 1-5 h. Hepatotoxicity was quantitated by measuring leakage of enzymes from cells into surrounding medium and the damage to the plasma cell membrane seen under surface scanning electron microscopy. Only the cells exposed to erythromycin estolate showed significantly greater enzyme leakage than controls and appeared severely affected by cytopathic changes when observed under scanning electron microscopy.

Animals↗

PubMedDate not supplied

Absorption of erythromycin stearate and enteric-coated erythromycin base after a single oral dose immediately before breakfast.

To study the absorption of different preparations of erythromycin in the fasting state, 500 mg stearate (tablets) and 500 mg base (enteric-coated pellets) were given immediately before a standardised breakfast to 24 young, healthy volunteers in an open, random, cross-over trial. The serum peak concentration appeared earlier and was higher after intake of the stearate tablets than after intake of the base pellets; however, there was no difference in the area under the serum concentration vs. time curves (AUC) between the two preparations. The bioavailability of erythromycin stearate in tablet form and of erythromycin base in the form of enteric-coated pellets thus appears comparable when taken on an empty stomach.

Absorption↗

PubMed1988

High-performance liquid chromatography of erythromycin propionyl ester and erythromycin base in biological fluids.

The simultaneous determination of erythromycin propionate and erythromycin base in serum and urine by high-performance liquid chromatography using oleandomycin as internal standard is described. The separation was achieved on a reversed-phase C18 column employing acetonitrile-0.05 M phosphate buffer (65:35), adjusted to pH 7.0, as the mobile phase with coulometric detection. Hydrolysis of the ester during blood sample collection was minimised by immediate high-speed centrifugation of collected blood samples, followed by separation and immediate freezing of the serum fraction. A solid-phase extraction procedure, combined with a simple phase-separation step was used prior to chromatographic analysis. The method has the necessary precision, sensitivity and accuracy to allow the simultaneous determination of both components in serum and urine following a single 500-mg oral dose of erythromycin estolate.

Chromatography, High Pressure Liquid↗

PubMed1999

Physiological role of the N-terminal processed P4501A1 targeted to mitochondria in erythromycin metabolism and reversal of erythromycin-mediated inhibition of mitochondrial protein synthesis.

Recently, we showed that the major species of beta-naphthoflavone-inducible rat liver mitochondrial P450MT2 consists of N-terminal truncated microsomal P4501A1 (+33/1A1) and that the truncated enzyme exhibits different substrate specificity as compared with intact P4501A1. The results of the present study show that P450MT2 targeted to COS cell mitochondria by transient transfection of P4501A1 cDNA is localized inside the mitochondrial inner membrane in a membrane-extrinsic orientation. Co-expression with wild type P4501A1 and adrenodoxin (Adx) cDNAs resulted in 5-7-fold higher erythromycin N-demethylation (ERND) in the mitochondrial fraction but minimal changes in the microsomal fraction of transfected cells. Erythromycin, a potent inhibitor of bacterial and mitochondrial protein synthesis, caused 8-12-fold higher accumulation of CYP1A1 mRNA, preferential accumulation of P450MT2, and 5-6-fold higher ERND activity in the mitochondrial compartment of rat C6 glioma cells. Consistent with the increased mitochondrial ERND activity, co-expression with P4501A1 and Adx in COS cells rendered complete protection against erythromycin-mediated mitochondrial translation inhibition. Mutations that specifically affect the mitochondrial targeting of P4501A1 also abolished protection against mitochondrial translation inhibition. These results for the first time suggest a physiological function for the xenobiotic inducible cytochrome P4501A1 against drug-mediated mitochondrial toxicity.

Animals↗