Search PubMed⌕ Search

SEARCH · Search PubMed

Results for “ERYTHROMYCIN”

Search indexed PubMed citations on genomics, clinical trials, systematic reviews and public health. Explore titles, authors and supplied subject terms, then open the PubMed record.

Quote a phrase for an exact phrase match. Source license links do not imply unrestricted reuse.

At least 1,063 records · Page 59Linked to original sources
PubMed1984

Erythromycin in the treatment of otitis media with effusion (OME).

Previous studies have shown erythromycin to penetrate into both the middle-ear effusion and the adenoid tissue in children with Otitis Media with Effusion (OME). The levels obtained were similar to the plasma levels. Cultures in long-standing cases of OME have yielded respiratory pathogens--Haemophilus influenzae, Streptococcus pneumoniae and Branhamella catarrhalis--in the nasopharynx in 79 per cent and in the middle-ear effusion in 18 per cent. In the present investigation a group of children with OME of more than three months' duration were given erythromycin (Abboticin) in standard dosage for the last 10 days prior to scheduled operation (paracentesis or tympanostomy). Resolution was determined as normalization of the middle ear status, and this led to cancellation of surgery. The rate of resolution--12/26 (45 per cent)--was significantly higher than in a similar group of children not treated with erythromycin--11/72 (15 per cent). There are thus rational reasons for using erythromycin in OME, in many cases as an alternative to tympanostomy.

Child↗
PubMed1998

Review of the evidence for the use of erythromycin in the management of persons exposed to pertussis.

We assessed the quality of evidence for the use of erythromycin in preventing secondary transmission of pertussis to close contacts of primary cases. A literature search was undertaken and identified papers were reviewed critically. Thirteen original papers and 1 manuscript met the inclusion criteria for review (3 randomized controlled trials, 4 analytical studies and 7 descriptive studies). Evidence from both experimental and analytical studies showed little effect of the use of erythromycin in preventing secondary transmission. Its effect is at best modest when compared with the protection conferred by use of good quality whole cell vaccine. Three studies reported adverse events with erythromycin prophylaxis; these were mainly nausea, vomiting and abdominal pain. In countries where effective pertussis vaccines are in use, erythromycin use should be confined to close contacts of cases, particularly unimmunized children or partially immunized infants who would be most susceptible to the complications of pertussis, or adults who come into close contact with vulnerable children.

Adult↗
PubMed1977

Interaction between the erythromycin and chloramphenicol binding sites on the Escherichica coli ribosome.

The effects of chloramphenical on the binding kinetics of a fluorescein isothiocyanate derivative of 9(S)-erythromycylamine with 70S and 50S ribosomes have been studied by direct fluorimetric measurements. While chloramphenicol had little effect on the second-order 70S binding rate of the erythromycin analogue, it substantially reduced the dissociation rate of the fluorescent antibiotic-70S ribosome complex. This could be explained by simultaneous binding of both antibiotics to the 70S ribosome. The kinetic results suggest that chloramphenicol-saturated 70S particles bind the erythromycin analogue four times stronger and this was confirmed by direct binding studies. In additon, chloramphenicol causes a twofold increase in the intrinsic fluorescence of the 70S-bound analogue. This increase in fluorescence was used to study the kinetics of chloramphenicol binding to 70S ribosomes containing the fluorescent derivative. The fluorescence change followed first-order kinetics, suggesting that chloramphenicol induces a conformational change in the 70S particle. This could explain both its effect on erythromycin binding and on the fluorescence of bound analogue. Less detailed results with the 50S particle indicate a qualitively similar picture of erythromycin-chloramphenicol interactions.

Anti-Bacterial Agents↗
PubMedDate not supplied

Improved bioconversion of 15-fluoro-6-deoxyerythronolide B to 15-fluoro-erythromycin A by overexpression of the eryK Gene in Saccharopolyspora erythraea.

The bioconversion of a 6-deoxyerythronolide B analogue to the corresponding erythromycin A analogue (R-EryA) by a Saccharopolyspora erythraea mutant lacking the ketosynthase in the first polyketide synthase module was significantly improved by changing fluxes at a key branch point affecting the erythromycin congener distribution. This was achieved by integrating an additional copy of the eryK gene into the chromosome under control of the eryAIp promoter. Real-time PCR analysis of RNA confirmed higher expression of eryK in the resulting strain, S. erythraea K301-105B, compared to its parent. In shake flasks, K301-105B produced less of the shunt product 15-fluoro-erythromycin B (15F-EryB), suggesting a shift in congener distribution toward the desired product, 15-fluoro-erythromycin A (15F-EryA). In bioreactor studies, K301-105B produced 1.3 g/L of 15F-EryA with 75-80% molar yield on fed precursor, compared with 0.9 g/L 15F-EryA with 50-55% molar yield on fed precursor by the parent strain. At higher precursor feed rates, K301-105B produced 3.5 g/L of 15F-EryA while maintaining 75-80% molar yield on fed precursor.

Bacterial Proteins↗
PubMed2005

Accelerated transformation and deactivation of erythromycin in superheated water. 1. Temperature effects, transformation rates, and the impacts of dissolved organic matter.

The presence of antibiotics and other pharmaceuticals in the environment is of increasing concern. The stringent treatment of point discharges of antibiotic wastes holds promise as an approach for curtailing growing trends of microbial resistance. The work described in this two-part series explores the use of superheated water as a medium forthe accelerated transformation and deactivation of a specific target antibiotic, erythromycin. Part 1 of the series focuses on parent compound conversion, and Part 2 examines transformation mechanisms and reaction products. This paper, Part 1, highlights the results of reactor studies performed in both batch and flow-through modes. The data presented confirm that accelerated conversion of erythromycin, based on parent compound disappearance as measured by high-pressure liquid chromatography, occurs in water under superheated conditions. Given an initial erythromycin concentration of 50 mg/L, greaterthan 85% apparent conversion was achieved within 30 min in the batch system at all temperatures investigated in the range from 125 to 200 degrees C. The presence of dissolved organic matter extracted from two natural soil materials, at concentrations of 2.5-20 mg/L, was shown to have little effect on the overall extent of transformation of erythromycin in the batch system. The rates of decomposition observed were found to be best described by a psuedo-first-order expression, one in which the rate coefficient increased linearly with increasing initial concentration of the antibiotic. First-order rate behavior was verified in subsequent flow reactor experiments. The temperature dependence of rate was also examined, and an activation energy of 68.8 kJ/mol was determined.

Anti-Bacterial Agents↗
PubMed2005

Simple confirmatory method for the determination of erythromycin residues in trout: a fast liquid-liquid extraction followed by liquid chromatography-tandem mass spectrometry.

In recent years, erythromycin has received considerable attention for its therapeutic efficacy against some bacterial kidney diseases in aquaculture and, therefore, suitable and sensitive analytical methods to monitor erythromycin residues in fish are required. A fast sample treatment followed by an LC-ESI-MS/MS method is described for the purification, identification, and quantification of erythromycin A residues in fish. After two extractions with acetonitrile, samples were defatted with n-hexane, filtered, and analyzed by tandem mass spectrometry. Three characteristic transition reactions (m/z 734 --> 716, 734 --> 576, and 734 --> 558) in multiple reaction monitoring were tested for the determination and confirmation of erythromycin A. The method was in-house validated through the determination of precision, accuracy, specificity, stability, calibration curve, decision limit (CCalpha), and detection capability (CCbeta), in accordance with European Commission Decision 657/2002. The coefficients of variation ranged from 1.8 to 9.4% and from 7.5 to 10.9% for intra- and interday repeatability, respectively. Recovery data were also satisfactory, with values varying from 85 to 97%. The method was specific, stable, and robust enough for the required purposes. The calibration curve showed a good linearity in the whole range of the tested concentrations (0-1000 microg kg(-1)) with a correlation coefficient (r2) equal to 0.9956. CCalpha and CCbeta were found to be 220 and 238 microg kg(-1), respectively.

Animals↗
PubMed1989

Synthesis and biological activity of photoactive derivatives of erythromycin.

Five photoactive derivatives of erythromycin have been synthesized by linking to 9(S)-aminoerythromycin either an aryl azide or a p-nitrophenyl ether. One derivative is an amide formed by reaction with (5-azido-2-formyl-phenoxy)acetic acid. Three derivatives are also amides, synthesized with 4-(p-nitroguaiacoxy)butanoic acid as a photoreactive group either directly or by interposing an amino acid (glycine or tyrosine). The last derivative is the product of the aldehyde condensation of aminoerythromycin with 10-(p-nitroguaiacoxy)decanal. Two of these derivatives can easily be made radioactive for affinity labeling studies either by reduction with [3H]borohydride (aryl azide derivative) or by 125I iodination (4-(p-nitroguaiacoxy)tyrosyl derivative). Although affected to different extents, the five erythromycin derivatives are biologically active and bind to the erythromycin-specific site on the bacterial ribosomes. In addition, the introduction of these groups changes the erythromycin inhibition pattern of peptide bond model reactions.

Aminoglycosides↗
PubMed1996

Topical delivery of erythromycin from various formulations: an in vivo hairless mouse study.

Topical products containing erythromycin, a macrolide antibiotic with poor aqueous solubility, are usually formulated as high alcohol content solutions or gels. In this study, we evaluated the deposition of erythromycin base into various strata of hairless mouse skin following topical in vivo application from various low- and nonalcoholic formulations. The formulations tested included nonionic liposomal formulation composed of glyceryl dilaurate, cholesterol, and polyoxyethylene-10-stearyl either at a weight ratio of 57:15:28, two nonionic oil-in-water (o/w) liposomal emulsions containing isopropyl myristate or light mineral oil as the oil phase, a conventional o/w emulsion, a 40% hydroalcoholic solution, and two commercially available topical products. Eight hours after topical administration of these formulations, the efficiency of uptake of erythromycin into the living skin strata was in the order: liposomal isopropyl myristate emulsion > > liposomal mineral oil emulsion > > nonionic liposomes approximately Emgel approximately Theramycin-Z > > conventional emulsion > > hydroalcoholic solution. Alcohol-free liposomal systems are shown to be as efficient as high alcohol content products in facilitating permeation of erythromycin through the stratum corneum into living skin tissue.

Administration, Cutaneous↗
PubMed1998

Effects of octreotide and erythromycin on gastric myoelectrical and motor activities in patients with gastroparesis.

Simultaneous recordings of gastric manometry and myoelectrical activity were made in 10 patients with gastroparesis. Intravenous erythromycin (100 mg) was administered in the fasting state for a period of 30 min. Subcutaneous injection of octreotide (100 microg) was administered before one of the four identical test meals. It was found that octreotide significantly decreased the antral motility index (30-min fasting: 4.51+/-1.04 vs 1.75+/-0.97, P < 0.02; 60-min fed: 5.16+/-1.44 vs 3.4+/-1.41, P < 0.05) and the dominant power of the EGG (fasting power: 35.19+/-1.54 vs 30.84+/-1.57 dB, P < 0.004; postprandial power increase: 5.52+/-1.06 vs -0.27+/-0.87, P < 0.001). Erythromycin significantly increased the antral motility index (3.16+/-0.96 vs 9.5+/-0.61, P < 0.001) and the dominant power of the EGG (28.86+/-1.57 dB vs 33.55+/-1.59 dB, P < 0.005) in the fasting state. An improvement in the regularity of the gastric slow wave was also noted with erythromycin. It was concluded that: (1) the inhibitory effect of octreotide on postprandial gastric motility and myoelectrical activity suggests that caution should be exercised when octreotide is used in patients with gastroparesis; and (2) the stimulatory effect of erythromycin on gastric myoelectrical activity may enhance gastric motility and gastric emptying in patients with gastroparesis.

Adult↗
PubMed2003

Characterization of the inhibitory effects of erythromycin and clarithromycin on the HERG potassium channel.

Both erythromycin and clarithromycin have been reported to cause QT prolongation and the cardiac arrhythmia torsade de pointes in humans, however direct evidence documenting that these drugs produce this effect by blocking human cardiac ion channels is lacking. The goal of this study was to test the hypothesis that these macrolide antibiotics significantly block the delayed rectifier current (IKr) encoded by HERG (the human ether-a-go-go-related gene) at drug concentrations, temperature and ionic conditions mimicking those occurring in human subjects. Potassium currents in HEK 293 cells stably transfected with HERG were recorded using a whole cell voltage clamp method. Exposure of cells to erythromycin reduced the HERG encoded potassium current in a concentration dependent manner with an IC50 of 38.9 +/- 1.2 microM and Hill Slope factor of 0.4 +/- 0.1. Clarithromycin produced a similar concentration-dependent block with an IC50 of 45.7 +/- 1.1 microM and Hill Slope factor of 1.0 +/- 0.1. Erythromycin (25-250 microM) and clarithromycin (5 or 25 microM) also produced a significant decrease in the integral of the current evoked by an action potential shaped voltage clamp protocol. The results of this study document that both erythromycin and clarithromycin significantly inhibit the HERG potassium current at clinically relevant concentrations.

Action Potentials↗
PubMed1981

Depression of theophylline elimination by erythromycin.

The elimination of a single oral dose of theophylline was studied in 12 healthy subjects before and after 250 mg erythromycin every 8 hr for 10 days. Serum theophylline elimination half-life rose from 4.79 +/- 0.43 hr before to 7.53 +/- 0.71 hr after erythromycin. Theophylline clearance decreased from a mean of 91.6 +/- 27.0 to 54.8 +/- 10.0 ml/kg/hr after erythromycin and the mean apparent volumes of distribution were much the same before and after the antibiotic. The excretion of theophylline and its metabolites was studied in the urine of three of the subjects. In each case the amount of 3-methylxanthine and 1,3-dimethyluric acid decreased after antibiotic. Adjustments of the theophylline dosage may be necessary for patients who take theophylline and erythromycin concurrently to minimize the risk of theophylline toxicity.

Administration, Oral↗
PubMed1990

The erythromycin breath test as a predictor of cyclosporine blood levels.

The daily dose of cyclosporine required to attain a desired blood level can vary greatly among patients. Because elimination of cyclosporine depends on its metabolism in the liver by an enzyme (cytochrome P-450IIIA) that also demethylates erythromycin, we reasoned that the ability of patients to demethylate a test dose of erythromycin might be useful in estimating their appropriate daily doses of cyclosporine. Accordingly, the [14C-N-methyl] erythromycin breath test was administered to 32 patients before they received 3.0, 5.0, or 7.5 mg/kg/day cyclosporine to treat psoriasis. We found that a simple mathematical equation incorporating just the 14CO2 production, the age of the patient, and the daily dose of cyclosporine accounted for almost 80% (R2 = 0.78) of the interpatient variability in cyclosporine blood levels we observed. Our data indicate that P-450IIIA activity largely accounts for the relationship between dose of cyclosporine and blood levels for an individual patient. We conclude that the erythromycin breath test may be a convenient guide for cyclosporine dosing.

Adult↗
PubMed1992

Changes in the pharmacokinetics and electrocardiographic pharmacodynamics of terfenadine with concomitant administration of erythromycin.

Terfenadine is a nonsedating H1-antagonist that when overdosed, used with hepatic compromise, or when given with ketoconazole results in accumulation of parent terfenadine, prolongation of the QT interval, and torsades de pointes in susceptible patients. Nine subjects were given the recommended dose of terfenadine (60 mg every 12 hours) for 7 days before initiation of oral erythromycin (500 mg every 8 hours). All subjects increased metabolite concentrations after the addition of erythromycin for 1 week. The maximum concentration of metabolite increased by a mean of 107% and the mean metabolite area under the concentration-time curve increased by 170%. Three subjects accumulated unmetabolized terfenadine after administration of erythromycin for 1 week. Electrocardiographic data revealed changes in QT intervals and ST-U complexes in a subset of subjects who accumulated terfenadine. We conclude that erythromycin alters the metabolism of terfenadine, leading to accumulation of terfenadine in certain individuals that is associated with altered cardiac repolarization.

Administration, Oral↗
PubMed1995

Comparative efficacy of oral doses of clindamycin and erythromycin in the prevention of bacteraemia.

Two antibiotics, clindamycin and erythromycin, were compared in a double-blind trial to test their efficacy in the prevention of post-dental extraction bacteraemia with streptococci in a group of 40 healthy patients. Tolerance to the oral doses was tested by questionnaire. Levels of drug in the serum were estimated using a microbiological assay. An in-vitro blood culture system was used as an analogy of the persistence of a bacteraemia in the presence of high levels of antibiotic. Isolates of streptococci were identified to species level. Minimum inhibitory concentrations of clindamycin and of erythromycin for each isolate were estimated. Results showed satisfactory levels of antibiotics in the blood for activity against oral streptococci. Clindamycin was slightly more effective than erythromycin in the prevention of post-extraction streptococcal bacteraemia but that efficacy was only 45%. Clindamycin as a single oral dose of 600 mg was well tolerated by patients compared with erythromycin 1.5 g.

Abdominal Pain↗
PubMed1997

Transdermal delivery of erythromycin lactobionate--implications for the therapy of gastroparesis.

BACKGROUND: The treatment of many diseases may be complicated by abnormalities in gastric emptying. Gastric motor dysfunction may lead to unpredictable food and medication delivery to the small intestine, their site of absorption. Prokinetic agents improve gastric motility, but orally administered drugs are unreliably absorbed, thereby limiting their effectiveness. A method of delivering prokinetic agents which bypasses the gastrointestinal tract could lead to more effective treatment. METHODS: Skin samples from rat, hairless mouse and man were placed in an in vitro diffusion chamber. The epidermal side of the skin was exposed to erythromycin lactobionate and passage of the drug across the skin sample monitored and quantitated by high-performance liquid chromatography with UV detection. RESULTS: Erythromycin passes across all skin types tested. Steady-state flux across hairless mouse skin was greater than for rat, full thickness human skin and human epidermis. In the first 3 h following introduction of erythromycin lactobionate, 1.85 mg/cm2 crossed human epidermis. Given that a dose of 50 mg may exert prokinetic effects in vivo in man, increasing the patch size to approximately equal to 28 cm2 should provide therapeutic levels of drug within 3 h. CONCLUSIONS: Erythromycin lactobionate, when administered transdermally, can be delivered at levels sufficient to treat gastroparesis. This technique warrants in vivo investigation.

Administration, Cutaneous↗
PubMed1999

Interspecies complementation in Saccharopolyspora erythraea : elucidation of the function of oleP1, oleG1 and oleG2 from the oleandomycin biosynthetic gene cluster of Streptomyces antibioticus and generation of new erythromycin derivatives.

Two glycosyltransferase genes, oleG1 and oleG2, and a putative isomerase gene, oleP1, have previously been identified in the oleandomycin biosynthetic gene cluster of Streptomyces antibioticus. In order to identify which of these two glycosyltransferases encodes the desosaminyltransferase and which the oleandrosyltransferase, interspecies complementation has been carried out, using two mutant strains of Saccharopolyspora erythraea, one strain carrying an internal deletion in the eryCIII (desosaminyltransferase) gene and the other an internal deletion in the eryBV (mycarosyltransferase) gene. Expression of the oleG1 gene in the eryCIII deletion mutant restored the production of erythromycin A (although at a low level), demonstrating that oleG1 encodes the desosaminyltransferase required for the biosynthesis of oleandomycin and indicating that, as in erythromycin biosynthesis, the neutral sugar is transferred before the aminosugar onto the macrocyclic ring. Significantly, when an intact oleG2 gene (presumed to encode the oleandrosyltransferase) was expressed in the eryBV deletion mutant, antibiotic activity was also restored and, in addition to erythromycin A, new bioactive compounds were produced with a good yield. The neutral sugar residue present in these compounds was identified as L-rhamnose attached at position C-3 of an erythronolide B or a 6-deoxyerythronolide B lactone ring, thus indicating a relaxed specificity of the oleandrosyltransferase, OleG2, for both the activated sugar and the macrolactone substrate. The oleP1 gene located immediately upstream of oleG1 was likewise introduced into an eryCII deletion mutant of Sac. erythraea, and production of erythromycin A was again restored, demonstrating that the function of OleP1 is identical to that of EryCII in the biosynthesis of dTDP-D-desosamine, which we have previously proposed to be a dTDP-4-keto-6-deoxy-D-glucose 3, 4-isomerase.

Chromatography, High Pressure Liquid↗
PubMed2001

Erythromycin inhibition of 50S ribosomal subunit formation in Escherichia coli cells.

The effects of erythromycin on the formation of ribosomal subunits were examined in wild-type Escherichia coli cells and in an RNase E mutant strain. Pulse-chase labelling kinetics revealed a reduced rate of 50S subunit formation in both strains compared with 30S synthesis, which was unaffected by the antibiotic. Growth of cells in the presence of [14C]-erythromycin showed drug binding to 50S particles and to a 50S subunit precursor sedimenting at about 30S in sucrose gradients. Antibiotic binding to the precursor correlated with the decline in 50S formation in both strains. Erythromycin binding to the precursor showed the same 1:1 stoichiometry as binding to the 50S particle. Gel electrophoresis of rRNA from antibiotic-treated organisms revealed the presence of both 23S and 5S rRNAs in the 30S region of sucrose gradients. Hybridization with a 23S rRNA-specific probe confirmed the presence of this species of rRNA in the precursor. Eighteen 50S ribosomal proteins were associated with the precursor particle. A model is presented to account for erythromycin inhibition of 50S formation.

Endoribonucleases↗
PubMed1998

Changes in pyloric resistance induced by erythromycin.

Erythromycin increases gastric emptying but the characteristics of transpyloric flow and the contribution of pyloric resistance to the mechanisms of increased flow are unknown. Transpyloric outflow and gastroduodenal pressures were studied in eight anaesthetized pigs during intravenous infusion of erythromycin (10 mg kg-1). Erythromycin increased emptying of saline through an increased stroke volume of individual flow pulses (13.7 +/- 1.24 vs. 3.6 +/- 1.30 mL) rather than by decreasing the interval between flow pulses (3.9 +/- 0.55 vs. 3.2 +/- 0.30 pulse.min-1). This flow pattern was associated with more frequent antral contractions of larger amplitude originating from the upper part of the gastric antrum, suppression of isolated pyloric pressure waves and significant reduction of the pyloric resistance to flow (2.3 +/- 0.21 vs. 4.6 +/- 0.46 mmHg mL-1 s-1). The decreased resistance originated from a different temporal relationship between antropyloric pressure event and flow pulses that occurred almost simultaneously during erythromycin.

Animals↗