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At least 775 records · Page 43Linked to original sources
PubMed1998

Chlamydia in pregnancy: a randomized trial of azithromycin and erythromycin.

OBJECTIVE: To determine side effect profiles and cure rates of azithromycin compared with erythromycin in the treatment of chlamydial cervicitis complicating pregnancy. METHODS: Pregnant patients with positive DNA antigen assays for Chlamydia trachomatis were randomized to either azithromycin, 1 g oral slurry in a single dose, or erythromycin, 500 mg every 6 hours for 7 days. Repeat assays were planned for 3 weeks after therapy. Side effects, compliance, and treatment efficacy were assessed. RESULTS: One hundred six women were enrolled, and eighty-five women completed the protocol. Significantly fewer gastrointestinal side effects were noted in the azithromycin group than in the erythromycin group (11.9% versus 58.1%, P < or = .01). Enhanced compliance was noted with azithromycin, because it was given in a single observed dose. Similar treatment efficacy was noted between azithromycin and erythromycin (88.1% versus 93.0%, P > .05). CONCLUSION: Compared with erythromycin, azithromycin is associated with significantly fewer gastrointestinal side effects in pregnancy. This association, along with the ease of administration and similar efficacy, suggests that azithromycin should be considered for the initial treatment of chlamydial cervicitis in pregnancy.

Adult↗
PubMed1993

Semi-synthetic derivatives of erythromycin.

Semi-synthetic derivatives of erythromycin have played an important role in antimicrobial chemotherapy. First generation derivatives such as 2'-esters and acid-addition salts significantly improved the chemical stability and oral bioavailability of erythromycin. A second generation of erythronolide-modified derivatives: roxithromycin, clarithromycin, azithromycin, dirithromycin and flurithromycin, have been synthesized and have exhibited significant improvements in pharmacokinetic and/or microbiological features. In addition, erythromycin itself has expanded its utility as an effective antibiotic against a variety of newly emerged pathogens. As a result of these developments, macrolide antibiotics have enjoyed a resurgence in clinical interest and use during the past half-dozen years, and semi-synthetic derivatives of erythromycin should continue to be important contributors to this macrolide renaissance. Despite these recent successes, other useful niches for macrolide antibiotics will remain unfilled. Consequently, the search for new semi-synthetic derivatives of erythromycin possessing even better antimicrobial properties should be pursued.

Erythromycin↗
PubMed2002

Comparison of single-dose azithromycin and 12-dose, 3-day erythromycin for childhood cholera: a randomised, double-blind trial.

BACKGROUND: Cholera is a major public-health problem, with children most affected. However, effective single-dose antimicrobial regimens have been identified only for adults. Our aim was to compare the efficacy of azithromycin and erythromycin regimens in the treatment of children. METHODS: We did a double-blind, randomised study of 128 severely dehydrated children (age 1-15 years) with cholera, treated at one of two treatment centres in Bangladesh in 1999. Children were assigned single-dose azithromycin (20 mg/kg bodyweight, maximum individual dose 1 g; n=65) or 12.5 mg/kg erythromycin (maximum dose 500 mg; n=63) every 6 h for 3 days. Patients stayed in hospital for 5 days. We measured fluid balance every 6 h, and obtained a rectal swab or stool sample for culture daily. Our primary outcome measures were clinical success of treatment-ie, cessation of watery diarrhoea within 48 h-and bacteriological success-ie, absence of Vibrio cholerae O1 or O139 from cultures of stool or rectal swab samples after study day 2. Analysis was per protocol. FINDINGS: Two children in both groups withdrew from the study, and we excluded one child in the erythromycin group. Treatment was clinically successful in 48 (76%) patients who received azithromycin and 39 (65%) who received erythromycin (difference 11%, 95% CI -5 to 27, p=0.244); and bacteriologically successful in 45 (71%) and 49 (82%) patients, respectively (10%, -5 to 25, p=0.261). Patients treated with azithromycin had a shorter duration of diarrhoea (median 24 h vs 42 h; difference 12 h, 0-18 h, p=0.019) and fewer episodes of vomiting (1 vs 4; difference 1 episode, 0-3 episodes, p=0.023). INTERPRETATION: Single-dose azithromycin is as effective for treatment of cholera in children as standard erythromycin therapy, but is associated with less vomiting.

Adolescent↗
PubMed1982

Double-blind placebo controlled trial of erythromycin for treatment of Campylobacter enteritis.

Although most strains of Campylobacter jejuni are susceptible in vitro to erythromycin and the drug has been recommended for treatment of campylobacter enteritis, prospective controlled trials have not been done. Erythromycin (250 mg 6-hourly for adults and 40 mg/kg daily for children) has been compared with placebo in a double-blind trial of 5-day therapy for acute campylobacter enteritis. The mean number of days of illness at onset of therapy was 5.6 for the treatment group (n = 15) and 6.5 for the placebo group (n = 14). There were no differences in temperature, symptoms, and stool characteristics between the two groups. The mean duration of unformed stools after treatment was 4.1 days in the erythromycin group and 3.5 days in the placebo group. Fever, when present, abated within 48 h in all but two patients in each group. Follow-up faecal cultures 2 days after completion of therapy, however, were negative in all 15 of the erythromycin-treated patients compared with 6 out of 14 controls. Thus erythromycin promptly eradicates C. jejuni from the faeces but does not alter the natural course of uncomplicated campylobacter enteritis when therapy begins 4 or more days after the onset of symptoms.

Campylobacter Infections↗
PubMedDate not supplied

Clinical comparison of cefaclor twice daily versus amoxicillin-clavulanate or erythromycin three times daily in the treatment of patients with streptococcal pharyngitis.

The present study was undertaken to compare the efficacy and safety of a new regimen of cefaclor (25 mg/kg BID) with amoxicillin-clavulanate and erythromycin TID at standard doses for the treatment of pediatric patients with acute pharyngotonsillitis (APT). A total of 673 children (age range, 2 to 12 years) with signs and symptoms of APT were enrolled; 245 of these children who had a positive throat culture for group A beta-hemolytic streptococci (GABHS) entered the study and were randomly assigned to receive cefaclor 25 mg/kg BID, amoxicillin-clavulanate 15 mg/kg TID, or erythromycin 15 mg/kg TID. A 10-day antibiotic course was prescribed for each patient. Clinical and bacteriologic responses were assessed at the end of treatment (day 10) and at the follow-up visit (day 30). All GABHS strains isolated from throat cultures were tested for in vitro sensitivity to the antibiotics used in the study. Side effects (mainly nausea) were rare and mild in each group and did not require discontinuation of therapy. No GABHS strain was resistant to cefaclor or to amoxicillin-clavulanate; 37.9% of the strains were resistant to erythromycin. The results indicated that cefaclor given BID seems to be as effective as amoxicillin-clavulanate given TID (cure rate, 91.9% and 90.5%, respectively) and more effective than erythromycin given TID (cure rate, 76.8%) for the treatment of patients with APT. Erythromycin resistance among GABHS is an emerging problem in many geographic areas.

Amoxicillin-Potassium Clavulanate Combination↗
PubMed1986

Comparative efficacy of oral erythromycin versus oral tetracycline in the treatment of acne vulgaris. A double-blind study.

The efficacy of erythromycin base (E-Mycin tablets, 333 mg) and the efficacy of tetracycline hydrochloride (Panmycin tablets) were compared in this double-blind, randomized study. Two hundred patients with moderate to moderately severe acne vulgaris were randomly assigned to the study. One hundred patients received 1 gm of erythromycin base by mouth per day for 4 weeks, followed by 333 mg/day for 8 weeks, plus placebo for tetracycline. The second group of patients received 1 gm of tetracycline by mouth per day for 4 weeks, followed by 500 mg/day for 8 weeks, plus placebo for erythromycin. Both drugs reduced acne severity to the same extent. Pustules, papules, and open comedo counts decreased significantly over the 12-week period. Seventy-seven percent of the erythromycin-treated patients and 89% of the tetracycline-treated patients stated that their acne was markedly improved or improved by week 12. Most of the side effects in patients treated with erythromycin were gastrointestinal symptoms. Among the side effects in patients treated with tetracycline were Candida vaginitis in one patient and pseudotumor cerebri in one patient.

Acne Vulgaris↗
PubMed1997

Determination of erythromycin in urine and plasma using microbore liquid chromatography with tris(2,2'-bipyridyl)ruthenium(II) electrogenerated chemiluminescence detection.

Erythromycin is determined in both urine and plasma samples using microbore reversed-phase liquid chromatography with tris(2,2'-bipyridyl)ruthenium(II) [Ru(bpy)3(2+)] electrogenerated chemiluminescence (ECL) detection. Ru(bpy)3(2+) is included in the mobile phase thus eliminating band broadening caused by post-column reagent addition. Extra column band broadening is an important concern in microbore liquid chromatography due to the small peak volumes. Erythromycin was studied in both water and biological samples. The detection limit for erythromycin in standards is 0.01 microM or 50 fmol injected with a S/N of 3 and a linear working range that extends four orders of magnitude. Human urine and blood plasma were also studied. Urine samples were diluted and filtered before injection. Ultrafiltration was used to remove protein from blood plasma samples prior to injection. Erythromycin was selectively detected in the body fluid samples without any further sample preparation. The detection limits obtained for erythromycin in urine and plasma are 0.05 and 0.1 microM, respectively, for 5 microl injected on a 150x1 mm I.D. C18 column.

2,2'-Dipyridyl↗
PubMed1997

Determination of erythromycin and related substances by capillary electrophoresis.

Current compendial methods of assay for the analysis of erythromycin and its related substances involve the use of microbiological techniques. These techniques are non-selective and tedious, thus there is a need for the development of highly specific, quantitative analytical methods. Erythromycin was analysed in a 50 mM phosphate buffer (pH 7.5) and run at an applied voltage of 20 kV. Detection sensitivity was enhanced by using a wavelength of 200 nm and selecting an injection solvent of lower conductivity than the electrolyte: acetonitrile-water (20:80, v/v). In order to facilitate the separation of erythromycin and its related substances, the organic solvent ethanol (35%, v/v) was incorporated into a modified 150 mM phosphate buffer (pH 7.5) and run at an applied voltage of 30 kV. Resolution of all the compounds was achieved in approximately 45 min. The methods described are accurate and precise and thus suitable for the quantitative determination of erythromycin and the related substances, erythromycin C, anhydroerythromycin and N-demethylerythromycin A.

Buffers↗
PubMed1999

The formulation and stability of erythromycin-benzoyl peroxide in a topical gel.

The combination of benzoyl peroxide and erythromycin is used for the local treatment of acne and available as a commercial preparation. Because of the stability problems of erythromycin an extempore preparation is required. The influence of storage temperature and non active ingredients on the stability of benzoyl peroxide and erythromycin in topical gel preparations for extempore compounding is described. A microbiological and an HPLC method were used to determine the erythromycin and the benzoyl peroxide concentrations, respectively. For a formulation compounded with hydroxyethylcellulose no stability problems were observed. For the formulation containing Carbopol 940, the levels of erythromycin varied over a wide range due to precipitation and aggregation of the drug during compounding.

Acrylic Resins↗
PubMed2000

Investigation of the chemical stability of an erythromycin-tretinoin lotion by the use of an optimization system.

A combination of 2% erythromycin and 0.05% tretinoin in an alcohol-isopropanol lotion was prepared. Two parameters were investigated for their influence on the stability of erythromycin and/or tretinoin, namely pH and the concentration of butylhydroxytoluene (BHT) as antioxidant. To investigate these two parameters, an optimization technique was used with two factors (pH and concentration of BHT) at two levels. Accelerated stability analysis was performed at 45 degrees C in the dark to exclude isomerization of tretinoin. To analyse erythromycin and tretinoin in the combination preparation, a TLC method, previously developed in the laboratory, was used. The degradation of erythromycin seemed to be much faster than the tretinoin degradation. Optimal stability is shown in the pH range of 8.2-8.6 for erythromycin and 7.2-8.2 for tretinoin while the concentration of BHT had no significant influence.

Anti-Bacterial Agents↗
PubMed1997

Protective effect of Livex, a herbal formulation against erythromycin estolate induced hepatotoxicity in rats.

Livex, a compound herbal formulation, was investigated for its possible hepatoprotective effect in Wistar rats against erythromycin estolate induced toxicity. Oral administration of Livex significantly prevented the occurrence of erythromycin estolate induced hepatic damage. The increased level of serum enzymes (aspartate transaminase, alanine transaminase, alkaline phosphatase), bilirubin, serum and tissue cholesterol, triglycerides, phospholipids and free fatty acids observed in rats treated with erythromycin estolate were very much reduced in rats treated with Livex and erythromycin estolate. These biochemical observations were supplemented by histopathological examination of liver sections. Results of this study revealed that Livex could afford a significant protection against erythromycin estolate induced hepatocellular damage.

Administration, Oral↗
PubMed2003

Antagonism between penicillin and erythromycin against Streptococcus pneumoniae: does it exist?

Penicillin and erythromycin are commonly used for the treatment of serious infections caused by Streptococcus pneumoniae and combined as empiric therapy of community-acquired pneumonia. A concern about potential antagonism between these drugs prompted a protocol designed to test the hypothesis in timed kill curve experiments with several interpretive criteria applied. Four clinical isolates of S.pneumoniae from the United States referred to the SENTRY Antimicrobial Surveillance Program and one QC strain (ATCC 49619) were tested. Minimum Inhibitory Concentration (MIC) and Minimum Bactericidal Concentration (MBC) were determined for each isolate using reference dilution methods (NCCLS). Penicillin MBC results matched very closely to the MIC values. Penicillin and erythromycin were tested at clinically relevant concentrations of 10 and 1 microg/ml, respectively, alone and in combination. Interpretations were calculated comparing the penicillin + erythromycin killing effect versus penicillin or erythromycin rates tested alone. There was consistent bactericidal activity against S. pneumoniae by each drug alone and combined over the monitored five-hour period, except for an erythromycin induced-resistant isolate. Drug interactions ranged from synergy to antagonism, depending on the criteria applied. Antagonism risk of macrolide-penicillin combinations appeared to be minimal and method-dependent by in vitro tests.

Animals↗
PubMed1998

Comparative in vitro and in vivo efficacy of roxithromycin and erythromycin against a strain of methicillin-susceptible Staphylococcus epidermidis.

The in vitro and in vivo efficacy of roxithromycin was compared with that of erythromycin, against a methicillin-susceptible strain of Staphylococcus epidermidis. We performed standard in vitro testing (MIC, MBC, and time-kill kinetics) for roxithromycin, erythromycin, and rifampin. Both macrolides were bacteriostatic in vitro. There was no significant difference in microbial survival between erythromycin and roxithromycin groups in the time-kill kinetics (p = 0.3). For the in vivo experiments, using the rabbit experimental endocarditis model, roxithromycin was found to be inferior to erythromycin in decreasing the microbial burden of the endocardial vegetations (p < 0.05). Rifampin was highly effective, both in vitro and in vivo. In conclusion, the efficacy of roxithromycin was poor and inferior to erythromycin against a strain of methicillin-susceptible S. epidermidis.

Analysis of Variance↗
PubMed2001

Rapid detection of mutations associated with resistance to erythromycin in Campylobacter jejuni/coli by PCR and line probe assay.

Mutation of 23S rDNA is one of the mechanisms of erythromycin resistance. PCR and line probe assay (PCR-LiPA) with ten oligonucleotide probes were developed to detect the mutations associated with macrolide resistance at positions of 2072, 2073 and 2074 in 23S rDNA of Campylobacter jejuni/coli. A2074-->G mutation was detected in 12 of 25 isolates, which were resistant to erythromycin. No other mutations in 23S rDNA were detected. The rest of the strains were susceptible to erythromycin and no mutation in 23S rDNA was detected. Six laboratory induced erythromycin resistant mutants had no mutations in 23S rDNA. PCR-LiPA is a useful and rapid method to detect mutations in 23S rDNA associated with erythromycin resistance in C. jejuni/coli.

Base Sequence↗
PubMed1997

In vitro analysis of the activity of the major human hepatic CYP enzyme (CYP3A4) using [N-methyl-14C]-erythromycin.

Although the N-demethylation of erythromycin has found widespread use in a noninvasive assay with which to phenotype hepatic CYP3A function, currently, the routine in vitro analysis of erythromycin N-demethylase activity relies on the quantitation of liberated formaldehyde by relatively labor-intensive and insensitive colorimetric or fluorimetric detection. This report describes the development of a rapid, sensitive, and reproducible radioassay for human CYP3A4 using solid-phase extraction (SPE). The kinetics of erythromycin N-demethylation were best described by a one-site Michaelis-Menten model with autoinhibition and the apparent kinetic parameters for pooled human liver microsomes (HLM; Km=88 microM, Vmax=345 pmol/min/mg) and expressed CYP3A4 (Km=33 microM, Vmax=130 pmol/min/ mg) were in good agreement. Erythromycin N-demethylase activity was found to vary 14-fold in HLM and correlated with the rate of testosterone 6beta-hydroxylation (r2=0.92, p < 0.001; N=9). Ketoconazole was a potent inhibitor of the N-demethylation of erythromycin, and the estimated IC50 value (104+/-23 nM) agreed well with that obtained using testosterone as a probe for CYP3A (71+/-4 nM). The addition of this radioassay to those established for human CYP1A2, 2C9, 2D6, and 2E1 and its subsequent automation should enable the routine use of this methodology in the analysis of CYP-dependent reactions.

Aryl Hydrocarbon Hydroxylases↗
PubMed2003

Evaluation of the antibacterial potential of tetracycline or erythromycin mixed with calcium hydroxide as intracanal dressing against Enterococcus faecalis in vivo.

OBJECTIVE: We evaluated the intracanal antibacterial potential of tetracycline or erythromycin mixed with calcium hydroxide (CH) against enterococci in vivo. STUDY DESIGN: Fifty-five teeth in which enterococci were present were dressed for 1 month with either tetracycline (28 teeth) or erythromycin (27 teeth) mixed with CH. RESULTS: The tetracycline mixture was effective against enterococci in 22 teeth (79%). In 7 teeth, other microorganisms were recovered, resulting in a total antimicrobial effect of 54%. The corresponding results for erythromycin were 96% and 56%. CONCLUSIONS: The antimicrobial treatment of CH in combination with either erythromycin or tetracycline had a significant effect on enterococci, but the overall antimicrobial effect was relatively weak. Erythromycin mixed with CH seems to be a valuable option in the battle against monoinfections of enterococci.

Adult↗
PubMed2000

Acid-catalyzed degradation of clarithromycin and erythromycin B: a comparative study using NMR spectroscopy.

One of the major drawbacks in the use of the antibiotic erythromycin A is its extreme acid sensitivity, leading to degradation in the stomach following oral administration. The modern derivative clarithromycin degrades by a different mechanism and much more slowly. We have studied the pathway and kinetics of the acid-catalyzed degradation of clarithromycin and of erythromycin B, a biosynthetic precursor of erythromycin A which also has good antibacterial activity, using (1)H NMR spectroscopy. Both drugs degrade by loss of the cladinose sugar ring and with similar rates of reaction. These results suggest that erythromycin B has potential as an independent therapeutic entity, with superior acid stability compared with erythromycin A and with the advantage over clarithromycin of being a natural product.

Acids↗
PubMed1997

Solid-state investigations of erythromycin A dihydrate: structure, NMR spectroscopy, and hygroscopicity.

The crystal structures of the commercially available form of erythromycin A dihydrate and clarithromycin anhydrate, in addition to the structure of erythromycin B dihydrate, are reported in this paper. In light of the crystallographic data, analysis of the structural information provides insight into the physical properties of these pharmaceuticals. The propensity of these pharmaceuticals to form solvated structures is discussed and the hygroscopicity of erythromycin A dihydrate is investigated. Solid-state 13C NMR was used to monitor changes that occur when the dihydrate form of erythromycin A is stored under conditions of low relative humidity. Although erythromycin A dihydrate retains its crystallographic order at low humidity, as indicated by its X-ray powder diffraction pattern, the local chemical environment is dramatically influenced by the loss of the water molecules and results in dramatic changes in its solid-state 13C NMR spectrum.

Anti-Bacterial Agents↗