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At least 1,783 records · Page 99Linked to original sources

Topical erythromycin solution in acne. Results of a multiclinic trial.

In a multiclinic double-blind trial, 253 patients with moderate to severe acne vulgaris were treated with erythromycin, 1.5% topical solution (n = 127), or the vehicle (n = 126). The preparations were applied twice daily for 12 weeks. The response to treatment was evaluated by lesion counts and overall clinical judgment at 2, 4, 8, 10, and 12 weeks after initiation of treatment. The reduction in the number of inflammatory lesions, papules, and pustules was significantly greater (p less than 0.01) in the erythromycin-treated group. The global evaluation of the clinical response correlated well with the reduction in the lesion counts. No serious adverse effects were encountered.

Acne Vulgaris↗

Topical erythromycin with zinc in acne. A double-blind controlled study.

This double-blind controlled study investigated the effectiveness of 4% topical erythromycin liquid with 1.2% zinc acetate and 4% topical erythromycin gel with 1.2% zinc octoate applied twice daily in comparison with 250 mg of oral tetracycline twice daily and placebo. One hundred forty-nine patients began and one hundred forty-one completed the study. Three judges recorded acne measurements of severity grade, papule counts, pustule counts, comedo grades, and comedo counts without mutual consultation on visits at 0, 2, 4, 6, 8, and 10 weeks. Analysis of the reduction in the acne severity grade and papule count showed that the erythromycin/zinc liquid and gel were statistically significantly better than placebo and as effective as the oral tetracycline. Analysis of comedo grades showed that at weeks 8 and 10 the 4% topical erythromycin/zinc liquid showed a reduction statistically better than placebo.

Acne Vulgaris↗

An evaluation of a 2% erythromycin ointment in the topical therapy of acne vulgaris.

Two hundred eight patients completed a 12-week, multicenter, double-blind, controlled study comparing a 2% erythromycin ointment to its vehicle. Patients were evaluated by inflammatory lesion counts and Cook acne severity grade at the initial visit and at weeks 2, 4, 8, 10, and 12. The 2% erythromycin ointment proved to be statistically more effective than the vehicle in reducing lesion counts and acne severity grade at weeks 4, 8, 10, and 12. The ointment caused few side effects and was well tolerated by most patients.

Acne Vulgaris↗

Use of rifampin with penicillin and erythromycin in the treatment of psoriasis. Preliminary report.

The addition of 5 days of rifampin therapy to a 10- or 14-day course of penicillin or erythromycin therapy has been shown to reduce greatly the rate of chronic streptococcal carriage. The empiric use of rifampin in combination with penicillin or erythromycin in nine of nine patients with streptococcal-associated psoriasis appeared to coincide with a marked improvement in their skin.

Adult↗

[Purification of the bacterial ribosome using chloramphenicol and erythromycin columns].

Chloramphenicol and erythromycin are antibiotics whose target is the bacterial ribosome. We have studied the possibility of isolating the bacterial ribosome by affinity chromatography on chloramphenicol and erythromycin columns. Several columns have been prepared using different spacers and methods of attachment of the ligands (cyanogen bromide, bis-expoxyde). The efficiency and specificity of these columns is discussed. Ethylene diamine is not always suitable as a spacer, because it presents non specific affinity for the ribosome. Pure tight ribosomes have been prepared by ultracentrifugation. They have been compared to ribosomes from affinity columns. These columns have no denaturing effect on ribosomes. They allow a good purification of ribosomes starting from crude bacterial extracts, but the separation of tight couples from loose subunits is not possible.

Chloramphenicol↗

Concentration of azidocillin, erythromycin, doxycycline and clindamycin in dental alveolar serum after single oral doses.

Treatment of osteitis in the mandible after surgery is still a clinical problem. Levels of four antibiotics--azidocillin, erythromycin, doxycycline, and clindamycin--were measured in serum and dental alveolar serum in 42 patients undergoing oral surgery. The systemic serum concentrations were higher than the dental alveolar serum concentrations in all patients. The maximal concentration in the alveolar serum for azidocillin was 6.0-12.0 microng/ml, for erythromycin 0.7-1.3 microng/ml, for doxycycline 2.8-3.6 microng/ml, and for clindamycin 2.0-2.8 microng/ml. When the dental alveolar serum concentrations of the various antibiotics were related to their range of inhibitory concentrations for microorganisms isolated from mandibular osteitis, it was noticed that each drug achieved levels sufficient to inhibit most strains.

Administration, Oral↗

The effect of low-dose erythromycin on whole gastrointestinal transit time of preterm infants.

UNLABELLED: The aim of the study was to determine the effect of a low oral dose of erythromycin on whole gastrointestinal transit time [WGTT]. Erythromycin [EM] [1.5 mg/kg, 6 hourly] or placebo was given first over 7 days in a double blind randomized crossover study of 21 preterm infants with feed intolerance. Median [range] birth weight was 1420 [690, 2200] g and postconceptual age 32. 5 [20, 36.4] weeks. WGTT was assessed on day 3 of each treatment, by timing the transit of carmine red through the gut. Treatments were compared using Student's paired t test. RESULTS: WGTT was significantly shorter following EM treatment as compared to placebo: mean [SD] 10.16 [4.6] h vs. 15. 9 [7.2] h, p<0.01. CONCLUSION: Oral low-dose EM significantly shortens WGTT of feed-intolerant preterm infants.

Anti-Bacterial Agents↗

Determination of erythromycin base and 2'-acetylerythromycin in human plasma using high-performance liquid chromatography with electrochemical detection.

A high-performance liquid chromatographic method for the determination of plasma concentrations of erythromycin base and 2'-acetylerythromycin, an ester prodrug of erythromycin, is described. tert.-Butyl methyl ether extracts of 1-ml plasma samples (pH 10) were chromatographed on a C18 reversed-phase column. A three-electrode coulometric detector (oxidation potentials +0.65 and +0.85 V) was used for quantitation. Oleandomycin was used as an internal standard. The method has good precision and accuracy, is linear in the range 0.25-7.5 mg/l and has proved to be suitable for pharmacokinetic studies in humans. Correlation with a microbiological assay was satisfactory (r greater than or equal to 0.95), but the chromatographic method gave ca. 30% higher values.

Biological Availability↗

Sensitive determination of erythromycin in human plasma by LC-MS/MS.

A liquid chromatography-tandem mass spectrometry (LC-MS/MS) method for the analysis of erythromycin in human plasma (EDTA as anticoagulant) was developed and validated. The concentration ranges were 0.5-50 and 50-5000 ng ml-1. The procedure involved alkalization of 0.5 ml of plasma, one step liquid-liquid extraction, dryness of the extract and reconstitution in 80:20 water:acetonitrile. An Inertsil ODS-2 5 microns, 3.0 x 50 mm column (Metachem) with a C8 guard column and isocratic mobile phase were used for liquid chromatography. The mobile phase consisted of 1:1 acetonitrile:water with 2 mM NH4OAc and 0.1% HOAc. A flow rate of 0.7 ml min-1 was used. The analysis time on LC-MS/MS for one sample was approximately 2 min. A Turbo-Ionspray source was interfaced between the HPLC and triple quadrupole mass spectrometer (Sciex API III Plus). MS/MS analysis used Multi-Reaction Monitoring (MRM) mode. The lowest limit of quantitation (LOQ) was 0.5 ng ml-1 with all Quality Control (QC) sample recoveries varying between 88 and 105%. Nine intraday and interday calibration curves were generated yielding correlation coefficients ranging from 0.995 to 1.000. Average recovery for erythromycin at 1 ng ml-1 was 105% (+/- 4.5%). Average recovery for the internal standard was 83-103%. Short-term and long-term stability in the freezer (-20 degrees C), bench stability, and stability after 3 freeze/thaw cycles at -20 and -80 degrees C were conducted. The samples were found to be stable under all conditions. The method developed and validated proved useful for clinical pharmacokinetic study sample analysis with high throughput due to its high sensitivity and very short analysis time.

Anti-Bacterial Agents↗

Argentinian collaborative study on prevalence of erythromycin and penicillin susceptibility in Streptococcus pyogenes. The Argentinian Streptococcus Study Group.

Two monthly studies on the prevalence of penicillin and erythromycin susceptibility of Streptococcus pyogenes were performed in May and October of 1994 in Argentina. A total of 58 centers from 27 cities participated in these studies. A total of 1072 isolates were tested by a diffusion method, although 595 isolates were tested both by the diffusion and an agar dilution method (n = 1767 isolates). No penicillin-resistant streptococci were found in our study (MIC100 = 0.03 microgram/ml). Only four isolates were confirmed as erythromycin resistant S. pyogenes (prevalence 0.14 and 0.28% in May and October 1994, respectively). Resistance in three isolates was due to an inducible mechanism, although in one strain a different phenotype was observed.

Anti-Bacterial Agents↗

In vitro activity of gatifloxacin, compared with ciprofloxacin, clarithromycin, erythromycin, and rifampin, against Legionella species.

Gatifloxacin, a new advanced-generation, 8-methoxy fluoroquinolone, has shown efficacy against a broad spectrum of microorganisms. In this study, the in vitro activity of gatifloxacin was compared with that of ciprofloxacin, clarithromycin, erythromycin, and rifampin against 214 Legionella spp. Species tested in order of frequency were: L. pneumophila serogroups 1 to 9 (181 strains); L. dumoffii (10 strains); L. micdadei (9 strains); L. longbeachae (7 strains); and other Legionella spp. (7 strains). MICs were determined by a standard dilution procedure using buffered yeast extract agar. Gatifloxacin and rifampin were the most active agents against all strains of Legionella tested. Moreover, against L. pneumophila strains tested, gatifloxacin was found to be more active (highest MIC90 = 0.03 mg/L) than ciprofloxacin (highest MIC90 = 0.06 mg/L) and clarithromycin (highest MIC90 = 0.12 mg/L). L. pneumophila serogroups 1 to 4 and 6 to 9 (MIC90 = 0.016 mg/L) were more susceptible to gatifloxacinthan L. pneumophila serogroup 5 (MIC90 = 0.03 mg/L). The activity of gatifloxacin against L. micdadei was equal to that of ciprofloxacin (MIC90 = 0.016 mg/L) and greater than that of erythromycin (MIC90 = 1.0 mg/L). The activity of gatifloxacin against L. dumoffii and L. longbeachae was equal to that of ciprofloxacin (MIC90 = 0.03 mg/L). The activity of gatifloxacin was similar against isolates obtained from both patients and environmental sources.

Anti-Bacterial Agents↗

Evolution of penicillin and erythromycin co-resistance in Streptococcus pneumoniae in Spain.

The temporal dynamics of penicillin and erythromycin co-resistance in Streptococcus pneumoniae based on two extensive multicentre Spanish surveillance SAUCE studies (1996-1997 and 1998-1999) is presented. Erythromycin resistance among penicillin non-susceptible isolates seems to have reached a limit as evidenced by a null increase between the two surveys, whereas it is growing among penicillin-susceptible pneumococci.

Drug Resistance, Bacterial↗

Ring-chain tautomerism in solid-phase erythromycin A: evidence by solid-state NMR.

Chemical shift modeling, utilizing the DFT B3LYP/D95** method, provides the spectral assignment of the 35 visible 13C resonances from the solid-phase erythromycin A dihydrate. A new resonance at 110.8ppm is observed in the high-resolution 13C CP/MAS spectrum upon the application of heat or sample desiccation. With the use of the dipolar-dephasing spectral editing technique, this resonance is identified as a hemiketal carbon and the alternative hypothesis, a conformational change to the anomeric carbon of the desosamine sugar, is ruled out. Hence, the formation of a cyclic hemiketal in erythromycin A while in the solid phase is proven by solid-state NMR. The principal components of the 13C chemical-shift tensor corresponding to this hemiketal are reported. This is the first measurement of hemiketal 13C principal values. The delta11 and delta22 components are unique compared to anomeric carbon values reported in the literature.

Erythromycin↗

Comparative study on the macrolides erythromycin and clarithromycin: antibacterial activity and influence on immune responses.

The in vitro activity of erythromycin and clarithromycin (a new macrolide antibiotic) on clinical bacterial isolates as well as their effects on the cellular and humoral immune responses in BALB/c-mice and on human granulocytes/monocytes was investigated. Treatment of BALB/c-mice for 7 days with these drugs did not influence the delayed type hypersensitivity to oxazolone nor the production of IgG and IgM immunoglobulins. In vitro, exposure of granulocytes to erythromycin resulted in increased phagocytosis only in higher concentrations (20 mcg/ml), whereas clarithromycin enhanced chemiluminescence response of granulocytes in concentrations ranging from 2.5-20 mcg/ml. Subinhibitory concentrations of both substances modified Staphylococcus aureus and made them more susceptible for granulocyte phagocytosis.

Animals↗

Effect of compression force on the crystal properties of erythromycin acistrate tablets.

The crystal properties of compressed and powdered erythromycin acistrate tablets were studied by the X-ray powder diffraction (XRPD) method. Detailed analysis of X-ray powder diffraction line profiles was performed. Diffraction peak intensities and full width at half maximum (FWHM) values of the peaks corresponding to three different crystal lattice directions were determined. Crystallite size was calculated by Scherrer's equation using the data of integral breadth of the peaks. The preferred orientation of the crystallites is also discussed. According to the results, the crystallite size increased on the tablet surface after a small compression force (4 kN) in all crystal lattice directions studied. Even small compression forces caused recrystallization. With higher compression forces (8-18 kN) the crystallite size and the FWHM values remained rather constant. After the compression force of 18 kN the peaks in different crystal lattice directions behaved differently. In the lattice directions of diffraction maxima 2 and 3, the effect was the same with the small (4 kN) and the high compression force (22 kN). Further recrystallization occurred with 22 kN. However, in the crystal lattice direction of diffraction maximum 1 at the compression force of 8 kN the crystallite broke and crystallinity decreased. These were not seen in the powdered tablet samples. It could be concluded that the effect of compression force on the crystal properties of erythromycin acistrate tablets was seen on the tablet surface but not in the powdered tablets. Compression force also affected the preferred orientation of crystallites on the tablet surface and especially in the lattice direction of diffraction maximum 3. This was not seen in the powdered tablets.

Chemistry, Pharmaceutical↗

Dependence between dissolution rate and porosity of compressed erythromycin acistrate tablets.

The correlation between dissolution rate and porosity of compressed erythromycin acistrate tablets was studied. The total porosity of the tablets, the pore size distribution and the specific surface area of the pores were determined using high-pressure mercury porosimetry. The particle size and specific surface area of the raw material and of the dry granulated mass of the tablets were also determined. The results show that the pore size distribution, showing the differences in pore structure, is more informative than total intruded volume of mercury. However, it is very difficult to explain the dissolution behaviour of erythromycin acistrate tablets only by porosity results of the tablets, and more work is still needed in this field.

Erythromycin↗

Synthesis and antibacterial activity of HMR 3647 a new ketolide highly potent against erythromycin-resistant and susceptible pathogens.

In the search for new ketolides with improved activities against erythromycin-resistant S. pneumoniae and H. influenzae we synthesized a new 11,12 carbamate ketolide substituted by an imidazo-pyridyl side chain: HMR 3647. This compound demonstrated a potent activity against erythromycin susceptible and resistant pathogens, including penicillin G/erythromycin A-resistant S. pneumoniae and H. influenzae. In vivo, HMR 3647 displayed good pharmacokinetic parameters (Cmax = 2.9 microg/ml, bioavailability=49%, AUC0.8 = 17.2 microg.h/l, t1/2=1h) and was shown to have a high therapeutic efficacy in mice infected by various respiratory pathogens, including multi-resistant S. pneumoniae and Gram negative bacteria such as H. influenzae. HMR 3647 appears to be a very promising agent for the treatment of respiratory infections and is currently in clinical trials.

Animals↗

Tc-99m erythromycin lactobionate inhalation scintigraphy in parenchymal lung diseases.

We have investigated Technetium 99m erythromycin lactobionate (Tc 99m EL) clearance from the lungs after inhalation, in the presence of an alveolitis. Eighteen patients (6 sarcoidosis, 7 idiopathic fibrosis, and 5 miliary tuberculosis) were imaged after the patients inhaled 1,110 MBq of Tc 99m EL. Clearance half time for the first 45 min, for 24 h, and retention at 24 h correlated with percentage of lymphocytes in bronchoalveolar lavage fluid (BAL) (r = .729, r = .883, and r = .826, respectively). There was a positive correlation between peripheral penetration (PP) and forced expiratory volume in 1 s (FEV1) (r = .806) and forced vital capacity (FVC) (r = .781). Retention was more marked in sarcoidosis compared with tuberculosis (0.025 < p < or = 0.05). Radioaerosol lung imaging may reflect the pulmonary function impairment in parenchymal lung diseases. Retention of Tc 99m EL may be related to number of BAL cells or presence of a lymphocytic alveolitis. Long residency time of Tc 99m EL in the lungs implies that erythromycin can also be administered by inhalation for therapeutic purposes.

Administration, Inhalation↗