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PubMed1977

Extrachromosomal inheritance in Schizosaccharomyces pombe. IV. Isolation and genetic characterization of mutants resistant to chloramphenicol and erythromycin using the mutator properties of mutant anar-8.

Spontaneous chloramphenicol (capr)- and erythromycin (eryr)-resistant mutants were isolated from strain ade7-50 h- and the antimycin-resistant mutant anar-8 ade 7-50 h- of Schizosaccharomyces pombe (Sch. p.). By mitotic segregation analysis all 154 capr- and 120 eryr-mutants derived from ade 7-50 h- proved to be recessive chromosomal, whereas all 108 capr- and 200 eryr-mutants originating from anar-8 were extrachromosomally inherited. The rate of spontaneous capr- and eryr-mutants was about hundredfold in anar-8 compared to ade 7-50 h-. Growth of capr- and eryr-mutants was not inhibited by chloramphenicol or erythromycin, respectively, in glucose-medium and only slightly in glycerol-medium at concentrations which completely inhibited anar-8. By mitotic segregation-, tetrad-, and mitotic haploidization-analysis the extrachromosomal inheritance of mutants derived from anar-8 was established. Segregational patterns of capr- and eryr-determinants during mitosis, meiosis, and mitotic haploidization of diploids are discussed.

Ascomycota↗
PubMed1989

A single nucleotide substitution at the rib2 locus of the yeast mitochondrial gene for 21S rRNA confers resistance to erythromycin and cold-sensitive ribosome assembly.

We have studied a mutation (cs23) in the mitochondrial gene for 21S rRNA that affects the peptidyl transferase center of the ribosome and conditionally blocks the assembly of the 54S ribosomal subunit. Strains carrying this mutation are resistant to erythromycin and cold-sensitive for growth on nonfermentable carbon sources (Singh et al. 1978) Mitochondria isolated from mutant cells grown on glucose at 20 degrees C, the nonpermissive temperature, were depleted of the 54S subunit and instead contained a novel 45S ribosomal particle. After mutant cells were shifted from 20 degrees C to 32 degrees C, 54S subunits were assembled, apparently from the 45S particles and pre-existing ribosomal proteins. DNA sequencing revealed that the mutant phenotype is a consequence of a C to A transversion at position 3993 of the 21S rRNA gene. Previously, C to U and C to G mutations have been identified at the same position in the 21S rRNA sequence. This position corresponds to C-2611 in the E. coli 23S RNA, a nucleotide that appears to be conserved in the large rRNA of all erythromycin-sensitive ribosomes.

Base Sequence↗
PubMed1983

Erythromycin absorption in healthy volunteers from single and multiple doses of enteric-coated pellets and tablets.

The absorption of erythromycin from two different enteric-coated preparations was evaluated in three groups of healthy volunteers. After a single dose, taken after an overnight fast, absorption was significantly better from enteric-coated pellets than from tablets; both the mean peak serum concentration and the peak mean level were higher (p less than 0.01) in all three groups, and the mean area under the serum concentration-time curve (AUC) was at least 65% larger. Eight out of 23 subjects showed no or only a very low serum concentration after the enteric-coated tablets. In a follow-up study, 250 mg doses were given 6-hourly for 3 days, and again the mean maximum serum concentration was significantly higher (p less than 0.05) after the pellets. In conclusion, enteric-coated pellets led to more regular and predictable absorption of erythromycin than did coated tablets.

Adult↗
PubMed1982

Should erythromycin dose be altered in haemodialysis patients?

Erythromycin kinetics were studied in 17 patients with end stage renal failure treated with maintenance haemodialysis and 9 normal volunteers to discover if dialysis patients needed a modified dose. The elimination half life in dialysis patients (on dialysis days) was similar to that reported in normal subjects. Only small amounts of drug appeared in the dialysate, no patient loosing more than 9 mg in one dialysis. Both patients and volunteers had similar plasma concentrations 8 h after the end of a 5-day course. Protein-binding did not change significantly during dialysis and was similar to that reported in normal subjects. We conclude that dialysis patients requiring 1.5 g of erythromycin stearate daily or less can be given normal doses.

Adult↗
PubMed1985

Effect of concomitant food intake on absorption kinetics of erythromycin in healthy volunteers.

The steady state absorption of erythromycin from enteric-coated pellets of erythromycin base was compared with that from enteric-coated tablets in a randomized, two-way cross-over study in 24 healthy adult volunteers. A higher mean individual peak concentration (p less than 0.01), and a greater mean area under the serum concentration-time (0-8 h) curve (AUC, p less than 0.01) was produced by the enteric-coated pellets, when the preparations were administered 1 hour before breakfast. No significant differences in the kinetic parameters between the two preparations were observed when they were taken during a non-standardized breakfast, as concomitant food intake was found to reduce both the peak levels and the AUC-values (p less than 0.01) produced by the pelleted preparation.

Adult↗
PubMed1995

Vinblastine and erythromycin: an unrecognized serious drug interaction.

Vinblastine and erythromycin are among the most commonly used chemotherapeutic and antimicrobial agents, respectively. No interaction between the two has ever been reported. Towards the end of a phase I study of vinblastine plus oral cyclosporin (to reverse multidrug resistance), three patients also received erythromycin to raise their cyclosporin levels. All developed severe toxicity consistent with a much higher vinblastine dose than was actually given. This apparent potentiation of vinblastine toxicity has not been previously described.

Aged↗
PubMed1979

Single-dose fasting bioequivalence assessment of erythromycin stearate tablets in man.

The bioequivalence of film-coated erythromycin stearate tablets produced by five different manufacturers was evaluated in a balanced incomplete block design involving the five formulations given to 30 fasted subjects over a 3-week study period. Serum levels of erythromycin activity were determined microbiologically. Statistical analysis of variance was performed on the observed bioavailability parameters: maximum serum concentration (Cmax), time to maximum serum concentration (Tmax), and area under the serum concentration-time curve (AUC). There was no statistical difference between formulations for the Tmax parameter. Formulation differences were found, however, based on the analysis of variance of the Cmax and AUC parameters. Two products, although not significantly different from one another, showed significantly greater Cmax and AUC values than the other three products.

Adult↗
PubMed1994

[Fluorimetric determination of erythromycin residues in foods of animal origin after derivatization with FMOC and HPLC separation].

A high-performance liquid chromatographic (HPLC) method for the determination of the macrolide antibiotic erythromycin in eggs, milk, swine muscle, kidney and liver was developed. The drug was extracted from the matrix with acetonitrile. The raw extract was purified by liquid-liquid partitioning and fractionation by reversed-phase HPLC for additional cleanup. Erythromycin was reacted in a pre-column procedure with 9-fluorenylmethylchloroformate (FMOC) to enable fluorimetric detection (excitation 255 nm, emission 315 nm) after isocratic separation on an analytical RP-18 HPLC column. Mean recoveries ranged from 99% at fortification levels of 0.03 mg/kg in egg to 38% at 0.06 mg/kg in liver. With the exception of liver all detection limits were below 0.01 mg/kg and precision for all other matrices and tested concentrations (0.015-0.09 mg/kg) better than 20% (coefficient of variation).

Animals↗
PubMed1982

[The pharmacokinetics of 1,000 mg erythromycin lactobionate i. v. in patients with respiratory tract infections (author's transl)].

Pharmacokinetic data were determined in 16 patients with respiratory tract infections who had received 1,000 mg erythromycin lactobionate i. v. The infusion lasted 60 or 30 minutes. The peak concentrations were 33.3 mg/l (60 min group) and 34.4 mg/l (30 min group). The elimination half-lives were 2.0 h and 1.9 h. The concentrations are considerably higher than those found following the peroral administration of erythromycin. We did not find a cumulative effect after four administrations at 12-hour intervals. The clinical efficacy was good.

Administration, Oral↗
PubMed1988

In vitro activity of azithromycin and erythromycin against organisms associated with bacterial vaginosis and chancroid.

The in vitro activity of the new macrolide azithromycin and erythromycin against Haemophilus ducreyi, Gardnerella vaginalis, Bacteroides spp. and Mobiluncus spp. was compared. Gardnerella vaginalis, Mobiluncus spp. and Haemophilus ducreyi were highly susceptible to both agents but azithromycin was more effective overall against all three groups of organisms. The activity of both antibiotics against Bacteroides spp. varied greatly, but azithromycin was again more active. Collectively, 62% of all Bacteroides strains were susceptible to erythromycin (MIC 1 mg/1) and 74% were susceptible to azithromycin.

Azides↗
PubMed1990

Comparative in vitro activity of azithromycin, clarithromycin, erythromycin and lomefloxacin against Mycoplasma pneumoniae, Mycoplasma hominis and Ureaplasma urealyticum.

The in vitro activity of three macrolides, azithromycin, clarithromycin and erythromycin and a new fluoroquinolone, lomefloxacin, against pathogenic mycoplasma (16 to 18 strains of Mycoplasma pneumoniae, 41 to 77 strains of Mycoplasma hominis, 65 to 104 strains of Ureaplasma urealyticum) was compared. The three macrolides were highly active against Mycoplasma pneumoniae. Clarithromycin was the most active macrolide against Ureaplasma urealyticum whereas azithromycin was somewhat more active than erythromycin against Mycoplasma hominis. Lomefloxacin was moderately active against all three mycoplasma species.

4-Quinolones↗
PubMed1990

Intraphagocytic activity of erythromycin, roxithromycin and azithromycin.

The intraphagocytic activity of erythromycin, roxithromycin and azithromycin against phagocytosed Staphylococcus aureus was compared. Erythromycin and roxithromycin both acted bacteriostatically at concentrations corresponding to 10 X MIC. Azithromycin, however, did not prevent intracellular proliferation of the staphylococci. On comparison of the pH dependency of the antibacterial activity of the three drugs, azithromycin was found to be inactivated earlier in an acidic milieu.

Azithromycin↗
PubMed1993

Erythromycin-associated ergotamine intoxication: arteriographic and electrophysiologic analysis of a rare cause of severe ischemia of the lower extremities and associated ischemic neuropathy.

Vasospasm associated with ergotamine is a well-known phenomenon. In this case report we present a rare drug interaction between erythromycin and ergotamine at normal doses causing lower extremity ischemia in a 36-year-old woman. Nitroprusside proved to be the treatment of choice. The response was dramatic and took place in a matter of hours in this patient. Ischemic monomelic neuropathy is a recently described entity in which axonal necrosis is caused by a loss of distal extremity blood flow. The association between erythromycin and ergotamine may be a dangerous pharmacologic combination; drugs that have a hepatic cycle with ergotamine derivatives must be used with caution.

Adult↗
PubMed1982

Flavobacterium meningosepticum ventriculitis: in vivo and in vitro results with the combinations rifampicin-erythromycin and mezlocillin-cefoxitin.

A case of Flavobacterium meningosepticum ventriculitis is described in which the failure of therapy with a combination of rifampicin and erythromycin is attributed to inadequate antibiotic levels in cerebrospinal fluid. The successful eradication of the organism was achieved with the use of mezlocillin and cefoxitin given by the intravenous and intraventricular route. In vitro sensitivity tests of recently isolated strains of Flavobacterium meningosepticum suggested that the combination mezlocillin and cefoxitin is more often synergistic than rifampicin and erythromycin.

Anti-Bacterial Agents↗
PubMed1982

Effects of subminimal inhibitory concentrations of chloramphenicol, erythromycin and penicillin on group A streptococci.

Group A streptococci strains were grown in broth containing subminimal inhibitory concentrations of chloramphenicol, erythromycin and penicillin, and tested for possible changes in colonial morphology, activity and amount of cellular and extracellular components. The following components were tested: T protein, M protein, opacity factor, lipoteichoic acid, hyaluronic acid, streptolysin S, streptolysin O, DNase, hyaluronidase and NADase. Sub-MICs of these drugs produced variable changes in the bacteria. They increased the amount of hyaluronic acid and hyaluronidase, decreased the amount of M protein, and enhanced phagocytosis and the release of lipoteichoic acid. The results indicate that sub-MICs of chloramphenicol, erythromycin and penicillin may affect the pathogenicity and toxinogenicity of group A streptococci.

Chloramphenicol↗
PubMed1987

Disk diffusion and disk elution tests with A-56268 and erythromycin.

Zones of inhibition around 15 micrograms A-56268 disks were essentially the same size as those around 15 micrograms erythromycin disks. If the same MIC breakpoints are to be used for defining susceptible categories for both macrolides, interpretive zone size standards for erythromycin disk tests may also be used for A-56268 disk tests. Against anaerobic bacteria, the two macrolides were only marginally effective when broth dilution tests were incubated in anaerobic jars. The aerobically incubated thioglycolate broth disk elution test indicated that both macrolides were much more effective against anaerobes. Three 15 micrograms disks eluted in 5 ml thioglycolate provided satisfactory results.

Bacteria↗
PubMed1995

Efficacy and safety of azithromycin versus benzylpenicillin or erythromycin in community-acquired pneumonia.

Azithromycin, a recently introduced antibiotic, offers the potential advantages of short-course administration and lower toxicity compared to other macrolides. Approved for the treatment of mild pneumonia, this drug was investigated in a study of patients hospitalized for community-acquired pneumonia. In an open-labelled randomized study, oral azithromycin was compared with intravenous benzylpenicillin in patients suspected to have pneumococcal pneumonia. Azithromycin was also compared with erythromycin, both administered orally, in all other patients. Three hundred thirty-four patients with community-acquired pneumonia were hospitalized, 108 of whom were randomized; 104 could be evaluated. A need for intravenous therapy was the most common reason for exclusion. In the pneumococcal group, 35 patients received azithromycin and 29 benzylpenicillin. The clinical and radiological success rate achieved with azithromycin (83%) was considerably higher than that achieved with benzylpenicillin (66%), though the difference was not significant. In the non-pneumococcal group, 19 patients received azithromycin and 21 erythromycin; no differences in the success rate were found (79% and 76%, respectively). Eight patients on azithromycin had a blood culture positive for Streptococcus pneumoniae; in three of these patients therapy was changed. None of the five patients with pneumococcal bacteraemia who received benzylpenicillin required a change in therapy. It is concluded that oral azithromycin, administered as short-course therapy, is an appropriate antibiotic for treating patients with community-acquired pneumonia. However, it is not yet certain that azithromycin is a good choice for patients with pneumococcal bacteraemia.

Administration, Oral↗