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PubMed1976

Multiple drug-resistance in staphylococci, an analysis of all-nation computer-processed data.

In a previous communication from this Institute it was assessed that multiple drug resistance plays a decisive role in overall antibiotic resistance of staphylococci and that true data of the extent of multiresistance depend decisively on sufficient number of antibiotics toward which strains of a given species is tested. It was found, by analysis of more than 60 000 staphylococcal strains isolated by Public Health Laboratories in the Slovak Socialist Republic (S.S.R.) during the period of one year, that triple and quadruple resistance is the most prevalent one in staphylococci - not regarded, however, the penicillin resistance which is absolutely predominant. Present analysis also shows that resistances to streptomycin, tetracyclines, erythromycin and kanamycin (STEK type) are both most frequent and mutually selective, i.e. strains resistant to any of these drugs (and also to penicillin, i.e. PSTEK type) show resistance also to other antibiotics of this group. In contrast, chloramphenicol resistance seems not to be connected with resistance to these substances nor is resistance to newer specific anti-staphylococcal antibiotics, used only recently in this country, as is oxacillin, lincomycin and cefaloridin. Nevertheless, lincomycin seems to select a co-resistance as many lincomycin-resistant strains were resistant also to oxacillin but not vice versa. Increasing resistance of staphylococci in S.S.R. to kanamycin and particularly to erythromycin, and their frequent occurrence in multiresistance types is a warning feature which might lead to an increase of therapeutic crisis in staphylococcal infections.

Anti-Bacterial Agents↗
PubMed1999

Sites and mechanisms of antibiotic-induced neuromuscular block: a pharmacological analysis using quantal content, voltage clamped end-plate currents and single channel analysis.

Since the original observation of Vital Brazil and Corrado (1957) concerning the antibiotic induced neuromuscular block produced by streptomycin, there has been considerable interest in the mechanisms responsible for not only neuromuscular block but also the effects of antibiotics on different systems. We used the voltage clamped end-plate of transacted skeletal muscle to examine the concentration-dependent actions of several groups of antibiotics. The aminoglycoside antibiotics, neomycin and streptomycin, were both more effective at reducing quantal release of acetylcholine (ACh) than interacting with the postjunctional ACh receptor-channel complex. Neomycin was approximately 10 X more potent prejunctionally than streptomycin and the prejunctional effects of each antibiotic were reversed competitively by raising extracellular calcium. Both neomycin and streptomycin also had postjunctional actions at higher concentrations. Neomycin interacted with the open state of the ACh receptor ion channel complex while streptomycin blocks the ACh receptor. The lincosamide antibiotics, lincomycin and clindamycin produced their neuromuscular block postjunctionally by interacting with the open state of the ACh-receptor channel complex. Clindamycin is approximately 20 X more effective at blocking the open channel than was lincomycin. Using cell attached patch clamp recordings in cultured rat myotubes, we demonstrated a lincosamide-induced block of open ion channels with clindamycin having a much slower unblocking rate than lincomycin. Using epimers of the lincosamides, we demonstrated that lipophilicity of the molecule, rather than stereochemical considerations, is important for open channel blockade affecting primarily the "off" rate of channel blocking. This mechanism appears important for not only the lincosamide antibiotics but also for the postjunctional actions of the aminoglycoside antibiotics, particularly neomycin.

Animals↗
PubMed1975

Studies of the enterohepatic circulation of morphine in the rat.

The disposition of 14C-morphine was studied after gastrointestinal and subcutaneous administration to female Sprague-Dawley rats. Morphine was found to be rapidly and nearly completely absorbed from the small intestine. After s.c. administration, approximately half the 5 mg/kg dose of morphine was excreted via the bile into the intestinal tract, largely as morphine glucuronide. Unlike morphine, the glucuronide conjugate in bile was poorly absorbed from the small intestine where its hydrolysis occurred slowly. After administration into the cecum, however, hydrolysis of the conjugate was rapid, and the rate of absorption of radioactive material was similar to that of free morphine. Treatment of rats with lincomycin (500 mg/1 in drinking water and 25 mg twice a day by gastric intubation for 4 days) significantly decreased cecal hydrolysis of the conjugate and the cecal absorption of radioactive material. Lincomycin treatment also increased fecal excretion of the conjugate in rats given morphine s.c. (5 mg/kg). These findings indicated that hydrolysis of morphine glucuronide is dependent upon the status of enteric bacteria and is a prerequisite to the enterohepatic circulation of morphine. In addition, after lincomycin treatment, a greater percentage of radioactivity excreted in the urine was associated with free morphine. This finding could be expained by the demonstration of pH dependence of renal excretion of morphine and a first-pass effect for this drug.

Ammonium Chloride↗
PubMed2003

[Efficacy of treatment of chronic destructive forms of apical periodontitis using oral decontamination antibiotic therapy].

The efficiency of preventive oral antibiotic therapy before the root channel filling was evaluated in 78 patients with granulating and granulomatous chronic periodontitis. Positive clinical changes were observed after lincomycin or rondomycin therapy (p = 0.017). The number of complaints was also less in the latter group (p > 0.05). The incidence of x-ray restoration of periapical foci of bone tissue destruction during 6 and 12 months was significantly higher (p < 0.05 and p < 0.01) after preventive treatment with lincomycin or rondomycin, characterized by potent osteotropic effects (decontamination with rondomycin 81.8%, with lincomycin 70.3% vs. 31.0% without decontamination therapy).

Administration, Oral↗
PubMed1992

[Eremomycin in the treatment of antibiotic-associated colitis in golden hamsters].

The efficacy of eremomycin, a new glycopeptide antibiotic, was studied on a model of antibiotic-associated colitis in golden hamsters. The colitis was induced by intraperitoneal or intragastric administration of lincomycin. In a dose of 100 mg/kg administered orally once a day for 5 days eremomycin protected the animals from the lincomycin-induced colitis: some animals survived, the others died in later periods. When the animals were infected with a pathogenetic strain of Clostridium difficile followed by exposure to lincomycin the use of eremomycin produced the similar effect.

Administration, Oral↗
PubMedDate not supplied

A comparison of three different prophylactic parenteral antibiotic regimens in colorectal surgery: a prospective study.

A double-blind, prospective, randomized study was performed with 90 patients undergoing colorectal surgery, to ascertain the prophylactic effect of three different parenteral antibiotic programs. The patients were divided into three groups. The patients in group 1 received 80 mg Gentamycin and 600 mg Lincomycin intramuscularly, two hours preoperatively, and every eight hours postoperatively for three days. In group 2, the treatment was similar to group 1 but the Lincomycin was replaced by 600 mg Clindamycin. In Group 3, the treatment was also similar to group 1, but 500 mg Metronidazole given over 20 minutes replaced the Lincomycin. The present study, the first comparing three antianaerobic antibiotics and an aminoglycoside in the prophylaxis of infection in colorectal surgery, shows certain clinical and socioeconomic benefits, although not statistically significant to be found in the group 3 program (Gentamycin plus Metronidazole) as compared with the other programs. This advantage was no doubt due to the use of Metronidazole (used in group 3 only), because of its effectiveness against anaerobic bacteriae.

Adult↗
PubMed1982

[Effect of antibiotic and vaccine therapies on the succinate dehydrogenase and phosphatase activity of liver cells of mice infected with Staphylococcus].

Changes in the activity of succinate dehydrogenase (SDH), total and acid phosphatase (TP and AP) were studied in treatment of laboratory animals with rifampicin, lincomycin and with inactivated staphylococcal vaccine used alone or in combinations. It was shown that immunization of the animals with inactivated staphylococcal vaccine under conditions of experimental staphylococcal infection promoted stimulation of the enzyme activity. Rifampicin and lincomycin used for the treatment of such animals lowered the activity of the enzymes. The suppressing effect of the antibiotics increased with an increase in the period of their use. It should be noted that the inhibitory effect of rifampicin on the activity of SDH, TP and AP was less pronounced than that of lincomycin. The combined use of the vaccine and antibiotics for the treatment of the animals promoted an increase in the enzyme activity as compared to the use of the antibiotics alone. Sometimes the activity of SDH, TP and AP reached the control levels in such animals or the levels observed in the animals treated with the vaccine alone. Stimulation of the enzyme activity was more pronounced when the vaccine was used in combination with rifampicin.

Animals↗
PubMed1983

[Effect of antibiotic therapy and vaccine therapy on the phagocytic reaction in mice infected with Staphylococcus].

The time course of changes in the activity, intensity and completeness of phagocytosis with leukocytes of the peritoneal exudate was studied on mice with experimental staphylococcal infection treated with rifampicin, lincomycin and inactivated staphylococcal vaccine used alone or in combination. It was shown that immunization of the animals with inactivated staphylococcal vaccine promoted stimulation of the phagocytic defense. Rifampicin and lincomycin applied therapeutically induced a decrease in the activity, intensity and completeness of phagocytosis. It should be noted that rifampicin had a less pronounced inhibitory effect than lincomycin. The combined use of vaccine and antibiotics with therapeutic purposes promoted an increase in phagocytosis as compared to the use of the antibiotics alone. The combined therapy sometimes resulted in completeness of phagocytosis making it reach the control values (the 10th and 15th days, rifampicin and vaccine). It should be noted that a more pronounced stimulation of the activity, intensity and completeness of the phagocytosis was observed with the use of the combination of rifampicin and the vaccine.

Animals↗
PubMed2001

Applications of a copper microparticle-modified carbon fiber microdisk array electrode for the simultaneous determination of aminoglycoside antibiotics by capillary electrophoresis.

A copper microparticle-modified carbon fiber microdisk array electrode was fabricated and employed in capillary electrophoresis for the simultaneous determination of the five aminoglycoside antibiotics (AGs) including netilmicin, tobramycin, lincomycin, kanamycin and amikacin. The array electrode exhibited high catalytic activity for AGs, good reproducibility and stability. Under the optimum separation conditions (separation voltage of 6.2 kV, electrophoretic medium of 125 mM NaOH), the five AGs above were baseline separated within 20 min. At a working electrode potential of 0.7 V (versus saturated calomel electrode), the calibration curves were linear over two orders of magnitude of concentration, and the detection limits (SIN=3) were below 2 microM except for lincomycin (6.7 microM). The developed method was successfully employed for the simultaneous determination of the five AGs studied in pharmaceutical injections. The feasibility of this method for the simultaneous determination of lincomycin, kanamycin and amikacin in urine sample was also demonstrated.

Aminoglycosides↗
PubMed2002

Comparative pulsed-field gel electrophoresis typing of gentamicin-resistant and -susceptible methicillin-resistant Staphylococcus aureus strains isolated in France between 1991 and 1998. Changes in antibiotic susceptibility.

Using macrorestriction of genomic DNA and pulsed-field gel electrophoresis, we examined 504 non-redundant, infection-causing human isolates of methicillin-resistant Staphylococcus aureus susceptible (G(S): 238 isolates) or resistant to gentamicin (G(R): 266 isolates). The strains were isolated at Albert Chenevier Hospital (Créteil, France) between 1 January 1991 and 31 December 1998. Their susceptibility to erythromycin, lincomycin, tetracycline, rifampicin, fusidic acid and fosfomycin was also studied. Seventy-six genotypes were identified (percentage similarity<80). Ten types, each containing at least eight strains, predominated. G(R) strains showed higher genetic polymorphism than G(S) strains: the 266 G(R) isolates belonged to 67 genotypes, five of which predominated (44, 42, 38, 30 and 15 isolates); the 238 G(S) isolates belonged to only 18 types, four of which predominated (112, 83, 11 and 10 isolates). Fifty-six percent of G(R) strains (34 Gt) were resistant to erythromycin, lincomycin, tetracycline and rifampicin, and were isolated at relatively stable frequencies. Resistance to five antibiotics studied (susceptible to fusidic acid) was observed among 16.5% of G(R) strains. The frequency of strains with this profile diminished from 30% in the early 1990s to 10% in 1998. One hundred and twenty-six G(S) isolates were susceptible to all six antibiotics; this profile was only found from 1993 onwards, and was increasingly frequent (60% of G(S) strains in 1996). Resistance to erythromycin and lincomycin only was found in 70 G(S) isolates; this profile accounted for approximately half the isolates in 1992/1993 and only one-third in 1998. These results, obtained over an eight-year period, show an overall increase in antibiotic susceptibility. They confirm the spread of two major clones of MRSA-G(S) and support the hypotheses that G(S) strains derive from G(R) strains that have lost the aac6'-aph2" gene; and that G(S) strains are genetically related to those that were present before the use of gentamicin and persisted at a low frequency until 1992-1993.

Anti-Bacterial Agents↗
PubMed2006

Antimicrobial susceptibility testing of Brachyspira intermedia and Brachyspira pilosicoli isolates from Australian chickens.

Susceptibilities of predominantly Australian isolates of the pathogenic intestinal spirochaetes Brachyspira intermedia (n = 25) and Brachyspira pilosicoli (n = 17) from chickens were tested in agar dilution against four concentrations each of the antimicrobials tiamulin, lincomycin, tylosin, metronidazole, tetracycline and ampicillin. Based on available minimum inhibitory concentration (MIC) breakpoint values for Brachyspira hyodysenteriae or other Gram-negative enteric veterinary pathogens, isolates of both species generally were susceptible to tiamulin, lincomycin, metronidazole and tetracycline. Although not classed as resistant, four isolates of B. intermedia had an elevated MIC range for tiamulin (1 to 4 mg/l), 11 isolates of B. intermedia and five of B. pilosicoli had an elevated MIC range for lincomycin (10 to 50 mg/l), one isolate of B. pilosicoli had an elevated MIC range for tetracycline (10 to 20 mg/l), and one isolate of B. intermedia and five of B. pilosicoli had an elevated MIC range for ampicillin (10 to 50 mg/l). A clear lack of susceptibility to tylosin (MIC > 4 mg/l) was seen in 11 isolates each of B. intermedia and B. pilosicoli, and to ampicillin (MIC > 32 mg/l) in two isolates of B. pilosicoli. These data suggest that some resistance to common antimicrobials exists among intestinal spirochetes obtained from laying hens and supports the need of MIC data for clinical isolates before any treatment is considered.

Animals↗
PubMed2006

Resistance to macrolides, lincosamides, streptogramins, and linezolid among members of the Staphylococcus sciuri group.

This study aimed to characterize the resistance profiles of the Staphylococcus sciuri group members to macrolides, lincosamides, streptogramins (MLS antibiotics), and linezolid upon analysis of large series of isolates that included 162 S. sciuri isolates, nine S. lentus, and one S. vitulinus. The evaluation of their susceptibility by disk diffusion and agar dilution methods, along with PCR detection of the resistance genes erm(A), erm(B), erm(C), mef(A), lnu(A), and lnu(B), were performed. Resistance to macrolides was detected in 10 (5.8%) tested strains, with three and six isolates exhibiting constitutive and inducible MLS(B) resistance phenotypes, respectively. Resistance mediated by active efflux was detected in one strain. The presence of genes conferring resistance, namely erm(B) or erm(C), was detected in two strains. All tested strains were susceptible to pristinamycin and linezolid. Of 172 tested strains, 70.9% were resistant and 26.2% had intermediary resistance to lincomycin, whereas 1.7% were resistant and 50% had intermediary resistance to clindamycin. The lnu(A) gene was detected in two strains only. The great majority of the tested S. sciuri strains (153 out of 162; 94.4%) presumably exhibited LS(A) phenotype because they did not carry lnu genes nor displayed constitutive MLSB resistance, but still showed intermediate resistance or resistance to lincomycin (MICs of 4, 8, 16, and 32 microg/ml). The results obtained indicate that S. sciuri may be naturally resistant to lincomycin. Expression of a novel type of inducible resistance to lincosamides, induced by erythromycin in erythromycinsusceptible strains, was observed in the S. sciuri group isolates.

Acetamides↗
PubMed2004

Phenotypic and molecular characterization of macrolide and streptogramin resistance in Streptococcus mitis from neutropenic patients.

OBJECTIVES: To determine the prevalence of macrolide and streptogramin resistance in Streptococcus mitis isolates from neutropenic patients and to identify mechanisms of macrolide and streptogramin resistance in resistant isolates. METHODS: MICs of erythromycin, spiramycin, lincomycin and pristinamycin were determined for S. mitis isolates. Macrolide-resistance genes were characterized by PCR and ribosomal mutations by sequencing. RESULTS: A total of 169 S. mitis isolates were recovered from 66 patients at the Tunisian Bone Marrow Transplant Centre. Of these, 120 (70%) were non-susceptible to erythromycin and one was resistant to pristinamycin; 48.5% of isolates had an MLSB phenotype with cross-resistance between erythromycin, spiramycin and lincomycin, 4% had a dissociated MLSB phenotype with resistance to erythromycin and spiramycin but apparent susceptibility to lincomycin and 47.5% displayed the M phenotype. Resistance determinants were characterized in 33 isolates. Ten of 14 isolates with the cross MLSB resistance contained an ermB-like gene and four a combination of ermB- and mefA-like genes. Four of the five isolates with a dissociated MLSB phenotype contained ermB-like and one a combination of ermB- and mefA-like genes. All the 14 isolates with an M phenotype contained mefA-like genes. The pristinamycin-resistant strain had G105 and A108 substitutions in the conserved C terminus of the L22 ribosomal protein. CONCLUSIONS: The prevalence of macrolide resistance is high in S. mitis from neutropenic patients and is due to the spread of ermB- or mefA-like genes alone or combined. Resistance to streptogramins is rare and in this case associated with ribosomal mutation.

Amino Acid Sequence↗
PubMed2003

Contribution of photosynthetic electron transport, heat dissipation, and recovery of photoinactivated photosystem II to photoprotection at different temperatures in Chenopodium album leaves.

Temperature dependence of photoinhibition and photoprotective mechanisms (10-35 degrees C) was investigated for Chenopodium album leaves grown at 25 degrees C under 500 micro mol quanta m(-2) s(-1). The fraction of active photosystem II (PSII) was determined after photoinhibitory treatment at different temperatures in the presence and absence of lincomycin, an inhibitor of chloroplast-encoded protein synthesis. In the absence of lincomycin, leaves were more tolerant to photoinhibition at high (25-35 degrees C) than at low (11-15 degrees C) temperatures. In the presence of lincomycin, the variation in the tolerance to photoinactivation became relatively small. The rate constant of photoinactivation (k(pi)) was stable at 25-35 degrees C and increased by 50% with temperature decrease from 25 to 11 degrees C. The rate constant of recovery of inactivated PSII (k(rec)) was more sensitive to temperature; it was very low at 11 degrees C and increased by an order of magnitude at 35 degrees C. We conclude that the recovery of photoinactivated PSII plays an essential role in photoprotection at 11-35 degrees C. Partitioning of light energy to various photoprotective mechanisms was further analyzed to reveal the factor responsible for k(pi). The fraction of energy utilized in photochemistry was lower at lower temperatures. Although the fraction of heat dissipation increased with decreasing temperatures, the excess energy that is neither utilized by photochemistry nor dissipated by heat dissipation was found to be greater at lower temperatures. The k(pi) value was strongly correlated with the excess energy, suggesting that the excess energy determines the rate of photoinactivation.

Adaptation, Physiological↗
PubMed1999

Plastid translation is required for the expression of nuclear photosynthesis genes in the dark and in roots of the pea lip1 mutant

The expression of nuclear photosynthesis genes in pea seedlings requires both light and a postulated signal produced by developing plastids. The requirement for the plastid signal for the accumulation of transcripts of Lhcb1, RbcS, PetE, and AtpC genes was investigated in the pea mutant lip1, which shows light-independent photomorphogenic development. Lincomycin and erythromycin, inhibitors of plastid translation, decreased the accumulation of transcripts of nuclear photosynthesis genes in shoots of light-grown wild-type and lip1 seedlings, indicating that the plastid signal is required in the lip1 mutant. Treatment with lincomycin or erythromycin also reduced the accumulation of transcripts in shoots of dark-grown lip1 seedlings, indicating that light is not an obligate requirement for the synthesis or activity of the plastid signal. Lincomycin had a similar effect on the accumulation of Lhcb1 transcripts in dark-grown cop1-4 seedlings of Arabidopsis. Accumulation of transcripts of nuclear photosynthesis genes was also observed in roots of light-grown lip1 seedlings, and this accumulation, which was associated with the development of chloroplasts, was again dependent on plastid translation. The plastid signal therefore regulates the expression of nuclear photosynthesis genes in the dark and in roots of the lip1 mutant.

Journal Article↗
PubMed1977

Drug resistance in Streptococcus pyogenes isolated in Japan.

Drug resistance of Streptococcus pyogenes strains isolated during 1974 and 1975 in various districts in Japan were surveyed and compared with an earlier survey of 1970 to 1973. Of 1,021 strains, tetracycline-, macrolide antibiotic-, lincomycin-, and chloramphenicol-resistant strains were demonstrated at frequencies of 80.3, 62.3, 60.8, and 57.9%, respectively. Distinct group resistances to penicillin and aminoglycoside antibiotics could not be identified among the strains examined. It was characteristic that quadruple and triple resistances were manifested among the strains resistant to macrolide antibiotics, lincomycin, tetracycline, and chloramphenicol, and they were confined to the T-type 12. The emergence of multiply resistant streptococcal strains was due mostly to the rapid increase in isolation frequency of macrolide antibiotic- or macrolide antibiotics-lincomycin-resistant strains.

Anti-Bacterial Agents↗
PubMed1973

Susceptibility of Bacteroides fragilis to six antibiotics determined by standardized antimicrobial disc susceptibility testing.

The susceptibility of 100 or more strains of Bacteroides fragilis to six antibiotics was determined by standardized agar dilution and disc diffusion tests. Good correlation of results of the two methods was obtained with chloramphenicol, clindamycin, lincomycin, penicillin, and vancomycin. Correlation of results with erythromycin was not as good. A great deal of overlapping of zone diameters among strains classed as susceptible, intermediate, and resistant occurred with both erythromycin and lincomycin, making interpretation of disc diffusion tests difficult. All strains tested were susceptible to chloramphenicol; 94% were susceptible to clindamycin at concentrations readily achieved with ordinary dosage, and all strains were inhibited by 6.2 mug/ml, a level which is achieved with somewhat more intensive therapy. Only 7% were shown to be susceptible to erythromycin and 13% to lincomycin under the conditions of our testing procedure. Only a small percentage of the strains were susceptible to penicillin, and none was susceptible to vancomycin.

Anti-Bacterial Agents↗
PubMed1989

Comparison of four charcoal media for the isolation of Bordetella pertussis.

Charcoal-horse blood agar with 40 micrograms of cephalexin per ml, charcoal-horse blood agar with 3 micrograms of lincomycin per ml, charcoal agar with 3 micrograms of lincomycin per ml, and Legionella (buffered charcoal-yeast extract) agar with 3 micrograms of lincomycin per ml were compared for isolation of Bordetella pertussis. Charcoal-horse blood agar with 40 micrograms of cephalexin per ml gave the best results, with a B. pertussis recovery rate of 100%. Growth was most rapid and the mean number of colonies was highest on this agar, and growth of pharyngeal flora was completely suppressed.

Agglutination Tests↗