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PubMed1985

Plasmid-mediated resistance to lincomycin by inactivation in Staphylococcus haemolyticus.

Staphylococcus haemolyticus BM4610 was resistant to high levels of lincomycin and susceptible to macrolides, clindamycin, and streptogramins. This resistance phenotype, not previously reported for a human clinical isolate, was due to inactivation of the antibiotic. The gene conferring resistance to lincomycin in strain BM4610 was carried by a 2.5-kilobase plasmid, pIP855, which was cloned in Escherichia coli. Plasmid pIP855 caused inactivation of both lincomycin and clindamycin in S. haemolyticus and in E. coli but conferred detectable resistance to lincomycin only in S. haemolyticus and to clindamycin only in E. coli.

Clindamycin↗
PubMed1997

The oxazolidinone eperezolid binds to the 50S ribosomal subunit and competes with binding of chloramphenicol and lincomycin.

The oxazolidinones are a novel class of antibiotics that act by inhibiting protein synthesis. It as been reported that the drug exerts its primary activity on the initiation phase of translation. In order to study the possibility of direct interaction between the drug and the ribosome, we have developed a binding assay using 14C-labelled eperezolid (PNU-100592; formerly U-100592). Eperezolid binds specifically to the 50S ribosomal subunit of Escherichia coli. The specific binding of eperezolid is dose dependent and is proportional to the ribosome concentrations. Scatchard analysis of the binding data reveals that the dissociation constant (Kd) is about 20 microM. The binding of eperezolid to the ribosome is competitively inhibited by chloramphenicol and lincomycin. However, unlike chloramphenicol and lincomycin, eperezolid does not inhibit the puromycin reaction, indicating that the oxazolidinones have no effect on peptidyl transferase. In addition, whereas lincomycin and, to some extent, chloramphenicol inhibit translation termination, eperezolid has no effect. Therefore, we conclude that the oxazolidinones inhibit protein synthesis by binding to the 50S ribosomal subunit at a site close to the site(s) to which chloramphenicol and lincomycin bind but that the oxazolidinones are mechanistically distinct from these two antibiotics.

Acetamides↗
PubMed2005

New lnu(C) gene conferring resistance to lincomycin by nucleotidylation in Streptococcus agalactiae UCN36.

Streptococcus agalactiae UCN36 was resistant to lincomycin (MIC = 16 microg/ml) but susceptible to clindamycin (MIC = 0.12 microg/ml) and erythromycin (MIC = 0.06 microg/ml). A 4-kb HindIII fragment was cloned from S. agalactiae UCN36 total DNA on plasmid pUC18 and introduced into Escherichia coli AG100A, where it conferred resistance to lincomycin. The sequence analysis of the fragment showed the presence of a 1,724-bp element delineated by imperfect inverted repeats (22 of 25 bp) and inserted in the operon for capsular synthesis of S. agalactiae UCN36. This element carried two open reading frames (ORF). The deduced amino acid sequence of the upstream ORF displayed similarity with transposases from anaerobes and IS1. The downstream ORF, lnu(C), encoded a 164-amino-acid protein with 26% to 27% identity with the LnuA(N2), LnuA, and LnuA' lincosamide nucleotidyltransferases reported for Bacteroides and Staphylococcus, respectively. Crude lysates of E. coli AG100A containing the cloned lnu(C) gene inactivated lincomycin and clindamycin in the presence of ATP and MgCl2. Mass spectrometry experiments demonstrated that the LnuC enzyme catalyzed adenylylation of lincomycin.

Anti-Bacterial Agents↗
PubMed1975

Susceptibility of various serogroups of streptococci to clindamycin and lincomycin.

The minimal inhibitory concentration of lincomycin and clindamycin for a large number of strains from multiple serogroups of streptococci was determined. The median minimal inhibitory concentration for streptococci from groups A, B, C, F, G, H, L, and M and nongroupable organisms ranged from 0.02 to 0.39 mug of lincomycin per ml and from </=0.01 to 0.09 mug of clindamycin per ml. Among the group D strains, Streptococcus faecium and Streptococcus faecalis were resistant to lincomycin and clindamycin, whereas Streptococcus bovis and four American strains of Streptococcus durans resembled nongroup D isolates in their susceptibility to these agents. Occasional strains of nongroup D streptococci were highly resistant to lincomycin and clindamycin.

Clindamycin↗
PubMed1968

Effect of inoculum size on in vitro susceptibility testing with lincomycin.

There is disagreement in the literature as to whether lincomycin is primarily a bacteriostatic or a bactericidal agent against gram-positive cocci and also regarding the levels of activity of this agent against susceptible microorganisms. These questions were examined in a study of the effect of inoculum size on the results of tube dilution susceptibility determinations with lincomycin against 49 clinical isolates of Staphylococcus aureus and 25 strains of streptococci and pneumococci. Lincomycin was both highly active and bactericidal when tested against 40 strains of S. aureus with inocula containing a maximum of 10(4) cells per ml [median minimal inhibitory concentration (MIC), 0.78 mug/ml; median minimal bactericidal concentration (MBC), 1.56 mug/ml]. With inocula of 10(5) cells per ml, lincomycin was primarily bacteriostatic (median MIC, 1.56 mug/ml; median MBC, 12.5 mug/ml). There were further decreases in inhibitory levels and significant losses of bactericidal activity when inocula containing more than 10(7) cells were tested (median MIC, 3.13 mug/ml; median MBC > 100 mug/ml). Similar measurements with streptococci and pneumococci revealed a lesser effect of inoculum size. The mean MBC value for alpha-hemolytic streptococci increased from 0.40 to 1.05 mug/ml with an increase in inocula from 10(4) to 10(6) cells per ml, but without a marked increase in MIC values. Similar results were obtained for beta-hemolytic streptococci and pneumococci.

Bacteriological Techniques↗
PubMedDate not supplied

Comparative neuromuscular effects of lincomycin and clindamycin.

The effects of lincomycin and clindamycin on neuromuscular transmission in vitro were studied. Standard microelectrode technics were used to measure miniature endplate potential (MEPP) amplitude and frequency, and endplate sensitivity to acetycholine on the frog sartorius muscle. Twitch tension and nerve terminal acetycholine release were also studied. In the drug concentration range where twitch tension changes occurred, both drugs caused marked decreases in MEPP amplitude and decreases in endplate sensitivity to iontophoretically applied acetylcholine. Lincomycin did not alter MEPP frequency but decreased acetylcholine release. Clindamycin increased MEPP frequency and increased acetylcholine release. The study shows that both lincomycin and clindamycin cause blockade of neuromuscular transmission through a postsynaptic action. However, at high concentrations, lincomycin has a nerve-terminal depressant effect, while clindamycin has a marked presynaptic stimulatory effect.

Acetylcholine↗
PubMed1978

Osteomyelitis after operative fracture treatment. A report of 62 cases treated with radical surgery and lincomycin (Lincocin).

During the years 1967--1975 a total of 62 patients were treated for postoperative osteomyelitis. The lower extremities had been fractured in 89 per cent of the cases and 54 per cent were closed injuries. The fractures, mostly caused by traffic accidents and falls, had been immobilized by plates in 30 and by intramedullary nails or pins in 25 patients. Staphylococcus aureus was cultured in 80 per cent, 68 per cent of them were resistant to penicillin, but in 84 per cent the organisms were highly lincomycin sensitive and only three patients with four osteomyelitic lesions presented lincomycin resistance. The treatment consisted chiefly of sequestrectomies and saucerizations supported by 3--12 months of lincomycin treatment. In 30 operations a closed irrigation-suction technique was used, perfusing the wound with lincomycin solution. Stable implants should be left in place until the fracture is clinically solid whereas unstable osteosyntheses should be replaced by rigid internal or extraskeletal fixation. At follow-up, the results were judged as good in 74 per cent, fair 8 per cent and poor 18 per cent. The amputation rate was 13 per cent. Plates should not be used in the treatment of comminuted tibial fractures with considerable soft tissue damage.

Adult↗
PubMed1983

Lincomycin dose response for treatment of necrotic enteritis in broilers.

A dose response study was conducted to determine the appropriate (optimal) lincomycin concentration in drinking water for the treatment of necrotic enteritis (NE) in broilers. The study was replicated twice over time using a total of 2,895 broilers. Birds were raised in a facility containing a built-up litter from a source that experienced NE. They were commingled from 1 day of age until NE was observed. Lincomycin was mixed in drinking water at a rate of 0, .528, 2.114, 8.454, or 33.818 mg/liter for a period of 7 days. The study was terminated 3 weeks after initiation of therapy. Necrotic enteritis was diagnosed by mortality and pathological findings. The data on mortality were analyzed statistically using analysis of variance procedures. The Walker-Carmer technique was applied to estimate the appropriate lincomycin concentration. Lincomycin was effective for the treatment of NE in broilers at concentrations of greater than or equal to 2.114 mg/liter of drinking water. The minimal effective dose that would achieve maximal treatment response (optimal dose) against NE in broilers was estimated to be 16.9 mg lincomycin/liter of drinking water.

Animals↗
PubMed1983

Therapeutic effect of optimal lincomycin concentration in drinking water on necrotic enteritis in broilers.

The efficacy of 16.9 mg lincomycin/liter of drinking water was evaluated for the treatment of necrotic enteritis (NE) in 743 broiler-type chickens. Birds were raised in a facility containing a built-up litter obtained from a source that experienced NE. They were commingled from 1 day of age until NE was observed. Two groups of 6 pens each were given 0 or 16.9 mg lincomycin/liter of drinking water. Water medication was offered fresh daily for 7 days and the study was terminated 3 weeks after initiation of therapy. The susceptibility of Clostridium perfringens to lincomycin was determined in vitro. The test organism was susceptible to lincomycin as reflected by minimal inhibitory concentration and minimal lethal concentration of .156 microgram/ml. Mortality attributed to NE was 0% in lincomycin treated birds and 14% in nonmedicated control birds (P less than .01). Lincomycin water medication was highly effective for the treatment of NE in broilers.

Animals↗
PubMed1977

Incidence of antibiotic-related diarrhoea and pseudomembranous colitis: a prospective study of lincomycin, clindamycin and ampicillin.

An existing intensive drug monitoring system was used to study the occurrence of pseudomembranous colitis and diarrhoea in 100 patients treated with lincomycin and clindamycin. In order to give perspective to the results an equal number of matched patients treated with ampicillin were also studied. The incidences of diarrhoea in both groups were similar (11% in the lincomycin-clindamycin group and 8% in the ampicillin group). One patient developed pseudomembranous colitis associated with two prolonged courses of lincomycin therapy. The results suggest that the risks associated with the use of lincomycin are acceptable if the drug is given for the approved specific indications.

Adult↗
PubMed1988

Effects of lincomycin on synthesis of TEM beta-lactamase by Escherichia coli.

Sub-inhibitory concentrations of lincomycin slightly inhibit growth of Escherichia coli carrying plasmid RP4 and cause a 2-fold increase in TEM-2 beta-lactamase. To analyze this effect, cultures were pulse-labeled with [3H]leucine, chased with non-radioactive leucine and immunoprecipitated with anti-beta-lactamase antiserum. The synthesis rate of beta-lactamase was two times higher in inhibited cultures than in control cultures. No significant decrease of labeled enzyme occurred during the 30 minutes chase, indicating no degradation of beta-lactamase. The rate of maturation of pre-beta-lactamase was determined by measuring the decrease in the amount of pre-beta-lactamase after a 1-minute labeling interval. There was no significant difference between the control and lincomycin-treated cultures, indicating that posttranslational translocation is not involved in the stimulation. Both plasmid encoded and chromosomally encoded TEM-1 beta-lactamase increased in the presence of lincomycin. The effects of other protein synthesis inhibitors on the synthesis of TEM-1 beta-lactamase were examined. The stimulation of beta-lactamase synthesis by lincomycin appears to be specific for macrolide and related antibiotics and is not a general phenomenon resulting from partial inhibition of protein synthesis.

Anti-Bacterial Agents↗
PubMed2001

Gene lmrB of Corynebacterium glutamicum confers efflux-mediated resistance to lincomycin.

The lmrB gene of Corynebacterium glutamicum, which confers specific resistance to lincosamides, such as lincomycin and clindamycin, was isolated. C. glutamicum cells, carrying the lmrB gene in a multicopy plasmid, showed increased resistance to lincomycin with a MIC of 230 microg/ml, which is a 9-fold increase compared to that of the wild type. The lmrB-disrupted mutant became sensitive to the compound. No difference in sensitivity to erythromycin, penicillin G, tetracycline, chloramphenicol, spectinomycin, nalidixic acid, gentamicin, streptomycin, ethidium bromide, and sodium dodecyl sulfate was observed. The protonophore carbonyl cyanide m-chlorophenylhydrazone abolished the lincomycin-resistance of lmrB-carrying cells. The putative protein product of the gene contained 14-transmembrane regions and showed high amino acid-sequence homology to the drug efflux pumps of other organisms. In addition, the putative protein contained a motif for major facilitators, suggesting a role in efflux-mediated resistance to lincomycin.

Amino Acid Sequence↗
PubMed2002

[The application of nanofiltration membrane in the concentration and separation of lincomycin wastewater].

Two spiral nanofiltration membranes, MPS-44 (1.4 m2) and DLNF2-30 (0.24 m2), were connected in series to test the concentration process of lincomycin wastewater. Results indicated when the water inflow concentration was about 200 mg/L, the lincomycin concentration can reach 2000 mg/L after being concentrated for about 10-20 times. Such concentration can reach the demand of reuse, and the concentrating time was 60-70 h. During the concentration process, the CODCr retention was always above 80%, and the lincomycin retention was always over 90%, and the lincomycin recycle rate was over 90%.

Anti-Bacterial Agents↗
PubMed1991

A pilot study of parenteral lincomycin therapy in soft tissue infections.

From our study it is clear that lincomycin, given 300 mg intra muscularly daily in a single dose, is effective in a wide range of soft tissue infections especially those involving the head and neck region. An overall success rate of 88.8 per cent was observed in the 150 patients selected for the study. It is significant that in none of the subjects was any untoward reaction observed or reported. Hitherto all the previous systematic surveys on lincomycin appear to have been carried out on bone infections where, undoubtedly, lincomycin is highly effective. This pilot study furnishes an encouraging report on the successful treatment of soft tissue infections with parenteral lincomycin.

Adolescent↗
PubMed1989

Comparative antimicrobial activities of ribostamycin, gentamicin, ampicillin and lincomycin in vitro and in vivo.

The antimicrobial activity of ribostamycin, a unique aminoglycoside antibiotic possessing a neutral sugar component, was compared with those of gentamicin, ampicillin and lincomycin in vitro and in vivo. Ribostamycin showed comparable or slightly weaker in vitro activity than the reference antibiotics against Gram-positive bacteria. Against Gram-negative bacteria, ribostamycin was less active than gentamicin, but comparable to or more active than ampicillin. Lincomycin was less active or inactive to Gram-negative bacteria. Ribostamycin was active against some gentamicin-resistant bacteria, especially K. pneumoniae possessing the aminoglycoside-modifying enzymes AAC(3)-l and AAD(2"). The in vivo activity of ribostamycin was weaker than that of gentamicin, but comparable to that of ampicillin and lincomycin against Gram-positive bacteria, and superior to that of ampicillin against Gram-negative bacteria. The in vivo activity of ribostamycin was characterized by (i) and ED50 value not so affected by the challenge inoculum as that of ampicillin; (ii) a lower ED50 value by bolus administration than that by divided administration of the same dosage; and (iii) a lower ED50 value than that expected from the MIC value as compared with that of ampicillin and lincomycin. These characteristics are explained by the rapid and potent bactericidal activity of ribostamycin at high inoculum and high drug concentration, assisted by high serum concentration in mice.

Ampicillin↗
PubMed1988

[Effect of lincomycin and staphylococcal vaccine on the course of experimental staphylococcal sepsis].

Therapeutic efficacy of lincomycin used alone and in combination with inactivated staphylococcal vaccine and the effect of these agents on synthesis of antibodies and their content in blood serum were investigated. Lincomycin was shown to inhibit septic processes in the host. After its administration the number of the pathogens in the blood and organs markedly decreased. At the same time, lincomycin lowered antibody synthesis in the lymphoid organs and the content of alpha-antitoxins in blood serum. The use of lincomycin in combination with inactivated staphylococcal vaccine promoted an increase in the number of the antibody forming cells in the spleen and lymph nodes and the content of the antibodies to the staphylococcal alpha-toxin in blood serum of the animals with staphylococcal sepsis.

Animals↗
PubMed1988

[Intramolecular hydrogen bonds and conformation of the lincomycin molecule in organic solvents].

IR spectra (1600-1800 and 3000-3650 cm-1) of lincomycin base solutions in inert (CCl4 and C2Cl4), proton acceptor (dioxane, dimethylsulfoxide and triethyl amine) and proton donor (CHCl3, CD3OD and D2O) solvents were studied. Analysis of the concentration and temperature changes in the spectra revealed that association in lincomycin in the inert solvents was due to intramolecular hydrogen linkage involving amide and hydroxyl groups. Disintegration of the associates after the solution dilution and temperature rise was accompanied by formation of intramolecular bonds stabilizing the stable conformation structure of the lincomycin molecule. The following hydrogen linkage in the conformation was realized: NH...N (band v NH...N at 3340 cm-1), OH...O involving the hydroxyl at C-7 and O atoms in the D-galactose ring (band v OH...O at 3548 cm-1), a chain of the hydrogen bonds OH...OH...OH in the lincomycin carbohydrate moiety (band v OH...O at 3593 cm-1 and v OH of the end hydroxyl group at 3625 cm-1). Bonds NH and C-O of the amide group were located in transconformation. Group C-O did not participate in the intramolecular hydrogen linkage.

Hydrogen Bonding↗
PubMed1978

[Results of 10 years of use of lincomycin (1966-1976) in the clinics of the N. N. Priorov Central Research Institute of Traumatology and Orthopedics].

During 10 years 1063 patients were treated with lincomycin used parentally or orally at the N. N. Priorov Central Research Institute of Traumatology and Orthopedy. The doses and the rate of its use depended on the state of the patient, its age and weight. Lincomycin was used for the treatment of patients with osteomyelitis or purulent wound infection, as well as for prophylaxis of suppuration. The drug was used for a long period of time under conditions of the same hospital, and it was shown that it remained up to the present days highly effective in therapy of infections and especially bone infections caused by staphylococci sensitive to it. The 10-year study of staphylococcal sensitivity to lincomycin revealed an insignificant increase in the development of resistance to it. The paper presents data on the importance of adequate surgical interventions in addition to the antibiotic therapy in cases with bone infections. A possibility of lincomycin combined use with other antibiotics and gentamicin or kanamycin in particular was shown. Complications, such as diarrhea and urticaria were registered in 11 patients.

Adult↗