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PubMed1978

Therapeutic effects of various concentrations of lincomycin in drinking water on experimentally transmitted swine dysentery.

Three experimental studies were conducted in 232 growing pigs (8 to 12 weeks old) to evaluate the therapeutic effects of various concentrations of lincomycin in drinking water, against swine dysentery experimentally transmitted, by oral inoculation or by contact-commingling exposure. Four or 5 concentrations of lincomycin were used in each experiment (132, 66, 33, 16.5 or 0.0 mg/L of drinking water). Medication was initiated 7 to days after exposure and was continued for 6 to 10 days. Both methods of exposure were capable of transmitting the disease successfully. A more marked dose response was noticed in pigs inoculated orally than in pigs that were exposed by contact. All concentrations of lincomycin were effective for the treatment of swine dysentery by oral or by contact exposure. At the smaller concentration of 16.5 mg/L of drinking water, lincomycin was less effective for treating the disease than it was at greater concentrations. The suggested optimal concentration was 33 mg of lincomycin/L of drinking water for the treatment of swine dysentery.

Administration, Oral↗
PubMed1965

Lincomycin in hospital practice.

The usefulness of the new antibiotic, lincomycin, was assessed on both bacteriological and clinical grounds. Of 3200 strains of staphylococci isolated from clinical material, only 40 were resistant to lincomycin. These 40 were all of the same phage type and in fact almost all represented different isolations of the same staphylococcus which had spread to cross-infect various patients. Sixteen of 22 patients with staphylococcal infections, nine of 14 with pneumonia, 15 of 17 with acute exacerbations of bronchitis and two patients with other bacterial infections recovered completely with lincomycin therapy. The only side effect was diarrhea in four of the 42 patients given the drug by mouth. The place of lincomycin in therapeutics seems to be principally in the treatment of chronic osteomyelitis and, in patients allergic to the penicillins, in the treatment of staphylococcal, respiratory and other infections for which penicillin is usually employed.

Bronchitis↗
PubMed1984

[Experimental study of lincomycin ointment and gel].

The pharmacokinetics and safety of the lincomycin ointment and gel were studied. It was shown that diffusion of lincomycin through the skin was satisfactory. Investigation of their general toxicity and organotropic properties revealed neither irritating effect nor changes in the internal organs associated with the toxic effect of the drugs. On the basis of the data on the stability of the lincomycin ointment and gel obtained on their storage the lincomycin ointment was recommended for industrial production.

Administration, Topical↗
PubMedDate not supplied

Gas chromatographic-mass spectrometric detection and quantitation of lincomycin in animal feedingstuffs.

A substantially improved assay was developed for lincomycin A in animal feedingstuffs. The assay allows unambiguous quantitation of at least 0.1 ppm in feed. Lincomycin B did not interfere because of differences in both retention time and mass of the main fragment ion in electron impact (EI) spectra. The assay using single ion monitoring with EI detection would not discriminate between lincomycin A and clindamycin. The presence of the latter was easily confirmed by using gas chromatography-mass spectrometry in the chemical ionization mode. The assay for lincomycin A was linear in the range 0-40 ng applied to the gas chromatographic column. The recovery was 93.4 +/- 4.2% at 1 and 5 ppm and 86.2 +/- 5.5% at 0.1 ppm in feed. The coefficient of variation of the assay was 4.8% at both 1 and 5 ppm, and was 6.43% at 0.1 ppm.

Animal Feed↗
PubMed1981

Adverse reactions to parenteral lincomycin.

Lincomycin use has not been reported exclusively in children and inasmuch as it has been extensively used at our institution, a chart review of 265 patients who received parenteral lincomycin at a dose of 100 mg/kg/day in four divided doses for five days or longer was undertaken. The following conditions were diagnosed: cellulitis, 39%; septic arthritis, 21%; osteomyelitis, 16%; abscess, 13%; lymphadenitis, 9%; and pneumonia, 1%. Cures were achieved in all. The majority of organisms cultured were Staphylococcus aureus and Streptococcus pyogenes. Duration of therapy ranged from five to 63 days, with a mean of 15 days. The lincomycin dose ranged from 75 to 2,400 mg every six hours. The majority of patients received the drug intravenously, but 25.7% received it only intramuscularly. There were no adverse reactions at the administration sites. Only 3% of the patients developed diarrhea, which was not felt to be secondary to the drug. There were no cases of pseudomembranous colitis. Therefore parenteral lincomycin in children appears to be a safe and effective antibiotic when used for infections due to Gram-positive cocci.

Abscess↗
PubMed1977

[Lincomycin concentration in human serum and pulmonary tissue].

Lincomycin levels in the blood serum and lung tissue were determined in 17 patients after surgical operations because of the lung diseases, the drug being administered in a dose of 500 mg. In 45 to 330 minutes after administration of the antibiotic its concentration in the blood serum and lung tissue was 4.6 +/- 10 lambda/ml(average 7.7 lambda/ml) and 1.4-8 lambda/gm (average 4.4 lambda/gm) respectively. The lincomycin level in the lung tissue amounted to 61 per cent of that in the blood setum. The concentration of lincomycin the lung tissue was several times higher than the minimum level necessary for inhibition of the strains included in the antibiotic antibacterial spectrum. Therefore, lincomycin is an important drug in the treatment of infections of the respiratory tract.

Adult↗
PubMed1965

DRUG ANTAGONISM BETWEEN LINCOMYCIN AND ERYTHROMYCIN.

An antagonistic action can be demonstrated between lincomycin, a new antibiotic, and erythromycin, when the two drugs are allowed to diffuse into the same area of an agar plate seeded with a strain of Staphylococcus which is resistant to erythromycin but sensitive to lincomycin. The increase in the minimum inhibitory concentrations of lincomycin in the presence of erythromycin may be significant in clinical application. The antagonism does not depend on a reaction between the two antibiotics, but appears to be the result of an altered metabolism stimulated by erythromycin on erythromycin-resistant staphylococci.

Anti-Bacterial Agents↗
PubMed1964

LINCOMYCIN: A NEW ANTIBIOTIC ACTIVE AGAINST STAPHYLOCOCCI AND OTHER GRAM-POSITIVE COCCI: CLINICAL AND LABORATORY STUDIES.

Preliminary results suggest that the antibiotic lincomycin (a product of Streptomyces lincolnensis var. lincolnensis) possesses certain valuable properties which include good in vitro activity against many strains of hospital staphylococci resistant to many other antibiotics. During a study of this agent, a selected series of severe staphylococcal infections due to resistant organisms were treated with lincomycin, with encouraging responses. Favourable results were also noted in seven cases of osteomyelitis. Lincomycin may be administered by the oral or parenteral routes to adults and infants and satisfactory serum blood levels obtained. So far as the authors' limited experience enables them to conclude, and at the dose range tested, this antibiotic promises to be one of low toxicity.

Anti-Bacterial Agents↗
PubMed1965

LINCOMYCIN AND STAPHYLOCOCCAL INFECTIONS: A CLINICAL STUDY OF 18 CASES.

Lincomycin, a chemically new antibiotic effective against Gram-positive organisms, was evaluated in vitro and tested clinically. In vitro testing indicated that lincomycin is especially effective against Staphylococcus aureus. Clinical testing showed that lincomycin was free of toxicity in a series of 18 cases of staphylococcal infection. Of particular interest was its pronounced effectiveness in nine cases of chronic osteomyelitis, one of which was of 15 years' duration and unresponsive to all other forms of antibiotic and surgical treatment. The only side effect noted was loose stools in the occasional patient.

Abscess↗
PubMed1979

Intraocular penetration of topically applied lincomycin hydrochloride in rabbits.

Ocular penetration of lincomycin hydrochloride in albino rabbits was determined by bioassay. On topical application, the frequency of multiple instillation of drops played an important role in producing therapeutic levels in the anterior chambers. Therapeutic levels were attained in the cornea, aqueous humor, and iris-ciliary body, with peak values occurring at 30 to 45 minutes. Varying the pH of the dosing solution did not change ocular absorption and distribution substantially. Removal of corneal epithelium, however, greatly enhanced absorption. Relative to clindamycin, lincomycin hydrochloride had longer onset of peak values and lower overall concentration in ocular tissues. Intravitreous injection of lincomycin hydrochloride produced therapeutic and steady levels of antibiotic in anterior chambers. Injection produced a concentration in aqueous humor twice that achievable topically. The major route of elimination from the posterior chamber was through retina-choroid.

Administration, Topical↗
PubMed2005

Determination of lincomycin and tylosin residues in honey by liquid chromatography/tandem mass spectrometry.

A simple and rapid analytical method was developed for the determination of lincomycin and tylosin residues in honey as part of field studies examining the efficacy and target animal safety of these antibiotics to control American foulbrood disease in honey bees. Residues of the antibiotics were determined using liquid chromatography/electrospray ionization tandem mass spectrometry (LC/ESI-MS/MS). Honey samples were diluted and injected directly into the LC/MS/MS system without additional cleanup by solid-phase extraction or liquid-liquid partitioning. A six-port valve system was utilized to selectively route eluant from the LC column into the mass spectrometer only during a relatively short portion of the chromatographic run corresponding to the elution of the analytes of interest. Minimal contamination of the MS source chamber was observed despite the analysis of large numbers of samples. Using internal standard quantitation, excellent accuracy and precision were obtained with no apparent matrix-to-matrix variation. Based on the analysis of fortified replicates, the mean percent deviation from the theoretical concentration and the percent relative standard deviation were both less than 10% for tylosin over an analytical range of 10-1000 microg/kg. Slightly higher mean percent deviations and relative standard deviations were observed for the analysis of lincomycin in fortified replicate samples. The method detection limits were determined to be 5 and 2 microg/kg for lincomycin and tylosin, respectively.

Anti-Bacterial Agents↗
PubMed1974

Genetics of resistance to macrolide antibiotics and lincomycin in natural isolates of Streptococcus pyogenes.

Of 5 clinically isolated strains of Streptococcus pyogenes, 3 showed high-level resistance to erythromycin and lincomycin that was inducible by subinhibitory concentrations of these drugs (IR strains) while 2 strains exhibited constitutive erythromycin and lincomycin resistance (CR strains) which was expressed without prior exposure to low drug concentrations. The CR strain 15346 showed spontaneous loss of resistance whereas resistance in the other strains was quite stable even under curing conditions. The IR strain 13234 was found to be polylysogenic for at least 4 different phages designated P13234ma, mi, mu, and mo. Phage mo, antigenically distinct from the other three, was shown to mediate the transfer of the resistance determinant ERL1 of strain 13234. ERL1 if borne by appropriate strains was also transducible by the virulent phage A25. ERL1 behaved as a discrete genetic unit in transduction experiments, was not linked to either of two chromosomal regions governing resistance to antibiotics that affect the ribosome, could be transferred to recombination deficient hosts, represented a relatively large UV inactivation target, and showed no stimulation of transduction by low UV doses. These findings suggest that resistance to erythromycin and lincomycin in certain natural isolates of S. pyogenes is specified by, or under the control of, a plasmid.

Bacteriophages↗
PubMed1979

Analysis of lincomycin resistance mutations in Escherichia coli.

High level lincomycin resistant strains of Escherichia coli were isolated and screened for altered ribosomal proteins and functions. Amongst 58 strains investigated by electrophoresis one had an altered ribosomal protein S7, another one a mutated L14 and two showed altered L15 proteins. A correlation between these alterations and lincomycin resistant growth could not be demonstrated by genetic analysis for any of the mutants. In vitro, however, extracts from the two L15 mutants were less sensitive to inhibition by the drug. A gene locus (linR) responsible for the lincomycin resistance phenotype was mapped at min 30 of the Escherichia coli chromosome near tyrR; it seems to be identical to the previously described linB locus (Apirion, 1967); however, in contrast to these reports it does not seem to alter any ribosomal function.

Bacterial Proteins↗
PubMed2003

Lincomycin, cultivation of producing strains and biosynthesis.

Lincomycin and its derivatives are antibiotics exhibiting biological activity against Gram-positive bacteria. The semi-synthetic chlorinated lincomycin derivative is used in clinical practice. The chemical structure of lincosamide antibiotics, cultivation of producing strains and analytical procedures used for separation and isolation of these compounds are described in this review. Biosynthesis of lincomycin and related compounds and its genetic control are briefly discussed.

Biomass↗
PubMed2004

Lincomycin, clindamycin and their applications.

Lincomycin and clindamycin are lincosamide antibiotics used in clinical practice. Both antibiotics are bacteriostatic and inhibit protein synthesis in sensitive bacteria. They may even be bactericidal at the higher concentrations that can be reached in vivo. Clindamycin is usually more active than lincomycin in the treatment of bacterial infections, in particular those caused by anaerobic species; and it can also be used for the treatment of important protozoal diseases, e.g. malaria, most effectively in combination with primaquine. Resistance to lincomycin and clindamycin may be caused by methylation of 23S ribosomal RNA, modification of the antibiotics by specific enzymes or active efflux from the periplasmic space.

Animals↗
PubMed2004

Crystal and molecular structure and absolute configuration of lincomycin hydrochloride monohydrate.

Lincomycin is a broad-spectrum antibiotic synthesized by Streptomyces lincolnensis that is particularly active against Gram-positive bacteria. It is widely used in human and veterinary applications. The crystal structure of lincomycin has been undertaken with a view to obtain the conformational and structural features of the drug in order to afford a comparison of its structural features with other aminoglycoside antibiotics. We report here the details of its structural and conformational features as determined by single-crystal X-ray crystallography. Crystals of lincomycin hydrochloride are orthorhombic, space group P2(1)2(1)2, with the cell dimensions a=18.5294(3) Angstroms, b=20.5980(4) Angstroms, c=6.17380(10) Angstroms, V=2356.35(7) Angstroms3. The structure was solved using X-ray diffraction data and refined to a final R-value of 0.0391 for 2321 reflections (I > or = 2sigma). The absolute configuration was established using the anomalous dispersion of the sulfur and chlorine atoms in the structure. The molecule consists of an amino acid linked by an amide group to a monosaccharide of galactose stereochemistry. A network of hydrogen-bonds stabilizes the crystal structure.

Crystallization↗
PubMed2006

Lincomycin solar photodegradation, algal toxicity and removal from wastewaters by means of ozonation.

Antibiotic molecules have been reported among the xenobiotics present at trace levels in sewage treatment plant (STP) effluents and aquatic environment. Lincomycin, one of the most used in clinical practices whose presence in the STP effluents has been often documented, is submitted to an extensive investigation to assess its persistence in the environment and toxicity towards different algal strains. The possibility to remove the lincomycin from water by means of ozonation is demonstrated and a reduction of toxicity of ozonated solutions on S. leopoliensis, with respect to untreated solutions containing this compound, is obtained even just for 1h of treatment. Kinetic constants for the attack to lincomycin of ozone (from 1.53 x 10(5) M(-1)s(-1) at pH = 3.0 and 4.93 x 10(5) M(-1)s(-1) at pH = 6.7) and OH radicals (4.37 x 10(9) M(-1)s(-1) at pH = 5.5 and 4.59 x 10(9) M(-1)s(-1) at pH = 7.5) are also evaluated.

Anti-Bacterial Agents↗
PubMed2001

Copper(II)-lincomycin: complexation pattern and oxidative activity.

Coordination of Cu(II) to lincomycin was studied by potentiometry, UV-Vis, circular dichroism (CD), EPR, NMR, cyclic voltammetry (CV) and ESI-MS. Only mononuclear complexes of stoichiometries ranging from CuL to CuH(-3)L were found. In the main species present at neutral pH, CuH(-2)L, lincomycin bonds Cu(II) through both of its nitrogen donors, and a deprotonated oxygen donor at C4 of the sugar moiety. High pressure liquid chromatography (HPLC) of products of 2'-deoxyguanosine (dG) oxidation and agarose gel electrophoresis of plasmid DNA confirmed that lincomycin complexes effectively facilitate dG oxidation by H2O2, but are not able to cleave double-stranded plasmid DNA.

Anti-Bacterial Agents↗