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PubMed1976

Antibiotic susceptibilities of streptococci from the mouth and blood of patients treated with penicillin or lincomycin and clindamycin.

Patients undergoing dental extractions were non-randomly allocated to three groups, one of which received no antibiotic, one benzylpenicillin followed by oral penicillin for 5 days, and the third intramuscular lincomycin followed by oral clindamycin. Dental extraction was performed at the beginning of the course of chemotherapy. Streptococci were isolated from the extracted teeth, from blood cultures collected before and immediately after dental extraction, and from sutures removed from the gums 5-7 days after the operation. The species of these organisms was determined, and their susceptibilities to penicillin, clindamycin, cephaloridine, erythromycin and tetracycline were assessed. The majority of streptococci isolated from teeth belonged to the species Streptococcus sanguis, S. mitior, S. mutans and S. milleri. Occasional isolates of each of these organisms collected before the antibiotic could take effect were resistant to penicillin. Three of these species, but not S. mutans, were the commonest streptococci to be isolated from the blood after dental extraction. Penicillin completely suppressed dental bacteriaemia under the conditions of our investigation, and lincomycin reduced the incidence by about 60 per cent. The commonest streptococci from sutures were also S. sanguis, S. mitior, S. mutans and S. milleri. S. faecalis was also isolated, but only in patients who had received antibiotics. Among the non-faecalis organisms, penicillin resistance was significantly more frequent among isolates from patients given penicillin than from patients not given this antibiotic, and clindamycin resistance was significantly more frequent among isolates from patients given lincomycin and clindamycin than from patients not given these antibiotics.

Anti-Bacterial Agents↗

PubMed1977

The mechanism of lincomycin-induced diarrhoea.

Metabolic studies were performed before and seven days after treating rats orally with lincomycin. Following the treatment the mean faecal weight increased from 302.2 g/72 hr +/- 3.8 (S.D.) to 65.5 +/- 8.2. The faecal fat excretion was unchanged, and the weight increase was mainly due to increased water content. To find whether the watery diarrhoea was due to bile acid malabsorption, the absorption rate of [14C]-taurocholic acid was measured in untreated rats and rats treated with lincomycin using an in vivo perfusion technique. There was no significant difference in bile acid absorption rate measured at three different concentrations of bile acid in the perfusate. Alternative mechanisms of lincomycin-associated diarrhoea are discussed.

Animals↗

PubMed1992

Molecular cloning and characterization of two lincomycin-resistance genes, lmrA and lmrB, from Streptomyces lincolnensis 78-11.

Two different lincomycin-resistance determinants (lmrA and lmrB) from Streptomyces lincolnensis 78-11 were cloned in Streptomyces lividans 66 TK23. The gene lmrA was localized on a 2.16 kb fragment, the determined nucleotide sequence of which encoded a single open reading frame 1446 bp long. Analysis of the deduced amino acid sequence suggested the presence of 12 membrane-spanning domains and showed significant similarities to the methylenomycin-resistance protein (Mmr) from Streptomyces coelicolor, the QacA protein from Staphylococcus aureus, and several tetracycline-resistance proteins from both Gram-positive and Gram-negative bacteria, as well as to some sugar-transport proteins from Escherichia coli. The lmrB gene was actively expressed from a 2.7 kb fragment. An open reading frame of 837 bp could be localized which encoded a protein that was significantly similar to 23S rRNA adenine(2058)-N-methyltransferases conferring macrolide-lincosamide-streptogramin resistance. LmrB also had putative rRNA methyltransferase activity since lincomycin resistance of ribosomes was induced in lmrB-containing strains. Surprisingly, both enzymes, LmrA and LmrB, had a substrate specificity restricted to lincomycin and did not cause resistance to other lincosamides such as celesticetin and clindamycin, or to macrolides.

Amino Acid Sequence↗

PubMed1975

Lincomycin in selective medium for the isolation of Neisseria gonorrhoeae.

For the isolation of gonococci, the selective culture medium containing colistin, vancomycin, nystatin and trimethoprim which is usually employed has been changed by substituting lincomycin for vancomycin. The best result was obtained if a concentration of 1/2 mug lincomycin/ml medium was used. This is a concentration of lincomycin considerably lower than that which by other investigators is considered most suitable for the purpose. However, the culture medium used by the latter did not contain trimethoprim. The use of 1/2 mug lincomycin/ml instead of vancomycin 3 mug/ml in the medium caused a slightly more pronounced growth of unwanted organisms. In spite of this, the results obtained by the medium containing lincomycin showed that the number of samples positive for gonococci was 7 per cent higher, and that the number of patients with gonococcal infections to be discovered was 4 per cent higher than the numbers obtained by the medium containing vancomycin. The results were considered highly favourable and, accordingly, by now our laboratory uses 1/2 mug lincomycin/ml medium in the routine isolation of gonococci.

Culture Media↗

PubMed1974

Rosamicin: evaluation in vitro and comparison with erythromycin and lincomycin.

Rosamicin is a new macrolide antibiotic produced by Micromonospora rosaria. It shares certain chemical and biological characteristics with erythromycin. Activity against gram-positive strains was assayed by broth dilution and compared to that of erythromycin and lincomycin. Rosamicin was bacteriostatic and inhibited most strains of Staphylococcus aureus, Staphylococcus epidermidis, enterococci, viridans streptococci, and group A streptococci in concentrations of 0.02 to 4.0 mug/ml. Results were similar for erythromycin and for lincomycin (excluding enterococci). Cross-resistance of gram-positive organisms to these three antimicrobial agents was incomplete. Rosamicin was more active than erythromycin against Enterobacteriaceae and Pseudomonas at pH 7.2. Alkalinization of the medium enhanced the activity of both rosamicin and erythromycin; however, rosamicin was still more active than erythromycin against all gram-negative strains at pH 7.6 and 8.0. In view of the high degree of in vitro activity of rosamicin against gram-positive organisms, lack of complete cross-resistance with erythromycin and lincomycin, and the greater activity of rosamicin than erythromycin against gram-negative organisms, further investigation of this macrolide is warranted.

Anti-Bacterial Agents↗

PubMed1975

Effect of lincomycin and clindamycin on peptide chain initiation.

Lincomycin does not affect initiation factor-dependent formation of 70S initiation complexes formed with fmet-tRNA(F), the initiation triplet A-U-G, and 70S ribosomes, whereas its 7-chloro-derivative clindamycin substantially stimulates this process. Conversely, lincomycin stimulates nonenzymatic formation of the 70S complex, but clindamycin does not. Both antibiotics stimulate the assembly of non-enzymatically formed 70S initiation complexes with R(17) phage ribonucleic acid and exert little effect on those formed in the presence of initiation factors. The formation of 30S initiation complexes is stimulated or remains unaffected by lincomycin or clindamycin except when initiation occurs in the presence of very low Mg(2+) concentrations. In this case, both antibiotics inhibit the assembly of the 30S complexes regardless of the messenger present.

Clindamycin↗

PubMed1966

Action of lincomycin on staphylococci.

On a solid medium, 0.1 to 1 mug/ml of lincomycin hydrochloride had a bacteriostatic effect upon 95 of 100 strains of staphylococci. Using cellophane transfers, we observed a bactericidal effect upon 54 of these strains after 3 to 14 hr of contact with 1 mug/ml. Five staphylococcal strains resistant to 100 mug/ml of lincomycin were also resistant to penicillin G, streptomycin, erythromycin, tetracycline, chloramphenicol (three strains), and rovamycin (three strains). Other staphylococcal strains resistant to methicillin, ampicillin, tetracycline, streptomycin, chloramphenicol, and erythromycin were sensitive to lincomycin.

Anti-Bacterial Agents↗

PubMed1970

In vitro activity of lincomycin and spectinomycin against serotypes of avian mycoplasma.

Twenty strains of avian mycoplasma, representing 12 serotypes, were tested in vitro for their susceptibility to the action of lincomycin and spectinomycin alone and in combination. They varied in their sensitivity pattern. The ranges of minimal inhibitory concentration were 1 to 20 mug/ml for lincomycin or spectinomycin alone and 0.5/1 to 3/6 mug/ml for the lincomycin and spectinomycin combination. The ranges of minimal lethal concentration were greater with either single antibiotic than with the antibiotic combination. The amount of each antibiotic required to achieve mycoplasmacidal action of the relatively resistant strains was less with the antibiotic combination than with the single antibiotics.

Air Sacs↗

PubMed1970

In-vitro comparison of erythromycin, lincomycin, and clindamycin.

The in-vitro antibacterial activities of erythromycin, lincomycin, and clindamycin, a new derivative of lincomycin, were compared. Clindamycin was always more active than lincomycin, and was either as active as erythromycin or more so against betahaemolytic streptococci, Streptococcus viridans, Str. pneumoniae, and erythromycin-sensitive Staphylococcus aureus. It was also fully active against most erythromycin-resistant strains of Staph. aureus. On the other hand, it was somewhat less active than erythromycin against Haemophilus influenzae and considerably less active than erythromycin against Str. faecalis and Neisseria gonorrhoeae.Clinical trials seem to be justified in infections with sensitive organisms for which erythromycin might have been indicated.

Bacteria↗

PubMed1973

Pharmacological studies with lincomycin in late pregnancy.

The placental transmission of lincomycin was studied in 60 patients in late pregnancy. A peak maternal blood level of 12.5 mug/ml was recorded 45 minutes after injection, and detectable levels were still present up to 42 hours after a single injection. A peak cord blood level of 2.7 mug/ml was recorded 55 minutes after injection; cord blood levels were about a quarter of the maternal blood levels, and in most cases no levels were detectable 24 hours after a single injection. The passage of lincomycin into and out of the liquor was slower and more variable, but some hours after injection the liquor levels were always higher than the maternal or cord blood levels, and detectable levels were still present in the liquor 52 hours after a single injection. Repeated injections did not lead to any significant accumulation of lincomycin. The only side effect was a possible case of neuromuscular block in a mother delivered by caesarean section. No infant was adversely affected.

Amniotic Fluid↗

PubMed1987

Effects of lincomycin on the immune system.

The effects of lincomycin on the immune system were studied on patients suffering from chronic bronchitis by means of phagocytosis, chemotaxis and natural-killer tests. The tests were performed before and 2, 4, 8, 12 and 24 h after administration of 600 mg lincomycin i.m. in a single dose. The results indicate that lincomycin stimulates phagocytosis, expressed as enhanced superoxide production (O2-), chemotaxis and the activity of natural killer cells, measured on the basis of their ability to perform a lysis on the K562 tumoral target labelled with 51Cr. The stimulating effects on chemotaxis appear already 2 h after the administration of the drug, while the same effect on phagocytosis and natural-killer activity occurs after 4 h. The maximal stimulating activity on all three parameters can be shown at 8 h and disappears at 24 h.

Adult↗

PubMed1976

The penetration of lincomycin into normal human bone. Determination of penetration into compact bone, spongy bone and bone marrow.

The penetration of lincomycin into normal bone was studied in 10 patients with fracture of the neck of the femur, a separate determination being made of the lincomycin concentration in serum, bone marrow, spongy bone and compact bone. The concentration of lincomycin in bone marrow was found to be at the same level as that in the serum. The concentration in spongy bone amounted in most cases to 50 to 75 percent of the concentration in the serum, whereas the concentration in compact bone varied from 0 to 15 percent of that in the serum.

Aged↗

PubMed1992

Isolation and identification of 3-propylidene-delta 1-pyrroline-5-carboxylic acid, a biosynthetic precursor of lincomycin.

An accumulated lincomycin intermediate in UC 8292, a lincomycin nonproducing strain of Streptomyces lincolnensis, has been isolated and purified by employing an assay system based on complementation of UC 11066, another lincomycin nonproducing strain of S. lincolnensis. The structure of the purified intermediate is shown to be 3-propylidene-delta 1-pyrroline-5-carboxylic acid, or 1, 2, 3, 6-tetradehydro-propylproline by mass spectrometry and NMR spectroscopic studies. Based on the structure of this newly found intermediate, a biosynthetic pathway for propylproline is proposed as tyrosine-->L-3-hydroxytyrosine (Dopa)-->-->-->-->3-propylidene-delta 1-pyrroline-5-carboxylic acid-->3-propyl-delta 2-pyrroline-5-carboxylic acid-->propylproline.

Fermentation↗

PubMed1975

Granuloma inguinale in Vietnam: successful therapy with ampicillin and lincomycin.

Thirty-six patients having granuloma inguinale were treated at the 483 USAF Hospital, Cam Ranh Bay, Republic of South Vietnam between October 1970 and September 1971. In 24 cases biopsy of the genital ulcerations revealed Donovan bodies pathognomonic for the disorder. The lesions generally did not heal during tetracycline therapy. All but 2 of the 31 cases treated primarily with ampicillin responded with complete healing of the local lesions which occurred primarily on the penis or in the groin. Of the remaining 2 patients, one responded to a second course of ampicillin and the other patient responded to a two week course of lincomycin after dorsal slit had been performed for partial phimosis and balanoposthitis. The 5 patients who were allergic to penicillin were treated primarily with lincomycin and all responded with complete healing. No previous reference could be found in the literature for the successful use of lincomycin in patients with granuloma inguinale. Further clinical trials with this medication are indicated.

Ampicillin↗

PubMed1992

Utilization of the protoplast fusion technique to explore directional altering lincomycin producing microorganism.

Interspecific protoplast fusion between Streptomyces lincolnensis var. lincolnensis (LM gamma, CTC gamma, producing lincomycin) protoplast and Streptomyces aureofaciens (LM gamma, CTC gamma, producing chlorotetracycline) protpolast which had been treated with UV radiation 40 min for inactivation was performed with PEG 6000, the fusants were obtained by directly selecting from the regeneration plates containing CTC 50 micrograms/ml, the fusion frequency was about 9.05 x 10(-5). From many fusants, only 4 stable recombinants were obtained. These species produced antibiotics which are different from lincomycin and chlorotetracycline. Preliminary identification of the antibiotic synthesized by one of the recombinants suggests that its basic structure might be similar to that of lincomycin. The fermentation product of recombinant No. 2 showed new chromatographic spot which is similar to that of clindamycin. Though the products remain to be identified further, this strategy seems to be worthy of exploring for screening new antibiotics.

Anti-Bacterial Agents↗

PubMed1992

[The efficacy of lincomycin in tick-borne encephalitis].

Lincomycin was found to inhibit tick-borne encephalitis (TBE) virus. To test antiviral potential of this drug, a clinical trial was initiated entering TBE patients from known focuses of the disease (Novosibirsk, Kemerovo, Perm and Irkutsk Provinces). The drug was given to 23 patients with meningeal and meningoencephalitic TBE. A control group of 22 matched subjects received specific immunoglobulin. Resultant efficacy of lincomycin appeared not inferior to that of anti-TBE immunoglobulin. Lincomycin can be successfully introduced in the treatment of meningeal and meningoencephalitic TBE.

Adolescent↗

PubMed1976

[Study of C1. perfringens resistance to lincomycin].

A possibility of developing resistant forms of C1. perfringens during treatment of experimental anaerobic (gaseous) infection with lincomycin was studied. It was shown that treatment of the animals for 7 days resulted in an increase in the resistance by 33-41 times. It was noted that strains with decreased sensitivity to lincomycins had changed morphology and biochemical activity (decreased lecitinase activity, changed biochemical properties), decreased virulence and pathogenicity for animals. So as to obtain the protective effect of the antibiotics in experimental anaerobic (gaseous) infection caused by resistant variants of C1. perfringens it was necessary to increase 1.5-3 times the doses of lincomycin or chlolincocin as compared to the processes induced by sensitive strains.

Animals↗

PubMed1991

Lincomycin injections for upper respiratory tract infections: a comparison of findings in a rural clinic with analysis of a national data base.

A review of the records of patients attending a rural family practice clinic indicated that 13% had received "cold shots" (lincomycin with or without chlorpheniramine). The providers who assumed management of the clinic when the previous physician retired judged these injections inappropriate, but patients believed that they were effective and expected to continue to receive them. This study included 51 consecutive patients seen in the clinic for treatment of a cold and compared those who expected an injection with those who did not. Thirty-four patients (67%) expected an injection but instead received education about upper respiratory tract infections and symptomatic treatment. Half of these patients (17) were not satisfied with this alternative, and 10 reportedly went to another provider for an injection. Compared with patients who did not expect an injection, patients who did were older (P less than .001), had longer duration of symptoms (P less than .02), and were more likely to have tried nonprescription remedies (P less than .001). Analysis of the 1985 National Ambulatory Medical Care Survey indicates that the administration of lincomycin is not uncommon (an estimated 800,000 injections were given in 1985) and that lincomycin is more likely to be administered by a rural solo physician practicing in the north central or southern regions of the United States.

Adolescent↗