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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

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

Effects of lincomycin and tetracycline on production and properties of enterotoxins of enterotoxigenic Escherichia coli.

Enterotoxigenic Escherichia coli grown in the presence of lincomycin and tetracycline produced an increased amount of heat-labile enterotoxin (LT). These antibiotics increased the production of not only extracellular LT but also intracellular LT. On the other hand, lincomycin did not stimulate the production of heat-stable enterotoxin by enterotoxigenic E. coli. The extracellular LTs produced in the presence of lincomycin and tetracycline were purified and analyzed by sodium dodecyl sulfate-polyacrylamide gel disc electrophoresis. Results showed that the A subunits of the purified LTs were not nicked, unlike that of extracellular LT produced in the absence of the antibiotics.

Anti-Bacterial Agents

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

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

Sideroblastic anaemia associated with lincomycin therapy.

Sideroblastic anaemia developed after lincomycin therapy in a 58-year-old woman. The anaemia proved completely reversible after termination of lincomycin therapy and the introduction of pyridoxine. The patient also had pseudomembranous enterocolitis, a well-known side effect of lincomycin.

Anemia, Sideroblastic

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

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

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

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

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

[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

[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

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

Randomised comparative efficacy of clindamycin, metronidazole, and lincomycin, plus gentamicin in chronic suppurative otitis media.

Chronic suppurative otitis media is major health problem seen frequently in the ENT clinics in Nigeria and the outcome of most medical management in the past have been disappointing. A comparative randomised clinical trial involving combination therapies with systemic clindamycin, metronidazole, lincomycin, each with gentamicin, was conducted on a total of 14 patients. At the end of one week, and three-week, follow-up end points the clinical response with bacteriological cure were, for clindamycin and gentamicin 21%, metronidazole and gentamicin 33%, lincomycin and gentamicin 22%, and the control (aural toilet alone) 14%. However, when the clinical response was measured only by the ceasation of discharge, the outcome was more impressive. By this assessment the clinical response with clindamycin and gentamicin was 52% of the 140 patients, metronidazole and gentamicin 69%, lincomycin and gentamicin 47%, and the control 24%. The metronidazole and gentamicin regime was significantly more effective than the other regimes and it is suggested for use in prophylactic treatment of CSOM patients undergoing surgical procedures.

Clindamycin

[Production of lincomycin by Micromonospora halophytica culture].

A Micromonospara culture designated as 991/78 with activity against gram-positive cocci and bacteria was isolated from samples of silt-covered substrates from the Amu-Darya. Directed screening on a selective medium supplemented with lincomycin in an amount of 50-100 micrograms/ml was used. Identification of the antibiotic produced by the culture showed it to be lincomycin. By its taxonomic features the culture was classified as belonging to Micromonospora (subgroup II, Cinnamomea) and in particular to M. halophytica (Weinstein, Luedemann, Oden, Wagman, 1968). Up to now, it was known that lincomycin was produced only by Streptomyces cultures.

Agar

[Lincomycin therapy of streptococcal and staphylococcal mastitis in cattle].

Lincomycin has a good influence on mastitis caused by gram positive bacteria especially streptococci and staphylococci. Applied parenterally lincomycin is very toxic. Therefore it is not a regular therapeutic drug. The tubes for intramammary application are completely non-toxic. Lincomycin is very useful for treating dairy herds with galt mastitis.

Animals

Drug residues in milk after intrauterine injection of oxytetracycline, lincomycin-spectinomycin, and povidone-iodine in cows with metritis.

A study was conducted to document the maximum retention times of antimicrobial residues in milk after their use in intrauterine treatment of metritis in lactating cows and to evaluate several risk factors hypothesized to influence the retention time of these drugs. Oxytetracycline (3 g), lincomycin-spectinomycin (2 g of one-third lincomycin and two-thirds spectinomycin), or povidone-iodine (6 g) were given to cows with metritis by intrauterine route. The Bacillus stearothermophilus var calidolactis disk assay was performed on each milk sample. Of the 61 cows treated with oxytetracycline, 30 had residues in their postinjection milk for variable periods (range, 12.5 to 44.0 hours; mean, 26.6 +/- 10.3). Of the 47 cows treated with lincomycin-spectinomycin, 17 had residues in their postinjection milk for various periods (range, 14.5 to 24 hours; mean, 19.5 +/- 8.9). Povidone-iodine was not detected in milk. Because a high number of cows (n = 61) were treated with oxytetracycline, only data from these cows were used in testing the influence of 3 factors (severity of metritis, time after parturition when cows with metritis were treated, and parity) on maximum retention of the drug in milk. Severity of metritis did not have a significant influence (P greater than or equal to 0.1) on the maximum retention time of the drug. The retention time decreased linearly with the increase of time after parturition when the cow with metritis was treated. First lactation cows had a significantly (P less than or equal to 0.01) shorter retention time than did older cows.

Animals