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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↗

Lincomycin increases synthetic rate and periplasmic pool size for cholera toxin.

Increased enterotoxigenicity of Vibrio cholerae 569B grown with low concentrations of lincomycin, previously described in terms of increased extracellular biological activity (capillary permeability factor and fluid accumulation in ligated rabbit ileal loops), was further characterized. Polyacrylamide gel electrophoresis and single radial immunodiffusion showed that lincomycin-stimulated cells produced increased molar quantities of cholera toxin (CT) both extra- and intracellularly. The intracellular CT was released in comparable amounts by sonication, deoxycholate extraction, and polymyxin B treatment. Polymyxin B release of CT was nearly complete under conditions wherein only 6% of total cellular beta-galactosidase was released, implying a periplasmic pool of CT in stimulated cells. No intracellular choleragenoid (CT subunit B) was found in stimulated cells by polymyxin B release. No proteolysis of 14C-labeled CT was detected after prolonged incubation with sonicated nonstimulated cultures or sonicated concentrated cells. These data support the conclusion that the stimulatory effect of lincomycin involves an increase in the rate of synthesis of the CT molecule, and argue against alternative models involving inhibition of putative normal degradation of CT, increased release of otherwise cell-bound CT, or activation of inactive, or less active, forms of CT.

Cholera Toxin↗

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↗

A comparison of lincomycin hydrochloride and clindamycin hydrochloride in the treatment of superficial pyoderma in dogs.

Thirty dogs with superficial pyoderma were randomly allocated to treatments with either lincomycin hydrochloride (22 mg/kg twice daily) or clindamycin hydrochloride (11 mg/kg once daily), initially for three weeks. Samples were taken from pustules, from adjacent apparently uninvolved skin, and from the nares. These were submitted for bacterial culture and sensitivity testing. The dogs were re-examined after three weeks treatment and samples for bacteriology were taken from the nares, from any pustules that were present or from skin in the area that was previously affected; the treatment was extended if necessary. Seventy-one per cent of the dogs given lincomycin hydrochloride responded within three weeks compared with 81 per cent of the dogs treated with clindamycin hydrochloride. The overall response rates, including those given longer courses of treatment were 93 per cent for those treated with lincomycin hydrochloride and 94 per cent for those treated with clindamycin hydrochloride, and there was no statistically significant difference between the groups either after three weeks treatment or after extended treatment. The microbiological results demonstrated that Staphylococcus intermedius was present on the skin adjacent to pustules and suggested that the nasal carriage of S intermedius was a result of cutaneous colonisation.

Administration, Oral↗

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↗