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[Pharmacokinetic research on Pharmachem's lincomycin hydrochloride in pigs].

In the experiments lincomycin hydrochloride LMC "F" with activity 820 UI/mg was used. It was established that in pigs, 5% water solution of LMC "F", applied intramuscularly in doses of 5 and 10 mg/kg m. and internally in doses 50 and 100 mg/kg m., penetrates comparatively quickly in the blood serum, and yet in the first hour established maximal concentrations. Intramuscular injection of LMC "F" of pigs, in doses of 5 and 10 mg/kg m., creates bacteriostatic concentrations in the blood serum for 12 hours, regardless of the quantity of the dose, and applied internally has a longer duration of the retention. The biological half-life of LMC "F" after muscular application in pigs is accordingly 1.7 and 3.5 hours, and after internal application 2.3 and 2.8 hours. Applied a single time intramuscularly in pigs in doses of 5 and 10 mg/kg m., LMC "F" is resorbed from the place of application and after 3 hours is established in most high quantities in the kidney in the lungs, the liver, the bile and in the urine. Mainly it is extracted with the urine in high concentrations--about 190 mg/cm3 (on the 3-rd hour), after intramuscular injection in dose of 10 mg/kg m. The longest time the antibiotic remains in the lungs, the urine and in the bile (up to 96 hours).

Administration, Oral↗

Study of the use of lincomycin aerosols in dogs.

This paper reports studies on different aspects of the administration of lincomycin by aerosol in dogs.The purpose of the study was to determine the depth of penetration of the drug into the lungs and its transfer into the blood, urine and tissues when administered as an aerosol.Special consideration was given to the possibility of side effects at the level of the bronchial mucosa, since this study was viewed as preliminary to the use of the antibiotic in humans.

Aerosols↗

[Tissue levels in human tonsils (tonsillae palatinae) following administration of different antibiotics (penicillin G, ampicillin, lincomycin)].

For determination of tissue levels of different antibiotics in human tonsils penicillin G, ampicillin or lincomycin is given i.v. to patients before tonsillectomy. The concentration of the individual substances is determined in tonsils and serum by agar diffusion method. The results are compared by diagrams of tissue and serum levels and statistically assessed. For therapeutic evaluation the absolute tissue levels at tonsillectomy are compared to the values of minimum inhibitory concentration (MIC) for most frequent germs in the stomato-maxillo-facial region. According to these results recommendations for antibiotic therapy of inflammatory processes of buccal cavity are given.

Ampicillin↗

Efficacy of lincomycin-spectinomycin water medication on Mycoplasma meleagridis airsacculitis in commercially reared turkey poults.

A field trial was conducted to compare the efficacy of a combination of the drugs lincomycin and spectinomycin (LS) with Tylan (tylosin, T) against Mycoplasma meleagridis (MM) airsacculitis in 50,320 commercially reared turkey poults in Ohio. Both drugs were administered at 2 g per gallon of drinking water for the first 5 days of life. The poults were allotted randomly to two treatment groups with 8 or 5 replicates each. Initially, 250 poults were weighed, necropsied, and examined microbiologically and grossly for airsacculitis. At 3 weeks of age, 33 poults from each replicate were randomly selected, necropsied, and examined for airsacculitis. The data indicate that LS is superior to T as an aid in the control of MM airsacculitis in poults, as reflected by fewer air-sac lesions and greater improvement in weight gain (P less than 0.05).

Air Sacs↗

[Study of lincomycin concentrations in hepatocystic duct].

Penetration of lincomycin (LCM) in choledochal and cholecystic bile as well as in the gallbladder tissue and liver tissue was investigated together with bacteria detectable in the bile in order to evaluate basically usefulness of this antibiotic in the treatment of infections of the hepatocystic duct. Intravenous drip infusion of LCM 1.5 g (in 500 ml of 5% glucose solution) over 1.5--2 hours resulted in mean drug concentrations of 33.9 and 10.1 micrograms/ml in serum at 2 and 4 hours post start of infusion respectively; 215.5 micrograms/ml in choledochal bile at 3 hours 15 minutes; 252.7 micrograms/ml in cholecystic bile at 3 hours 36 minutes; 28.1 micrograms/g in gallbladder tissue at 2 hours 55 minutes; and 15.4 micrograms/g in liver tissue at 4 hours. A cross-over study of LCM and cefazolin (CEZ) in 2 cases where T-tubes were employed demonstrated evidently higher biliary levels of LCM than CEZ. Bacteriological examination showed that Hafnia alvei plus Streptococcus faecalis were presented in choledochal bile from just 1 of 4 cases while in cholecystic bile from 9 of 15 cases were detected 22 strains of organisms including Klebsiella pneumoniae (7 strains), Bacteroides fragilis (5), Escherichia coli (2), Citrobacter freundii (2) and Serratia marcescens (2). A total of 7 strains of anaerobes including B. fragilis was isolated. The above concentrations of LCM in the bile, gallbladder tissue and liver tissue sufficiently covered the MIC90 of this antibiotic determined by us in 1980 for major species of anaerobes including clinical isolates of B. fragilis.(ABSTRACT TRUNCATED AT 250 WORDS)

Adult↗

The effect of lincomycin-neomycin treatment on experimental anaerobic bacterial bovine mastitis.

Three healthy lactating quarters of a Friesland cow were each experimentally infected with a pure culture of a strain of either Bacteroides fragilis, Eubacterium lentum or a Peptostreptococcus sp. respectively. The onset and progression to clinical mastitis was monitored 12 hourly by examination for clinical signs of inflammation, bacterial culture, somatic cell counts and with a strip cup. All infected quarters developed clinical mastitis within 24 hours. The 2 quarters infected with B. fragilis and E. lentum respectively were treated 4 times consecutively at 12 hour intervals, commencing at 24 h by intramammary instillation of 10 ml of a mixture containing 200 mg lincomycin hydrochloride, 200 mg neomycin sulphate and 5 mg methylprednisolone (Lincocin Forte, Upjohn). Both quarters became clinically normal and no bacteria could be detected in the secretions 12 hours after the first treatment. At 36 hours the strip cup became negative, and the somatic cell count dropped to less than 500 X 10(3) at 72 hours after the initial treatment. The quarter infected with a Peptostreptococcus sp. was unable to overcome the infection by natural means when intramammary treatment was delayed for the first 36 hours after the onset of clinical mastitis. Subsequent treatment of this quarter gave results similar to those treated earlier.

Animals↗

[Damaging action of lincomycins on the intestines of experimental animals].

It was found that lincomycin and 7-chlor-7-desoxylincomycin administered 3 times induced severe enterocolitis accompanied by dysbacteriosis in a part of the experimental rabbits, while no such phenomenon was observed in the mice. Treatment of the animals with neomycin for 10 days protected them from death of severe forms of enterocolitis.

Animals↗

Effect of lincomycin on the dimorphic chloroplasts of Zea mays L. leaves.

The effect of lincomycin treatment on the ultrastructure, and on the absorption and fluorescence emission spectra, of mesophyll and bundle sheath chloroplasts of maize was investigated. The ultrastructural and absorption changes affected mainly the unstacked lamellae (photosystem 1) in the treated mesophyll and bundle sheath plastids, while the fluorescence emission spectra reflect a changed energy transfer between the chlorophyll a forms. The results provide additional evidence for the compositional and developmental similarity of the intergranal lamellae of mesophyll chloroplasts to the membranes of the nearly agranal bundle sheath chloroplasts.

Chlorophyll↗

[Experimental therapy of a local infectious-inflammatory process in rats using a lincomycin film].

Implantation of a lincomycin film in granulomotomy resulted in an intensified therapeutical process of a pyo-inflammatory proliferative focus caused by subcutaneous administration of pathogenic Staphylococci, Streptococci, and Pneumococci to albino rats. As compared to the routine surgical tools, this technique provided a two-fold reduction in the periods of healing of wounds and their dissemination. At the same time there was a decrease in the manifestation rate of the pyo-necrotic component of inflammation and an improvement of the general status of the experimental animals.

Animals↗

[The development of a technology for lincomycin biosynthesis with batch-type feeding of the substrates during the process].

It was shown possible to improve the process of lincomycin production by using batch-type feeding of the carbohydrate substrates during the biosynthesis. The optimal composition of the fermentation medium with lower concentrations of the carbohydrates was developed and batch-type feeding of the substrates was applied. The conditions of the substrate feeding were developed under laboratory conditions. Solutions of glucose or sugar supplemented with potassium sulfate were used for the feeding. The antibiotic yield under the optimal conditions of the substrate feeding and the process control was higher than that under the conditions of the batch fermentation by 23-24 per cent.

Bacteriological Techniques↗

Studies on the reaction model for the immobilized Streptomyces aureofaciens's protoplasts used to convert lincomycin.

A reaction kinetic model is proposed for immobilized S. aureofacien's protoplasts which can facilitate the conversion of lincomycin into clindamycin. The simulation result of the model has been given. Effects of various kinetic parameters of the reaction on the conversion rate are given in the formula. The formulas which can be used to calculate the maximum conversion rate and the optimal reaction time have been given. The results of model simulation are in good agreement with the experimental results.

Clindamycin↗

[Lincomycin formation by strain R-367 on a complex medium not containing corn steep].

A new complex medium for biosynthesis of lincomycin by strain R-367 was developed using one-factor experiments and mathematical schemes of planning. A complex of mineral salts containing nitrogen, sulphur, phosphurus, magnesium and trace elements was introduced into the content of the new medium. This provided elimination of corn steep liquor from the medium. The linomycin production level in the fermentation broth with the use of the new medium was at an average 2.5 times higher than that on the initial medium containing corn steep liquor.

Culture Media↗

Lincomycin-induced cholecystitis and gallstones in guinea pigs.

Guinea pigs given lincomycin 60 mg per kg per day showed a striking increase in the renewal of epithelial cells in the gallbladder. This was detectable after only 24 hr of treatment. By 48 hr a precipitate consisting predominantly of calcium and bilirubin had formed in the gallbladder. Gallbladder bile glycoprotein concentrations rose progressively. At 8 days epithelial dysplasia was marked. Treatment was discontinued at 9 days. The guinea pigs that survived beyond 34 days showed that new tubuloalveolar glands had formed focally in the body and fundus of the gallbladder. Multiple calcium-containing stones were present. The failure to culture bacteria from bile, the failure of the bile salt pattern to change, and the progressive nature of the epithelial injury suggested that the changes resulted from a direct toxic effect and were not dependent on the antibiotic activity of this drug. It was concluded that damage to the epithelium of the gallbladder preceded the formation of a precipitate and initiated histological changes which culminated, at the time that the precipitate became organized into stones, in impressive glandular metaplasia.

Animals↗

[Effect of lincomycin on a cell culture].

Cumulative and toxic properties of lincomycin evident from increased numbers of pathological mitosis were found on three-fold treatment of various cell lines with the antibiotic in concentrations of 100 or 200 Units/ml for 1.5 years. The toxicity level was not high since the other indices of the mitotic regimen remained unchanged.

Cell Line↗