[Rapid determination of microbial sensitivity to antibiotics by using laser spectroscopy]. / Uskorennoe opredelenie chuvstvite'lnosti mikroorganizmov k antibiotikam s ispo'lzovaniem lazernoi spektroskopii.

A method of express-determination of the susceptibility of microbes to antibiotics is presented based upon the registration by the method of laser spectroscopy of changes of optic properties of cultures at early terms of their incubation in liquid nutrient media with addition of antibiotics. The method was elaborated in 13 standard strains of Staphylococcus aureus and Escherichia coli with antibiotics of different classes, tested on the microflora of pus of patients with sepsis, verified by the method of serial dilutions of the antibiotic. The method makes it possible to obtain the minimum inhibiting concentration of antimicrobial preparations 1 h after the moment of obtaining the native material.

[Effect of the proteinase isolated from a fungus on the kallikrein-kinin system]. / Vliianie proteinazy, vydelennoi iz griba, na kallikrein-kininovuiu sistemu.

Carboxyl proteinase (CP) with the isoelectric point of 6.3-6.4 was isolated from a fungus at the Laboratory of Enzymology of the All-Union Research Technological Institute of Antibiotics and Enzymes and its effect on the kallikrein-kinin system and trypsin caseinolytic activity was studied. Four lots of the preparation with the activity of 1116 to 2300 milk coagulating units per 1 mg were used. The kininogenase activity of kallikrein, bradykinin and trypsin was determined with the routine biological procedures and the trypsin caseinolytic activity was determined with the Kunitz method and the diffusion method on casein-containing agar. It was shown that CP inhibited the kininogenase activity of kallikrein in the secretion of the salivary glands of man and crystalline trypsin in aqueous media and blood serum. It also inactivated the bradykinin constrictor effect on the smooth muscle tissue of the uterus horn in rats. CP had a capacity for inhibiting the caseinolytic activity of crystalline trypsin. Possible use of CP in treatment of patients with diseases accompanied by impairment of the kallikrein-kinin system (increased activity) is discussed.

[Pharmacokinetics of amphoglucamine in an experiment]. / Farmakokinetika amfogliukamina v éksperimente.

The pharmacokinetics of amphoglucamine administered in a single dose or used for a treatment course orally or in the form of aerosols was studied on experimental animals. It was shown that amphoglucamine was absorbed after either its oral administration or its administration in the form of aerosols. The use of the drug during the treatment course resulted in an increase in the antibiotic levels and the period of its renal excretion in the animals.

[Aerobic and anaerobic microflora in experimental drug-induced enterocolitis]. / Aérobnaia i anaérobnaia mikroflora pri éksperimental'nom lekarstvennom énterokolite.

The results of studying aerobic and anaerobic intestinal microflora of rabbits with experimental enterocolitis caused by administration of 7-chlor-7-desoxylincomycin are presented. An increased number of E. coli and some other gram-negative bacteria was noted. It was shown that the quantitative and qualitative composition of the obligate anaerobic microflora was changed: the number of cells of the bacteroids, bifidobacteria, peptococci and peptostreptococci resistant to the antibiotic was low, but the number of clostridia cells resistant to the antibiotic was high. On the basis of a thorough investigation the latter cultures were classified as belonging to Cl. butyricum.

[Characteristics of lincomycin penetration into the organs and tissues of laboratory animals]. / Osobennosti proniknoveniia linkomitsinov v organy i tkani laboratornykh zhivotnykh.

The study on the pharmacokinetics of lincomycin and its 7-chloroderivative in rabbits and albino mice treated with the antibiotics in single and repeated doses administered parenterally or orally revealed significant differences in distribution of the drugs in the animals. The excretion rate of the lincomycins in the rabbits was much lower. They were mainly deposited in the intestine. This fact is probably one of the causes of diarrhea and colitis developing in the course of therapy with these drugs.

[Damaging action of lincomycins on the intestines of experimental animals]. / Povrezhdaiushchee deistvie linkomitsinov na kishechnik éksperimental'-nykh zhivotnykh.

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.

[Experimental characteristics of the antileishmaniasis action of amphotericin B]. / Eksperimental'naia kharakteristika protivoleishmanioznogo deistviia amfoteritsina B.

The efficacy of amphotericin B powder of the Soviet production was studied as a therapeutic agent in experimental zoonotic leishmaniosis of the skin form of mice and hamsters. Amphotericin B was administered per os and its action was compared with that of monomycin injected subcutaneously (50 mg/kg). Amphotericin B in a dose of 150 mg/kg administered for 30 days protected 96+/-0.07 and 76.4+/-0.9 per cent of the mice and hamsters respectively from development of the leishmaniosis clinical signs, 68.8+/-0.04 per cent of the animals being cured (in the treatment experiments). The effect of the antibiotic was analogous to that of monomycin administered parenterally. The study of the kinetics of amphotericin B showed that the antibiotic was well absorbed from the digestive tract of the animals into the blood which provided the chemotherapeutic effect.

[Pharmacokinetics of lincomycins in experimental staphylococcal sepsis]. / Farmakokinetika linkomitsinov pri éksperimental'nom stafilokokkovom sepsise.

Pharmacokinetics of lincomycin hydrochloride and 7-chlor-7-desoxylincomycin hydrochloride (chlolincocin) was studied on albino mice and rabbits with experimental staphylococcal sepsis caused by intravenous introduction of highly pathogenic cultures. The septic process was accompanied by impairement of the kidney function, the pathological changes in the kidneys being most pronounced. The antibiotic levels in the blood and tissues of the internal organs, i.e. liver, kidneys, lungs and spleen increased in the infected animals, while the content of the antibiotic in the urine decreased. Determination of the plasmatic, kidney and extrakidney clearance revealed the increasing role of the extrakidney clearance. The shudy of the concentrations of 7-desoxylincomycin in the bile of the animals subjected to cholecystostomy showed that the role of the liver in elimination of lincomycin increased in the animals with experimental staphylococcal infection. As the state of the animals improved the changes in the pharmacokinetics of lincomycin decreased.

[Distribution of polyene antibiotics in the cells of a tissue culture of puppy kidney]. / Raspredelenie polienovykh antibiotikov v kletkakh kul'tury tkani pochek shchenkov

The results of the studies on interacellular distribution of amphotericin AM-2, a wate soluble derivative of amphotericin in the cells of the puppy kidney tissue culture exposed to the antibiotic in a concentration of 50 gamma per 1 ml medium for 17 hours are presented. It was found that the antibiotic was firmly bound with the kidney cells: 15.4 per cent of the initial amount of the antibiotic was detected in the washed cells. Analysis of the antibiotic distribution in separate subcellular components showed that sorption of amphotericin AM-2 by the plasmic membranes, nuclei and cytoplasm was respectively 18.3, 35.6 and 9.7 per cent of the amount absorbed by the cells. Binding of a significant amount of the antibiotic absorbed by the plasmic membranes and nuclei with the above fractions was reversible. The results of the study provided a supposition that amphotericin AM-2 penetrated into the cells of the kidney tissue which adds some new findings to the studies on the mechanism of action of polyenic antibiotics in cells.

[Effectiveness of the inhalatory administration of chlolincocin in experimental staphylococcal pneumonia]. / Effektivnost' ingaliatsionnogo vvedeniia khlolinkomitsina pri éksperimental' noi stafilokkovoi pnevmonii

Administration of chlolincocin (7-chlor-7-desoxylincomycin) in the form of inhalation aerosol to albino mice in a dose of 200 Units/mouse provided the drug therapeutic concentrations in the lung tissue. The antibiotic was well adsorbed and detected in the blood, liver, kidneys and other biological substrates. Penetration of chlolincocin and lincomycin from the lungs into the blood was better in healthy animals. In animals with experimental staphylococcal infection their blood levels were 1.5--2 times lower. Repeated inhalations of chlolincocin resulted in an increase resulted in its levels in the lung tissue up to 8--10 Units/ml, however, its blood levels increased insignificantly. When chlolincocin and lincomycin were administered intravenously, their concentrations in the lung tissue were lower and detected for a shorter period of time than after the inhalation administration. The aerosols of chlolincocin markedly inhibited the growth of Staph. aureus in the lungs. The drug was 3--5 times more active than lincomycin. Inhalation administration of chlolincocin aerosol is supposed to be expedient for the treatment of inflammatory diseases of the respiratory organs caused by lincomycin sensitive flora.

[Chlorlincocin kinetics in animals with a disordered hormonal balance]. / Kinetika khlorlinkotsina u zhivotnykh s narushennym gormonal'nym balansom

Distribution of chlorlincomycin in intact rats and animals with an impaired hormonal balance was studied. Estradiol or hydrocortizon acetate were administered repeatedly to the animals in large doses with a purpose of inducing pathological conditions. Chlorlincomycin was administered intravenously for 11 days in a dose of 15 mg/kg. The antibiotic levels in the blood serum and organs of the rats were determined at various intervals after the drug administration. The hormones induced changes in the sexual cycle. Hydrocortizon acetate markedly changed the animal weight and the weight coefficient of the internal organs. The kinetics of chlorlincomycin in the animals with hormonal impairments induced by estradiol or hydrocortizon acetate changed insufficiently as compared to that in the intact rats. Individual fluctuations in the antibiotic distribution was observed in the animals treated with hydrocortizon acetate. The levels of chlorlincomycin in the blood of the weakest animals were higher. No cumulation of the drug was noted.