[Ultrastructural study of the action of cyclosporine on cells of the fungus Aspergillus niger].

Electron microscopy of the ultrastructure of the Aspergillus niger cells exposed to cyclosporine in acute experiments revealed changes in the mycelium morphology, hyphae growth and cell structure in the organism sensitive to cyclosporine. The analysis of the changes showed that the primary target of the cyclosporine action was the cell cytoplasmic membrane. The changes in the matrix of the cytoplasmic membrane, mitochondria and cell wall were likely mediated or secondary after the impairment of the cytoplasmic membrane.

[Cyclosporin A and the permeability of the cytoplasmic membrane in Aspergillus niger].

Cyclosporine A was shown to impair selective permeability of cytoplasmic membranes in Aspergillus niger thus inducing leakage of low molecular components of the intracellular fond from the cells. In this respect lyposomal cyclosporine had a more pronounced action than the free form. Cyclosporine was compared with amphotericin B and the latter in the free and lyposomal forms demonstrated a higher effect on the cell membranes of Asp.

[Comparative effectiveness of rifampicin for parenteral administration and internal dose in the treatment of experimental plague in albino mice].

The therapeutic effects of parenteral and oral rifampicins were studied comparatively in a model of experimental plague of albino mice infected subcutaneously and by aerosol. The study showed that in a dose of 25 mg/kg rifampicin was highly efficient in the treatment of the albino mice with experimental glandular plague when the drug was administered either parenterally or orally for 7 days (100-percent survival). The parenteral rifampicin was advantageous when used in lower doses (6.

[Comparative in vitro activity of ampicillin, cefoperazone, their combinations with sulbactam and other antibiotics with respect to staphylococci and pneumococci].

Antibiotic susceptibility of 225 Staphylococcus strains and 42 Pneumococcus strains was assayed with the method of serial microdilutions. Methicillin resistant Staphylococcus strains (S. aureus and coagulase negative strains) were characterized by high susceptibility to cephalosporins and ampicillin + sulbactam combination, as well as to ciprofloxacin, rifampicin and vancomycin (70 to 100 per cent of the susceptible strains).

[Comparative in vitro activity ampicillin, cefoperazone, their combinations with sulbactam, as well as that of other antibiotics against aerobic gram-negative microorganisms].

The activity of 12 antibiotics against 849 strains of gram-negative aerobes isolated in special and general hospitals of Moscow and Smolensk in 1992-1993 was assayed with the method of serial microdilutions. By the criteria of the activity (percentage of the susceptible strains by the NSSLS criteria) against the isolates the antibiotics were arranged as follows: ciprofloxacin (89.8 per cent) > imipenem (89.

[Effect of cyclosporin on various metabolic processes in fungi].

Sensitivity of the representatives of Aspergillus and Piricularia to various concentrations of cyclosporine (in the submerged culture) was studied for choosing the test object for the subcellular investigation of the mechanism of the cyclosporine antifungal action. Changes in the main physiological and biochemical parameters of the fungal cells under the action of cyclosporine in concentrations of 10 to 80 micrograms per 1 ml of the medium were characterized. Low concentrations of cyclosporine (10 to 20 micrograms/ml) did not inhibit the growth of Aspergillus niger but induced stimulation of the growth processes.

[A comparative study of liposome-incorporated beta-lactam antibiotics, fluoroquinolones and cephalosporin conjugates with fluoroquinolones].

Beta-lactam antibiotics (some penicillins and cephalosporins), a fluorquinolone (pefloxacin) and cephalosporin conjugates with fluorquinolones were liposome-encapsulated by the method of detergent dialysis. Under the experimental conditions the entrapment of the beta-lactams and pefloxacin to liposomes did not exceed 20 and 12.5 per cent of the initial quantity respectively.

[Semisynthetic penicillins: their importance in the current antibiotic therapy of infections. Penicillinase-resistant penicillins with predominantly antistaphylococcal action].

The status of isoxazolylpenicillins in the modern antibiotic therapy of staphylococcal infections is discussed from various viewpoints: the role and distribution of methicillin resistant staphylococci (MRSA), the methicillin tolerance, the clinical pharmacology and pharmacokinetics, the preferable administration routes and regimens depending on the disease severity and renal function, the prophylaxis of purulent infections, the indications to the combined therapy and possible side effects. It is indicated that one of the conditions providing the efficacy of penicillinase stable antistaphylococcal penicillins is the absolute knowledge of their properties and the joint efforts of the clinicians and bacteriologists in providing a rapid change of the drug after the detection of MRSA or methicillin tolerant staphylococci. This excludes any discredit of the drugs which are useful in the modern antistaphylococcal therapy.

[Antibiotic pharmacokinetic indices and their significance in working out antibacterial therapy regimens and predicting their efficacy].

The data on the value of pharmacokinetic parameters and pharmacologic properties of antibiotics for the development of optimal regimens of antibacterial therapy are presented. The impact of various symptoms and syndromes of purulent septic processes (uremia, anemia, obesity or hyperbilirubinemia) on antibiotic pharmacokinetics is discussed. Approaches to the improvement of schemes for antibiotic therapy of various pathological conditions are noted.

[Inactivation of free and liposome-encapsulated aminoglycosides by enzymes of resistant strains of bacteria].

Liposome-encapsulated gentamicin, sisomicin, paromomycin, amikacin, dibekacin and some other aminoglycoside antibiotics were prepared by the method of detergent dialysis. The entrapment level was higher with respect to paromomycin, gentamicin and sisomicin. After a 1-hour incubation of the liposome-encapsulated paromomycin in the presence of a cell-free preparation of 3'-1-phosphotransferase from Escherichia coli there was observed no inactivation of the antibiotic.

Use of gentamicin physiologically-based model for individual dosing.

A new approach to fixing initial doses of gentamicin (GM) for i.m. administration (that is most commonly used anyway) is discussed.