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PubMed1981

[Antibiotics as inhibitors of the prokaryotic protein biosynthesis: action and resistance mechanisms (author's transl)].

Most of the known antibiotics interfere with the translational apparatus due to the extraordinary complexity of the translational organelle, the ribosome. After a short survey on structure and function of the ribosome the action of some antibiotics is explained and integrated in an extended scheme of ribosomal functions. Furthermore, various resistance strategies of the translational apparatus against the antibiotics are described.

Anti-Bacterial Agents↗
PubMed1983

[Effect of glycodihydrofusidate, a structural analog of bile salts, on the hepatic transport of bromosulfophthalein in rats].

The interaction between bromosulfophthalein and glycodihydrofusidate in their transport by the liver were studied. In vitro, glycodihydrofusidate, a bile salt analogue, inhibited bromosulfophthalein uptake by isolated rat liver cells. This inhibition was similar to that previously described by adding sodium taurocholate to the medium; the inhibition was only partial and could no longer be detected at high bromosulfophthalein concentrations (20 microM). These results suggest that glycodihydrofusidate, like sodium taurocholate can compete with bromosulfophthalein for a common carrier in the liver cell membrane. In vivo, in the rat submitted to a saturating infusion of bromosulfophthalein, the addition of glycodihydrofusidate to the perfusate induced a 65 p. 100 decrease in the biliary excretion of bromosulfophthalein, a decrease in the water flow (47 p. 100) and a slight diminution in the bile salt output (14 p. 100). In experiments where glycodihydrofusidate-bromosulfophthalein interactions did not occur at the sinusoidal level, the biliary excretion of the dye was inhibited by glycodihydrofusidate. This suggests a common pathway for the two molecules. Our results are consistent with the existence of two different bromosulfophthalein carrier systems present at either pole of the hepatocyte. However only one is shared with bile salts and glycodihydrofusidate. This same hypothesis might account for many other experimental results as well.

Animals↗
PubMed1984

Acute osteomyelitis and septic arthritis in children. A simple approach to treatment.

A 12-month prospective study of 45 patients with bacteriologically proven acute osteitis and septic arthritis is presented. Sodium fusidate and erythromycin at the recommended dosage of 30 mg/kg/d for 3 weeks was found to be an effective first-line antibiotic regimen. The hazards of Haemophilus infection are emphasized. Immediate Gram staining is therefore strongly recommended. It was found that adequate drainage of a subperiosteal abscess without drilling of the bone always resulted in complete cure, while cases of septic arthritis consequent upon decompression of a contiguous metaphysitis were adequately treated by arthrotomy and irrigation alone. The authors believe that early limited surgery with adequate administration of antibiotics aided by early circumspect mobilization will provide a good functional and cosmetically acceptable result in most cases.

Acute Disease↗
PubMed1982

Antibiotic loaded plaster of Paris pellets: an in vitro study of a possible method of local antibiotic therapy in bone infection.

Plaster of Paris is an effective ancillary treatment in the surgery of infected cavities in bone. It is well tolerated and spontaneously absorbed over a period of weeks to months, being replaced by bone of normal architecture. It effectively obliterates much of the dead space, leaving little room for hematoma formation. It would appear logical to treat local infection, especially involving rigid walled cavities, by a locally diffused antibiotic. When incorporated into plaster of Paris pellets, two antibiotics, Fucidin and gentamicin, are capable of prolonged local release in bacteriocidal concentrations. On the basis of in vitro observations on bacterial cultures, it is proposed that antibiotic-plaster of Paris pellets might be a simple adjuvant technique to good surgical debridement in the treatment of bone infection. Plaster of Paris has the practical advantage over acrylic cement beads containing antibiotics in that it is resorbed and would not need a subsequent operation to be moved.

Anti-Bacterial Agents↗
PubMed1978

[Effect of antibiotics on the early stages of embryogenesis].

Tetracycline and Fusidin have the ability to flow through the placenta in a high quantity. It is proved, that these preparations in the early stage of ontogenesis developed considerable embryotoxic quality. High danger in the pregnancy is given with Tetracycline. Therefore the application of these antibiotics during the pregnancy is not indicated.

Abnormalities, Drug-Induced↗
PubMed1981

Antibiotics for gram-positive organisms.

Most infections due to Gram-positive organisms can be treated with quite a small number of antibiotics. Penicillin, cloxacillin, and erythromycin should be enough to cover 90 per cent of Gram-positive infections. The relatively narrow spectrum of these drugs should be the incentive to prescribers to use them selectively, together with adequate bacteriological investigation, in order to achieve effective treatment with a minimum of disturbance to the patient's normal bacterial flora and without any other harmful side effects.

Anti-Bacterial Agents↗
PubMed1993

Permeability enhancement in Caco-2 cell monolayers by sodium salicylate and sodium taurodihydrofusidate: assessment of effect-reversibility and imaging of transepithelial transport routes by confocal laser scanning microscopy.

The effects of sodium salicylate and sodium tauro-24,25-dihydrofusidate (STDHF) on the aqueous permeability of confluent monolayers of Caco-2 cells were studied. Measurements of transepithelial electrical resistance (TEER) showed a concentration-dependent effect of both compounds after apical incubation for 1 hr. Reductions in TEER resulting from EC50 concentrations (2.8 mM for STDHF; 173 mM for salicylate) were reversible within 5.75 hr. The transpithelial fluxes of two hydrophilic model compounds, sodium fluorescein F (molecular weight 376) and a fluorescein isothiocyanate-labeled dextran (mean molecular weight 4000) was significantly increased by STDHF (2.8 mM). Sodium salicylate (173 mM) only enhanced the transport of sodium fluorescein significantly. At the EC50 concentrations, confocal laser scanning microscopy (CLSM) visualized both fluorescent tracers mainly in the paracellular route. With higher enhancer concentrations (373 mM sodium salicylate and 8 mM STDHF), both transport markers appeared intracellularly as a result of cell death. STDHF rapidly extracted an exogenous lipophilic membrane probe, 5-(N-hexadecanoyl)aminofluorescein (HEDAF), from the apical part of Caco-2 plasma membranes, indicating qualitatively that STDHF interacts with the lipid portion of cell membranes. These results suggest that both sodium salicylate and STDHF can be used to reversibly increase paracellular permeability of Caco-2 cell monolayers, whereby STDHF appears to be advantageous compared to sodium salicylate. By adapting the Costar cell culture system to CLSM, we have shown that this technique is suitable to study membrane interactions qualitatively and for visualizing transport routes of hydrophilic tracers through nonfixed, filter-grown monolayers.

Adjuvants, Pharmaceutic↗
PubMed1995

Effects of sodium fusidate in animal models of insulin-dependent diabetes mellitus and septic shock.

We have evaluated the effects of the novel immunosuppressant sodium fusidate (fusidin) in the non-obese diabetic (NOD) mouse and in D-galactosamine (D-Gal)-presensitized BALB/c mice challenged with the bacterial superantigen, Staphylococcus aureus enterotoxin B (SEB) or with the endotoxin, Escherichia coli lipopolysaccharide (LPS). The NOD mouse model has clinical and histoimmunological features similar to those of human insulin-dependent diabetes mellitus (IDDM). The SEB- and LPS-treated BALB/c mouse models exhibit pathogenic similarities with human septic shock conditions. In the NOD mouse, fusidin suppressed the spontaneous development of insulitis (mean inhibition 73%) and hyperglycaemia (IDDM incidence 25% versus 0%) when administered at 40 mg/kg five times weekly for 8 consecutive weeks from the fourth week of age; concurrently treated animals exhibited reduced percentages of splenic T lymphocytes. This anti-diabetogenic effect was confirmed in the accelerated model of diabetes induced in the NOD mouse with cyclophosphamide (CY) (IDDM incidence 55% versus 21-6% using dosages of fusidin from 40 to 80 mg/kg five times weekly); protection from IDDM development was achieved even when the drug (80 mg/kg/day) was first administered 7 days after CY challenge. In contrast, fusidin did not reverse hyperglycaemia when administered to CY-treated animals within 3 days of IDDM development. In the two models of septic shock, prophylactic treatment with fusidin, 80 mg/kg given three times for 2 days prior to D-Gal/SEB or D-Gal/LPS challenge, drastically reduced the lethality compared with D-Gal/buffer-treated mice. This effect may depend on the inhibitory action of fusidin on the secretion of cytokines such as interferon-gamma and tumour necrosis factor-alpha, the serum levels of which were greatly diminished in the fusidin-treated mice (mean inhibition 50-90%). These results demonstrate that fusidin may have a role in the treatment of cell-mediated autoimmune diseases and cytokine-mediated infectious diseases in humans.

Animals↗