Fusidic Acid: a New Antibiotic

121

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confidence: 99%

Genetic and Phenotypic Identification of Fusidic Acid-Resistant Mutants with the Small-Colony-Variant Phenotype in Staphylococcus aureus

Norström

Lannergård

Hughes

2007

121

“…Fusidic acid is a steroid-like antibiotic isolated from the fermentation broth of the fungus Fusidium coccineum (8). It is active in vitro against Staphylococcus aureus, Clostridium spp., and corynebacteria (8,10,23).…”

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confidence: 99%

“…It is active in vitro against Staphylococcus aureus, Clostridium spp., and corynebacteria (8,10,23). Its antibacterial activity is the result of an inhibition of bacterial protein synthesis (1).…”

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confidence: 99%

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Pharmacokinetics of intravenous fusidic acid in patients with cholestasis

Peter

Jehl

Pottecher

et al. 1993

The pharmacokinetics of fusidic acid and 3-ketofusidic acid were investigated in cholestatic and noncholestatic patients after intravenous administration of single and multiple doses of 500 mg of sodium fusidate. The patients, all with low serum albumin levels, were divided into three groups. Group I consisted of six noncholestatic patients; group II consisted of nine mildly cholestatic patients with mild hepatic impairment (conjugated bilirubin, 47 pmol liter-l; alkaline phosphatase, 280 IU liter-'; y-tglutamyltranspeptidase, 190 IU liter-.); group m consisted of six benign intrahepatic cholestatic patients with high isolated conjugated hyperbilirubinemia (98.1 ,umol liter-'). Assays were performed by high-pressure liquid chromatography. At steady state, the mean peak concentrations in serum were 63.7, 44.9, and 92.2 tLg ml-l in groups I, II, and III, respectively; over a dosage interval, areas under the concentration-time curve were 411. 1, 238.7, and 603.4 t.g. h ml-' and the mean body clearances were 0.34, 0.53, and 0.25 ml min kg-' in groups I, II, and III, respectively. The accumulation ratio of fusidic acid increased from 2.8 and 2.4 in groups I and II to 4.2 in group II. At steady state, the ratios of the areas under the concentration-time curve from 0 to 8 h for 3-ketofusidic acid/fusidic acid were 0.11, 0.09, and 0.10 in the three groups, respectively. Only very small amounts of fusidic acid and 3-ketofusidic acid were found in urine. These results substantiate the following hypotheses. In group I and II patients the clearance is higher than that in healthy volunteers because of the increased free, unbound fraction of fusidic acid, a consequence of lower serum albumin concentrations, resulting in increased distribution in tissue and hepatic metabolism. In group MII patients, the higher bilirubinemia results in competition with fusidic acid for the limited glucuronidation mechanism, thus compensating for the increased elimination of fusidic acid because of the low serum albumin concentration. These results suggest that fusidic acid can be administered normally even to patients with high bilirubinemia because the postoperative serum albumin concentration is usually low.

“…Fusidic acid, produced by the fungus Fusidium coccineum, possesses a steroid structure and is chemically related to cephalosporin P1 (3). Unlike the cephalosporins, which inhibit cell wall synthesis, fusidic acid inhibits bacterial protein synthesis by interfering with the translocation enzyme and inhibiting the binding of aminoacyl transfer ribonucleic acid to ribosomes (2).…”

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confidence: 99%

In Vitro Activity of Sodium Fusidate Against Anaerobic Bacteria

Steinkraus

McCarthy

1979

The microtiter broth dilution method was employed to determine the in vitro susceptibility of 525 recent clinical isolates of anaerobic bacteria to sodium fusidate. The minimal inhibitory concentrations of sodium fusidate ranged from -0.06 to 1.0 ,ug/ml for 155 strains of anaerobic gram-positive rods and 130 strains of anaerobic gram-positive cocci. Minimal inhibitory concentrations ranging from s0.06 to 32 ,ug/ml were observed for 240 strains of anaerobic gram-negative rods.Among the latter group a minimal inhibitory concentration of 16 ,ug/ml or greater was encountered with 16% of 45 Bacteroides fragilis strains, 19% of 32 Bacteroides thetaiotaomicron, and all 7 strains of Fusobacterium necrophorum. Minimal inhibitory concentrations for Veillonella parvula, the only gram-negative coccus tested, ranged from 0.5 to 8.0 yig/ml.