Bactericidal Activity and Pharmacology of Cefazolin

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The activity of cefamandole was comparable to that of cephalothin, cefazolin, and cephaloridine against Staphylococcus aureus, Streptococcus pyogenes, and Diplococcus pneumoniae. In contrast, cefamandole was considerably more active than cephalothin, cefazolin, or cephaloridine against gram-negative facultative bacilli, including Haemophilus influenzae, the most striking disparities being noted with indole-positive Proteus and Enterobacter. Bacteroides fragilis was more susceptible to cefoxitin than to cefamandole or cefazolin (median minimal inhibitory concentration, approximately 8, 32, and 32 ,ug/ml, respectively); cephalothin exhibited still less activity against this species. The majority of other anaerobes were inhibited by relatively low concentrations of all four cephalosporins. The results indicate a potentially valuable role for cefamandole against facultative gram-negative bacilli, including H. influenzae, but no exceptional activity against anaerobes.

Section: Notes 853mentioning

confidence: 95%

“…Bacterial inocula, prepared from an overnight broth culture, contained 5 x 103 organisms per well. The minimal inhibitory concentration (MIC) and minimal bactericidal concentration (MBC) were determined as previously described (1).…”

mentioning

confidence: 99%

Activity of Cefamandole and Other Cephalosporins Against Aerobic and Anaerobic Bacteria

Ernst

Berger

Barza

et al. 1976

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“…The in vitro activities of P-lactam antibiotics and fusidic acid are diminished by plasma protein binding (2,4,5,15,20,25). The activities of seven penicillins have been closely related to plasma protein binding in experimental infections in mice as well (18).…”

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confidence: 99%

Influence of albumin on itraconazole and ketoconazole antifungal activity: results of a dynamic in vitro study

Schäfer‐Korting

Körting

Amann

et al. 1991

The relevance of intense protein binding to the antifungal activity of azole compounds is still a matter of debate. The influence of albumin on the antimicrobial activity of ketoconazole and itraconazole, which exhibit very strong plasma protein binding (99 and 99.8%), was evaluated in vitro. Candida albicans was exposed to continuously changing azole concentrations corresponding to drug levels in serum following an oral dose of 200 mg. Total as well as free drug levels in serum were simulated. The incubation medium was free of proteins or contained 4% human serum albumin. Itraconazole levels reflecting free drug concentrations in humans did not reduce the growth rate of C. albicans, as compared with controls (difference in the log CFU per milliliter at 12 h, 0.03 ± 0.09), whereas total drug levels were as active in the presence of 4% albumin (meah difference, -0.61) as in its absence (-0.75). The same was true for ketoconazole, except that free drug levels were also active (-1.21 versus -1.39 for total drug levels). This result was due to the higher ketoconazole levels in humans. Thus, in terms of routine susceptibility testing, in vitro total drug levels can be considered relevant.

“…Table 2 were reported by various investigators by a different methodology; however, there is general agreement among investigators (1,3,9,10). Cephalothin also penetrates the pleural fluid in therapeutic levels (4,6).…”

Section: Resultsmentioning

confidence: 99%

Penetration of Cefazolin into Pleural Fluid

Cole

Pung

1977

Single doses of cefazolin, 500 mg intramuscularly and 1 g intravenously, were administered to 16 patients having lung pathology who were scheduled for thoracic fluid aspiration. Pleural fluid and serum samples were taken at intervals of 30 to 240 min for determination of cefazolin levels. The levels obtained were variable; however, the levels of cefazolin in pleural fluid generally exceeded the reported minimal inhibitory concentration values for Staphylococcus pneumoniae and Staphylococcus, and group A beta-hemolytic streptococcus. In addition, the pleural fluid levels exceeded the minimal inhibitory concentration for cefazolin against most of the Klebsiella and Haemophilus influenzae strains. These data show that cefazolin, despite its comparative high protein binding, produces levels in the pleural fluid capable of inhibiting the organisms commonly found in respiratory tract infections.Cephalosporins such as cefazolin and cephalothin are used effectively to treat infections of the respiratory tract caused by Streptococcus pneumoniae, Klebsiella species, Staphylococcus aureus, group A beta-hemolytic streptococcus, and Haemophilus influenzae. Cefazolin and cephalothin have a similar broad spectrum of activity; however, cefazolin produces higher and longer-lasting blood levels than does cephalothin. On the other hand, cefazolin is more highly protein bound than cephalothin -86%