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PubMed1977

Cefoxitin activity against multiply antibiotic-resistance Klebsiella pneumoniae in vitro.

Due to the emergence of cephalothin- and gentamicin-resistant Klebsiella pneumoniae at this institution, we investigated the in vitro activity of two new cephalosporin compounds-cefoxitin and cefamandole. Whereas both drugs were active against cephalothin- and gentamicin-susceptible isolates of Klebsiella, only cefoxitin exhibited significant activity against cephalothin- and gentamicin-resistant isolates. Seventeen of 20 (85%) of the cephalothin- and gentamicin-resistant isolates were inhibited by </=12.5 mug of cefoxitin per ml. The minimum bactericidal concentration in broth of representative isolates equaled the agar dilution minimum inhibitory concentration. Kirby-Bauer disk susceptibility testing correlated well with the agar dilution minimum inhibitory concentration. Cephalothin and cefamandole resistance of isolates could be correlated with antibiotic degradation by beta-lactamase. Cephalothin and cefamandole evoked only a transient decrease in viable bacterial cell count with rapid inactivation of antibiotics, and full regrowth of the organisms. Cefoxitin, on the other hand, was quite effective in vitro against multiply resistant Klebsiella. No beta-lactamase degradation of cefoxitin was detected. Growth curves with antibiotics indicated rapid killing of cephalothin- and gentamicin-resistant isolates by cefoxitin.

Cefoxitin↗
PubMed1983

Particulate matter in four reconstituted cephalosporin injections.

The amount and size of particulate contamination in three commercially available cephalosporin injections and a new product, anophilized cephalothin sodium injection, were studied. Particles in reconstituted cephalothin sodium (commercially available and anophilized), cephapirin sodium, and cephradine injections were counted using two methods: (1) modified USP membrane-filtration technique and (2) Elzone computerized particle analyzer. The amount of particulate contamination in the ranges of 10-24 and greater than or equal to 25 microns was determined by both methods. In the 10-24-microns range, the cephalothin, cephapirin, and cephradine products had significantly greater particle counts than the anophilized cephalothin product. The greater than or equal to 25-microns particle counts showed that the cephapirin and cephradine products had particle counts greater than the anophilized cephalothin product, while total particle counts showed the same results as the 10-24-microns particle counts. A comparison of counting methods showed that the only significant difference between the number of particulates obtained using the modified USP and Elzone computer methods was with the cephalothin product. Anophilized cephalothin sodium injection has significantly fewer particles in the size ranges studied. No conclusion could be reached as to the more accurate method for counting particles.

Cephalosporins↗
PubMed1993

Characterisation of Yersinia species isolated from a kennel and from cattle and pig farms.

Between April 1984 and November 1986, 126 faeces samples were collected from puppies and bitches in a kennel and examined for Yersinia species; 45 (35.7 per cent) of them were positive. Thirty-eight isolates were Y enterocolitica, five were Y frederiksenii and two were Y intermedia. Twenty-one of the Y enterocolitica isolates belonged to serogroup 0:3 and 17 of these were L-sorbose negative; all these isolates were from puppies. One strain of Y frederiksenii and all the L-sorbose-negative Y enterocolitica serogroup 0:3 isolates were resistant to antimicrobial agents and showed four different patterns of resistance (ampicillin, cephalothin and tetracycline; ampicillin, cephalothin, streptomycin and tetracycline; ampicillin, chloramphenicol, cephalothin, streptomycin and sulfathiazole; and ampicillin, chloramphenicol, cephalothin, streptomycin, sulfathiazole and tetracycline. In January 1986, investigations were conducted on a cattle farm and a pig farm close to the kennel. Of 19 bovine faeces samples 11 (57.8 per cent) were positive for Yersinia species; eight yielded Y enterocolitica and four yielded Y frederiksenii. None of the Y enterocolitica isolates belonged to serogroup 0:3. Of 20 porcine faeces samples eight (40 per cent) were positive for Yersinia species; all eight yielded Y enterocolitica and four also yielded Y pseudotuberculosis. Two of the isolates of Y frederiksenii and two of the isolates of Y enterocolitica from the farms had the following resistance patterns: ampicillin, cephalothin and streptomycin; ampicillin, streptomycin and tetracycline; ampicillin, chloramphenicol, cephalothin, streptomycin, trimethoprim-sulphamethoxazole and tetracycline; and ampicillin, chloramphenicol, cephalothin, streptomycin, sulphatiazole, trimethoprim-sulphamethoxazole and tetracycline.(ABSTRACT TRUNCATED AT 250 WORDS)

Animals↗
PubMed1981

Antibiotic combination-associated nephrotoxicity in granulocytopenic patients with cancer.

Antibiotic combination-associated nephrotoxicity was reviewed in 491 granulocytopenic patients with cancer and fever. Nephrotoxicity was defined as a rise in the serum creatinine level of more than 0.4 mg/dL. The different aminoglycosides, when combined with ticarcillin disodium, were found to have an equivalent nephrotoxic potential and, for the purpose of analysis, were combined and termed "aminoglycoside plus ticarcillin" (Ags + ticarcillin). Groups treated with gentamicin or amikacin plus cephalothin sodium were combined and termed "aminoglycoside plus cephalothin" (Ags + cephalothin). The rate of nephrotoxicity was statistically less for the Ags + ticarcillin group, eight (3.1%) of 262 patients, than for the Ags + cephalothin group, 23 (18.3%) of 126 patients. Age greater than 50 years was a potentiating factor for the occurrence of nephrotoxicity in the Ags + cephalothin group. We have concluded that for granulocytopenic patients with cancer and fever, the antibiotic combination of the Ags + cephalothin should not be used as empiric antibiotic therapy.

Adolescent↗
PubMed1978

Interaction of cephalosporins with human and canine serum proteins.

The kinetic interaction of cephalothin and cefamandole with human serum protein and of cephalothin with canine serum protein was studied with use of a rate-of-dialysis method. Binding of antibiotic to serum proteins was complete in less than 1 min and was immediately reversible. Human serum bound 76.9% of cephalothin and 73.7% of cefamandole at 10 microgram/ml, and canine serum bound 41.3% of cephalothin at 10 microgram/ml when this technique was used. Quantitative binding determined by ultracentrifugation was 78.5% for cephalothin and 80.1% for cefamandole in human serum and 45.6% for cephalothin and 32.5% for cefazolin in canine serum. There was no delayed binding of these antibiotics to either human or canine serum. In addition, a large number of antibiotic-binding sites appeared to be present on both human and canine serum protein when the antibiotic concentration was increased to 10(5) microgram/ml.

Animals↗
PubMed1984

Endocarditis due to methicillin-resistant Staphylococcus aureus in rabbits: expression of resistance to beta-lactam antibiotics in vivo and in vitro.

Whether a strain of methicillin-resistant Staphylococcus aureus susceptible to cephalothin by the disk-diffusion method was also susceptible to cephalothin in vivo was evaluated in the rabbit model of endocarditis. Rabbits with aortic-valve endocarditis due to methicillin-resistant S. aureus that were treated for four days with cephalothin had the same numbers of organisms in vegetations as did untreated rabbits. Treatment with cephalothin caused emergence of a highly resistant subpopulation in aortic-valve vegetations. Organisms highly resistant to cephalothin were also highly resistant to nafcillin. Thus broth-dilution and disk-diffusion tests may not predict therapeutic failure for cephalothin against strains of methicillin-resistant S. aureus. Because of cross-resistances among beta-lactam drugs, these strains should be considered uniformly resistant to this general class of antimicrobial agents, regardless of results from these tests.

Animals↗
PubMed1984

Antibiotic prophylaxis for cardiovascular surgery. Efficacy with coronary artery bypass.

Two hundred twenty patients were randomly assigned to receive either ceforanide or cephalothin as perioperative antibiotic prophylaxis during cardiovascular surgery. More infections were seen among cephalothin recipients (8 deep, 32 total) than among ceforanide recipients (1 deep, 17 total). Among patients who had only coronary artery bypass grafting, more cephalothin recipients had infection than did ceforanide recipients (19 of 82 as opposed to 7 of 83; p = 0.001; relative risk, 2.7; 95% confidence interval, 1.22 to 6.18). The difference between the two regimens was attributable to fewer blood, wound, and urinary tract infections. Among patients who had other procedures, there was no difference in the efficacy of the two regimens. Cephalothin recipients who developed wound or blood stream infections had lower antibiotic levels in their atrial appendages than recipients not developing such infections (p = 0.02). If one assumes that cephalothin does not increase the risk of infection, then these data show that antibiotic prophylaxis prevents infection after coronary artery bypass surgery, and, in the dosages used, that ceforanide is superior to cephalothin.

Cefamandole↗
PubMed1972

Structure-activity relationships among a group of 7-(alpha-(N,N'-substituted-amidinothio)-acetamido) cephalosphoranic acids.

Structure-activity relationships were examined for a number of 7-[alpha-(N,N'-substituted-amidinothio)-acetamido] cephalosporanic acids, including several wherein the amidino group was cyclized into six, seven, and eight-membered rings and a series wherein alkyl, cycloalkyl, alkenyl, and alkynyl radicals were substituted on the nitrogens of the noncyclized amidino group. Derivatives containing an unsubstituted cyclized amidino group had comparable antibacterial activity in vitro and in general had a spectrum of activity broader than that of cephalothin, especially against cephalothin-resistant strains of Escherichia, Klebsiella, and Proteus. When administered parenterally, the cephalosporin with the six-membered cyclized amidino group was as effective as cephalothin in experimental infections of mice produced by cephalothin-sensitive gram-negative organisms and more efficacious in infections caused by cephalothin-resistant strains. Among the cephalosporins with noncyclized amidino groups, those with an ethyl substituent on one of the nitrogens and a C(2)-C(4) alkyl radical, particularly propyl on the other, were the most active. They not only had a better profile of activity in vitro than cephalothin and the cephalosporin derivatives having a cyclized amidino group, but were also more efficacious in infections of mice.

Acetamides↗
PubMed1973

Microbiological properties of a new cephalosporin, BL-S 339: 7-(phenylacetimidoyl-aminoacetamido)-3-(2-methyl-1,3,4-thiadiazol-5-ylthiomethyl)ceph-3-em-4-carboxylic acid.

BL-S 339 is a new broad-spectrum, parenterally effective cephalosporin whose expression of antibacterial activity in vitro is markedly affected by the nature of the assay medium. When assayed in nutrient agar, BL-S 339 was more active than cephalothin against strains of Diplococcus pneumoniae, Streptococcus pyogenes, Escherichia coli, Serratia marcescens, Klebsiella pneumoniae, Enterobacter, and indole-positive Proteus sp. However, when assayed in Mueller-Hinton medium, its activity, especially against gram-negative bacteria, was reduced substantially, whereas the activity of cephalothin was virtually unaffected by the assay medium. The in vivo activity of BL-S 339 correlated well with its activity in nutrient agar; when administered subcutaneously to mice, it was therapeutically more efficacious than cephalothin in infections caused by both gram-positive and gram-negative bacteria. When BL-S 339 was administered intramuscularly to mice, the concentrations achieved in the blood were three times those achieved with cephalothin. BL-S 339 was bound to human serum proteins to the same extent as cephalothin. Recovery of BL-S 339 in the urine within the 24-hr period after intramuscular administration to rats was three times that of cephalothin.

Animals↗
PubMed1986

Benefit from high intrarenal levels of gentamicin in the treatment of E. coli pyelonephritis.

The importance of high intrarenal levels of gentamicin on the outcome of experimental pyelonephritis was studied in rats receiving either a short course (three days) of gentamicin (G) alone or combined with a longer course (14 days) of ampicillin (A), cephalothin (C), or trimethoprim (T), or two weeks of therapy with ampicillin, cephalothin, trimethoprim and gentamicin given alone. While ampicillin, cephalothin and trimethoprim were undetectable in the medulla within six hours of cessation of therapy, gentamicin was still detectable in levels six folds above the MIC up to six months after treatment had ceased. Six months after the end of treatment, the percentage of sterile left kidneys in animals treated with ampicillin (50%), cephalothin (15%), trimethoprim (20%) was lower than the percentage of animals receiving 14 days of gentamicin (100%), or the combinations AG:89%, CG:67% and TG:60%, P less than 0.01. Following three days of gentamicin, 50% of the left kidneys were sterilized. When compared to ampicillin, cephalothin or trimethoprim alone, combined therapies significantly reduced the number of CFU in the kidneys P less than 0.01. These combinations were almost as effective as two weeks of therapy with gentamicin. Short-term therapy (three days) with an aminoglycoside which concentrates in the renal parenchyma, combined with an antibiotic which will accumulate in other parts of the nephron, may result in "pharmacological synergy". This new approach to therapy of pyelonephritis may be promising.

Acute Disease↗
PubMed1976

Characteristics of biliary excretion of cefazolin and other cephalosporins with reference to the relationship between serum levels and administration conditions.

The biliary excretion of cefazolin was compared with that of cephalothin and cephaloridine in rats and man. In rats, the biliary levels were dose-related with cefazolin and cephalothin but not with cephaloridine. Biliary levels were higher than serum levels after injection of 10--80 mg/kg of cefazolin and cephalothin, whereas serum levels of cephaloridine after injection were higher than biliary levels. The highest biliary levels of cefazolin were obtained by intravenous injection, followed by intramuscular injection and drip infusion. In man, a crossover study was made to compare biliary levels of cefazolin with those of cephaloridine and cephalothin. After a single 1-gram intravenous injection, the peak levels of cefazolin ranged from 0.85 to 21 mug/ml and those of cephaloridine varied from 0.55 to 3.9 mug/ml. After a 3-gram intravenous injection, the peak biliary levels of cefazolin ranged from 35.5 to 270 mug/ml and those of cephalothin from 0.3 to 64 mug/ml. The chemotherapeutic biliary levels of cefazolin able to inhibit susceptible organisms were obtained by 3-gram intravenous injections.

Animals↗
PubMed1975

A new parenteral cephalosporin. SK&F 59962: in vitro and in vivo antibacterial activity and serum levels in experimental animals.

SK&F 59962, a new parenteral cephalosporin was found to have a high order of in vitro and in vivo antibacterial activity against a broad-spectrum of clinical isolates. When tested in vitro against gram-negative organisms, SK&F 59962 was consistently more active than cefazolin and far superior to cephalothin. This new antibiotic had activity equal to that of cephalothin against gram-positive bacteria. Enterobacter species were found to be susceptible to SK&F 59962. In mouse infection studies using bacterial pathogens, SK&F 59962 had protective activity of the order of that of cefazolin and superior to that of cephalothin. Following parenteral administration the serum profile of SK&F 59962 in the mouse, dog and squirrel monkey was similar to that of cephalothin. SK&F 59962 and cephalothin had lower peak serum concentrations and shorter biologic half-lives than those of cefazolin.

Animals↗
PubMed1984

7-(D,L-alpha-fluoro-2-thienylacetamido)cephalosporanic acid (L 14655), a new semisynthetic cephalosporin. Synthesis and preliminary biological evaluation.

We describe the synthesis and some preliminary antimicrobial and enzymatic properties of 7-(D,L-alpha-fluoro-2-thienylacetamido)cephalosporanic acid (L 14655), a fluorinated derivative of cephalothin. L 14655 had antimicrobial activity similar to that of cephalothin. Cell-free studies demonstrated that L 14655 was very stable to hydrolysis by type Ia beta-lactamase (325 times more than cephalothin) but not to TEM enzyme. In addition, L 14655 was 480 times more active than cephalothin in preventing the hydrolysis of nitrocephin by type Ia enzyme. Preliminary studies in intact beta-lactamase-producing cells did not however produce evidence of enhanced activity of L 14655 relative to cephalothin.

Anti-Bacterial Agents↗
PubMed1977

Reliability of the microdilution technic for detection of methicillin-resistant strains of staphylococcus aureus.

To determine whether the microdilution technic for antimicrobic susceptibility testing could detect the hetero-resistance of "methicillin"-resistant Staphylococcus aureus, 100 stock cultures (54 methicillin-susceptible and 46 methicillin-resistant) were tested against methicillin, oxacillin, nafcillin and cephalothin. Each drug was diluted in Mueller-Hinton broth and in Mueller-Hinton broth with 5% NaCl. Minimum inhibitory concentration (MIC) determinations were made after 20-24 hours at 35 C and again after 48 hours of incubation. With one exception, methicillin resistance was detected in Mueller-Hinton broth when the trays were reincubated and read after 48 hours. Earlier detection of methicillin resistance was possible when the penicillinase-stable penicillins were diluted in broth containing 5% NaCl. Further studies suggest that the addition of NaCl to the broth medium might improve the stabilities of methicillin, oxacillin, and nafcillin during storage of the frozen microdilution trays. Either nafcillin or oxacillin would appear to be the best representative of the penicillinase-stable penicillins. Standardized disk-diffusion tests with cephalothin disks indicated that most methicillin-resistant strains are susceptible to cephalothin. However, there is reason to believe that such in-vitro test results might be inappropriate. With microdilution tests, most methicillin-resistant isolates were more resistant to cephalothin than were the methicillin-susceptible strains, but the MIC's for both types of staphylococci were generally within the range of concentrations that can be obtained during therapy. The addition of NaCl to the microdilution tests with cephalothin did not alter the test results significantly.

Indicator Dilution Techniques↗
PubMed1976

Susceptibility of anaerobic bacteria to 23 antimicrobial agents.

The antimicrobial susceptibility of 492 anaerobic bacteria, the majority of which were recent clinical isolates, was determined by the agar dilution technique. Penicillin G was active against most of the strains tested at 32 U or less/ml, but only 72% of Bacteroides fragilis strains were susceptible at this level and 9% required 256 U or more/ml. Ampicillin was effective against most of the strains except B. fragilis at 16 mug or less/ml. Amoxicillin was active against only 31% of B. fragilis, 76% of other Bacteroides species, and 67% of Fusobacterium species at 8 mug/ml. Two new penicillins, mezlocillin and azlocillin, were similar to ampicillin in their activity. Carbenicillin and ticarcillin inhibited all but a few strains at 128 mug or less/ml. BLP 1654 was somewhat more active than penicillin G against B. fragilis but had similar activity against other anaerobes. Cephalothin was inactive against B. fragilis, and only 65% of other Bacteroides species were inhibited by 32 mug or less/ml. It was effective against all other anaerobes at that level. Cefamandole showed somewhat greater activity than cephalothin against B. fragilis but generally less activity against gram-positive organisms. Cefazaflur (SKF 59962) was comparable to cephalothin against B. fragilis. Cefoxitin was distinctly more active than cephalothin against B. fragilis. These latter two agents were less active than cephalothin against the gram-positive anaerobes. Chloramphenicol remains active against anaerobic bacteria at 16 mug or less/ml, with rare exceptions. Thiamphenicol was similar to chloramphenicol in its activity. Clindamycin was very active against most of the anaerobes at 8 mug or less/ml. Erythromycin and josamycin were also tested, with josamycin showing greater activity against B. fragilis than either erythromycin or clindamycin. A new oligosaccharide, everninomicin B, was less active than clindamycin against B. fragilis but more active against clostridia and some of the other strains tested. Most of the groups of bacteria tested demonstrated a trend toward resistance to tetracycline. Doxycycline and minocycline were somewhat more active than was tetracycline. Metronidazole was active against the majority of the anaerobes tested; resistance ws demonstrated by some of the gram-positive cocci and gram-positive, non-sporeforming bacilli.

Anaerobiosis↗
PubMed1978

Comparative in vitro activity of newer cephalosporins against anaerobic bacteria.

The in vitro susceptibilities of 408 recent clinical isolates of anaerobic bacteria against cefaclor, cephalexin, cephalothin, cefazolin, cefamandole, and cefoxitin were compared by an agar dilution technique. Against gram-positive bacteria, especially peptococci, peptostreptococci, and propionibacteria, cephalexin and cefaclor were significantly less active than cephalothin (P < 0.05). Cephalexin was also less active than cephalothin against clostridia and lactobacillus (P < 0.05). Against gram-negative bacteria, major differences were observed primarily with Bacteroides fragilis, against which cephalexin, cefazolin and cefoxitin were all significantly more active than cephalothin (P < 0.001). At concentrations of 16 mug per ml, however, all cephalosporins showed high in vitro activity, except against Lactobacillus species and B. fragilis. Cephalothin, cefazolin and cefamandole were considerably more active against the former, whereas cefoxitin was distinctly more active against the latter.

Anaerobiosis↗
PubMed1974

Characterization and prevalence of the different mechanisms of resistance to beta-lactam antibiotics in clinical isolates of Escherichia coli.

A survey of clinical isolates from a hospital laboratory showed that Escherichia coli could be grouped into three classes of beta-lactam-antibiotic resistance by results of routine susceptibility testing to ampicillin, cephalothin, and carbenicillin. E. coli highly resistant to ampicillin and carbenicillin but not to cephalothin (class I) were found to have one of two levels of R factor-mediated, periplasmic-beta-lactamase which resembled R(TEM) and was located behind a permeability barrier to penicillins but not to cephalosporins. This permeability barrier appeared to act synergistically with the beta-lactamase in producing high levels of resistance to penicillins. E. coli highly resistant to ampicillin and cephalothin but not carbenicillin (class II) were found to have a beta-lactamase with predominantly cephalosporinase activity which was neither transferable nor releasable by osmotic shock. E. coli moderately resistant to one or to all three of these antibiotics (class III) were found to have low levels of different beta-lactamases including a transferable beta-lactamase which resembled R(1818). Thus, different mechanisms producing resistance to beta-lactam antibiotics could be deduced from the patterns of resistance to ampicillin, cephalothin, and carbenicillin found on routine susceptibility testing. E. coli of class I were much more prevalent than the other classes and the proportion of E. coli that were class I increased with duration of patient hospitalization. The incidence of class I E. coli rose only slightly over the past 7 years and that of class II E. coli remained constant despite increased usage of both cephalothin and ampicillin. These observations emphasize that the properties of the apparently limited number of individual resistance mechanisms that exist in a bacterial flora, such as their genetic mobility and linkages and the spectrum of their antibiotic inactivating enzymes and permeability barriers, may govern the effect that usage of an antibiotic has upon the prevalence of resistance to it and to other antibiotics.

Amidohydrolases↗
PubMed1976

Relative inactivation by Staphylococcus aureus of eight cephalosporin antibiotics.

These studies extend the recent observation that cefazolin is inactivated to a greater extent than cephaloridine by some strains of penicillinase-producing Staphylococcus aureus, whereas cephalothin undergoes little if any inactivation. In Mueller-Hinton broth (inoculum, 3 x 10(6)) 100 recently isolated strains had minimal inhibitory concentrations (MICs) </= 2 mug/ml for cephalothin and cephaloridine, whereas in Trypticase soy broth (TSB) 50% had MICs > 2 mug/ml and 10% (designated "resistant" strains) were >8 mug/ml for cephaloridine but remained </=2 mug/ml for cephalothin. A large inoculum (3 x 10(7)) of strains with high MICs in TSB almost completely inactivated 50 mug of cefazolin per ml in 6 h, with progressively less inactivation, in the following order, of cephaloridine, cephalexin, cephradine, cephapirin, and cefamandole; cefoxitin and cephalothin underwent little if any inactivation. The greater inactivation in TSB than in Mueller-Hinton broth appeared to be due to a greater production of beta-lactamases by each colony-forming unit, since the inoculum size in the two broths was not significantly different. In contrast, "susceptible" strains (MICs </= 2 mug/ml in both broths) inactivated cephaloridine more than cefazolin, and equal amounts of powdered bacterial extracts confirmed the fact that qualitatively different beta-lactamases were produced by the susceptible and resistant strains. Disk diffusion tests were unreliable in separating the two groups of staphylococci. The clinical significance of inactivation by strains with high MICs is not known but, unless susceptibility can be clearly established, cephalothin appears preferable for severe staphylococcal infections, since it undergoes little if any inactivation by any strains of staphylococci.

Cephalosporins↗