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PubMed1986

Evaluation of aztreonam, cefoperazone, latamoxef and ceftazidime in the hamster colitis model.

Aztreonam, ceftazidime, cefoperazone and latamoxef (moxalactam) were evaluated in a hamster model for antibiotic-associated colitis. Aztreonam, a novel monocyclic beta-lactam antibiotic specifically directed against aerobic Gram-negative bacteria with limited activity against Gram-positive and anaerobic bacteria did not cause haemorrhagic caecitis and death in hamsters when administered intraperitioneally or orally. Quantitative caecal cultures showed no changes in the anaerobic caecal microflora of hamsters treated intraperitoneally with aztreonam and only a temporary decrease in anaerobic Gram-negative bacilli in hamsters treated orally. Clostridium difficile and its cytotoxin were not present in these animals. Parenteral administration of ceftazidime also did not affect the anaerobic caecal microflora or cause caecitis. However, when given orally, ceftazidime suppressed the anaerobic caecal microflora and a lethal C. difficile-induced caecitis developed. Latamoxef or cefoperazone given parenterally resulted in caecitis and death in five days with marked changes in the anaerobic caecal microflora and C. difficile present in the caecal contents of these animals. The lethal haemorrhagic caecitis observed in this study was indistinguishable from that seen in the clindamycin-induced colitis model in the hamster. The possible correlation of these findings to gastrointestinal disturbances as a complication of antibiotic therapy in humans is discussed.

Administration, Oral↗
PubMed1992

The in-vitro antibacterial activity of a combination of cefpirome or cefoperazone with vancomycin against enterococci and Staphylococcus aureus.

Cefpirome, cefoperazone and ceftazidime were tested for their in-vitro activity against Enterococcus faecalis and methicillin-resistant Staphylococcus aureus (MRSA) isolates. Cefpirome was the most active cephalosporin followed by cefoperazone. Ceftazidime had only very limited activity against these strains. In experiments with cefpirome/vancomycin and cefoperazone/vancomycin combinations, synergy was detected against most MRSA strains and some enterococci. Antagonism did not occur.

Cefoperazone↗
PubMed1993

An open trial of cefoperazone plus sulbactam for the treatment of fever in cancer patients.

Cancer patients received cefoperazone plus sulbactam for 673 febrile episodes presumed to be caused by infection. Overall, 415 (76%) of the 545 evaluable episodes responded. There were 213 responses (84%) amongst the 254 fevers of unknown origin and 202 responses (69%) amongst the 291 documented infections. Fifty-one (61%) of the 83 episodes pneumonia and 74 (64%) of the 115 episodes of bacteraemia responded. Only 39 (58%) of the 67 infections caused by Gram-positive bacteria responded compared with 55 (86%) of 64 Gram-negative infections which included seven of eight caused by Pseudomonas aeruginosa. Eighteen (67%) of 27 polymicrobial infections responded to the regimen. Response rates were significantly lower amongst the 125 patients whose neutrophil counts decreased during therapy than amongst the 158 patients whose neutrophil counts increased. Adverse events which were possibly or probably related to antibiotic therapy were observed during 73 of the episodes; the most commonly reported side-effects were diarrhoea and skin rash. Six patients developed a coagulopathy without haemorrhage and two experienced anaphylactic reactions. In this open trial cefoperazone plus sulbactam proved to be an effective regimen for initial therapy of fever in cancer patients. It should be combined with a glycopeptide in those institutions where infections caused by methicillin-resistant staphylococci are frequently encountered.

Adolescent↗
PubMed1985

Coagulopathy and hemorrhage associated with cefoperazone therapy in a patient with renal failure.

We have reported life-threatening gastrointestinal hemorrhage with hypoprothrombinemia in a patient treated with cefoperazone for a urinary tract infection. The coagulation abnormality was rapidly corrected with administration of vitamin K and discontinuation of the antibiotic. This complication of cefoperazone therapy is not widely recognized and may be seen more frequently with increased use of the drug.

Aged↗
PubMed1988

Chemical stabilities of cefoperazone sodium and ceftazidime in 5% dextrose and 0.9% sodium chloride injections.

The chemical stabilities of cefoperazone and ceftazidime solutions in 5% dextrose and 0.9% sodium chloride injections have been studied using high-performance liquid chromatography methods. The solutions of cefoperazone were stable for 8 days (loss in potency of less than 10%) at 25 degrees C, for at least 80 days at 5 degrees C and for at least 96 days at -10 degrees C. The ceftazidime solutions were stable for only 2 days at 25 degrees C, for 21 days at 5 degrees C (28 days in normal saline) and for 90 days at -10 degrees C. Thawing the frozen solutions using a microwave oven did not cause degradation.

Cefoperazone↗
PubMed1988

Cefoperazone in the treatment of peritonitis in continuous ambulatory peritoneal dialysis patients.

Cefoperazone is a third-generation cephalosporin that is active against a broad spectrum of gram-positive and gram-negative bacteria. We added this antibiotic to peritoneal dialysis solution at a concentration of 62.5 mg/L to treat peritonitis in six continuous ambulatory peritoneal dialysis (CAPD) patients. Serum drug concentrations were obtained at 0, 0.5, 1, 2, 4, and 24 h after instituting antibiotic therapy. Rapid uptake by blood of the antibiotic across the peritoneal membrane occurred when the latter was inflamed. Adequate bactericidal serum levels for many bacteria were obtained in less than 4 h. Cefoperazone effectively eradicated peritonitis in all patients.

Cefoperazone↗
PubMed1980

In vitro evaluation of cefoperazone.

The activity of cefoperazone, a new broad-spectrum cephalosporin, was tested in vitro against 670 clinical isolates of gram-negative bacilli and gram-positive cocci. With the exception of Enterobacter spp., it inhibited the majority of all organisms tested at a concentration of 6.25 microgram/ml. Of particular interest is its good activity against Pseudomonas aeruginosa isolates which are usually very resistant to cephalosporins. When compared with other antibiotics, it was more active than any available cephalosporin against the Enterobacteriaceae, and its activity was comparable to the investigational drugs tested. Except against Pseudomonas, cefoperazone was less active than moxalactam (LY127935). No significant decrease in activity was noted in medium and pH variation studies. A considerable decrease in activity resulted when the size of the inoculum was incrased from 10(5) to 10(7) cells/ml. The minimal bactericidal concentrations were within one or two dilution values of the minimal inhibitory concentrations against the majority of isolates tested, except Staphylococcus aureus.

Bacteria↗
PubMed1980

Comparison of cefoperazone, cefotaxime, and moxalactam (LY127935) against aerobic gram-negative bacilli.

This study compares the minimum inhibitory concentrations of cefoperazone, cefotaxime, and moxalactam (LY127935) for 446 aerobic gram-negative bacillary isolates and further compares the minimum inhibitory concentrations of LY127935 and these third-generation cephalosporins with those of thienamycin for Pseudomonas aeruginosa. Each antibiotic at low concentrations inhibited nearly all Enterobacteriaceae tested. Minimum inhibitory concentrations for P. aeruginosa were higher, but for a majority of strains they fell below achievable serum levels. Thienamycin and cefoperazone showed significantly greater antipseudomonal activity than did cefotaxime or LY127935. Cefoxitin-inducible resistance to LY127935 and the two cephalosporins was demonstrated among Enterobacter species but did not occur with thienamycin.

Aerobiosis↗
PubMed1980

Comparative in vitro activity of moxalactam, cefotaxime, cefoperazone, piperacillin, and aminoglycosides against gram-negative bacilli.

The in vitro activities of four new beta-lactam antimicrobial agents (moxalactam, cefotaxime, cefoperazone, and piperacillin) and the aminoglycosides against 744 recent clinical isolates of facultative gram-negative bacilli were compared simultaneously by the agar dilution method. The major in vitro difference of these newer beta-lactam compounds appeared to be their antipseudomonal activity; cefoperazone was the most active, whereas cefotaxime had the least potency. The aminoglycosides, however, had the most effective in vitro activity on a weight basis against Pseudomonas aeruginosa.

Aminoglycosides↗
PubMed1980

Cefoperazone concentrations in bile and gall bladder wall after intravenous administration.

Cefoperazone concentrations in the common duct bile, gall bladder bile, and gall bladder wall were determined in four patients with cholelithiasis and one patient with carcinoma of the head of the pancreas, all of whom had normal renal functions. Within 65 min after a 1-g intravenous administration, maximum concentrations ranged from 373.4 to 3,100 micrograms/ml in common duct bile and from 6.8 to 680 micrograms/ml in gall bladder bile. Cefoperazone concentrations per gram of the gall bladder wall ranged from 16.8 to 48.0 micrograms.

Adult↗
PubMed1981

Comparative synergistic activity of cefoperazone, cefotaxime, moxalactam, and carbenicillin, combined with tobramycin, against Pseudomonas aeruginosa.

A broth dilution checkerboard synergy assay was used to assess the activity of cefoperazone, cefotaxime, moxalactam, and carbenicillin, in combination with tobramycin, against 38 strains of Pseudomonas aeruginosa. Synergy occurred significantly more often (P less than 0.001) when tobramycin was combined with cefotaxime (63%) than when it was combined with carbenicillin (26%), cefoperazone (21%), or moxalactam (18%). Of the 25 synergistically inhibited strains, the combination cefotaxime-tobramycin was synergistic against 24 and was the only synergistic combination against 10. Of six strains initially resistant to cefotaxime, five were susceptible to this agent (minimum inhibitory concentration, less than or equal to 32 micrograms/ml) when it was combined with tobramycin. Clinical trials are needed to determine the therapeutic efficacy of cefotaxime-aminoglycoside combinations in the treatment of serious Pseudomonas infections.

Anti-Bacterial Agents↗
PubMed1981

Pharmacokinetics of cefoperazone in patients with neoplastic disease.

The pharmacokinetics of cefoperazone, a new semisynthetic cephalosporin, were studied in 34 patients with neoplastic disease. This compound was administered in a variety of doses and schedules without observable toxicity in any patient. The mean peak serum concentration after a 15-min intravenous infusion of 2 g was 264 microgram/ml after the first dose; the serum half-life was 2.1 h. There was no significant change in half-life or serum concentrations after 4 or 7 days of therapy. The mean peak serum concentration after infusion of 1 g over 15 min was 133 microgram/ml, with a mean of 10.7 microgram/ml at 6 h. The serum half-life was 2 h. The mean peak serum concentration after infusion of 1 g over 0.5 h was 101 microgram/ml. When 8 g was subsequently administered daily by a continuous infusion schedule, levels were maintained at 80 microgram/ml. When the dose was increased to 16 g daily, serum concentrations were maintained at an average of 153 microgram/ml. Only 37% of cefoperazone was recovered in the urine in a 12-h period after the initial dose, suggesting the importance of other mechanisms of excretion; however, serum concentrations in one patient with renal insufficiency were significantly higher than serum concentrations in patients with normal renal function.

Adolescent↗
PubMed1981

Comparative in vitro activity of ceftizoxime, cefoperazone, and cefoxitin against anaerobic bacteria.

Against 482 obligate anaerobes studied by the agar dilution technique, ceftizoxime was significantly more active than both cefoxitin and cefoperazone (P less than 0.001); the latter two agents were comparable in activity. The enhanced activity of ceftizoxime, as compared with the activity of cefoxitin, was against both gram-positive and gram-negative anaerobes (especially Lactobacillus and bacteroides spp). Cefoperazone, however, was more active than cefoxitin against gram-positive anaerobes (particularly Lactobacillus spp.) but was less active than cefoxitin against gram-negative anaerobes (particularly Bacteroides fragilis and Veillonella spp.).

Anaerobiosis↗
PubMed1982

Aminoglycoside-resistant gram-negative bacilli in a community hospital: comparative in vitro activity of cefotaxime, moxalactam, cefoperazone, and piperacillin.

All aminoglycoside-resistant gram-negative bacilli isolated during 1 year at a community hospital were tested for in vitro sensitivity to cefotaxime, moxalactam, cefoperazone, and piperacillin. The majority of Enterobacteriaceae were susceptible to all four antibiotics. Cefoperazone and piperacillin were the most active for pseudomonas aeruginosa, and activity for other nonfermentative gram-negative bacilli was variable.

Aminoglycosides↗
PubMed1982

Impact of cefoperazone therapy on fecal flora.

To evaluate the effects of parenteral cefoperazone therapy upon human fecal flora, fecal specimens obtained from four patients before and during therapy (as well as after therapy for one patient) were cultured quantitatively for facultative, aerobic, and anaerobic bacteria and for fungi. Cefoperazone therapy was associated with major changes in fecal flora. There was suppression to undetectable levels or an appreciable reduction in all anaerobic bacteria as well as suppression of all initially detected Enterobacteriaceae. During therapy, there was acquisition or an increase in counts of Candida spp., so that these became the most numerous fecal microorganisms in all patients. In addition, Pseudomonas spp. and coagulase-negative Staphylococcus sp. were acquired by three patients. These marked alterations in flora have potentially important consequences.

Adult↗
PubMed1985

Penetration and clearance of cefoperazone and moxalactam in pleural fluid.

The penetration of cefoperazone and moxalactam into pleural fluid was studied in 11 patients after intravenous infusion of 2-g doses of these agents. Clearance of these agents from pleural fluid was studied in seven patients after instillation of 1-g doses into the pleural space. The concentrations in pleural fluid after intravenous infusion of 2-g doses reached a peak of 7 to 25 micrograms/ml for cefoperazone and 9 to 35 micrograms/ml for moxalactam at 4 to 6 h after administration. These levels exceeded reported MICs for most susceptible organisms. The elimination half-life of both agents was about two to five times longer in pleural fluid than in serum. These prolonged elimination rates of both agents might be of great advantage for killing bacteria in the pleural space.

Aged↗
PubMed1986

Pharmacokinetics of cefotaxime, moxalactam, and cefoperazone in the early puerperium.

Twelve parturient women volunteered to receive 1 g of cefotaxime on the second or third day postpartum by intravenous infusion over 3 min. Blood was taken from the antecubital vein of the contralateral arm at 0.25, 0.5, 0.75, 1, 2, 4, and 6 h. The concentration of cefotaxime in serum was assayed by agar diffusion, with Sarcina lutea ATCC 9341 as the indicator strain. The same 12 women received an identical dose of antibiotic 4 months after the first dose, and blood was taken at the same time intervals as in the first study to measure antibiotic levels. An additional 24 women participated in identical studies with either moxalactam or cefoperazone. Cefoperazone afforded the highest concentration in serum of the three drugs, followed by moxalactam. These differences in the concentration in serum were seen both early postpartum and 4 months later. However, the concentration in serum of all three drugs was diminished 2 and 3 days postpartum compared with 4 months postpartum. Most pharmacokinetic parameters were also significantly altered early in the puerperium relative to those obtained 4 months later. The altered pharmacokinetic behavior of antibiotics associated with pregnancy appears to persist into the early puerperium.

Adult↗