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PubMed1995

Synergistic enhancement of in vitro antimicrobial activity of imipenem and cefazolin, cephalothin, cefotiam, cefamandole or cefoperazone in combination against methicillin-sensitive and -resistant Staphylococcus aureus.

Synergistic enhancement of the in vitro antimicrobial activity of imipenem combined with cephalosporins against methicillin-resistant Staphylococcus aureus (MRSA) has been reported. In order to investigate which cephalosporin is more effective in enhancing the activity of imipenem against MRSA, the in vitro antimicrobial activities of imipenem, cefazolin, cephalothin, cefotiam, cefamandole and cefoperazone, alone and in combination, against methicillin-sensitive Staphylococcus aureus (MSSA) and MRSA were assessed. Using the checkerboard Mueller-Hinton agar dilution method, strong synergy was found in 97% to 100% of MRSA strains for imipenem and all tested cephalosporins except cefoperazone; fractional inhibitory concentration (FIC) indices were < or = 0.5. Among the cephalosporins studied, cefamandole most markedly increased the activity of imipenem against MRSA, followed, in order of decreasing effect, by cefotiam, cephalothin, cefazolin, and cefoperazone. The synergistic effect of imipenem combined with cefamandole or cefotiam was confirmed using the broth dilution method with 2% of NaCl.

Cefamandole↗

PubMedDate not supplied

[A trial of using Cefobid (cefoperazone) in treating infections of the skin and soft tissues].

A clinical laboratory investigation of cefoperazon in the treatment of 27 patients with burn traumata and purulent necrotic wounds of the soft tissues of various genesis and localization was carried out. The clinical efficacy of the treatment was 75-86.6 per cent. 4 patients with extended purulent wounds of the soft tissues and bone affections were treated with cefoperazon and local application of gentacicol (a dosage form of gentamicin based on collagen with prolonged action) which provided the clinical effect in all the cases. 226 isolates from the wounds, urine, blood, sputum, pleural fluid and other substrates were tested and a rather high activity of cefoperazon against many strains of gram-positive and gram-negative organisms including Staphylococcus spp., Pseudomonas aeruginosa, Escherichia coli, Providencia sp. and Proteus spp. was revealed. The tolerance of the drug in all the cases was good.

Adolescent↗

PubMed1979

[Pharmacokinetics of a new cephalosporin, cefoperazone].

Cefoperazone is a semi-synthetic cephalosporin for parenteral use with an extended antibacterial spectrum covering Pseudomonas aeruginosa, Enterobacter cloacae and Serratia marcescens. Its pharmacokinetic properties were studied in 8 healthy subjects after 2 intravenous infusions of 2 g of the drug at a 12-hour interval. The mean peak serum concentrations were 134 +/- 16 microgram/ml and 143 microgram/ml. Cefoperazone was shown to possess a long half-life for a cephalosporin (1.7 hours). In our concentration range the drug is 90% protein bound. The apparent volume of distribution was a mean 11.4 liters and the renal clearance 18 ml/min. The cumulative urinary excretion was small, viz. 23% in 12 hours, indicating that there should be no need to modify the dosage regimen in renal failure. Comparison of in vitro studies with the pharmacokinetic properties show that 2 g cefoperazone given intravenously twice a day should inhibit most sensitive bacteria.

Bacteria↗

PubMed1984

Pharmacokinetics of cefoperazone in patients undergoing chronic ambulatory peritoneal dialysis: clinical and pathophysiological implications.

The pharmacokinetics of cefoperazone after i.p. and/or i.v. administration were studied in 12 CAPD patients. After i.v. injection, the plasma half-life was 2.65 +/- 0.4 h, the total clearance amounting to 70.1 +/- 19.2 ml/min. Peritoneal clearance was calculated to be 6.9 +/- 1 ml/min. After peritoneal instillation, the bioavailability was 63.9 +/- 5%. After repeated i.p. administration, no accumulation of the drug in the body was observed. Thus, cefoperazone can be safely administered for the treatment of peritonitis in CAPD patients.

Cefoperazone↗

PubMed1982

Antibacterial activity of N-formimidoyl thienamycin in comparison with cefotaxime, lamoxactam, cefoperazone, piperacillin gentamicin.

The in vitro activity of N-formimidoyl thienamycin (MK 0787), a new stable derivative of thienamycin was compared with that of lamoxactam, cefotaxime, cefoperazone, piperacillin and gentamicin against 410 clinical isolates of common bacteria. In comparison with the other agents, MK 0787 was more or equally active against Staphylococcus aureus, Streptococcus faecalis, Escherichia coli, Citrobacter spp., Klebsiella spp., and Serratia spp. It inhibited all isolates at a concentration of 0.5 mg/l, but was less active than cefotaxime and lamoxactam against Proteus mirabilis and less active than cefotaxime, lamoxactam and cefoperazone against Beta-lactamase positive Haemophilus influenzae. Strains of Pseudomonas aeruginosa were more susceptible to N-formimidoyl thienamycin than to other antibiotics.

Anti-Bacterial Agents↗

PubMedDate not supplied

Lung tissue concentrations of cefoperazone.

The following lung tissue concentrations of cefoperazone were found in 20 patients after a 2 g single dose: 45.3-113.3 mg/kg after one hour and 20.5-68.1 mg/kg after two hours. The respective serum levels were measured in parallel determinations for comparison purposes. All determinations were carried out by means of high pressure liquid chromatography. The results suggest that cefoperazone has a rapid and sustained concentration ability in the lung tissue. The drug is therefore suitable for perioperative prophylaxis in lung surgery.

Cefoperazone↗

PubMed1991

Comparison of two schedules of cefoperazone plus aztreonam in the treatment of neutropenic patients with fever.

Cancer patients were randomized to receive an every 4 hour or every 8 hour schedule of cefoperazone plus aztreonam during 617 febrile episodes. The overall response rate for the 478 evaluable episodes was 76% and there was no difference in response rate between the two schedules. The response rate was 79% for cases of pneumonia and 63% for cases of bacteremia. Only 50% of the microbiologically documented infections caused by gram-positive organisms responded whereas 95% of gram-negative infections, including all of those caused by Pseudomonas aeruginosa, responded. Response rates were lower among patients whose neutrophil counts decreased during therapy than among those whose neutrophil counts increased (64% vs. 85%, p = 0.008). Side-effects that were possibly or probably related to antibiotic therapy were observed during 11% of the episodes. The most common side-effects were diarrhea and rashes including one case of Stevens-Johnson syndrome. Three patients developed a coagulopathy during therapy. Cefoperazone plus aztreonam proved to be an effective combination for treatment of gram-negative infections and fever of unknown origin in cancer patients and an every 8-hour schedule of administration was as effective as an every 4-hour schedule. Approximately half of the patients with gram-positive infections required additional antibiotics for successful therapy.

Aztreonam↗

PubMed1988

Cefoperazone in the treatment of infections in cancer patients.

Cefoperazone appears to be one of the cephalosporins with the most promise in granulocytopenic patients, regardless of whether it is used in combination or as monotherapy. It has the broad spectrum of antimicrobial activity necessary to inhibit the organisms commonly encountered in patients with cancer, as well as the ability to achieve high serum levels for sustained periods of time. Administration of cefoperazone should provide effective therapy in the overall management of most infections encountered in patients with neoplastic diseases.

Bacterial Infections↗

PubMed1982

Cefoperazone concentrations in human aqueous humor after intravenous administration.

Twenty-four patients about to undergo elective cataract surgery received either a 2-g (ten patients) or a 4-g (14 patients) intravenous infusion of cefoperazone one to six hours before surgery. The 4-g dose produced a mean peak aqueous humor concentration of 2.93 micrograms/ml at one hour; the mean concentration remained higher than 2 micrograms/ml for at least four hours. These levels, however, were never more than 90% of the minimum inhibitory concentration of cefoperazone for common bacterial ocular pathogens.

Aqueous Humor↗

PubMed1982

Antibiotic management of surgically treated gangrenous or perforated appendicitis. Comparison of gentamicin and clindamycin versus cefamandole versus cefoperazone.

A study of 130 adult patients with surgically treated gangrenous or perforated appendicitis was undertaken to evaluate the efficacy of three antibiotic regimens. Forty-eight patients received cefamandole, 40 were given the combination of clindamycin and gentamicin, and 42 were treated with cefoperazone. Side effects from these antibiotics were infrequent and mild. When all cases were compared for infectious failure, clindamycin-gentamicin showed a clear advantage over cefamandole. Because of the heterogeneity of the total study population, patients with perforation and peritonitis were compared separately. This analysis confirmed the advantage of clindamycin-gentamicin over cefamandole. In addition, it appears that clindamycin-gentamicin is more efficacious than cefoperazone.

Adolescent↗

PubMed1995

NMR study of whole rat bile: the biliary excretion of cefoperazone and benzyl chloride by an isolated perfused rat liver.

1H NMR spectroscopy at 400 MHz has been applied to the analysis of whole bile samples produced by the isolated perfused rat liver. Using relatively simple NMR experiments biliary excretory products of cefoperazone and benzyl chloride were identified as cefoperazone itself and a benzyl-glutathione conjugate, respectively. Our use of 13C isotopic labelling demonstrates how 1H/13C heteronuclear NMR techniques can be used to produce uncrowded and informative spectra from whole bile. From the use of a HMQC-COSY experiment the structure of a benzyl-glutathione conjugate contained in whole bile was confirmed.

Animals↗

PubMed1987

Effect of beta-lactamase inhibitors on the antimicrobial activity of cefoperazone, cefotaxime, and ceftizoxime against aerobic and anaerobic beta-lactamase producing bacteria.

Clavulanic acid (2.0 micrograms/ml) lowered the minimal inhibitory concentrations (MICs) of ceftizoxime and cefotaxime against 49 strains of the Bacteroides fragilis group by a mean of 4.0 and 3.4 log2 concentrations, respectively. Sulbactam plus ceftizoxime gave almost identical results. Sulbactam lowered cefoperazone MICs by a mean of 2 log2 concentrations. Against 52 aerobic and facultative isolates producing a variety of beta-lactamase types, the use of beta-lactamase inhibitors (sulbactam) was most effective in reducing the MICs of cefoperazone.

Bacteria, Aerobic↗

PubMed1984

Changing patterns of resistance to new beta-lactam antibiotics. In vitro efficacy of cefoperazone against bacterial pathogens.

No evidence for significant increase in resistance to cefoperazone was detected in susceptibility test surveillance programs or in the literature through 1983, but rare endemic resistance to cefoperazone and some other newer beta-lactams was found. Medical centers contemplating the use of a third-generation drug for cost-containment should be aware of the susceptibility of isolates in their hospitals, and the drug's ability to withstand beta-lactamase hydrolysis by local pathogens. The possible dangers of inducible cephalosporins in certain Enterobacteriaceae and strains of Pseudomonas aeruginosa are discussed in the light of the physical and chemical characteristics of the newer antimicrobial agents. Criteria for judging the values of investigational beta-lactams are presented. These focus on the interaction of antimicrobial agents with host defense mechanisms and circulating blood elements.

Anti-Bacterial Agents↗

PubMed1988

Placental transfer of cefoperazone and sulbactam in the isolated in vitro perfused human placenta.

The transfer of cefoperazone and sulbactam across the human placenta was studied qualitatively and quantitatively with the isolated in vitro bidirectionally perfused human placental lobule. Clearance indexes for both cefoperazone and sulbactam were derived. The absence of active transport and facilitated diffusion were documented, implying simple diffusion as the mechanism of placental transfer for both drugs. Placental tissue levels were also studied.

Biological Transport↗

PubMed1992

Peritoneal absorption of cefoperazone in rats.

The peritoneal absorption of cefoperazone, administered by intraperitoneal (ip) perfusion in a large volume (100 mg/40 ml), was investigated in rats. Its pharmacokinetics was also studied after ip or intravenous (iv) injection of 100 mg/kg in two groups of rats. The peritoneal uptake after the two modes of ip administration was rapid, peaking in less than 20 minutes and the means of peak concentrations were similar. The peak remained high in the group perfused with a large volume for at least 4 hours, which was the end of sample collection. In addition, the absorption half-life and the fraction (F) reaching systemic circulation were calculated and found to be 10.0 +/- 2.5 min and 0.93, respectively. A brief distribution phase (t1/2 alpha 8.0 +/- 0.67 minutes) appeared only after the iv bolus. Otherwise the decline in serum concentration was monoexponential with half-lives of 39.0 +/- 4.0 and 63.6 +/- 7.5 min for the iv and ip injected groups, respectively. The stability of cefoperazone in plasma was also investigated in this study. It was found to be unstable at physiological pH even at -30 degrees C and the samples collected should be buffered in acidic media to optimize stability. The degradation process is likely to contribute to its elimination kinetics during in vivo administration.

Absorption↗

PubMedDate not supplied

Differences among moxalactam, cefoperazone, and cefotaxime in activity against multiple-antibiotic-resistant gram-negative bacteria.

In vitro evaluations have shown that moxalactam, cefoperazone, and cefotaxime, three new beta-lactam antibiotics, have certain potency and antibacterial spectral characteristics in common. Results of parallel tests of these antibiotics against routine clinical isolates have suggested that these compounds could be tested with one disk that is representative of this spectral class. The key requirement for this class concept in disk testing is that there be no bacterial resistance mechanism that can operate against one, but not all, members of the proposed class. The results of an 11-center study of approximately 500 isolates of multiple-antibiotic-resistant Enterobacteriaceae responsible for nosocomial infections illustrated that cross-resistance to moxalactam, cefoperazone, and cefotaxime is highly variable from center to center. Thus, the spectral class concept of disk susceptibility testing would be inappropriate for this group of drugs.

Bacteria↗

PubMed1983

Effect of cefoperazone on faecal flora.

The effect of cefoperazone on the intestinal flora was investigated in 29 patients receiving the drug for 7 to 14 days. Faecal specimens were cultured quantitatively for aerobic and anaerobic micro-organisms before, during and after therapy. The cefoperazone treatment was associated with major changes in the faecal flora. There was marked suppression of enterobacteria, staphylococci, streptococci, anaerobic cocci, bacteroides, fusobacteria, bifidobacteria, eubacteria and lactobacilli. The number of enterococci increased in most patients and the number of clostridia remained constant. Eight patients had cultures positive for Clostridium difficile during or after treatment. The marked changes in the intestinal flora can have important clinical consequences.

Adolescent↗

PubMed1984

The serum bactericidal activity of latamoxef (moxalactam), cefoperazone and cefotaxime.

We determined the serum bactericidal activity 1 h after the end of 2 g, 30 min infusions of latamoxef, cefoperazone and cefotaxime in six volunteers against six strains each of Escherichia coli, Klebsiella pneumoniae, Staphylococcus aureus and Pseudomonas aeruginosa. All produced excellent serum bactericidal activity against E. coli. Latamoxef and cefotaxime were superior for K. pneumoniae. Cefoperazone produced the highest titres against Staph. aureus. None of these agents produced sufficient bactericidal activity against Ps. aeruginosa to be useful in initial single agent therapy for the septic, granulocytopenic cancer patient.

Adolescent↗