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PubMed1984

Serum bactericidal activity of aztreonam, cefoperazone, and amikacin, alone or in combination, against Escherichia coli, Klebsiella pneumoniae, Serratia marcescens, and Pseudomonas aeruginosa.

Serum samples from volunteers receiving (per kilogram) 20 mg of aztreonam, 20 mg of cefoperazone, 7.5 mg of amikacin, 20 mg of cefoperazone plus 20 mg of aztreonam, or 20 mg of aztreonam plus 7.5 mg of amikacin were evaluated for bactericidal activity against Escherichia coli, Klebsiella pneumonia, Serratia marcescens, and Pseudomonas aeruginosa. Serum bactericidal activities were similar for aztreonam alone or in combination but were lower for amikacin and cefoperazone alone, especially against S. marcescens and P. aeruginosa. Killing studies, performed with serum samples diluted 1:8, demonstrated a high killing rate for aztreonam plus amikacin, especially against P. aeruginosa.

Amikacin↗

PubMed1985

Assessment of serum bactericidal activity after administration of cefoperazone, cefotaxime, ceftizoxime, and moxalactam to healthy subjects.

Bactericidal activity in serum produced after administration of 1-g intravenous doses of cefoperazone, cefotaxime, ceftizoxime, and moxalactam was ascertained in six healthy subjects. The assay organisms were a strain of Staphylococcus aureus which was moderately susceptible to the drugs (MBC, 2 to 8 micrograms/ml) and an isolate of Escherichia coli which was highly susceptible (MBC, 0.08 to 0.3 microgram/ml). Drug concentrations and bactericidal titers were measured from samples taken for up to 12 h after the dose. No bactericidal activity against the S. aureus strain was found at 4 to 6 h and beyond for any of the drugs. Ranking of the in vivo bactericidal activity of the drugs was cefoperazone = cefotaxime greater than ceftizoxime = moxalactam. Against the E. coli isolate, bactericidal activity was present for 8 h for cefotaxime, and for 12 h for the other drugs. Ranking of the drugs in terms of extent and duration of in vivo bactericidal activity versus E. coli was moxalactam = ceftizoxime greater than cefoperazone greater than cefotaxime. After administration of 1-g doses of these new beta-lactams, bactericidal activity in serum was maintained for 12 h against highly susceptible bacteria. More frequent (6 to 8 h) or higher (greater than or equal to 2 g) dosing appears to be necessary to achieve prolonged serum bactericidal activity against less susceptible isolates (MBC, greater than or equal to 2 to 8 micrograms/ml).

Adult↗

PubMed1989

Influence of protein binding on therapeutic efficacy of cefoperazone.

The effect of protein binding of cefoperazone (89.3% bound to rabbit serum) on antibacterial activity in serum was tested in a model that simulated a closed-space infection in a neutropenic host. Four gram-negative bacilli were tested in the model with cefoperazone doses of 20 and 200 mg/kg administered intramuscularly every 6 h for 16 doses. Cefoperazone efficacy was measured at 92 h by determining the log10 decrease in bacterial count from that of the control for five paired studies with three isolates. A significantly better response was demonstrated when the free (non-protein-bound) drug concentration exceeded the MICs and MBCs for the infecting microorganisms at the infection site at all times (P less than 0.005). This supports the concept that free (unbound) drug is the active component in treating bacterial infections.

Animals↗

PubMed1992

Pharmacokinetic disposition and bactericidal activities of cefepime, ceftazidime, and cefoperazone in serum and blister fluid.

Cefepime is a new broad-spectrum cephalosporin with excellent gram-positive and gram-negative activity including activity against Staphylococcus aureus, Pseudomonas aeruginosa, and Enterobacter cloacae. The pharmacokinetic disposition of cefepime is similar to that of ceftazidime. We compared the pharmacokinetic characteristics and the extent and duration of bactericidal activity in serum and suction-induced blister fluid after single 2-g intravenous doses of cefepime, ceftazidime, and cefoperazone given to healthy subjects. One clinical isolate each of E. cloacae, P. aeruginosa, and S. aureus was used to assess bactericidal activity. Results of the pharmacokinetic analysis were similar to previously reported data for these drugs. The high serum protein binding of cefoperazone (approximately 90%) contributed to poor blister fluid penetration. The other drugs penetrated well into this fluid compartment. Cefepime showed significantly greater bactericidal activity in serum and blister fluid against E. cloacae than the other study drugs, ceftazidime was significantly better in serum and blister fluid against P. aeruginosa, and cefoperazone was significantly better against S. aureus only in serum. None of the study drugs had significant bactericidal activity in blister fluid against S. aureus. Cefepime is a promising antimicrobial agent for the treatment of infections due to E. cloacae.

Adult↗

PubMed1986

Pharmacokinetics of cefoperazone in the cow by the intramammary route and its effect on mastitis pathogens in vitro.

The pharmacokinetic and microbiological properties of a new third generation cephalosporin, cefoperazone, when given by the intramammary route to the cow are described. Cefoperazone is excreted from the udder over a three- to five-day period following a single infusion of 250 mg in an oil base into each of all four quarters. By the fifth milking after treatment the mean bucket (composite) concentration of cefoperazone was below 0.01 microgram/ml. The minimal inhibitory concentrations for 470 pathogens isolated from cases of mastitis were determined. A few exotic species were resistant but all the usual isolates were sensitive. No signs of transferable drug resistance from known multiple drug-resistant strains were detected.

Animals↗

PubMed1985

Cefoperazone therapy of complicated urinary tract infections: pharmacokinetics in renal transplant recipients.

Cefoperazone was used to treat patients with complicated urinary tract infections due to multiple antibiotic-resistant gram-negative rods who had failed prior courses of intravenous antibiotic therapy. Cure was achieved in 44% (4/9) of cases; 44% of patients improved but relapsed and 11% (1/9) of patients were reinfected. Relapse and reinfection were associated with Pseudomonas aeruginosa and/or with conditions not normally responsive to medical therapy alone including prostatitis, reflux and chronic indwelling Foley catheters. The pharmacokinetics of cefoperazone were studied in renal transplant recipients. Peak serum concentrations (range 146-241 micrograms/ml) and 2-hour noncumulative urine concentrations (range 161-291 micrograms/ml) exceeded the minimal inhibitory concentrations of the bacteria in all cases. There was no accumulation of cefoperazone despite the presence of impaired renal function.

Adult↗

PubMed1981

Cefoperazone: spectrum of antibacterial activity and disc diffusion testing.

Cefoperazone is a new cephalosporin with a very wide spectrum of antibacterial activity, including Enterobacteriaceae, Pseudomonas aeruginosa, staphylococci, streptococci (other than serological group D strains), Neisseria and Haemophilus species (including beta-lactamase positive strains) and some anaerobes. On testing more than 8700 clinical isolates, approximately 93% were inhibited by 16 micrograms/ml of cefoperazone, 95% by 32 micrograms/ml and 98% by 64 micrograms/ml. The drug is less active on Acinetobacter and group D streptococci. We recommend that a disc containing 75 micrograms of cefoperazone be used in the diffusion test with 'breakpoints' of less than or equal to 14 mm for resistant, 15-17 mm for intermediate, and greater than or equal to 18 mm for susceptible bacteria.

Bacteria↗

PubMed1981

Cefoperazone in Klebsiella meningitis: a case report.

A 51-year-old man with meningitis due to Klebsiella pneumoniae was treated with cefoperazone 6 to 8 g/day intravenously and was cured. Simultaneous blood and cerebrospinal fluid levels were measured. Trough levels of cefoperazone in cerebrospinal fluid were 9 and 12 mg/L. Cefoperazone should be considered for meningitis due to susceptible organisms resistant to customarily used antibacterial drugs.

Cefoperazone↗

PubMed1981

A clinical trial with cefoperazone in pneumonia and pyelonephritis.

15 cases of pneumonia and 15 cases of pyelonephritis were included in a clinical trial of parenteral cefoperazone. The organisms isolated from patients with bacterial pneumonia were: Staphylococcus aureus (6), Klebsiella pneumoniae (5), Diplococcus pneumoniae (3), Pseudomonas species (2), and 6 others. Amongst those with pyelonephritis, Escherichia coli (12), Enterobacter (1), and 3 other pathogens, were isolated. All were sensitive to cefoperazone. The efficacy of cefoperazone in patients with pneumonia was: good in 11 (73%), fair in 3, and poor in 1. In pyelonephritis, 12 (80%) responded well and in the other 3 response was fair. There were no significant side effects or hypersensitivity reactions.

Adult↗

PubMed1981

Cefoperazone in lower respiratory tract infections.

17 hospitalised patients with a wide variety of common lower respiratory tract infections received at least 6 days of intravenous bolus cefoperazone 1.0g 12-hourly. Disease was caused by Haemophilus influenzae, Streptococcus pneumoniae, Staphylococcus aureus, and mixed anaerobes in 1 patient. All isolates were sensitive to cefoperazone. 11 patients were cured, 4 improved, and 2 failed (1 of whom had an anaerobic empyema). Toxicity and side effects were infrequent. In general cefoperazone was effective therapy for these infections.

Adult↗

PubMed1981

Cefoperazone: A review of its in vitro antimicrobial activity, pharmacological properties and therapeutic efficacy.

Cefoperazone is a new 'third generation' semisynthetic injectable cephalosporin. It has a broad spectrum of antibacterial activity which includes Pseudomonas aeruginosa (unlike older cephalosporins), along with the Enterobacteriaceae and other Gram-negative bacteria, Gram-positive bacteria and anaerobic bacteria. Unlike other cephalosporins, cefoperazone is excreted to a considerable extent by extrarenal mechanisms. Given by intravenous or intramuscular injection, cefoperazone is effective against a wide variety of infections caused by Gram-negative or Gram-positive aerobes, including infections of the biliary tract, and in many anaerobic infections. It is generally well tolerated, diarrhoea and skin rashes being the most frequently reported side effects.

Anti-Bacterial Agents↗

PubMed1999

Imipenem-cilastatin versus sulbactam-cefoperazone plus amikacin in the initial treatment of febrile neutropenic cancer patients.

The treatment of infectious complications in cancer patients has evolved as a consequence of the developments in the chemotherapy of cancer patients. In this prospective, randomized study, we compared imipenem-cilastatin and sulbactam-cefoperazone with amikacin in the empiric therapy of febrile neutropenic (< 1000/mm3) patients with liquids and solid tumours. Of 30 evaluable episodes, 15 were treated with imipenem-cilastatin and 15 were treated with sulbactam-cefoperazone plus amikacin. 73% of episodes were culture-positive: gram-positive pathogens accounted for 62% of the isolates. Bacteremia was the most frequent site of infection. The initial clinical response rate for both regimens was 60% (p > 0.05). No major adverse effects occurred. This study demonstrated that imipenem-cilastatin monotherapy and combination therapy of sulbactam-cefoperazone plus amikacin were equally effective empiric therapy for febrile granulocytopenic cancer patients.

Adolescent↗

PubMed2001

[Characterization of cefoperazone resistance gene on plasmid pFC in E. coli HX88108].

OBJECTIVE: To investigate the characterization of cefoperazone resistance gene (CPZr) on plasmid pFC in E. coli HX88108 and inquire into the mechanism of resistance to CPZ at the molecular level. METHODS: E. coli HX88108 strain which demonstrated high-level resistance to cefoperazone (MIC, > 512 micrograms/ml) was isolated from a severely infected patient in 1988. Five plasmids coexisting in the strain were designated pFC, pFT1; pFT2, pFT3 and pFX, respectively. Four plasmids except pFX conferred CPZ resistance. Cefoperazone resistance gene (CPZr) has been cloned from plasmid pFC. beta-lactamase assays with Nitrocefin were performed. RESULTS: The expression product of CPZr was beta-lactamase. The high level beta-lactamase enzymatic activities against cephaloridine of CPZr transformants which were detected spectrophotometrically at 260 nm wave length demonstrated high level similarities to that of pFC. MICs of 18 antibiotics were determined according to a guideline of NCCLS by broth dilution method. CPZr transformants showed moderate level resistance to ampicillin, cefazolin, cefazolin, cefamandole and CPZ (MIC, 64 micrograms/ml). Meanwhile, susceptibility testing results demonstrated that the level of resistance to CPZ of pFC transformant in this study (MIC, 64 micrograms/ml) was much lower than that in 1988 (MIC, > 512 micrograms/ml) and resistance to nofloxacin and aminoglycosides was not observed. Induction experiment and temperature-sensitive mutation of CPZ resistance were performed. CPZr colonal strains revealed the higher-level of resistance to CPZ (MIC, 512 micrograms/ml) due to antibiotic CPZ induction rather than temperature sensitive mutation. CONCLUSION: This observation suggests that resistance to antibiotics encoded by plasmid might have been lower or lost under no antibiotic stress in a certain period, but higher under heavy stress.

Cefoperazone↗

PubMed1992

[Experience with using cefoperazone in cancer patients after bone marrow transplantation].

Cefoperazone is a semisynthetic cephalosporin of the 3rd generation (cefobid, Pfizer, USA). It was used in monotherapy of 12 oncological patients during ++post-cytostatic aplasia of the bone marrow and peripheral pancytopenia after bone marrow transplantation. The results were favourable in 67 per cent of the patients: the body temperature normalized and no signs of any infection were evident. In 25 per cent of the patients the monotherapy failed and it was necessary to combine cefoperazone with aminoglycosides. Therefore, cefoperazone proved to be an efficient antibacterial drug, whose use was possible in the monotherapy of oncological patients after transplantation of the bone marrow.

Adolescent↗

PubMed1992

[Cefoperazone in a multi-profile surgical clinic].

The results of the clinical trials of cefoperazone (cefobid, Pfizer, USA), a 3rd generation cephalosporin, carried out at the Research Centre of Surgery are presented. The antibiotic was used to treat and prevent postoperative infections in 44 patients. Good and satisfactory results were observed in 43 out of the 44 patients (99.9 per cent). Antimicrobial activity of cefoperazone against 182 bacterial strains isolated from the patients was assayed and compared with that of other cephalosporins i.e. cefotaxime, ceftriaxone and ceftazidime. The cefoperazone pharmacokinetics was studied in the patients with normal renal functions after surgical operations on the organs of the chest and abdominal cavity. The antibiotic was shown useful in the monotherapy of mixed infections involving anaerobic pathogens.

Adolescent↗

PubMedDate not supplied

[Does glycemic level influence the pharmacokinetics of an antibiotic (cefoperazone)?].

Hyperglycemia may modify pharmacokinetics of some antibiotics as shown in the literature. We studied the influence of glycaemic levels on pharmacokinetics properties of cefoperazone in 12 type 1 insulin dependent diabetic patients. Hyperglycaemia was obtained by a reduction of one quarter of their usual insulin dosage and normoglycaemia by an artificial pancreas (Biostator GCIIS). Cefoperazone had a high protein affinity and a high biliary elimination. Pharmacokinetic study was performed during a 8 hour period following one gram intravenous bolus. We did not found any influence of glycaemic level (normoglycaemia or hyperglycaemia) on the pharmacokinetic parameters of cefoperazone.

Blood Glucose↗

PubMed1990

Comparative susceptibility studies of clinically isolated Pseudomonas aeruginosa, Escherichia coli and Klebsiella spp to cefoperazone and cefotaxime.

The in-vitro activity of cefotaxime and cefoperazone were compared using clinically isolated Escherichia coli, Klebsiella spp and Pseudomonas aeruginosa. Cefotaxime was found on a weight to weight basis, to be much more active than cefoperazone. All the three species studied show the presence of cefoperazone-resistant population which were sensitive to cefotaxime. The possible mechanisms of resistance to these antibiotics were discussed.

Cefoperazone↗

PubMed1987

[Prophylactic antibiotherapy in biliary surgery, cefazolin versus cefoperazone. Randomized comparative open study in a population at risk for infection].

Sixty patients having to undergo a biliary operation with high risk of infection (Keighley's criterions) received at random either cefazolin (CFZ) or cefoperazone (CFP) as a prophylactic antibiotherapy. Postoperative courses were fairly normal: a peak of temperature on day 5 for one case and a digestive bleeding due to hypoprothrombinemia for another case. No further complication occurred. Patient discharge was two days shorter with cefoperazone and biliary positive cultures were in favour of cefoperazone (21% with CFZ, 11% with CFP) but without statistically significant level. Consequently, this trial should be carried out on a larger scale.

Adolescent↗