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PubMed2000

Simultaneous determination of unbound cefoperazone in rat blood and brain using microdialysis.

A sensitive microbore HPLC method was developed for the simultaneous determination of unbound cefoperazone in rat blood and brain using microdialysis. Two microdialysis probes were inserted into the jugular vein/right atrium and brain striatum of Sprague-Dawley rats. Cefoperazone (50 mgkg(-1), i.v.) was then administered via the femoral vein. Blood and brain dialysates were collected and eluted with a mobile phase containing methanol-100 mM monosodium phosphoric acid (30:70, v/v, pH 5.5). The wavelength of the UV detector was set at 254 nm. The detection limit of cefoperazone was 20 ng mL(-1). Isocratic separation of cefoperazone was achieved within 10 min. The intra- and inter-assay accuracy and precision of the analyses were < or =10% in the range of 0.05-10 microg mL(-1). The ratio of the area under the concentration curve of cefoperazone in rat brain and blood was estimated to be about 7-8%. It is concluded that cefoperazone is capable of penetrating the blood-brain barrier.

Animals↗
PubMed1999

Effect of acute renal failure on the disposition of cefoperazone.

The effect of acute renal failure on the disposition of cefoperazone was investigated. Rats, 3 days after uranyl nitrate treatment, were used to model acute renal failure. Although plasma-protein binding of cefoperazone decreased significantly in acute renal failure compared with control rats, the plasma clearance of total (bound plus unbound) drug after intravenous administration (50 mg kg(-1)) did not differ significantly between the two groups (5.61+/-2.37 mL min(-1) for control and 4.75+/-2.82 mL min(-1) for acute renal failure). Consequently the plasma clearance of the unbound drug in acute renal failure (6.14+/-1.16 mL min(-1)) was significantly lower than in control rats (15.6+/-3.7 mL min(-1), P < 0.025). Plasma clearance of the drug (both total and unbound) was also dependent on bile flow, and clearance of the unbound drug in acute renal failure rats was lower than in control rats with identical bile flow rates. To examine the mechanism of reduced unbound cefoperazone clearance, an in-vitro experiment using a simultaneous perfusion system of rat liver and kidney was performed. By changing perfusate plasma protein from bovine serum albumin to human serum albumin, the plasma clearance of the total cefoperazone changed to one-sixth in proportion to the unbound cefoperazone in the perfusate plasma. On the other hand, the plasma clearance of the total and unbound drug in acute renal failure rats decreased significantly compared with controls. These results demonstrate that the plasma clearance of unbound cefoperazone, which is mainly eliminated by the liver, decreased in acute renal failure in rats, probably due to changes in hepatic transport.

Acute Kidney Injury↗
PubMed2004

Acute interstitial nephritis due to cefoperazone.

OBJECTIVE: To describe a case of cefoperazone-induced acute interstitial nephritis (AIN) in which the diagnosis was supported by renal biopsy. CASE SUMMARY: A 35-year-old woman presented to our hospital with decreased urine output and no past history of renal problems. Fifteen days prior to presentation, she had started treatment with intramuscular cefoperazone 1 g/day for a scalp infection. On day 12 of therapy, the patient noted decreased urine output, anorexia, and weakness, but she continued taking cefoperazone for 3 more days. Hemodialysis and oral prednisolone 1 mg/kg (30 mg twice daily) were started. Renal function returned to normal after 2 months of prednisolone treatment. DISCUSSION: Although AIN has been linked with other cephalosporins, as of June 18, 2004, to our knowledge, this is the first report of a cefoperazone-induced case. We based our diagnosis on the features of acute-onset renal failure, abnormal urinalysis findings, eosinophilia, inflammatory infiltrate in the interstitium, and recovery from renal failure after initiation of corticosteroid treatment. Application of the Naranjo probability scale indicated a probable relationship between the acute renal failure secondary to the possible AIN and cefoperazone therapy in this patient. CONCLUSIONS: This case indicates that cefoperazone, like other cephalosporins, can cause AIN. We recommend close monitoring of renal function in patients who are prescribed this drug.

Acute Disease↗
PubMed1981

Clinical experience with cefoperazone in biliary tract infections.

The biliary excretion of cefoperazone in experimental animals, and humans, was investigated. Biliary excretion of cefoperazone in rats, rabbits, dogs, and monkeys was always higher than that of cephazolin. Biliary excretion was markedly reduced in experimentally-produced liver cirrhosis in rats. Comparing the biliary excretion of cefoperazone and cephazolin in a crossover study in patients, the excretion of cefoperazone was shown to be much higher than that of cephazolin. In clinical studies in 116 patients with biliary tract infections such as cholecystitis, cholangitis, and liver abscess, cefoperazone was effective in 90 (78%). The incidence of side effects was low. In conclusion, cefoperazone was considered to be effective in treating biliary tract infections because of its broad antibacterial spectrum and high penetration into bile.

Adult↗
PubMed1991

Beta-lactam antibiotic therapy in febrile granulocytopenic patients. A randomized trial comparing cefoperazone plus piperacillin, ceftazidime plus piperacillin, and imipenem alone.

OBJECTIVE: To compare the efficacy, toxicity, and cost-effectiveness of double beta-lactam therapy with monotherapy. DESIGN: A randomized, controlled trial. PATIENTS: Febrile, granulocytopenic patients (429). INTERVENTIONS: Patients were randomly assigned to receive iv cefoperazone (3 g every 12 hours) plus piperacillin (75 mg/kg body weight every 6 hours), ceftazidime (2 g every 8 hours) plus piperacillin (75 mg/kg every 6 hours), or imipenem alone (1.0 g or 0.5 g every 6 hours). Patients also received prophylactic vitamin K. MEASUREMENTS: Clinical improvement, eradication of the infecting organism, and toxicity in 403 evaluable patients with one or more infections. MAIN RESULTS: Cefoperazone and ceftazidime, when given in combination with piperacillin, were equally effective (response rates of 75% (104 of 138 patients) and 74% (101 of 137 patients), respectively). Monotherapy with imipenem had a response rate of 82% (111 of 136 patients) and was as effective as double beta-lactam therapy. Overall antibiotic-related toxicity was minimal, although seizures were associated with high doses of imipenem. Seizures occurred in 3 of 29 patients (10.3%) who were receiving 4 g/d of imipenem, in 3 of 136 patients (2.2%) who were receiving cefoperazone plus piperacillin, in 0 of the 132 patients who were receiving ceftazidime plus piperacillin, and in 1 of 106 patients (0.9%) who were receiving 2 g/d of imipenem (P less than 0.005). The 2-g daily dose of imipenem was as effective as the 4-g daily dose. Diarrhea was more frequent in patients receiving cefoperazone, whereas nausea occurred more often with imipenem. No antibiotic-related hemorrhage or nephrotoxicity was observed. Superinfections caused by beta-lactam-resistant, gram-negative bacilli were uncommon but occurred more frequently with double beta-lactam therapy than with imipenem monotherapy (11 of 268 patients compared with 1 of 135 patients; P = 0.06). Xanthomonas maltophilia superinfections occurred only in patients receiving imipenem (3 of 135 patients compared with 0 of 268 patients; P = 0.03). Imipenem monotherapy was the least expensive therapy. CONCLUSIONS: Cefoperazone and ceftazidime were equally effective when used in combination antibiotic therapy with piperacillin. Twice-daily cefoperazone is less expensive than ceftazidime given three times daily. Monotherapy with imipenem, at a daily dose of 2 g, is as efficacious as double beta-lactam therapy and costs less than combination therapy.

Adolescent↗
PubMed1986

Study of in vitro selected resistance of Pseudomonas aeruginosa to cefoperazone, ceftazidime, azthreonam and imipenem.

Ten strains of Pseudomonas aeruginosa were plated on agar containing cefoperazone, ceftazidime, azthreonam or imipenem alone and in combination with ampicillin or cefoxitin as inducers, and/or amikacin (MIC/4), according to Szybalsky. Regrowing colonies were randomly selected for MIC and MBC determinations. The numbers of regrowing colonies were occasionally increased by a beta-lactamase inducer, although amikacin significantly reduced it. Some 243 colonies were further studied. The most frequent phenotypes of resistance (195 mutants) were: resistance to cefoperazone, ceftazidime, azthreonam (99 regrowing colonies); resistance to cefoperazone, azthreonam (36); resistance to cefoperazone (17); resistance to cefoperazone, ceftazidime, azthreonam, imipenem (17). A total of 28/31 R mutants retained their phenotype after 15 subcultures in antibiotic-free medium. The mutants R cefoperazone, ceftazidime, azthreonam were studied by quantitative beta-lactamase evaluation in agar with substrate and non-substrate antibiotics, substrate profile study spectrophotometrically, crypticity study by comparing beta-lactamase activity of intact and sonicated cells spectrophotometrically, isoelectric focusing of sonicate extracts and dialysis experiments for trapping evaluation. These mutants were characterized by a 240-fold increase in beta-lactamase production (Pi = 8.7) and unchanged permeability. beta-lactamase trapping was demonstrated but could not explain alone the phenotype of resistance. These studies suggest that mutants constitutive for beta-lactamase production were easily selected in vitro. Amikacin was able significantly to prevent their emergence.

Amikacin↗
PubMed1987

Biliary secretion of cefoperazone and its inter-relationship with bile acid transport in the rat.

Cefoperazone is a third generation cephalosporin which is secreted predominantly in bile. This study set out to examine the effect of stimulating bile choleresis on the biliary secretion of cefoperazone. Stimulation of both bile acid-dependent and independent bile flow (phenobarbitone pretreatment) hastened the peak appearance of a pulse of cefoperazone into bile. Although the biliary secretion rate of cefoperazone was enhanced by bile acid infusion, the % recovery and maximal biliary concentration were reduced. The reciprocal effect of continuous cefoperazone infusion on the rate of biliary transport of a pulse of bile acid was examined. Cefoperazone infusion hastened the biliary transport of glycocholate. Net recovery of glycocholate was unaffected.

Animals↗
PubMed1984

Multicenter clinical trials of cefoperazone in Japan.

The safety and clinical efficacy of cefoperazone were evaluated at 149 institutions in Japan. A total of 979 hospitalized patients were treated with cefoperazone alone for 1,059 infections. In the 984 infections evaluated, there was an overall satisfactory clinical response in 824 (83.7%). Cefoperazone was effective in 83.0% of the respiratory tract infections, 84.9% of urinary tract infections, and 89.6% of hepatobiliary tract infections. Clinical response was satisfactory in 90% or more of the cases in which Escherichia coli, Serratia sp, Haemophilus influenzae or Staphylococcus sp were isolated. Sixty percent to 90% of the infections with Klebsiella sp, Enterobacter sp, Proteus sp, and Pseudomonas aeruginosa responded satisfactorily to cefoperazone. Cefoperazone was effective in 76.2% of 260 evaluated cases that had failed to respond to prior treatment with other cephalosporins. The adverse reactions that occurred in 19 (1.9%) of the 979 patients included rash (1%), diarrhea (0.6%), and fever (0.4%). Cefoperazone appears to be extremely useful in the treatment of various infections in hospitalized patients.

Adult↗
PubMed1980

Clinical comparison of cefoperazone in complicated urinary tract infections using a double-blind method.

A comparative double-blind study of the clinical efficacy of cefoperazone against chronic, complicated urinary tract infections was performed using carbenicillin as a control. Cefoperazone was administered at 2 gm/day and carbenicillin at 4 gm/day, in two divided doses, for five consecutive days, and the clinical efficacy was determined. A total of 283 patients were treated, of which 45 were subsequently excluded as unassessable ans six were dropped owing to side effects, leaving 232 evaluable patients, 116 on each drug. There were no significant differences between the two drug groups with respect to patients' sex, age, body weight, and catheterization. The overall efficacy rates were: cefoperazone, excellent in 24 and moderate in 45 cases, for an overall clinical effectiveness rate of 59%; carbenicillin, excellent in 14 and moderate in 21 cases, for an overall effectiveness rate of 30%. With respect to bacteriological activity, 68.2% of 154 strains treated with cefoperazone were eradicated, compared with 50.3% of 169 strains treated with carbenicillin. The corresponding eradication rates were 84% and 40% for Escherichia coli, 50% and 16% for Serratia sp, and 54% and 55% for Pseudomonas sp, respectively. Cefoperazone caused side effects in only four cases, and carbenicillin in three, all of which were mild in nature, with no significant toleration differences between the two groups. A total of 11 abnormal laboratory test results were obtained in patients treated with cefoperazone; nine such results were recorded for carbenicillin-treated individuals. None were of clinical significance.

Aged↗
PubMed1980

In vitro activity of a new semisynthetic cephalosporin: cefoperazone.

Cefoperazone is a new semisynthetic cephalosporin with excellent antibacterial activity. This study included more than 1,500 clinical isolates whose susceptibility to cefoperazone was determined by minimal inhibitory concentration (MIC) and minimal bactericidal concentration (MBC). Cefoperazone was highly active against Enterobacteriaceae including indolepositive Proteus, Serratia and Enterobacter sp. Particularly noteworthy was the high activity of cefoperazone against Pseudomonas and Acinetobacter strains, which are usually resistant to first- and second-generation cephalosporins. The activity of cefoperazone against Staphylococcus aureus, Staphylococcus epidermidis, group D streptococci and Haemophilus was also determined. In general, the differences between MIC and MBC were minimal. Additional studies were carried out to determine the effect of inoculum size on cefoperazone activity.

Bacteria↗
PubMed1982

[Pharmacokinetic study of a cephalosporin: cefoperazone in patients with a Kehr drain].

Cefoperazone is a semi-synthetic cefalosporine for parenteral use which has an excellent activity against a wide range of grampositive and gramnegative bacteria, especially Pseudomonas aeruginosa, Enterobacter, Proteus indole positive and Serratia marcescens. The pharmacokinetics of the new antibiotic have been studied in patients who had undergone cholecystectomy and choledochotomy for lithiasis and who required T-tube drainage of the bile duct. Five patients were anicteric and one was icteric. Mean serum concentration of cefoperazone determined by a microbiological method) measured after a two-hour intravenous perfusion of 2 g cefoperazone was 198.6 microgram/lm; this level is higher than the mean level measured in normal subjects (134 microgram/ml) but lower than the mean level measured in patients with hepatic insufficiency (208 microgram/ml). Apparent half life of elimination was longer (mean 4.1 hours) in the patients than in controls (mean 1.6 hours) and compares with that of patients with hepatic insufficiency (mean 4.3 hours). The distribution volume and renal clearance are similar to that in healthy volunteers and patients with hepatic insufficiency. Extrarenal clearance of cefoperazone was significantly lower in our patients (15.8 ml/min), as it is in patients with hepatic insufficiency (7.3 ml/min), than in the control group (59.4) ml/min). Cefoperazone concentrations in the bile were 10-20 times higher than those in the serum; in the icteric patient the concentrations achieved were still higher than the MIC values for organisms commonly encountered in the bile. These results open the way to the use of cefoperazone to treat infectious biliary diseases, particularly angiocholitis, which need a high biliary antibiotic concentration.

Adult↗
PubMed1979

In vitro antibacterial activity of cefoperazone (T-1551), a new semisynthetic cephalosporin.

Cefoperazone, a new semisynthetic cephalosporin, has a broad spectrum of antibacterial activity. It is as active as cefazolin and cefamandole against gram-positive bacteria and is more active than cefazolin and cefamandole against such gram-negative bacilli as Escherichia coli, Klebsiella pneumoniae, Proteus species, Pseudomonas aeruginosa, Citrobacter freundii, Enterobacter cloacae, and Serratia marcescens. The superiority of cefoperazone over cefazolin and cefamandole with respect to activity against P. aeruginosa by more than 200-fold was especially remarkable. As with other beta-lactam antibiotics, there was only a small spread between the minimum inhibitory concentrations and the minimum bactericidal concentrations of cefoperazone and a significant decrease in activity with an increase in inoculum size. Activity was not altered significantly by the addition of human serum to the test medium. Cefoperazone is relatively stable to hydrolysis to beta-lactamases produced by gram-negative bacteria. Relative rates of hydrolysis of cefoperazone by cephalosporinases are 7.0 to 0.01, with reference to cephaloridine hydrolysis (base, 100). Cefoperazone is also more stable than penicillin G and cephaloridine to various types of penicillinases.

Bacteria↗
PubMedDate not supplied

Comparative study of the serum bactericidal activity of cefoperazone alone and in combination with amikacin or mezlocillin against gram-negative bacilli and Staphylococcus aureus.

Serum bactericidal activity (SBA) was studied in vitro after intravenous administration of cefoperazone alone or in combination with mezlocillin or amikacin to human volunteers. One hour after the infusion, cefoperazone (2 g), cefoperazone + mezlocillin (5 g) and cefoperazone + amikacin (500 mg) achieved comparable activity against Escherichia coli and Klebsiella pneumoniae (100% of the strains being killed by a 1:8 or greater dilution). The activity of the three regimens was also similar against Pseudomonas aeruginosa (87-96% of the sera had an SBA greater than or equal to 1:8) and somewhat less for Staphylococcus aureus (52-60% with SBA greater than or equal to 1:8). Six and ten hours after administration, the SBAs were much lower for all regimens; a small advantage for cefoperazone + mezlocillin against K. pneumoniae could be shown in comparison to the other regimens.

Amikacin↗
PubMed2006

Efficacy and safety of intravenous moxifloxacin versus cefoperazone with azithromycin in the treatment of community acquired pneumonia.

To compare the efficacy, safety, and tolerability of intravenous moxifloxacin with those of a commonly used empirical antibiotic regimen, cefoperazone and azithromycin in the treatment of community acquired pneumonia (CAP) in adult patients requiring initial parenteral therapy, 40 patients with CAP were divided into two groups, a moxifloxacin group (n = 20) and a control group (n = 20), which were treated for 7 to 14 days. The patients in the moxifloxacin group were intravenously given 400 mg of moxifloxacin (Avelox) once a day. Patients in the control group were administered 2.0 g of cefoperazone twice a day and azithromycin 0.5 g once a day. Clinical, bacteriological, and laboratory examinations were performed before the treatment, and at the end of the treatment. Our results showed that there was no significant difference in the clinical efficacy rate between two treatment groups at end of therapy (90% for moxifloxacin, 95% for cefoperazone plus azithromycin) (P > 0.05). The bacteriologic eradication rate at the end of treatment was 90% in the moxifloxacin group and 80% in the cefoperazone-plus-azithromycin group, whereas there was no significant difference between the two groups (P > 0.05). In addition, both drugs were well-tolerated in this trial, with the number of drug-related adverse events being comparable. It is concluded that moxifloxacin is an effective and well-tolerated treatment for CAP and was equivalent to the commonly used empirical treatment of cefoperazone plus azithromycin. Moxifloxacin is likely to offer clinicians an alternative for reliable empirical CAP treatment in the face of increasing antibiotic resistance.

Adolescent↗
PubMed1988

Cefoperazone versus combination antibiotic therapy of hospital-acquired pneumonia.

Cefoperazone monotherapy was compared with combination antibiotic therapy in a randomized prospective evaluation of patients with hospital-acquired pneumonia. Cefoperazone was as effective as either clindamycin/gentamicin or cefazolin/gentamicin (cure rate: 45 of 52 cefoperazone-treated patients [87 percent], versus 44 of 61 combination-therapy patients [72 percent], p = 0.069). With the exception of hypoprothrombinemia in those patients who did not receive prophylactic vitamin K, there was no difference in the incidence of side effects. In addition, no difference was noted in the incidence of superinfections or secondary pneumonias. When antibiotic costs, administration costs, and laboratory costs were considered, cefoperazone monotherapy was the least expensive antibiotic regimen. Cefoperazone is a suitable alternative to combination antibiotic therapy for the treatment of hospital-acquired pneumonia.

Anti-Bacterial Agents↗
PubMed1988

Cefoperazone plus tobramycin versus ticarcillin plus tobramycin in febrile granulocytopenic cancer patients.

Cefoperazone plus tobramycin was compared in a prospective, randomized trial with our standard regimen of ticarcillin plus tobramycin as empiric therapy of fever in granulocytopenic patients with cancer. Patients who received cefoperazone were also given vitamin K (5 mg orally twice a week). Of 39 microbiologically and clinically documented infections treated with ticarcillin plus tobramycin, 28 (72 percent) showed improvement. Of 27 microbiologically and clinically documented infections treated with cefoperazone plus tobramycin, 21 (78 percent) showed improvement. The overall response rates were similar (40 of 53, or 74 percent, for ticarcillin plus tobramycin versus 38 of 48, or 79 percent for cefoperazone plus tobramycin). There was no difference in response between groups according to site of infection. Serious side effects were minimal with both regimens. There were no enterococcal superinfections in patients receiving cefoperazone. These results suggest that the overall efficacy and toxicity of study regimens are similar.

Adolescent↗
PubMed1988

Comparative susceptibility patterns of common clinical isolates to cefoperazone: 1981 to 1987.

It has been postulated that the widespread use of broad-spectrum cephalosporins might lead to increased bacterial resistance to such agents. To determine if such increased resistance to cefoperazone might be detectable, the susceptibility patterns of common clinical isolates to cefoperazone were examined from the Pathology Laboratories at Baptist Medical Center, Jacksonville, Florida, from 1981, prior to approval by the Food and Drug Administration, to the present. Gram-negative aerobic and facultative anaerobic organisms, staphylococci, and members of the Bacteroides fragilis group were included in the analysis. The data obtained were compared with results of similar published studies nationwide. No significant decrease in susceptibility to cefoperazone was detected for any gram-negative species examined. A steady increase in the percentage of staphylococci (both coagulase positive and especially coagulase negative) resistant to cefoperazone was demonstrable at this institution. This was a direct function of the concomitant rise in the percentages of staphylococci resistant to methicillin observed over the testing interval. Anaerobic susceptibility patterns of the members of the B. fragilis group were also relatively constant during this period of time. The concentrations of antibiotic inhibiting 50 percent (MIC50) and 90 percent (MIC90) of B. fragilis isolates as determined by an agar dilution technique were 16 micrograms/ml and 64 micrograms/ml, respectively, both in 1981 and in 1987. No change in the national susceptibility patterns of common bacterial isolates to cefoperazone was demonstrable in the five-year period during which the antibiotic has been available for clinical use.

Bacteria↗
PubMed1992

Cefoperazone versus ceftriaxone monotherapy of nosocomial pneumonia.

Ceftriaxone and cefoperazone monotherapy was compared in a multicentered, randomized, nonblinded, prospective study of patients with nosocomial pneumonia. These antibiotics were equally effective, with an overall successful treatment rate of 48 (80%) of 60 for the cefoperazone-treated patients and 35 (70%) of 50 for the ceftriaxone-treated patients. Patients with nursing-home-acquired pneumonia had similar bacterial pathogens and an almost identical cure rate to those patients with hospital-acquired infection. There was no statistical difference in the incidence of side effects of superinfections. The development of secondary pneumonia with resistant bacteria was low, 3% with cefoperazone and 4% with ceftriaxone. When antibiotic, administrative, and laboratory costs were calculated, cefoperazone was slightly less expensive than ceftriaxone. Both cefoperazone and ceftriaxone are effective therapy for the treatment of nosocomial pneumonia.

Adult↗