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PubMed1987

Hypoprothrombinemia associated with cefoperazone therapy.

Cefoperazone, a beta-lactam antibiotic with a methylthiotetrazole side chain, has been reported infrequently to cause hypoprothrombinemia and hemorrhage. We retrospectively analyzed the records of 80 patients who had been given this drug for more than 72 hours. Nine patients received vitamin K1 (phytonadione) prophylaxis and had no evidence of hemorrhage. Of the remaining 71 patients, 32 had prothrombin times measured; 14 of them had hypoprothrombinemia. Prothrombin times ranged from 14.8 to 97.3 seconds at a mean of 6.2 days after initiation of therapy. Seven of the 14 patients had clinically significant hemorrhage and five required transfusions. Two patients with clinically evident hemorrhage died during or immediately after cefoperazone therapy. Prothrombin times rapidly returned to normal in all patients treated with phytonadione. We believe hypoprothrombinemia is a more common complication of cefoperazone therapy than is generally acknowledged, and is preventable. Unless clinically contraindicated, we recommend that all patients treated with cefoperazone receive phytonadione prophylaxis.

Aged↗
PubMed1984

Serum and sputum concentrations of azlocillin, cefoperazone and ceftazidime in patients with cystic fibrosis.

Single-dose pharmacokinetics of azlocillin, cefoperazone and ceftazidime were studied in 17 patients with cystic fibrosis (CF). All patients had broncho-pulmonary infections caused by Pseudomonas aeruginosa. Three groups of five, six, and six patients were treated with azlocillin, cefoperazone, or ceftazidime, respectively. The size of the single dose was 133 mg/kg for azlocillin, 66.7 mg/kg for ceftazidime and 66.7 mg/kg for cefoperazone. The clearance values for the three antibiotics calculated from the single-dose data were, on the average, higher than the values previously reported for normal subjects. After the first dose, the patients received a repeated-dose treatment with the same antibiotic. During the first 5 days of therapy, a complement postural drainage of sputum was obtained four times a day for each patient. Cefoperazone could be measured in 47 (39.2%) of the 120 sputum samples assayed while ceftazidime was shown to be present in all 120 sputum samples examined. Azlocillin was not detected in any of the 100 sputum samples assayed.

Adolescent↗
PubMed1980

Cefoperazone (T-1551), a new semisynthetic cephalosporin: comparison with cephalothin and gentamicin.

The in vitro activity of cefoperazone (T-1551) against almost 9,000 recent clinical isolates at six institutions was tested and compared with that of cephalothin and gentamicin. The modal minimum inhibitory concentrations of cefoperazone were 16- and 4-fold less than those of cephalothin and gentamicin, respectively, against 5,503 strains of Enterobacteriaceae. Species normally resistant to cephalothin, such as indole-positive protease and enterobacters, were almost universally susceptible to cefoperazone. Cefoperazone demonstrated activity comparable to gentamicin against Pseudomonas aeruginosa and other pseudomonads.

Bacteria↗
PubMed1980

Influence of inoculum size on activity of cefoperazone, cefotaxime, moxalactam, piperacillin, and N-formimidoyl thienamycin (MK0787) against Pseudomonas aeruginosa.

Forty clinical isolates of Pseudomonas aeruginosa were tested for their susceptibility to cefoperazone, cefotaxime, moxalactam, piperacillin, N-formimidoyl thienamycin (MK0787), and gentamicin at three different inocula. At an inoculum of 5 x 10(3) colony-forming units (CFU) per ml, the minimum inhibitory concentrations (in micrograms per milliliter) for 90% of isolates (MIC90) were as follows: gentamicin, 1; N-formimidoyl thienamycin, 2; cefoperazone, 4; piperacillin, 8; moxalactam, 16; and cefotaxime, 16. When the inoculum was increased to 5 x 10(5) CFU/ml, the MIC90 for all drugs tested increased. Among the beta-lactam antibiotics, N-formimidoyl thienamycin and cefoperazone had the lowest MIC90 (8 micrograms/ml) at this inoculum. When the inoculum was increased further to 5 x 10(7) CFU/ml, an MIC90 could be determined only for gentamicin and N-formimidoyl thienamycin (4 and 8 micrograms/ml, respectively). Indeed, the MIC50 for moxalactam, cefotaxime, cefoperazone, and piperacillin was 128 micrograms/ml or more at this inoculum. The minimum bactericidal concentration for 90% of isolates (MBC90) at an inoculum of 5 x 10(5) CFU/ml ranged from 8 micrograms/ml for gentamicin and N-formimidoyl thienamycin to 128 micrograms/ml for cefotaxime. At the highest inoculum, however, whereas the MBC90 for gentamicin and N-formimidoyl thienamycin remained at 8 micrograms/ml, the MBC90 for each of the other drugs was greater than 128 micrograms/ml. N-Formimidoyl thienamycin was the only drug tested for which an MIC100 and MBC100 (MIC and MBC for 100% of isolates) could be determined, and these were not significantly different from the MIC90 and MCB90.

Anti-Bacterial Agents↗
PubMed1983

Cefoperazone pharmacokinetics in normal subjects and patients with cirrhosis.

The pharmacokinetics of cefoperazone were studied and compared in six normal subjects and six patients with severe liver disease. All subjects received a 2-g intravenous infusion of cefoperazone over 15 min. Significantly different results were noted between normal subjects and patients with cirrhosis (range [mean]) for the following: peak serum concentrations (203 to 345 [239] versus 82 to 206 [141] micrograms/ml; P less than 0.01); serum beta half-lives (1.0 to 1.8 [1.5] versus 2.3 to 9.9 [4.5] h; P less than 0.05); renal excretion (17 to 27 [21] versus 32 to 60 [50]%; P less than 0.01); and apparent volumes of distribution at steady state (4.1 to 7.8 [6.3] versus 12.7 to 23.8 [15.9] liters/1.73 m2; P less than 0.01). Lower peak serum levels in the patients with cirrhosis were probably related to an increased apparent volume of distribution secondary to ascites and to decreased serum protein binding of cefoperazone. Longer beta half-lives in the patients with cirrhosis were probably secondary to both decreased hepatic excretion caused by severe liver disease and to increased apparent volume of distribution. However, the longest beta half-life among the patients with cirrhosis was in a subject with a serum creatinine level of 2.1 mg/dl. We conclude that, although mild to moderate impairment of cefoperazone excretion occurs in patients with hepatic disease, adjustment of dosage may be necessary only with concomitant renal insufficiency.

Adult↗
PubMed1987

Comparison of difloxacin, enoxacin, and cefoperazone for treatment of experimental Enterobacter aerogenes endocarditis.

This study compared difloxacin administered orally, enoxacin administered orally, and cefoperazone administered intramuscularly for the treatment of experimental Enterobacter aerogenes endocarditis. Difloxacin significantly reduced bacterial counts of vegetations, as compared with enoxacin and cefoperazone. Enoxacin and cefoperazone did not differ significantly. This study demonstrated that difloxacin was significantly more effective than enoxacin and cefoperazone for the treatment of E. aerogenes endocarditis in rabbits.

Animals↗
PubMed1988

Pharmacokinetics of cefoperazone (2.0 g) and sulbactam (1.0 g) coadministered to subjects with normal renal function, patients with decreased renal function, and patients with end-stage renal disease on hemodialysis.

The single-dose pharmacokinetics of intravenously administered cefoperazone (2.0 g) and sulbactam (1.0 g) were studied in normal subjects and in patients with various degrees of renal failure. In an open, parallel experimental design, six normal subjects (creatinine clearance, greater than 90 ml/min), two patients with mild renal failure (creatinine clearance, 31 to 60 ml/min), eight patients with moderate renal failure (creatinine clearance, 7 to 30 ml/min), and four functionally anephric patients (creatinine clearance, less than 7 ml/min) were studied. The functionally anephric patients were given two test doses to allow study of drug disposition both on and off hemodialysis. Serial blood and urine samples were collected from time zero to 12 h after dosing in normal subjects and from 0 to 72 h in renal patients. Serum concentrations of both drugs declined biexponentially. For cefoperazone, the terminal elimination half-lives averaged from 1.6 to 3.0 h and were similar in subjects and patients. No cefoperazone pharmacokinetic parameters were appreciably altered by renal failure or hemodialysis, and there was no correlation between the total body clearance of cefoperazone and estimated creatinine clearance. In contrast, the sulbactam total body clearance was highly correlated with estimated creatinine clearance (r = 0.92, P less than 0.01) and was significantly higher in normal volunteers than in the renally impaired groups (P less than 0.01). The sulbactam terminal elimination half-life in functionally anephric patients (9.7 +/- 5.3 h) differed significantly from that of normal volunteers (1.0 +/- 0.2 h) and patients with mild renal failure (1.7 +/- 0.7 h, P less than 0.05).(ABSTRACT TRUNCATED AT 250 WORDS)

Adult↗
PubMed1988

Multiple-dose pharmacokinetics of intravenously administered cefoperazone and sulbactam when given in combination to infected, seriously ill, elderly patients.

The pharmacokinetics of cefoperazone and sulbactam in combination were evaluated in six, elderly, seriously ill patients treated with the drug combination for intra-abdominal infections. After giving informed consent, three males and three females aged 63.5 to 77.5 (mean 67.9) years and weighing 54.5 to 86.8 (mean, 67.6) kg were treated with cefoperazone (2.0 g) and sulbactam (1.0 g) infused intravenously every 12 h for at least 5 days. Cefoperazone and sulbactam pharmacokinetics were characterized on both days 1 and 5 of treatment. Eleven serial blood samples were obtained just prior to and following dose 1 on days 1 and 5 of treatment. Mean estimates of cefoperazone maximal concentration in plasma (Cmax), area under the curve of drug concentration in plasma versus time (AUC), half-life (t 1/2), apparent volume of distribution by the area method (Varea), apparent volume of distribution at steady state (Vss), and total body clearance (CL) for day 1 (day 5) were 297.5 237.5) micrograms/ml, 1,247 (1,063) micrograms.h/ml, 7.0 (4.9) h, 16.1 (13.4) liter, 13.1 (14.4) liter, and 28.9 (34.2) ml/min, respectively. Day 1 (day 5) mean values for sulbactam Cmax, AUC, t 1/2, Varea, Vss, and CL were 110.3 (78.0) micrograms/ml, 228 (217) micrograms.h/ml, 3.4 (2.5) h, 26.1 (18.5) liter, 18.9 (15.4) liter, and 97 (94) ml/min, respectively. Both drugs evidenced slower elimination and greater pharmacokinetic variability in these patients compared with values previously reported for normal volunteers. As patients improved during the course of therapy, the only pharmacokinetic parameter significantly changed between days 1 and 5 was a shortened sulbactam t 1/2. Our inability to find substantial evidence of pharmacokinetic normalization may have been related to sample size and study duration. Both drugs were present in potentially therapeutic concentrations for the entire 12-h dosing interval, but without undue accumulation from days 1 to 5.

Abdomen↗
PubMed1992

Use of a predictor panel for development of a new disk for diffusion tests with cefoperazone-sulbactam.

The proper disk mass for diffusion susceptibility tests with cefoperazone-sulbactam was determined by using a predictor panel of clinical isolates that included staphylococci and gram-negative bacteria intrinsically susceptible, intrinsically resistant, and of various susceptibilities because of the production of different types and amounts of beta-lactamase. A primary panel of 24 isolates was used to screen various disk masses of cefoperazone and sulbactam in disk diffusion susceptibility tests. Regression analyses were performed for each combination by comparing MICs to zone diameters. Analysis of each component demonstrated that decreasing the disk mass of cefoperazone shifted the regression line to the left while decreasing the disk mass of sulbactam diminished the slope of the line. Ten candidate disks that adequately separated susceptible and resistant strains among the primary panel were identified, and these 10 disks, along with the previously proposed 75/30-micrograms disk, were then tested against an expanded panel of 265 isolates. Results indicated that a 30/20-micrograms cefoperazone-sulbactam disk provided the best separation between susceptible and resistant strains when interpretive criteria of less than or equal to 15 mm for resistance, 16 to 19 mm for moderate susceptibility, and greater than or equal to 20 mm for susceptibility were used. They also identified discrepancies between agar and broth microdilution MICs of sufficient size to warrant separate interpretive criteria for the two methods. Overall, the use of a predictor panel to develop interpretive criteria for susceptibility tests appeared to be a very useful approach, especially when antibiotics designed to be used against drug-resistant organisms are involved.

Bacteria↗
PubMed1984

Assessment in the mouse of cefoperazone as a treatment for mastitis.

The value of cefoperazone in mastitis therapy was assessed in the mouse model of mastitis primarily by its effect on bacterial cell numbers in the gland. In addition histological studies showed that the drug was not an irritant in the mammary gland. Pharmacokinetic studies showed that it was slowly absorbed from the gland (six days to absorb 500 micrograms) but was easily removed by milking. In ascending order of efficacy cefoperazone (500 micrograms/gland) was active against four-hour-old intramammary infections caused by Pseudomonas aeruginosa, Staphylococcus aureus, Escherichia coli, Streptococcus agalactiae and Strep uberis. The effect against Staph aureus was titrated down to a dose of 50 micrograms/gland. Cefoperazone was not bactericidal against intracellular staphylococci but it did sensitise them to the action of lytic enzyme. Cefoperazone and cloxacillin behaved similarly against progressive staphylococcal mastitis. Both antibiotics significantly reduced the bacterial numbers when four-hour-old infections were treated but the effect on 26-hour-old infections was perceptible only when each antibiotic was assayed against saline treatment in the mouse. The results suggest that further studies in dairy cattle should be undertaken.

Animals↗
PubMed1982

In vitro activity of moxalactam and cefoperazone against Streptococcus pneumoniae with differing susceptibilities to penicillin.

In vitro studies were performed to examine the potential usefulness of two new drugs, moxalactam and cefoperazone, for the treatment of infections caused by Streptococcus pneumoniae. 34 isolates of S. pneumoniae with differing susceptibilities to penicillin were examined by disk diffusion, agar and microbroth dilution methods. Isolates highly resistant to penicillin (MIC greater then 1 microgram/ml) were also resistant to moxalactam (MIC = 128 micrograms/ml) but were sensitive to cefoperazone (MIC = 2--4 micrograms/ml). All isolates relatively resistant to penicillin (MIC 0.25--0.5 micrograms/ml) were sensitive to cefoperazone (MIC 0.25--1 microgram/ml) and had moxalactam MICs of 4--16 micrograms/ml for 10/12 isolates. The disk diffusion test was unreliable for detecting strain relatively resistant to moxalactam. These studies showed that cefoperazone is more active than moxalactam in vitro against S. pneumoniae regardless of the penicillin susceptibility of these bacteria.

Cefoperazone↗
PubMed1988

Cefoperazone compared with chloramphenicol in the treatment of typhoid fever.

The authors have conducted an open randomized study to compare the clinical efficacy and safety of cefoperazone with those of chloramphenicol in the treatment of typhoid fever. They studied 56 subjects (28 in each group), 36 males and 20 females, whose average age was 25.9 years. The diagnosis of typhoid fever was made when one of the at least three blood cultures performed was positive for Salmonella typhi and in the presence of a 'toxic'-like symptomatology and hyperpyrexia (39 degrees C). Moreover, several stool cultures were done and the signs and symptoms characteristic of the pathology in progress were monitored. Furthermore, the MICs of cefoperazone and chloramphenicol were determined for all the strains of S. typhi isolated in both groups. Cefoperazone was given at the mean dose of 2 g i.v. every 8 h, and chloramphenicol at the dose of 500 mg by oral route every 6 h. The results obtained were assessed statistically (Friedman's test and Fischer's test). The authors conclude that cefoperazone is as active as chloramphenicol, and the importance of this result should not be underestimated.

Adolescent↗
PubMed1981

The role of the laboratory in the planned use of cefoperazone for the treatment of difficult Pseudomonas infections.

Four cases are discussed illustrating the role of the laboratory in the treatment of difficult pseudomonas infections. Pseudomonas vertebral osteomyelitis, in a 76-year-old man with impaired renal function, was successfully treated with cefoperazone given for 7 weeks. A 73-year-old woman, who had recurrent pseudomonas septicaemia due to infected cardiac pacing wires (that could not be removed), was managed with long term daily intramuscular cefoperazone, and a 31-year-old woman with pseudomonas aortitis was treated with long term intravenous cefoperazone. A 47-year-old man, who developed a pseudomonas infection superimposed on chronic osteomyelitis of the femur prior to a free vascularised graft operation, was treated with cefoperazone and ticarcillin.

Adult↗
PubMed1981

Anomalous effect of serum on the antimicrobial activity of cefoperazone.

This study investigated the effect of added serum on cefoperazone activity in vitro. Due to protein-binding, an 8-fold difference would be expected between minimum inhibitory concentrations in broth and in broth plus 90% serum. Using supplemented Mueller-Hinton broth (sMH) and sMH plus 90% heat-inactivated human serum there were differences of 3.36 +/- 0.92 for Staphylococcus aureus strain ATCC1 25923, 1.39 +/- 0.47 for Escherichia coli strain ATCC 25922 and 1.43 +/- 0.39 for Pseudomonas aeruginosa strain ATCC 27853. Serum-related modal increases in minimum inhibitory concentrations of cefoperazone for clinical isolates were 4-fold versus Staphylococcus aureus (5 strains), Klebsiella species (5 strains) and Pseudomonas aeruginosa (8 strains), and 2-fold versus Escherichia coli (4 strains). On the addition of serum to 2 strains of Serratia marcescens, divergent effects were seen. Minimum lethal concentrations of cefoperazone were generally identical to, or a low multiple of, corresponding minimum inhibitory concentrations. Variables other than protein binding may account for the anomalous activity of antibiotics against organisms in serum. These factors favour the activity of cefoperazone against several clinically important species.

Bacteria↗
PubMed2006

Severe INR elevation in a patient with choledocholithiasis receiving cefoperazone.

Cefoperazone is a third-generation cefalosporin that contains the N-methyl- thio-tetrazole (NMTT) side chain, which inhibits vitamin K-dependent carboxylation. Administration of NMTT-containing cefalosporins can cause alterations in the hepatic glutathione redox state, resulting in a dose-related increase in oxidised glutathione, which is responsible for the inhibition of microsomal reduction of vitamin K epoxide. In addition, cefoperazone is not metabolised and is excreted predominantly through the bile. In patients with hepatic impairment, the clearance of cefoperazone has been shown to be significantly reduced and the half-life prolonged. We report a case of choledocholithiasis related to a prolonged prothrombin time and INR secondary to cefoperazone therapy.

Aged↗
PubMed1997

In-vitro susceptibility of Burkholderia pseudomallei to cefoperazone-sulbactam combination.

Melioidosis is endemic in Malaysia. Emerging resistance with new and current antimicrobial agents has underscored the need to look further for new antimicrobial agents for the treatment of melioidosis. Hence, we evaluated the in-vitro susceptibility of fifty locally isolated strains of Burkholderia pseudomallei, the causative agent of melioidosis to cefoperazone-sulbactam combination using the method of NCCLS. All the fifty strains tested were susceptible in-vitro to cefoperazone-sulbactam. The MIC90 of the organism for cefoperazone-sulbactam was 4 mg/L. The results of our findings suggested that cefoperazone-sulbactam may be useful in the treatment of melioidosis.

Burkholderia pseudomallei↗
PubMed1991

Compatibility of cefoperazone sodium and cimetidine hydrochloride in 5% dextrose injection.

The compatibility of cimetidine hydrochloride and cefoperazone sodium in 5% dextrose injection stored at two temperatures was studied. Cimetidine hydrochloride and cefoperazone sodium were reconstituted or diluted with 5% dextrose injection to form an admixture with a cimetidine concentration of 2 mg/mL and a cefoperazone concentration of 5 mg/mL. The admixture was stored in 100-mL vented i.v. containers in the dark at 4 and 25 degrees C; three containers were stored at each temperature. A 2-mL sample was taken from each container after 0.5, 0.75, 1, 6, 12, 24, and 48 hours of storage and visually inspected, tested for pH, and assayed by a stability-indicating high-performance liquid chromatographic method. Triplicate studies were done for each storage condition. At both temperatures, drug concentrations varied by less than 5% during the study period. No color change, precipitation, or cloudiness was observed for any of the solutions under any of the storage conditions. Cefoperazone sodium 5.0 mg/mL and cimetidine hydrochloride 2.0 mg/mL in admixtures in 5% dextrose injection are stable for 48 hours at 4 and 25 degrees C.

Cefoperazone↗
PubMed1990

In vitro antimicrobial activity of a novel aminothiazolylglycylcephalosporin, MT0703S, compared with that of ceftazidime, cefoperazone and aztreonam.

The antibacterial activity of a novel aminothiazolylglycylcephalosporin, MT0703S, possessing a dihydroxypyridone moiety was compared in vitro with the activity of ceftazidime, cefoperazone, aztreonam and other beta-lactam antibiotics using seven bacterial species of a clinical origin. MT0703S showed the most potent activity against P. aeruginosa, including the ceftazidime-resistant strains, E. coli, K. pneumoniae and C. freundii. MT0703S was comparable to aztreonam but more active than ceftazidime and cefoperazone in its activity against K. oxytoca and E. cloacae, and comparable to ceftazidime against S. aureus and S. marcescens. MT0703S was more active than cefoperazone against S. marcescens but less active against S. aureus. The stability of MT0703S against various beta-lactamases appeared to be intermediate between the stability of ceftazidime and that of cefoperazone. The antimicrobial activity of MT0703S increased in a low-iron environment and decreased in a high ferric ion concentration.

Aztreonam↗