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PubMed1981

Serum and urine concentrations of cefoperazone in severe chronic renal failure.

Two studies evaluating the efficacy of cefoperazone in patients with chronic renal failure are described. In study A, 10 patients with severe chronic renal failure were given 1 g of cefoperazone intravenously over 3 minutes. The mean serum cefoperazone concentration at 30 minutes was 119.3 +/- 15.7 microgram/ml, and at 6 hours was 35.9 +/- 5.7 micrograms/ml. The mean serum half-life using the method of least squares was 6.6 +/- 1.15 hours (range, 2.5 to 15.1). The mean half-life from 2 hours onwards was 12.2 +/- 3.51 hours (range, 2.3 to 42.9). The mean peak urinary concentration of cefoperazone was 192 microgram/ml with a very wide individual range of 20 to 920 microgram/ml which was reached 0.5 to 9 hours after injection. In study B, 8 patients with chronic renal failure were treated with 1 to 2 g of cefoperazone intravenously every 12 hours for 5 to 14 days for complicated urinary tract infections. Serum and urine concentrations of cefoperazone were measured 6 hours after each morning dose. The mean 6-hour serum and urine concentrations of cefoperazone for the 4 patients treated with 2 g daily were 63 +/- 11.7 and 87 +/- 11.1 microgram/ml, respectively. The corresponding values for the 4 patients treated with 4 g daily were 106 +/- 20 and 258 +/- 32 microgram/ml. No drug accumulation occurred in any patient. No deterioration in renal function was noted. In conclusion, cefoperazone promises to be an effective and safe broad-spectrum antibiotic for patients with all degrees of renal function impairment. A dosage schedule of 2 to 4 g daily will not lead to significant drug accumulation in the presence of severe renal failure.

Adult↗
PubMed1981

Cefoperazone in the treatment of severe or complicated infections.

We report the use of cefoperazone in 62 cases of serious infection, most of which occurred in patients with renal impairment. 43 severe or complicated urinary tract infections, 11 cases of pneumonia and 8 with other severe sepsis were treated with cefoperazone 1 to 2 g twice daily usually for 5 to 10 days. Of the patients with urinary tract infection, all who were symptomatic showed a rapid clinical response; 26 (61%) were cured including 11 of 16 with chronic renal failure; 12 relapsed and 5 were reinfected with a different pathogen. All of these patients were infected by organisms sensitive to cefoperazone by disc testing but in 5 of those who relapsed the cefoperazone MIC was in fact greater than or equal to 50 microgram/ml. Ten of 11 cases with radiologically confirmed pneumonia were cured with cefoperazone. 7 episodes of pneumonia were in patients with end-stage chronic renal failure (6 were on dialysis) and 1 was in a patient with acute renal failure. Seven of 8 cases with severe sepsis were cured with cefoperazone. 1 patient was withdrawn from the study when acute bronchospasm followed a 2 g intravenous dose. 2 of the successfully treated patients had functioning renal transplants, 2 of 3 with severe chronic renal failure were on dialysis and 1 had acute renal failure. Side effects included minor disturbances of liver function in 6 patients (11%), diarrhoea in 7 (13%) and marked alcohol intolerance in one, 4 patients with chronic renal failure developed a coagulation disorder which was corrected with vitamin K. None of the patients showed deterioration in renal function while receiving cefoperazone. Cefoperazone promises to be an effective drug for the treatment of a wide spectrum of severe infections in hospitalised patients including those with impaired renal function.

Adolescent↗
PubMed1981

Worldwide clinical experience with cefoperazone.

The safety and clinical efficacy of cefoperazone 1 to 2g 12-hourly was evaluated in clinical trials conducted in the United States, Europe, South and Latin America, and Japan. 1046 patients were treated in 4 comparative and 9 non-comparative studies. An overall satisfactory clinical response for cefoperazone therapy was achieved in 540 (88%) of the 615 evaluable patients. Cefoperazone was effective in 92% of lower respiratory tract infections, 81% of urinary tract infections, 98% of gynaecological infections and 90% of a mixture of intra-abdominal, wound and soft tissue infections. A satisfactory clinical response was obtained in over 90% of patients infected with organisms normally susceptible to cephalosporins, such as staphylococci, streptococci, Escherichia coli, Klebsiella and Proteus species. 50 to 90% of infections caused by organisms resistant to presently available cephalosporins, such as Enterobacter species, Proteus vulgaris, Providencia species, Morganella morganii, Serratia species, Pseudomonas aeruginosa, and Bacteroides fragilis responded satisfactorily to cefoperazone. In the 4 clinical trials comparing cefoperazone with cefamandole, cephazolin or carbenicillin, cefoperazone therapy resulted in a similar or higher rate of satisfactory clinical response. Adverse reactions related to cefoperazone occurred in 8% of patients and were mainly diarrhoea (4%), skin reactions (3%) and phlebitis (1%). Twice daily dosing with cefoperazone appears to be effective against numerous Gram-positive and Gram-negative bacteria in a variety of clinical infections.

Bacteria↗
PubMed1984

Influence of cefoperazone on ethanol and acetaldehyde metabolism in vitro.

The effect of cefoperazone on ethanol and acetaldehyde metabolism was studied in rat liver homogenates and with a purified aldehyde dehydrogenase. Rat liver homogenates were incubated with ethanol (30 mM) alone or in combination with cefoperazone (15 or 150 micrograms/g liver). Ethanol and acetaldehyde concentrations were determined at 6, 12, 18 and 24 minutes. Cefoperazone added to the incubation medium inhibited ethanol and acetaldehyde metabolism in a concentration-dependent manner. The addition of cefoperazone to rat liver homogenates incubated with acetaldehyde (300 microM), however, did not inhibit acetaldehyde disappearance for a period of 15 minutes. Purified aldehyde dehydrogenase was incubated with 300 microM acetaldehyde. When cefoperazone was added, acetaldehyde disappearance was significantly slower than without cefoperazone. The data indicate that cefoperazone inhibits ethanol metabolism in rat liver homogenates in a concentration-dependent manner. The effect of the antibiotic on acetaldehyde elimination in liver homogenate, however, depends on the concentration of acetaldehyde in the medium. The acetaldehyde dehydrogenase obtained from yeast is inhibited by cefoperazone.

Acetaldehyde↗
PubMed1987

Inhibition of biliary phospholipid and cholesterol secretion by cefoperazone.

The effect of cefoperazone, a third-generation cephalosporin, on biliary lipid secretion in rats was examined. Rats were anesthetized with ether and the mid-lumbar vein and common bile duct cannulated. Bile acid secretion was maintained by intravenous taurocholic acid infusion (28 mumol/hr). A 1-hr control period was followed by intravenous cefoperazone infusion at either submaximal (20 mumol/hr), or supramaximal (60 mumol/hr) concentrations. At the cefoperazone infusion rate of 20 mumol/hr (biliary secretion of 7.1 +/- 1.6 mumol/hr) phospholipid secretion fell 19% and cholesterol secretion fell 31%; at a cefoperazone infusion rate of 60 mumol/hr (biliary secretion rate of 27.1 +/- 5.1 mumol/hr) phospholipid and cholesterol secretion were further reduced 40% and 56%, respectively, of controls. All changes were significant (P less than 0.01). Inhibition of both cholesterol and phospholipid secretion paralleled each other, was dose-dependent, and reversible. Cefoperazone's inhibitory action was abolished at a bile acid infusion rate of 108 mumol/hr. Cefoperazone was not found to be associated with bile acid micelles or mixed micelles as determined by ultracentrifugation and gel filtration. Thus, the effect of cefoperazone on biliary lipid secretion is not due to the impairment of mixed micelle formation in the canalicular lumen but rather its inhibitory effect appears to be due to a presecretory event.

Animals↗
PubMed1987

Prophylactic antibiotics for patients undergoing elective biliary tract surgery: a prospective randomized study of cefotiam and cefoperazone.

Cefotiam, a second generation cephalosporin and cefoperazone, a third generation cephalosporin have a broad spectrum of activity against a majority of organisms commonly found in the bile. Although cefoperazone is excreted into the human bile to a greater extent than is cefotiam, there are no comparative data available that cefoperazone prophylaxis is safer and more effective than cefotiam for patients undergoing biliary tract surgery. A prospective randomized study was performed to compare the safety and efficacy of cefotiam with those of cefoperazone for prophylaxis in patients undergoing elective biliary tract surgery. The incidence of postoperative infection was not significantly different between the cefotiam group (n = 86) and the cefoperazone group (n = 86). The rate of side effects, however, was significantly different. In the cefotiam group, only one patient had diarrhea whereas in the cefoperazone group, eight had diarrhea and one skin eruption. Clostridium difficile cytotoxin was nil in those with diarrhea. Diarrhea in all patients was mild and recovery was rapid. Cefotiam is thus safer and as effective as cefoperazone in preventing postoperative infections following biliary tract surgery. We suggest that cefotiam is the first choice antibiotic for prophylaxis in biliary tract surgery.

Adult↗
PubMed1988

Cefoperazone plus piperacillin versus mezlocillin plus tobramycin as empiric therapy for febrile episodes in neutropenic patients.

The double beta-lactam combination of cefoperazone plus piperacillin was compared with an aminoglycoside-containing regimen of mezlocillin plus tobramycin in a prospective, randomized trial of empiric therapy for febrile neutropenic patients (neutrophils no more than 1,000/mm3). Thirty febrile episodes were treated with cefoperazone plus piperacillin and mezlocillin plus tobramycin, respectively. There was no significant difference between the two groups with respect to age, sex, pretherapy neutrophil count, and mean duration of therapy. The majority of patients had neutrophil counts of no more than 200/mm3 at the initiation of therapy. Only microbiologically and clinically documented infections were evaluated for efficacy. The cefoperazone plus piperacillin regimen appeared to have a comparable response rate with the mezlocillin plus tobramycin regimen (20 of 24 patients [83 percent] versus 16 of 23 patients [70 percent]). Gram-positive micro-organisms were seen predominantly in this study, with the cefoperazone plus piperacillin regimen achieving a bacteriologic response in 84 percent, as opposed to 60 percent for those organisms treated with the mezlocillin plus tobramycin regimen. Neither regimen was totally effective against coagulase-negative staphylococci. Eight superinfections occurred in the cefoperazone plus piperacillin arm, whereas 11 superinfections occurred in the mezlocillin plus tobramycin arm. Although fungal superinfections were most common, the number of gram-positive superinfections in the mezlocillin plus tobramycin arm exceeded those seen in the cefoperazone plus piperacillin arm. The incidence of antibiotic-related side effects was similar in the two groups. Hypokalemia was most frequently seen. Both skin rashes and nephrotoxicity were more common with mezlocillin plus tobramycin. Cefoperazone plus piperacillin was found to be effective empiric therapy in febrile neutropenic patients. This double beta-lactam combination may be particularly useful for patients who have or are at high risk for the development of renal insufficiency.

Adolescent↗
PubMed1983

Biliary excretion and pharmacokinetics of cefoperazone in humans.

Six patients, 40 to 81 years of age, requiring T-tube drainage of their common bile duct, were studied to assess the biliary tract excretion and pharmacokinetics of cefoperazone. Each patient received 2.0 g of cefoperazone iv over 15 min. Cefoperazone concentrations were determined in serum, urine and bile by means of bioassay and HPLC. The results were compared with a pharmacokinetic study in healthy volunteers. The mean total recovery rate of cefoperazone in urine and bile was with bioassay: 64.5 +/- 15.3% (HPLC: 62.4 +/- 15.5%) in 24 h. 18.6 +/- 14.0% (11.5 +/- 7.1%) were found in the bile and 45.9 +/- 16.2% (50.9 +/- 19.7%) in urine. Peak bile concentrations were 3642 +/- 2975 mg/l (2259 +/- 1337 mg/l) after 2-3 h. The serum levels of cefoperazone showed a slow decrease in patients with a long terminal half life (T1/2 gamma) of 380 min from 295 +/- 90 mg/l initially to 15.9 +/- 11.3 mg/l after 12 h. In normal subjects, serum concentrations decreased much faster (T1/2 gamma = 143.5 +/- 20.0 min) from 232.8 +/- 28.6 mg/l to 1.16 +/- 0.73 mg/l after 12 h. Recovery in urine was 21.4 +/- 5.6%. Using HPLC analysis, we found cefoperazone A in small concentrations in the serum and in higher concentrations in the bile and urine of the operated patients. It is debatable whether cefoperazone A is a true metabolite in vivo or a physical degradation product.

Adult↗
PubMed1983

Serum bactericidal activity of cefoperazone and ceftazidime at increasing dosages against Pseudomonas aeruginosa.

Serum bactericidal activity (SBA) greater than or equal to 1:8 correlates with the clinical effectiveness of antibiotics. Ten healthy young volunteers received iv on separate days cefoperazone 1, 2, or 3 g and ceftazidime 1, 2, or 3 g. The serum levels 1 and 6 h after the administration of cefoperazone 1, 2 and 3 g were respectively 52 and 7 mg/l, 122 and 13 mg/l, 190 and 22 mg/l. The serum levels of ceftazidime 1, 2 and 3 g, after 1 h and 6 h were 28 and 8, 56 and 9, 78 and 13 mg/l. The SBA was determined against seven strains of Pseudomonas aeruginosa with MBC of 1.6-12.5 mg/l of cefoperazone and 0.8-6.2 mg/l of ceftazidime. Increased dosage of cefoperazone and ceftazidime led to a significant increase in the SBA's greater than or equal to 1:8 at 1 h (P less than 0.01). In sera obtained 1 h and 6 h after the injection of the antibiotics, 97% and 51% of the strains were inhibited by ceftazidime 2 g, while 1 g was inhibitory on 84% (1 h) and 8% (6 h) of the strains. Ceftazidime 1 g produced SBA's greater than or equal to 1:8 significantly more often than did cefoperazone 3 g (P less than 0.01) at 1 h. The rate of killing with all ceftazidime regimens was similar and slightly higher than that of any cefoperazone regimen. Ceftazidime seems more effective than cefoperazone against Ps. aeruginosa; however, increased MBC values were observed during killing curves studies with both drugs.

Adult↗
PubMed1981

Comparative pharmacokinetics of cefoperazone and cefamandole.

The pharmacokinetics of cefoperazone, a new beta-lactam antibiotic, were studied in normal volunteers and compared with the pharmacokinetics of cefamandole. After a 30-min infusion of 2 g of cefoperazone, the mean serum level was 256 micrograms/ml; at 4 h, the serum level was 20 micrograms/ml, and at 24 h, the level was 1.25 micrograms/ml, compared with levels of cefamandole of 188 micrograms/ml at the end of infusion, 1.8 micrograms/ml at 4 h, and none detected thereafter. The mean half-life of cefoperazone was 1.6 h, compared with 0.7 h for cefamandole. The area under the curve was 356 micrograms/ml per h for cefoperazone, which was three times that for cefamandole. The apparent volume of distribution for cefoperazone was 9.9 liters/1.73 m2 compared with 12.5 liters/1.73 m2 for cefamandole. Serum clearance of cefoperazone was 85 ml/min, and renal clearance was 25 ml/min, compared with a serum clearance of 224 ml/min and a renal clearance of 213 ml/min for cefamandole. Urine levels exceeded 25 micrograms/ml in the first 8 h after injection. Renal recovery of cefoperazone was only 29%.

Adult↗
PubMed1982

Activity of cefoperazone and two beta-lactamase inhibitors, sulbactam and clavulanic acid, against Bacteroides spp. correlated with beta-lactamase production.

A total of 102 isolates of Bacteroides spp. were studied for beta-lactamase production and susceptibility to cefoperazone alone or in combination with either of the beta-lactamase inhibitors sulbactam and clavulanic acid. The geometric mean minimal inhibitory concentration of cefoperazone alone was 31.5 micrograms/ml and when combined with 10 micrograms of sulbactam per ml or 2 micrograms of clavulanic acid per ml was reduced to 5.4 and 9.2 micrograms/ml, respectively. When bacterial suspensions were tested for beta-lactamase production with nitrocefin, 91 (89.2%) of these isolates produced the enzyme. The geometric mean minimal inhibitory concentrations of cefoperazone rose only slightly for isolates with low or intermediate enzyme activity but rose significantly for those with high activity. The addition of EDTA to cefoperazone significantly more frequently enhanced the activity of cefoperazone against beta-lactamase-negative as opposed to beta-lactamase-positive isolates. Furthermore, EDTA resulted in synergistic activity of the cefoperazone-sulbactam combination on beta-lactamase-positive isolates for which the combination had previously not shown a synergistic effect. This study demonstrates the relationship between beta-lactamase production and the resistance of Bacteroides spp. to cefoperazone and shows that inhibition of these enzymes can reverse this resistance.

Anti-Bacterial Agents↗
PubMed1988

Pharmacokinetics and pharmacodynamics of cefoperazone-sulbactam in patients on continuous ambulatory peritoneal dialysis.

This study was conducted to determine the pharmacokinetics of the fixed combination antibiotic cefoperazone-sulbactam in patients receiving continuous ambulatory peritoneal dialysis (CAPD). In addition, the pharmacodynamic profile of this combination was determined by the use of mean bactericidal titers against selected bacterial strains. Six noninfected CAPD patients were given a fixed dose of cefoperazone (2 g) and sulbactam (1 g) either intravenously or intraperitoneally over 10 min in a randomized, two-way crossover fashion. The mean peak cefoperazone concentration in serum after intravenous administration was 280.9 micrograms/ml. The mean peak concentration in serum after intraperitoneal cefoperazone administration was 38.9 micrograms/ml and occurred 2 to 4 h postdose. The mean peak sulbactam concentration in serum after intravenous administration was 82.2 micrograms/ml. The mean peak concentration in serum after intraperitoneal sulbactam administration was 24.4 micrograms/ml and occurred at 6 h. The absolute bioavailability of the intraperitoneal dose was 61% for cefoperazone and 70% for sulbactam. Cefoperazone total body and renal clearances were unaffected by renal failure and dialysis. However, both clearance values for sulbactam were reduced markedly. Only intraperitoneal dosing provided peak inhibitory and bactericidal titers in dialysate for all organisms tested. Intravenous dosing provided satisfactory dialysate titers only for very susceptible bacterial strains. End-stage renal disease and CAPD do not alter cefoperazone pharmacokinetics; however, sulbactam dosing may need to be adjusted.

Adult↗
PubMed1988

Effect of protein binding on serum bactericidal activities of ceftazidime and cefoperazone in healthy volunteers.

The effect of protein binding on antibiotic efficacy is controversial. The pharmacologic effect of an antibiotic is believed to be related to its unbound concentration at the site of infection. It is unknown whether antibiotics with a low degree of serum protein binding are clinically superior to antibiotics that are highly protein bound. In a randomized, crossover investigation, the serum bactericidal activities of a single dose of ceftazidime (30 mg/kg) and cefoperazone (30 mg/kg) were studied in six healthy volunteers against three clinical isolates of Pseudomonas aeruginosa for which both antibiotics had similar MICs and MBCs. Serum samples were collected over 12 h. The total and unbound antibiotic concentrations were determined by high-pressure liquid chromatography. Mean peak total concentrations of ceftazidime and cefoperazone in serum were 101.7 +/- 18.6 and 264.1 +/- 149.6 micrograms/ml, respectively. Due to its lower protein binding (21 +/- 6%), ceftazidime had significantly higher unbound concentrations in serum than did the highly bound cefoperazone (91.5 +/- 2%). Mean peak unbound concentrations were 78.5 +/- 12.5 and 24.2 +/- 17.8 micrograms/ml for ceftazidime and cefoperazone, respectively. The unbound concentration of ceftazidime at each sampling time was higher than that of cefoperazone. Although total concentrations were consistently higher than the MICs, serum containing cefoperazone showed minimal bactericidal activity against the isolates. In contrast, despite lower total concentrations, ceftazidime had greater antibacterial activity than cefoperazone. Serum bactericidal activity was more closely related to unbound rather than total antibiotic concentrations. Our data support the concept that only the unbound drug is microbiologically active.

Adult↗
PubMed1996

Molecular aspects of high-level resistance to sulbactam-cefoperazone in Klebsiella oxytoca clinical isolates.

Nine Klebsiella oxytoca strains which demonstrated resistance to the combination of sulbactam and cefoperazone were isolated from geographically separate hospitals in Japan in 1995. Among them, K. oxytoca SB23 showed high-level resistance to sulbactam-cefoperazone (MIC > 128 micrograms/ml) and aztreonam (MIC, 128 micrograms/ml). The sulbactam-cefoperazone resistance was not transferred from strain SB23 to Escherichia coli CSH2 by conjugation, beta-Lactamase RbiA, produced by strain SB23, was purified, and the molecular mass was estimated to be 29 kDa by sodium dodecyl sulfate-polyacrylamide gel electrophoresis. Kinetic parameters for RbiA revealed that cefoperazone and aztreonam were hydrolyzed efficiently by this enzyme. Moreover, ceftazidime and imipenem were also hydrolyzed weakly by RbiA, although strain SB23 did not show any resistance to these agents. Clavulanate, sulbactam, and tazobactam failed to block the hydrolysis of cefoperazone by RbiA. The structural gene of RbiA (blaRBI) was cloned and sequenced, and the deduced amino acid sequence of RbiA demonstrated high-level similarities to those of the beta-lactamases found in K. oxytoca D488, E23004, and plasmid-mediated MEN-1, which have been classified into Bush functional group 2be. Although RbiA demonstrates high-level molecular similarity to the enzymes in group 2be, from an enzymological point of view, this enzyme might be differentiated from the enzymes in that group. Hybridization analysis revealed that beta-lactamase genes highly similar to blaRBI were generally encoded on the chromosome of the sulbactam-cefoperazone-resistant clinical isolates of K. oxytoca tested in the study, despite their different derivations. This observation suggests that sulbactam-cefoperazone-resistant A. oxytoca strains which produce RbiA-type beta-lactamases have been proliferating in many hospitals in Japan.

Amino Acid Sequence↗
PubMed1988

Criteria for disk susceptibility tests and quality control guidelines for the cefoperazone-sulbactam combination.

For in vitro susceptibility tests with cefoperazone and sulbactam (a beta-lactamase inhibitor), 75/30-micrograms disks may be used with the interpretive zone size breakpoints that are currently used for 75-micrograms cefoperazone disks. For dilution tests, a 2:1 ratio of cefoperazone to sulbactam is recommended. For quality control purposes, MIC limits that are used to monitor cefoperazone tests were also applied to tests with the combination of drugs. For gram-negative control strains, zone size limits were calculated to be 1 mm smaller than those used for cefoperazone disks. To monitor the sulbactam portion of the combination, Acinetobacter calcoaceticus subsp. anitratus ATCC 43498 was selected; zones with 75/30-micrograms disks were 26 to 32 mm in diameter, and broth microdilution MICs ranged from 1.0/0.5 to 8.0/4.0 micrograms/ml. With cefoperazone alone, MICs for Acinetobacter calcoaceticus subsp. anitratus were 16 to 64 micrograms/ml and zones ranged from 14 to 18 mm in diameter. For anaerobic dilution tests, only Bacteroides thetaiotaomicron ATCC 29741 is recommended for cefoperazone-sulbactam; MICs ranged from 8.0/4.0 to 32/16 micrograms/ml.

Bacteria, Anaerobic↗
PubMed2005

[The reaction mechanism between cefoperazone and human serum albumin].

The reaction mechanism between cefoperazone and human serum albumin (HSA) and the affinity between cefoperazone and beta-lactamase were investigated by spectrometry and spectrofluorimetry. The interaction dissociation constants of human serum albumin and cefoperazone have been determined from a double reciprocal Lineweaver-Burk plot. The binding distance and the transfer efficiency between cefoperazone and HSA were also obtained according to the theory of Förster' non-radiation energy transfer. The result suggested that the main binding force between cefoperazone and HSA is electrostatic force interaction. The high beta-lactamase stability of cefoperazone may be correlative with its molecular structure. The antibiotic activity and valency connect with transfer efficiency and dissociation constant. The effect of cefoperazone on the conformation of HSA was also analyzed using synchronous fluorescence spectrometry.

Algorithms↗
PubMed1989

Cefoperazone pharmacokinetics in patients with liver cirrhosis: a predictive value of the ujoviridin test.

Pharmacokinetics of cefoperazone was studied in 10 healthy volunteers and in 11 patients with liver cirrhosis. In the same persons, we also examined the clearance of ujoviridin--a preparation of indocyanine green. Within 12 h, 31.8 (+/- 7.6)% of the 2 g dose of cefoperazone was eliminated in the urine of healthy persons and 74.3 (+/- 7.9)% (mean +/- SD) was eliminated in the urine of cirrhotics. The biological half-life (beta-phase) of cefoperazone in healthy volunteers and in cirrhotics was 1.77 (+/- 0.25) and 4.29 (+/- 1.16) h, total clearance 1.009 (+/- 0.187) and 0.583 (+/- 0.169) ml/s and hepatic clearance 0.694 (+/- 0.174) and 0.152 (+/- 0.079) ml/s, respectively. The differences are statistically significant (p less than 0.001). We also found good correlation between total clearance of cefoperazone and clearance of ujoviridin (r = 0.842) and even better between hepatic clearance of cefoperazone and ujoviridin clearance (r = 0.957), both statistically significant. The findings suggest that the dosage of cefoperazone should be reduced in patients with liver cirrhosis and that the ujoviridin clearance test is a good indicator of impaired cefoperazone elimination.

Adult↗
PubMed1981

Clinical and laboratory evaluation of cefoperazone.

Cefoperazone, a third-generation cephalosporin derivative, has been reported to have excellent antibacterial activity against a wide range of gram-positive and gram-negative pathogens, including Pseudomonas aeruginosa. We treated 54 patients with a variety of clinical infections with cefoperazone and determined the susceptibilities of their 90 bacterial isolates. An additional 25 aerobic isolates obtained from patients treated with cefamandole in a comparison study were also tested for susceptibility to cefoperazone. Thus a total of 115 isolates were studied in vitro. One hundred nine (95%) of 115 bacterial isolates, including gram-positive and gram-negative aerobes and anaerobes, were susceptible to less than or equal to 32 microgram/ml. Only four isolates (three Escherichia coli and one Serratia marcescens) were highly resistant (minimal inhibitory concentration greater than or equal to 128 microgram/ml). We were able to assess clinical outcome of cefoperazone therapy in 53 patients; favorable responses (cure of improvement) were found in 48 (91%). P. aeruginosa was a major pathogen in three patients treated with cefoperazone; all three showed a favorable response. Side effects of cefoperazone therapy were noted in seven (13%) patients, and laboratory abnormalities were observed in 11 (20%) patients; all of these were mild and readily reversible. Cefoperazone thus appears to be safe, well tolerated, and suitable for use in a variety of human infections.

Bacterial Infections↗