Search PubMed⌕ Search

SEARCH · Search PubMed

Results for “Cefoperazone”

Search indexed PubMed citations on genomics, clinical trials, systematic reviews and public health. Explore titles, authors and supplied subject terms, then open the PubMed record.

Quote a phrase for an exact phrase match. Source license links do not imply unrestricted reuse.

At least 127 records · Page 7Linked to original sources

Economic examination of cefoperazone therapy.

Medical records of 1137 patients from 35 hospitals were reviewed to examine the total cost of care for patients receiving cefoperazone as initial therapy compared to a control group receiving alternative agents. The direct costs of care measurable through a retrospective review of patient records were examined, including the cost of antibiotic acquisition, drug administration, laboratory testing, and room and board. Results of a regression analysis show that cefoperazone as initial therapy is associated with lower costs for all factors studied except acquisition cost. Antibiotic acquisition averaged $24 per patient more for the cefoperazone group (p less than 0.01). However, for cefoperazone patients drug administration was $63 less (p less than 0.0001), laboratory testing costs averaged $9 less (p = 0.22), and costs associated with room and board charges were $80 less (p = 0.40). Total costs averaged $3073 per cefoperazone patient and $3228 per control patient (p = 0.20). These data suggest that the previously accepted definitions of antimicrobial costs (i.e., cost per gram, cost per dose, cost per day) may no longer be adequate in this era of cost containment. In order to make sound clinical decisions with lowest total costs, practitioners should identify how and where costs are incurred.

Anti-Bacterial Agents↗

Steady-state pharmacokinetics of cefoperazone and sulbactam in patients with acute appendicitis.

OBJECTIVE: To determine the steady-state pharmacokinetics of intravenously administered cefoperazone and sulbactam when given in combination to patients with acute appendicitis. METHODS: Six patients with normal renal and hepatic function received cefoperazone 2 g with sulbactam 1 g prior to appendectomy and then every 12 hours. Serial blood samples were collected after each patient received at least three doses of cefoperazone/sulbactam. RESULTS: Cefoperazone and sulbactam could be best described by a two-compartment model. Mean +/- SD values for cefoperazone steady-state volume of distribution (Vssd), elimination half-life (t1/2 beta), clearance (Cl), and area under the curve (AUC0-t) were 19.8 +/- 8.0 L, 3.97 +/- 1.06 h, 62.6 +/- 16.3 mL/min, and 556.9 +/- 122.0 mg.h/L, respectively. Sulbactam Vssd, t1/2 beta, Cl, and AUC0-t were 34.7 +/- 13.9 L, 1.39 +/- 0.4 h, 288.6 +/- 68.2 mL/min, and 64.8 +/- 24.5 mg.h/L, respectively. CONCLUSIONS: Compared with data from healthy volunteers, cefoperazone exhibited a decreased Cl and increased Vssd and t1/2 beta in patients with acute appendicitis. An increased Vssd also was observed for sulbactam. The disposition of cefoperazone/sulbactam is altered in this group of patients; however, these changes are not likely to warrant a dosage reduction.

Acute Disease↗

First occurrence of transferable extended-spectrum beta-lactamase hydrolyzing cefoperazone in multiresistant nosocomial strains of Klebsiella pneumoniae from two hospitals in Czech and Slovak Republics.

The occurrence of positive synergy between antibiotic discs of amoxicillin/clavulanate and cefoperazone was registered in two Klebsiella pneumoniae strains, isolated from hospitals in Czech and Slovak Republic, indicating the presence of genes coding for an extended-spectrum beta-lactamase active also against cefoperazone, a broad-spectrum cephalosporin. Sulbactam inhibited the hydrolysis of cefoperazone by cell-free lysates of these strains which substantiates its use in combination with cefoperazone. Resistance to cephalothin, cefotaxime, ceftazidime, cefoperazone, cefepime and aztreonam was transferred from K. pneumoniae isolates to Escherichia coli K-12 3110 and to Proteus mirabilis P-38 recipient strains.

Amoxicillin-Potassium Clavulanate Combination↗

Potential value of cefoperazone in bacterial meningitis: experimental studies.

To assess the potential value of cefoperazone in treating bacterial meningitis, its pharmacokinetics in the cerebrospinal fluid of rabbits were studied. Cefoperazone penetrated poorly into the cerebrospinal fluid of rabbits with uninflamed meninges, but in the presence of meningitis concentrations increased 2- to 3-fold. These concentrations were above the minimum inhibitory concentrations for the majority of Enterobacteriaceae, indicating the potential value of cefoperazone in treating bacterial meningitis. The half-lives of cefoperazone and moxalactam in cerebrospinal fluid, measured by a bioassay, were marked prolonged by meningeal inflammation. In contrast, the half-life of cefotaxime in cerebrospinal fluid was short. Consequently both cefoperazone and moxalactam provided significantly better antibacterial effect in cerebrospinal fluid than did cefotaxime.

Animals↗

[Comparative analysis of the effectiveness and costs of azithromycin and cefoperazone treatment of patients during COPD exacerbation].

UNLABELLED: The effectiveness and costs of azithromycin and cefoperazone treatment of COPD exacerbation have been analysed in this study. Forty patients at the mean age of 65.9 (+/- 11.5) years were enrolled. The subjects were randomly selected and treated either with cefoperazone 2 x 1.0 g i.v. daily (group I = 20 persons) or with azithromycin 1 x 0.5 g (group II = 20 persons), in sequential method. Body temperature, cough intensity, quality and quantity of expectorated sputum, number of breaths per minute and adverse events were recorded daily. The values of pulmonary function tests and leucocytosis were assessed three times during the study. Statistically significant differences between both groups have been found with respect to the mean time of staying in hospital (9.1 days--group I vs 6.1 days--group II), mean total duration of antibiotic therapy (10.1 days--group I vs. 6.6 days--group II) and duration of intravenous antibiotic therapy only [7.5 days (group I) vs 2.9 days (group II)] (p < 0.05). Taking into account the duration of hospitalization, it was shown that the mean total costs of treatment of COPD exacerbation with azithromycin was significantly lower than that of treatment with cefoperazone (2375.9 PLN and 1663.7 PLN, respectively) (p < 0.05). CONCLUSIONS: The effectiveness of treatment with azithromycin in patients with COPD exacerbation was evident. The total costs of treatment of COPD exacerbation with azithromycin is lower than with cefoperazone. Both azithromycin and cefoperazone are safe in the treatment of exacerbation of COPD.

Acute Disease↗

[Prevention and treatment with cefoperazone of postoperative suppurative complications in heart surgery].

Clinical trials of cefoperazone (cefobid, Pfizer, USA) were carried out in 49 patients with cardiovascular diseases who had undergone surgical operations. The pathogens of infectious complications were investigated bacteriologically. Good results of the treatment were observed in 43 patients. Allergic reaction developed in 1 patient. Cefoperazone was shown advantageous in treatment of pulmonary complications in the operated patients. It was found possible to use cefoperazone in combination with aminoglycosides. Cefoperazone was found to be one of the drugs of choice in the treatment of aerobic and anaerobic bacteriemia, as well as sepsis after surgical operations on the heart and great vessels. The results on the use of cefoperazone for short-term "perioperative" prophylaxis in cardiosurgery (in accordance with the WHO instructions) are also presented.

Aortic Valve↗

Compatibility of cefoperazone sodium and furosemide in 5% dextrose injection.

The compatibility of cefoperazone sodium and furosemide in 5% dextrose injection stored at two temperatures was studied. Cefoperazone sodium and furosemide were added to 5% dextrose injection to achieve a cefoperazone concentration of 10 mg/mL and a furosemide concentration of 0.2 mg/mL. The admixture was stored in 100-mL vented i.v. containers in the dark under refrigeration (4 degrees C) and at room temperature (25 degrees C); three containers were stored at each temperature. A 1-mL sample was taken from each i.v. container immediately after preparation and after 1, 2, 5, 10, 15, 20, and 25 days to be inspected visually, checked for pH value, and analyzed by a stability-indicating high-performance liquid chromatographic method. No color change or precipitation was observed in any sample at any time during the study. More than 95% of the initial concentrations of both drugs remained for five days at 4 degrees C but for only two days at 25 degrees C. Cefoperazone sodium was somewhat more stable than furosemide under the same storage conditions for 25 days; however, less than a 2% difference between the drugs was noted. Under the conditions of this study, cefoperazone sodium 10 mg/mL and furosemide 0.2 mg/mL in admixtures in 5% dextrose injection are stable for only two days at 25 degrees C and five days at 4 degrees C.

Cefoperazone↗

Reversal by cefoperazone of resistance to etoposide, doxorubicin, and vinblastine in multidrug resistant human sarcoma cells.

The cephalosporins are a family of semisynthetic antibiotics, some of which have structural features associated with substrates for the multidrug transporter, P-glycoprotein. The activity of a series of six cephalosporins in reversing multidrug resistance (MDR) was examined in MDR variants (Dx5 cells) of the human sarcoma line MES-SA. Dx5 cells express high levels of the mdr1 gene product P-glycoprotein and are 25- to 30-fold resistant to doxorubicin (DOX), etoposide (VP-16), and vinblastine (VBL). Cytotoxicity was measured by the MTT assay. Cefoperazone (1.0 mM) was the most effective modulator of MDR, lowering the IC50 for VP-16 by 29-fold (29x), for VBL by 16x, and for DOX by 14x. Ceftriaxone at 1.0 mM produced 10x modulation of VP-16 cytotoxicity, 8x for DOX, and 2x for VBL. The reversal of resistance was concentration dependent, decreasing to 4x and 5x, respectively, for DOX with 0.25 mM cefoperazone and ceftriaxone. No modulation of cytotoxicity was observed in the parental MES-SA cells, which do not express mdr1. Cefazolin, cefotetan, cephradine, and ceftazidime were ineffective, producing less than 5x modulation of DOX at 1.0 mM. Among these cephalosporins, cefoperazone and ceftriaxone were the most highly protein bound in the media (30 and 52%), and the most lipid soluble, with octanol/water partitioning coefficients of -0.49 and -0.60. Varying the serum concentration in medium from 5 to 50% had less than a two-fold effect on the modulation of MDR by ceftriaxone. The ability to reverse MDR among these agents is associated with lipid solubility, high protein binding, a polycyclic planar geometry, and the presence of the piperazine group in cefoperazone. These data and the potential for achieving high tissue concentrations indicate that cefoperazone merits further study as a modulator of MDR.

Cefoperazone↗

Pharmacokinetics of single doses of cefoperazone given by the intravenous and intramuscular routes to unweaned calves.

Cefoperazone pharmacokinetics were studied in unweaned calves. The antibiotic was administered to 10 calves intravenously, to eight calves intramuscularly at 20 mg kg-1 and to 10 calves intramuscularly at 20 mg kg-1 together with probenecid at 40 mg kg-1. Serum concentration versus time data were analysed by non-compartmental methods based on the statistical moment theory. The intravenous data were also fitted by a linear, open two-compartment model. The terminal halflife of cefoperazone was 127.9 +/- 28.2 min (mean +/- SD) after intravenous and 136.9 +/- 19.6 min after intramuscular administration. The t1/2 was increased to 257.3 +/- 127.3 min by the co-administration of probenecid. The total body clearance was 8.16 +/- 1.60 ml min-1 kg-1 and the volume of distribution at steady state was 0.713 +/- 0.167 litre kg-1. The mean residence time values were 87.2 +/- 10.6 min after intravenous and 140.3 +/- 20.6 min after intramuscular injection and were increased to 264.5 +/- 99.8 min by the co-administration of probenecid. The estimated mean absorption time was 53.1 min and the estimated bioavailability after intramuscular administration was 76.3 per cent. The minimal inhibitory concentration (MIC90) values of cefoperazone ranged from 0.5 to 2 micrograms ml-1 for Escherichia coli, salmonella groups C, D and E and Pasteurella multocida isolates. Salmonella group B strains appeared to be highly resistant to cefoperazone with MIC90 greater than 32 micrograms ml-1. There were no significant differences between the pharmacokinetic variables calculated by statistical moment theory or compartmental analysis indicating central compartment output of cefoperazone.(ABSTRACT TRUNCATED AT 250 WORDS)

Absorption↗

[Clinical studies on cefoperazone in renal transplantation].

Two grams of Cefoperazone was intravenously administered twice a day for 5 days by drip infusion to 10 donors and 9 recipients after renal transplantation. The concentration of cefoperazone in the blood after administration in both donors and recipients did not show any accumulation tendency. The urinary recovery rate of cefoperazone for 24 hours in donors was 8.8% and that in recipients was 8.1%. There was no change in the renal function in donors after administration of cefoperazone. No change was observed in blood examination, BUN or creatinine, but S-GOT and S-GPT showed a temporary increase in 1 donor and 1 recipient. It is considered that Cefoperazone is a very useful drug for prophylactic chemotherapy after renal transplantation.

Adolescent↗

[Comparative clinical trial of cefoperazone versus ampicillin + tobramycin in severe bronchopulmonary and pleural infectious pathology].

This study involved an open trial with parallel randomised series receiving either cefoperazone (2 g/d) or a combination of ampicillin (6 g/d) and tobramycin (3 to 4 mg/kg/d). The 30 patients included were of both sexes (male predominance), hospitalised, aged 62 +/- 11,5 years and suffering from a severe bronchopulmonary or pleural infection. Underlying pathology was serious (neoplasm, C.O.D.L., bronchiectasis, cardiac pathology). No significant difference was seen in the sampling of the two populations. Cefoperazone was prescribed in 2 infusions per 24 hours. Ampicillin was given as 3 infusions, followed by tobramycin administered by a similar number of injections. The duration of treatment was 16.8 +/- 9 days (cefoperazone) and 11,8 +/- 6,5 days (ampicillin + tobramycin). Overall evaluation (clinical, radiological and laboratory criteria) showed 88% (cefoperazone group) and 71% (ampicillin + tobramycin group) recovery and improvement rates. There were two failures in the cefoperazone group and 6 failures in the other group. These results were not statistically different. Three of the 6 failures could be attributed to resistance of the initial bacteria or selected by one or other type of treatment. None of the antibiotics prescribed raised any acceptability problems.

Aged↗

Asian multicenter trial of cefoperazone in respiratory tract infection.

The safety and clinical efficacy of cefoperazone were evaluated in a multicenter trial conducted at institutions in Japan, Korea, and Taiwan. Cefoperazone was given as the sole antibiotic for 481 respiratory tract infections in 476 patients. An overall satisfactory clinical response was achieved in 73.7% of patients. Cefoperazone was effective in 78.9% of cases of pneumonia, 81.1% of acute exacerbations of chronic bronchitis, and 69.4% of bronchiectasis with infection. A satisfactory bacteriological effect was obtained in 93.2% of cases in which Haemophilus influenzae was isolated, 70.2% of Klebsiella infections, and 84.6% of infections with Streptococcus pneumoniae. Although the eradication rate was only 38.6% in patients with Pseudomonas aeruginosa, the success rate increases to 59.1% if patients showing a decrease in the number of organisms are included. Cefoperazone was effective in 63.5% of the 148 cases that had failed to respond to treatment with other antibiotics. Adverse reactions occurred in 8.0% of patients and consisted primarily of rash, diarrhea, and fever. Cefoperazone appears to be an extremely useful injectable antibiotic for the treatment of respiratory tract infections in hospitalized patients.

Adolescent↗

[In vitro comparative activity of 4 beta-lactams against Pseudomonas aeruginosa. Role of cefoperazone].

The authors compared in vitro activity of cefoperazone, piperacillin, carbenicillin and ceftazidime against 100 clinical isolates of Pseudomonas aeruginosa. Minimal inhibitory concentrations (MICs) were determined by the agar dilution method. Minimal bactericidal concentrations were measured using microplates. Eighty-two percent of strains were susceptible or intermediate to cefoperazone, with MICs less than 30 micrograms/ml. The geometric mean of the MICs of cefoperazone was 14.3 micrograms/ml; MIC 50 was 6.9 micrograms/ml. Activity of cefoperazone was comparable to that of carbenicillin, to which eighty-three percent of strains were susceptible, with MICs less than or equal to 128 micrograms/ml. Ceftazidime was also highly active against Pseudomonas, with a mean MIC of 3.29 micrograms/ml. MIC 50 was 1.9 micrograms/ml. Piperacillin was slightly less active, with MICs less than or equal to 32 micrograms/ml for 35% of strains. Cefoperazone exhibited bactericidal activity on 50% of strains at a 28.8 micrograms/ml concentration. These values must be interpreted with caution as they do not allow for the phenomenon of regrowth of Pseudomonas aeruginosa due to the presence of microaggregates of the bacteria in vivo despite bactericidal concentrations of antibiotic.

Anti-Bacterial Agents↗

Cefoperazone pharmacokinetics and sputum levels after single/multiple i.m. injections in bronchopneumopathic patients and bone, pulmonary and prostatic tissue penetration.

Cefoperazone is a third-generation semisynthetic injectable cephalosporin. It has been reported that cefoperazone has beta-lactamase resistance and quite a broad antimicrobial spectrum against many Gram-positive and Gram-negative microorganisms and most anaerobes. In this study, the pharmacokinetics of cefoperazone were examined in a group of 10 patients suffering from acute exacerbations of chronic bronchitis, with purulent or mucopurulent expectorations. Cefoperazone was administered at the dose of 1 g i.m. every 12 hours. Serum and urinary parameters and the profile of bronchial mucus diffusion were assessed after the first administration and during the whole period of treatment which lasted for 7 days. In a second, third, and fourth group of volunteer patients who had to undergo surgical operations, bone, lung and prostatic penetration of cefoperazone was determined in correlation with serum levels.

Bone and Bones↗

Risk of bleeding and hypoprothrombinaemia associated with NMTT side chain antibiotics: using cefoperazone as a test case.

A retrospective cohort study was performed to determine the incidence of hypoprothrombinaemia and bleeding in patients receiving cefoperazone, a third-generation cephalosporin that contains an NMTT side chain. 374 patients receiving cefoperazone from February 1983 to March 1986 at a teaching hospital in Philadelphia were compared with 497 patients receiving either ceftizoxime or cefotaxime during the same period, and with 476 patients receiving ceftazidime from April 1985 to December 1987. Adverse events (any bleeding episodes, decrease in haemoglobin, prolongation of prothrombin time (PT), and prolongation of partial thromboplastin times (PTT)) were evaluated, if occurring during the period from the start of cephalosporin therapy, or the start of therapy with one of the two control drugs, for 14 days after the last date of the first course of therapy were recorded. An increased risk of hypoprothrombinaemia was associated with the use of cefoperazone: the prothrombin time was prolonged by 5 s or more in 12.3% of patients receiving cefoperazone vs. 5.8% of patients receiving ceftizoxime or cefotaxime, and vs. 5.8% receiving ceftazidime; the adjusted odds ratios (95% CIs) were 3.6 (1.7-7.4) and 3.8 (1.8-7.8), respectively, and these increased at higher doses of cephalosporin. No protection was apparent from the administration of vitamin K prior to or during the course of cephalosporin. No overall increased risks were observed for bleeding (adjusted odds ratios (95% CIs) were 1.1 (0.8-1.4) vs. ceftizoxime or cefotaxime, and 0.9 (0.6-1.2) vs. ceftazidime), decrease in haemoglobin, or increased partial thromboplastin time. In subgroup analyses, increased risks of bleeding were observed with high dose cefoperazone use [2.8 (1.5-5.5) vs. ceftizoxime or cefotaxime, and 2.3 (1.1-4.6) vs. ceftazidime]. Patients receiving NMTT side chain antibiotics should be monitored for hypoprothrombinaemia, but any increase in bleeding is likely to be small, and prophylactic vitamin K is probably not warranted.

Journal Article↗

Specific determination of unbound oxacillin in protein solution with cefoperazone by high-performance frontal analysis with chemiluminescence detection.

Unbound oxacillin concentrations in human serum albumin (HSA) solutions in the presence or absence of cefoperazone were determined using high-performance frontal analysis coupled with chemiluminescence detection (HPFA-CL). The HPFA was performed on an ISRP column with 67 mM potassium phosphate buffer of pH 7.4 and ionic strength of 0.17 as the mobile phase. The luminol-H(2)O(2)-Co(2+) system was employed in the chemiluminescence detection. The detection was highly specific for oxacillin in the presence of cefoperazone. Although both drugs in HSA solutions co-eluted in the same region in HPFA, cefoperazone did not interfere with the determination of unbound concentration of oxacillin. In the solution of 100 microM HSA and 11.33 micro M oxacillin the bound percentage of oxacillin to HSA was estimated as 80.5%. Addition of 30.98 micro M cefoperazone into the HSA-equilibrated solution produced little effect on the protein binding of oxacillin. In the presence of 154.9 micro M cefoperazone, however, the bound percentage of oxacillin was significantly reduced. This specific method could be applied to the investigation of drug-drug interaction in protein binding.

Chromatography, High Pressure Liquid↗

Rat renal organic anion transporter rOAT1 mediates transport of urinary-excreted cephalosporins, but not of biliary-excreted cefoperazone.

Most cephalosporin antibiotics are excreted into urine via glomerular filtration and active tubular secretion by renal organic anion transporters. In this study, we investigated the interaction of cephalosporins with rat organic anion transporter rOAT1, mainly expressed at the basolateral membrane of the renal proximal tubules, using Xenopus laevis oocytes, to assess the roles of rOAT1 in renal excretion of cephalosporin antibiotics. The expression of rOAT1 significantly stimulated the uptake of cefazolin, cefotiam and cephalexin into oocytes, but not of cefoperazone. The inhibition constants of these cephalosporins to rOAT1-mediated p-aminohippurate (PAH) uptake were 72 microM for cefazolin, 298 microM for cefoperazone, 718 microM for cefotiam and 6 mM for cephalexin. Eadie-Hofstee plot analysis revealed that cefoperazone as well as cefotiam inhibited rOAT1-mediated PAH uptake competitively. These results suggest that rOAT1 mediates basolateral uptake of cephalosporin antibiotics in the renal tubules. Furthermore, it is suggested that a minor contribution of the kidney to cefoperazone excretion could be related to the finding that cefoperazone is a poor substrate of rOAT1.

Journal Article↗

Antimicrobial activity, pharmacokinetics, adverse reactions, and therapeutic indications of cefoperazone.

Cefoperazone is a parenteral cephalosporin antibiotic that is pending approval by the U. S. Food and Drug Administration. Compared to most other cephalosporins cefoperazone has a greatly expanded spectrum of bactericidal activity that encompasses most aerobic gram-positive bacteria except enterococci, most aerobic gram-negative bacteria, including a majority of Pseudomonas aeruginosa strains, and a number of pathogenic anaerobic bacteria. Its long serum half-life, approximately two hours, permits a twelve hourly dosing schedule. No dosage modification is required in patients with renal insufficiency, and only minor modification is needed in patients with hepatic insufficiency or biliary obstruction. Clinical trials have established cefoperazone's efficacy in lower respiratory tract infections, urinary tract infections, and a variety of other bacterial infections. Adverse reactions have been infrequent, and few serious reactions have been identified. Cefoperazone is a promising new agent for the treatment of gram-negative bacillary and polymicrobial infections, especially in settings that require empiric therapy.

Bacteria↗