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PubMed1987

Cefoperazone therapy of bacterial meningitis: a preliminary report.

Eleven hospitalized patients with bacterial meningitis were treated with cefoperazone at daily dosage ranging between 3 and 8 g intravenously. Seven patients had proven Gram-negative bacterial infections, but in four patients the aetiological agent remained unknown. Eight patients completely recovered from infection and the pathogens were eradicated, in one patient the treatment failed and in two patients only some improvement was registered. Furthermore in five patients cefoperazone serum and cerebrospinal fluid levels were determined four times in the first week of treatment (1st, 3rd, 5th and 7th day). No side-effects were recorded. Cefoperazone can be considered as effective antimicrobial agent in the therapy of bacterial meningitis.

Adolescent↗

PubMed1985

[In vitro antibacterial activity of cefodizime (HR 221) on 323 hospital strains of Gram negative bacilli. Comparison with cefotiam, cefoperazone, cefotetan and cefotaxime].

In vitro activity of a new cephalosporin, cefodizime, was investigated by comparison with cefotiam, cefoperazone, cefotetan and cefotaxime. 291 Enterobacteriaceae strains belonging to 6 cephalosporin-resistance phenotypes and 32 strains of oxidative Gram negative bacilli were tested. With modal MICs of 0.25 to 4 mg/l, cefodizime is active on most phenotypes of resistance to first or second generation cephalosporins demonstrated in vitro in Enterobacteriaceae, including strains resistant to cefamandole and intermediate to cefoxitin. Cefodizime fails to inhibit strains resistant to third generation cephalosporins (E. cloacae, C. freundii, P. stuartii), except for those strains of S. marcescens belonging to this phenotype whose modal MIC is 4 mg/l. 85% of all tested Enterobacteriaceae are inhibited by 4 mg/l and 91% by 8 mg/l. Cefodizime exhibits little activity against A. calcoaceticus and P. aeruginosa. Comparison of activities of the five cephalosporins against Enterobacteriaceae shows that cefodizime out-strips cefotiam, cefoperazone and cefotetan as a result of its broader spectrum of activity against tested species. Cefotaxime, on the contrary, proves superior to cefodizime and is still the most potent drug against. A. calcoaceticus whereas cefoperazone has the greatest effectiveness against P. aeruginosa.

Cefoperazone↗

PubMed1985

Hypoprothrombinaemia and bleeding during administration of cefamandole and cefoperazone. Report of three cases.

Deficiency of vitamin K-dependent coagulation factors caused by the cephalosporin derivatives cefamandole, cefoperazone and moxalactam has been recently recognized. It has been suggested that this adverse reaction may result from vitamin K deficiency caused by eradication of the vitamin K producing intestinal bacteria or inhibition of action of vitamin K 1. Three patients are described in whom hypoprothrombinaemic bleeding developed during administration of cefamandole or cefoperazone. All patients were elderly, had previous malnutrition or had been on parenteral nutrition without vitamin K supplementation. One patient had renal failure. Bleeding manifested 5-14 days after the start of antibiotic treatment. Other causes of the bleeding were excluded. One case was fatal and in 2 cases the coagulopathy was corrected by administration of vitamin K 1 or fresh frozen plasma and cessation of the antibiotic. We recommend prophylactic administration of vitamin K 1 during cefamandole or cefoperazone treatment to patients at risk, i.e. elderly malnourished patients especially those with renal failure or on parenteral nutrition.

Aged↗

PubMed1985

Transfer of cefoperazone into human skin fluid.

The transfer of cefoperazone into exudates from excoriated skin wounds was studied in 13 adolescent and adult patients. Subjects were given an intravenous bolus injection of 50 mg/kg of body weight. Concentrations of cefoperazone in serum and in exudate fluids were determined by bioassay using Escherichia coli as the test organism. Mean (+/- SD) cefoperazone concentration in serum reached 333.3 +/- 103.3 micrograms/ml 30 minutes after the injection and decreased to 16.4 +/- 5.7 micrograms/ml eight hours after the injection. In exudate fluids, the peak value was 52.7 +/- 22.1 micrograms/ml at one hour. Eight hours after the injection, the mean concentration in the exudate was 10.7 +/- 7.2 micrograms/ml, which was considerably above the minimum inhibitory concentrations for important pathogens.

Adolescent↗

PubMed1984

In vitro susceptibility tests with cefoperazone compared with cefotaxime, cefoxitin, cefuroxime, cephaloridine and gentamicin.

Minimum inhibitory concentrations (MICs), minimum bactericidal concentrations (MBCs) and sensitivity disc tests of cefoperazone, cefotaxime, cefoxitin, cefuroxime, cephaloridine and gentamicin were determined from 300 Gram-positive and -negative isolates from kidney transplant recipients. Cefoperazone inhibited 50% of Pseudomonas aeruginosa strains at a concentration of 6.25 micrograms/ml. Only gentamicin had similar activity but if we consider the sources of our strains and the nephrotoxicity of the compound, its use is not suitable. Moreover, cefoperazone was able to inhibit from 50% to 90% of the other strains at variable concentrations between 0.39 micrograms/ml and 3.12 micrograms/ml.

Bacteria↗

PubMed1982

Cefoperazone therapy of serious infections.

Cefoperazone was evaluated as the therapeutic agent in 64 adults with serious infections. Included were pneumonias, urinary tract infections, septicemia, osteomyelitis, joint infections, and superficial infections. A total of 84 organisms, including many multiantibiotic-resistant strains, were designated as the etiological agents. In most patients therapy was initiated before information on cefoperazone sensitivity of the infecting organism was available. This proved suitable in most instances. Clinical response to therapy was excellent in these individuals. Bacteriological responses coincided with the problems of the patient but did not reflect inadequacy of the antibacterial effect of cefoperazone. Adverse effects on renal function, including already impaired function, were not observed.

Adolescent↗

PubMed1982

In vitro combination effects of cefsulodin, moxalactam and cefoperazone with four aminoglycosides on nonfermenting nosocomial gram-negative bacteria.

The activity of moxalactam, cefsulodin and cefoperazone on 67 non-fermenting gram-negative bacterial strains isolated from patients with nosocomial infections was tested either alone or in combination with gentamicin, tobramycin, amikacin and netilmicin, respectively, by use of the checkerboard agar dilution technique. Cefsulodin was most active against Pseudomonas aeruginosa, cefoperazone was the most active cephalosporin tested against Pseudomonas fluorescens-putida and Acinetobacter antitratus. Cefoperazone-aminoglycoside interactions were found to be synergistic in only 2--5% of all strains, cefsulodin and moxalactam in combination with aminoglycosides were most potent against P. aeruginosa. Cefsulodin-gentamicin interactions were superior to other cephalosporin-amino-glycoside combinations.

Aminoglycosides↗

PubMed1982

[Comparison of antimicrobial activity and stability to beta-lactamases of cefoperazone, cefotaxime, lamoxactam and ceftriaxon].

Ceftriaxon (Ro 13-9904) is a new cephalosporin, whose structure resembles cefotaxime. This study compares the minimal inhibitory concentrations (MIC-s) of Ceftriaxon, cefoperazone, cefotaxime, lamoxactam and gentamicin against 622 isolates of various Enterobacteriaceae, non-fermenters and Aeromonas hydrophila. Furthermore the minimal bactericidal concentrations (MBC-s) were determined for some organism; additionally destruction of beta-lactamantibiotics in the presence of beta-lactamases was studied by a bioassay technique. The in vitro activity of Ceftriaxon against gramnegative bacteria was found very similar to that of cefotaxime. The susceptibility of Enterobacter sp. to the three cephalosporines was exceeded by lamoxactam while cefoperazone was the most active beta-lactam-antibiotic against Pseudomonas. Lactamases, which inactivated cefotaxime also destroyed Ceftriaxon in a greater extend. No hydrolysis of lamoxactam and cefoperazone occurred by nearly all bacterial extracts tested.

Bacteria↗

PubMed1984

Clinical efficacy of cefoperazone in obstetric and gynecologic infections.

Compared with second-generation cephalosporins, cefoperazone, a third-generation cephalosporin, has demonstrated an extended antibacterial spectrum. In addition, it has a long serum half-life and requires only twice-a-day administration. In this study, 66 patients with clinically diagnosed obstetric and gynecologic infections were treated with cefoperazone, and 61 were evaluated for efficacy. An overall cure rate of 93% (57 patients) was achieved. In view of the excellent clinical response and convenience of twice-a-day administration, we conclude that cefoperazone is a clinically useful single agent for the initial empirical treatment of patients with obstetric and gynecologic infections.

Abortion, Septic↗

PubMed1980

Bactericidal activity of cefoperazone in comparison with other beta-lactam antibiotics and gentamicin.

Killing curves were employed to determine the in vitro bactericidal activity of cefoperazone against several aerobic bacterial species of clinical origin. Cefoperazone was bactericidal at concentrations equal to, or greater than, the minimal inhibitory concentration (MIC) but allowed regrowth of the organisms after four to six hours when tested in concentrations of one-fourth or one-half the MIC. Comparative studies with gentamicin, LY127935 (moxalactam), piperacillin, cefamandole, and cephalothin indicate that, in general, cefoperazone demonstrated similar killing activity as other beta-lactam compounds, with some strain differences noted. Gentamicin, as the representative aminoglycoside, demonstrated a greater rate of bactericidal activity than the beta-lactam compounds studied.

Cefoperazone↗

PubMed1980

Clinical trials with cefoperazone in the field of internal medicine in Japan.

A total of 466 patients were treated with cefoperazone. The drug was usually administered by drip infusion of 2 to 4 gm/day. Therapy was described as markedly effective and moderately effective in 64 of 77 patients (83.1%) treated for urinary tract infections; 253 of 316 patients (80.1%) treated for respiratory infections; 37 of 48 patients (77.1%) treated for liver biliary duct infections; ten of 16 patients (62.5%) treated for septicemia; and seven of nine patients (77.8%) being treated for other infections. Overall, cefoperazone was effective 79.6% of all patients treated. With respect to bacteriological activity, the overall eradication rate for gram-negative organisms (including Pseudomonas aeruginosa, Klebsiella sp, Escherichia coli, Haemophilus influenzae, Enterobacter sp, and Proteus sp) was 81% (182/225) and for gram-positive (Staphyloccocus aureus, Streptococcus pneumoniae and Streptococcus faecalis) 90% (36/40). Of 205 patients who failed to respond to previous antibiotic therapy, 67.8% were treated effectively with cefoperazone. Side effects, such as skin eruption, pyrexia and diarrhea, occurred in only 4.8% of patients treated, while laboratory abnormalities, such as elevated glutamic-oxaloacetic transaminase, glutamic-pyruvic transaminase, alkaline phosphatase, and eosinophil values, occurred in only 6.4% of the treated patients. None of these abnormal values were of clinical significance.

Adolescent↗

PubMed1980

Susceptibility of anaerobic bacteria to cefoperazone and other beta-lactam antibiotics.

The in vitro activity of cefoperazone was tested against 155 clinical isolates of anaerobic bacteria and compared to that of cefoxitin, LY127935 (moxalactam), cefotaxime, cefamandole, and cephalothin. Against the Bacteroides fragilis group, the compound was as active as LY127935, but less active than cefoxitin. Cefotaxime was less active than cefoperazone, cefoxitin, and LY127935. Cefoperazone, as well as cefoxitin, LY127935, and cefotaxime, exhibited excellent activity against all other anaerobic organisms tested. Cefamandole and cephalothin showed inferior activity when compared to the other four drugs.

Bacteroides↗

PubMed1981

[Pharmacokinetic study of a cephalosporin, cefoperazone, in liver failure].

The pharmacokinetics of cefoperazone, a semi-synthetic cephalosporin for parenteral use with a spectrum covering P. aeruginosa, E. cloacae, indole-positive Proteus and S. Marcescens, was studied after a 2-h intravenous infusion of 2 g of the drug in 6 patients with moderate liver function impairment (viral hepatitis in 4 cases, alcoholic fatty liver and cirrhosis in 2 cases). At the end of the infusion, mean serum concentrations (determined by a bioassay) were 208 microgram/ml in the patients and 134 microgram/ml in healthy volunteers. The half-life was 4.3 h in patients and 1.6 h in healthy volunteers. Volume of distribution and renal clearance were similar in the two groups. Extrarenal clearance of cefoperazone was lower in the patients (7.3 ml/min) than in the control group (59.4 mg/min). Urinary excretion of biologically active drug was markedly increased in the patients (79% of the dose) compared with healthy volunteers (24%). This study provides evidence that liver function impairment increases with both the apparent half-life of elimination and the urinary excretion of the drug. The results raise the question of the desirability of cefoperazone dosage adjustment in patients with hepatic diseases.

Adult↗

PubMed1981

[Investigation on the antimicrobial activity of cefoperazone (author's transl)].

Cefoperazone has the usual antimicrobial spectrum of the cephalosporins, but the ratios of resistance to the various bacterial strains - even if they are problematic-are very low. It remains to be seen, however, whether a widespread use of the drug induces an increase in the number of resistant strains. An outstanding advantage of cefoperazone is its efficacy against Pseudomonas aeruginosa; only one of 75 strains investigated was resistant. In the case of Providencia, an important germ in the field of urology that is often difficult to be affected by antibiotics, we could not find any resistant strains. We did, however, find moderate sensitive strains. Concerning Enterococci we did not find any resistant strains, but 96% of the strains were classified as moderate sensitive. That leads to the conclusion that the drug should only be effective in high dosage, when Enterococci are found. Even multi-resistant bacterial strains still respond considerably to cefoperazone. This applies in particular to Pseudomonas aeruginosa.

Anti-Bacterial Agents↗

PubMed1981

[Concentration of cefoperazone in various tissues of the urogenital system (author's transl)].

Within the framework of perioperative short-term prophylaxis against infections, serum and tissue concentrations were investigated after a single i.v. bolus injection of 2.0 g cefoperazone (Cefobis), a semisynthetic cephalosporin parenterally applicable, in 30 patients with a prostatic adenoma. The mean serum concentrations ranged from 82.0 micrograms/ml at 30 min to 41.9 micrograms/ml at 150 min following the injection decreasing continuously. The corresponding mean concentrations in the tissue of prostatic adenoma were 17.8 micrograms/g and 13.9 micrograms/g, the maximum concentrations were found 90 min after the injection with 21.6 micrograms/g. Most differing concentrations were found in 14 kidneys 90 min after injection. The individual values varied between 5.5 micrograms/g and 70.2 micrograms/g. These ranges of variation must be attributed to the differing clinical and histological diagnoses of the collected organs with highly differing degrees of function. Effective levels of 7.0 micrograms/g to 28.9 micrograms/g were found at different times in 13 testes of 14 patients undergoing plastic orchidectomy because of a carcinoma of the prostata. Average concentrations of 10.3 micrograms/g to 13.2 micrograms/g in the ureter, adipose tissue and muscle were within the therapeutically effective range. The high cefoperazone concentrations found in serum and different tissues lead us to expect successful therapy when cefoperazone is used to treat bacterial infections with sensitive pathogens in the urogenital tract.

Adenoma↗

PubMed1984

A multicenter clinical study of cefoperazone.

Thirty-five adult and 11 pediatric patients in nine Philippine hospitals were treated with cefoperazone for various moderate to severe infections. Adults received 1 to 8 gm/day and children received 0.450 to 4 gm/day in two divided doses, for a mean period of eight to nine days (ranges, 5 to 11 days for children and 5 to 30 days for adults). The efficacy rate (cured and improved) was 90.90% for pediatric patients and 85.72% for adult patients. In a group of patients shifted from other antibiotic regimens, efficacy rates were 100% for pediatric patients and 85% for adult patients treated with cefoperazone. No follow-up cultures were obtained from patients from whom 26 pathogens were isolated, but correlations between the isolates and clinical efficacy showed that cefoperazone had an efficacy rate of 92.3%.

Adolescent↗

PubMed1995

[Comparative in vitro activity of ampicillin, cefoperazone and their combinations with sulbactam, as well as that of other antibiotics against anaerobic organisms].

Susceptibility of 180 strains of anaerobic organisms to ampicillin, cefoperazone and their combinations with sulbactam, as well as that to cefoxitin, imipenem and metronidazole was studied with the method of serial microdilutions. 100 per cent of the strains was susceptible to the ampicillin + cefoperazone combination. Only 1 strain of Bacteroides fragilis was resistant to imipenem. 73.4 and 57.8 per cent of the B. fragilis strains were susceptible to cefoxitin and cefoperazone respectively. No resistance to metronidazole was detected. 100 per cent of the strains belonging to Bacteroides spp. fragilis (gr.) and Prevotella spp. was resistant to all the antibiotics except ampicillin. Gram-positive anaerobic cocci were susceptible to all the antibiotics. The strains of Actinomyces spp. and Propionibacterium acnes were resistant to metronidazole. Only 48.7 per cent the Actinomyces strains was susceptible to cefoxitin.

Ampicillin↗

PubMed1994

[Cefoperazone in the prevention and treatment of experimental plague caused by typical and fraction-free pathogen strains in white mice].

The high susceptibility of the plague microbe to cefoperazone (MIC of 0.1-0.25 microgram/ml) did not depend on the causative agent ability to produce fraction I. Cefoperazone, a 3rd generation cephalosporin, was highly active in the treatment of experimental plague caused by the plague microbe strain typical in the antigen composition: the drug daily dose of 250-500 mg/kg provided an 80-100 percent survival of the albino mice. The efficacy of cefoperazone lowered when the infection was caused by the strain defective in the capsule antigen. The use of the antibiotic for more prolonged periods provided better results of the etiotropic therapy.

Animals↗