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PubMed1983

Cefoperazone pharmacokinetics in acute childhood meningitis.

We studied the serum pharmacokinetics and cerebrospinal fluid concentrations of cefoperazone in 15 children with acute meningitis. Mean cefoperazone concentrations of 117 micrograms/ml in the serum and 3.8 micrograms/ml in the cerebrospinal fluid were noted 2 hours after a single 100 mg/kg dose. Following multiple 50 or 100 mg/kg doses, the mean peak serum cefoperazone concentrations were 232 and 498 micrograms/ml, respectively, with an overall mean elimination phase half-life of 2.12 hours. The data best fit a linear, two-compartment model. Cerebrospinal fluid concentrations 1.5 to 2.5 hours after the end of cefoperazone infusions ranged from 1.4 to 19.2 micrograms/ml for all doses and states of illness. This represented 1.2% to 6.4% of simultaneous serum values. The cerebrospinal fluid inhibitory titer was greater than or equal to 1:16 in 17 of 18 specimens tested against a strain of Haemophilus influenzae type b resistant to both chloramphenicol and ampicillin. In the doses given, cefoperazone produces adequate cerebrospinal fluid concentrations and bioactivity to treat the common bacterial forms of acute meningitis in infants and children.

Acute Disease↗
PubMed1996

A comparative study of the binding characteristics of ceftriaxone, cefoperazone and cefsulodin to human serum albumin.

The binding to human serum albumin of three cephalosporins of pharmacological interest: cefoperazone, ceftriaxone and cefsulodin was studied by ultrafiltration and differential scanning calorimetry methods. The identification of the binding sites in albumin was also performed using probes for the so-called sites I, II, bilirubin and fatty acids binding sites. Albumin showed two types of binding sites for cefoperazone and ceftriaxone, while for cefsulodin it showed a single type of binding site. The affinity values were: 5.6 10(4) M-1 and 3.1 10(4) M-1 for cefoperazone and ceftriaxone respectively, while cefsulodin showed low affinity (3.8 10(2) M-1). It was found that only cefoperazone interacted in a slight way with site I on serum albumin, while site II and the bilirubin binding site have capacity of binding the three cephalosporins assayed. Ceftriaxone and cefoperazone showed capacity to bind to the fatty acids binding site on albumin. These cephalosporins increased the thermal stability of the protein, suggesting that these ligands are favouring the compact structure of the native form of the protein more than the unfolded form.

Binding Sites↗
PubMedDate not supplied

Comparative pharmacokinetics of moxalactam, cefoperazone, and cefotaxime in normal volunteers.

The pharmacokinetic parameters of moxalactam were compared with those of cefoperazone and cefotaxime in normal volunteers in a crossover manner. Following 30-min intravenous infusions of 2 g of each of the three antibiotics, serum levels at 1 hr were slightly lower for moxalactam (88 micrograms/ml) than for cefoperazone (112 micrograms/ml) but more than three times those obtained for cefotaxime (29 micrograms/ml). By 8 hr, levels of moxalactam (9.2 micrograms/ml) were slightly higher than those of cefoperazone (6.5 micrograms/ml), and levels of cefotaxime in serum were unmeasurable (less than 1 micrograms/ml). These values reflect differences in half lives of the three agents. Peak serum levels following intramuscular injection and serum levels during constant intravenous infusion were similar for moxalactam and cefoperazone because of counterbalancing differences in the apparent volume of distribution and rates of elimination of the two antibiotics. Serum levels of cefotaxime were much lower than those of the other two antibiotics primarily because of the rapid elimination of cefotaxime from the body. The kidney was the major route of excretion of moxalactam, whereas extrarenal mechanisms were more important for elimination of cefoperazone. These differences in pharmacokinetics may have significant implications for the clinical use of these new antibiotics.

Adolescent↗
PubMedDate not supplied

Pharmacokinetics of cefoperazone in patients with normal and impaired hepatic and renal function.

The pharmacokinetics of cefoperazone in normal subjects and in patients with hepatic and renal dysfunction are reviewed. Peak serum concentrations and areas under serum level-time curves are linearly related to dose. The range of mean peak serum concentrations after a 2-g dose of cefoperazone is 202-375 micrograms/ml with iv injection or infusion and 111 micrograms/ml with im injection. The serum half-life is 1.6-2.6 hr. Urinary excretion is rapid, but only 15%-37% of the dose is recovered in urine. The drug is not metabolized significantly. Levels of drug in bile are many times higher than serum levels, and biliary excretion represents the major pathway of cefoperazone elimination. Serum kinetics of cefoperazone are not significantly altered by renal impairment. However, hepatic dysfunction is associated with a two- to fourfold increase in serum half-life. Even in these patients, drug accumulation was not observed after repeated administration of 1 g of cefoperazone at 12-hr intervals. Major dosage modification should only be required with concomitant renal and hepatic dysfunction.

Biliary Tract Diseases↗
PubMedDate not supplied

Use of cefoperazone in the empiric treatment of serious skin infections.

This report summarizes the results of a six-center clinical trial of cefoperazone as empiric therapy for hospitalized patients with serious infections of the skin and skin structures. Cefoperazone was administered in doses of 2-4 g once every 12 hr by iv infusion over 15-30 min or im injection. Results of therapy were evaluated for 39 of the 46 patients enrolled in the study. Of these 39 patients, 30 had a satisfactory clinical response to cefoperazone therapy, six had a partly satisfactory response, and three had an unsatisfactory response. A total of 78 pathogens were isolated from infected sites of the 39 patients, and MICs were determined for 62 of these pathogens. Of the 78 isolated pathogens, 63 (including five of eight isolates of Pseudomonas aeruginosa) were eradicated by cefoperazone. It is concluded that cefoperazone is a suitable antibiotic for empiric therapy for infections of the skin and skin structures of hospitalized patients.

Cefoperazone↗
PubMed1984

A comparison of cefotaxime and cefoperazone in respiratory tract infections.

The clinical efficacy and safety of cefotaxime and cefoperazone were evaluated in a comparative study. There were 18 adult males and 11 females. Their underlying disease was pneumonia (10), pleural empyema (2), bronchiectasis (6), bacterial bronchitis (9), lung abscess (2). Bacterial material included sputum, bronchial secretion gained by bronchoscopy or tracheal aspiration, and pleural punctures obtained up to 24 h before treatment. Most patients had Streptococcus pneumoniae or Haemophilus influenzae infections, although two patients in the cefoperazone group had infections caused by Pseudomonas aeruginosa, and another two anaerobic flora. Standard disc diffusion, and agar dilution susceptibilities were performed on all isolates. Patients received either cefoperazone (14) intravenously or intramuscularly in a dose range from 2 to 8 g/day or cefotaxime (15) 1 to 2 g intravenous or intramusculary at dosing intervals of 6 to 8 h (total 3 to 8 g/day), depending on the severity of the disease. Clinical improvement occurred in 14/15 (93%) of patients in the cefotaxime group, and 12/14 (86%) of patients treated with cefoperazone. Two failures in the cefoperazone group were secondary to superinfection (Acinetobacter and Ps. aeruginosa). Bacteriological and symptomatic failure, occurred in one patient with anaerobic lung abscess treated with cefotaxime. The results of this study indicate that cefotaxime is safe and effective in the therapy of acute bacterial lower respiratory tract infections.

Adult↗
PubMed1985

The effects of latamoxef, cefotaxime, and cefoperazone on platelet function and coagulation in normal volunteers.

A bleeding diathesis characterized by in-vitro platelet dysfunction and prolongation of the template bleeding time (TBT) has been reported in patients receiving latamoxef ('moxalactam'), but not cefotaxime or cefoperazone. Hypoprothrombinaemia has been associated with the use of both latamoxef and cefoperazone in seriously ill and malnourished patients. We administered either latamoxef, cefotaxime or cefoperazone intravenously, at dosages within the range recommended by each manufacturer, to 14 normal volunteers. Latamoxef caused a dose and time dependent defect in platelet function characterized in vitro by abnormalities in aggregation to adenosine diphosphate and in vivo by prolongation of the template bleeding time. In two out of two subjects, a single 4 g dose of latamoxef caused neither prolongation of template bleeding times nor aggregation abnormalities. Two out of two subjects receiving latamoxef 6 g/day for six days had progressive prolongation of bleeding times to 12 and 15 min. Two additional subjects receiving latamoxef 12 g/day for four days had prolongation of template bleeding times to greater than 20 min. Of four subjects receiving cefotaxime 12 g/day for seven days, none had prolongation of template bleeding times or abnormalities in platelet aggregations. Of four subjects receiving cefoperazone 6 g/day, none had significant prolongation of template bleeding times and one had abnormalities in aggregation attributed to inadvertent salicylate ingestion. Prolongation of the prothrombin time or activated partial thromboplastin time did not occur in any of the 14 volunteers. Latamoxef is more likely to interfere with platelet function than either cefotaxime or cefoperazone.

Blood Coagulation↗
PubMed1989

Prospective comparative trial of short course (four day) and continuous tobramycin in combination with cefoperazone or mezlocillin in febrile, granulocytopenic patients.

In a prospective, randomized trial of 195 febrile episodes in granulocytopenic patients short course aminoglycoside treatment (initial tobramycin and cefoperazone followed by tobramycin discontinuation at day four of therapy) was compared with two regimens (tobramycin plus cefoperazone and tobramycin plus mezlocillin) in which both drugs were continued for up to 26 days. All regimens were successful as empirical therapy with comparable response rates of just over seventy per cent. Fifty-three per cent of the initial episodes of fever were related to documented infections which responded less well (P = 0.007) than unexplained fever. Patients with bacteraemia, pneumonia or Gram-positive aerobic or Pseudomonas aeruginosa infections responded poorly to all regimens. The recovery from granulocytopenia was the most important determinant of successful response. Aminoglycoside discontinuation followed by cefoperazone monotherapy after day four was statistically as effective as the combination regimens. Short course tobramycin therapy eliminated the nephrotoxicity seen in the combination limbs. The use of cefoperazone was not associated with an increased incidence of hypoprothrombinemia; however, the only three bleeding episodes occurred in patients given cefoperazone but not vitamin K. Short course aminoglycoside therapy will reduce cost and nephrotoxicity when compared with prolonged combination therapy and should be further explored in this setting, with use of different agents and comparison with monotherapy.

Adolescent↗
PubMed1985

Pharmacokinetics of cefaronide, ceftriaxone and cefoperazone in sheep.

The pharmacokinetics of cefaronide (16 gm/kg dose), ceftriaxone and cefoperazone (47 gm/kg dose), after intravenous (i.v.) administration were determined in six Merino ewes. The mean values for terminal half life, steady state volume of distribution Vd(ss), renal clearance (ClR) and total body clearance (ClB) for cefaronide were 1.5 h, 0.39 l/kg, 0.06 l/h/kg and 0.16 l/h/kg, for ceftriaxone; 1.7 h, 0.30 l/kg, 0.08 l/h/kg, and 0.22 l/h/kg, and 0.7 h, 0.16 l/kg, 0.02 l/h/kg and 0.16 l/h/kg for cefoperazone, respectively. After 5.5 h, approximately 42% cefaronide, and after 8 h, approximately 37% ceftriaxone and 13% cefoperazone, was excreted in urine. The non-renal elimination of ceftriaxone and cefoperazone appeared to be more rapid in sheep than is reported in man. Cefaronide was excreted largely unchanged in the urine of sheep. Therefore, the elimination of cefaronide in sheep was similar to that found in man. Cefaronide was well distributed in sheep, whereas ceftriaxone and cefoperazone appeared to be distributed to a lesser degree. These findings underline the different disposition of drugs in different species.

Animals↗
PubMed1993

The use of intramuscular cefoperazone versus intramuscular ceftriaxone in patients with nursing home-acquired pneumonia.

OBJECTIVE: To compare the efficacy and safety of intramuscular cefoperazone and intramuscular ceftriaxone in the treatment of nursing home-acquired pneumonia in the nursing home setting. DESIGN: A randomized clinical trial. SETTING: Skilled nursing wards at the Veterans Home of California. PATIENTS: 104 residents of skilled nursing wards, aged 65 years or older. INTERVENTIONS: Intramuscular administration of either cefoperazone or ceftriaxone. MEASUREMENTS: The variables analyzed for baseline comparability were demographics (age, sex), clinical variables (duration in nursing home; presence of sputum, fever, cough, or leukocyte count), and clinical symptoms and signs. Efficacy was assessed by days of therapy, final maximum temperature, and clinical and bacteriological response. RESULTS: Fifty residents received cefoperazone, 1 gm every 12 hours, intramuscularly. Fifty-four residents received ceftriaxone, 1 gm every 24 hours, intramuscularly. The total duration of treatment was scheduled for 10 days. Clinical cure was seen in 45 (90%) of the cefoperazone treatment group and 51 (94%) of the ceftriaxone treatment group, with a mean duration of therapy of 10.30 and 9.90 days, respectively. Satisfactory sputum specimens were collected in 71% of the treated residents; the most common isolate was Streptococcus pneumoniae, followed by Haemophilus influenzae and Staphylococcus aureus, respectively. The overall mortality was 4.5% at long-term follow-up. Both agents were well tolerated and no therapy was discontinued due to intramuscular pain or abnormal laboratory values. CONCLUSIONS: Intramuscular cefoperazone and intramuscular ceftriaxone are safe and effective in the treatment of nursing home-acquired pneumonia. The clinical outcomes in both treatment groups support their use within this select population without the need for transferring the patient to an acute care hospital. Clinical studies are needed to evaluate the impact of such therapy on the control of health care expenditures within the nursing home facility.

Aged↗
PubMed1981

Cefoperazone treatment of experimental endocarditis.

Cefoperazone (10 mg/kg) and cephalothin (20 mg/kg) administered intramuscularly every 6 h were both effective in reducing the number of Staphylococcus aureus cells in vegetations in rabbits with endocarditis. Cefoperazone produced higher peak concentrations and greater bactericidal activity in serum than did cephalothin. Cefoperazone (40 mg/kg) administered every 6 h was significantly more effective than cefamandole (40 mg/kg) administered every 6 h in reducing the number of Enterobacter aerogenes cells in vegetations. Although cefamandole produced higher peak concentrations in serum, the serum bactericidal activity was greater with cefoperazone. The half-lives in serum were 0.64 h for cefoperazone and 0.46 h for cephalothin and cefamandole.

Animals↗
PubMed1983

Comparative pharmacokinetics of cefoperazone, cefotaxime, and moxalactam.

The pharmacokinetics of cefoperazone, cefotaxime, and moxalactam were compared in a cross-over randomized study in 10 healthy volunteers. Each subject received 1.0 g of the three drugs by bolus intravenous injection over 3 min. Serum and urine concentrations were assayed by a microbiological method and in addition by high-pressure liquid chromatography (HPLC) for cefotaxime in five subjects. Maximal concentrations in serum 5 min after the injection were 163 +/- 40.3 mg/liter for cefoperazone, 86.1 +/- 19.0 mg/liter for cefotaxime, and 95.5 +/- 21.1 mg/liter for moxalactam. After 12 h, 1.2 +/- 1.4 mg of cefoperazone per liter and 1.8 +/- 0.9 mg of moxalactam per liter could still be measured. Eight hours after the administration of cefotaxime, serum concentrations were below the detection limit of 0.3 mg/liter in most subjects. By HPLC analysis, the mean maximal concentration of desacetyl cefotaxime was 16.6 +/- 10.5 mg/liter 5 min after application; the metabolite exceeded the serum concentration of the parent compound after 1 to 2 h. Relevant pharmacokinetic parameters were calculated, using two- and three-compartment models. The terminal half-life was 144.1 +/- 37.3 min for cefoperazone, 76.1 +/- 32.0 min for cefotaxime, and 272.4 +/- 114.1 min for moxalactam. The apparent volume of distribution corresponded to the extracellular volume. Only 25.1 +/- 8% of cefoperazone could be detected in urine compared with 53.3 +/- 8.1% of cefotaxime and 61.0 +/- 9.2% of moxalactam in 24 h. A total of 89.6 +/- 11.4% of the cefotaxime dose could be recovered by HPLC in urine, 60.6 +/- 7.7% as cefotaxime and 29.1 +/- 7.0% as desacetyl cefotaxime.

Adult↗
PubMed1984

Penetration of cefoperazone into surgical wound drainage in patients undergoing head and neck surgery.

Cefoperazone penetration into skeletal muscle and wound drainage in patients undergoing major surgery of the head and neck was measured by high-pressure liquid chromatography. Cefoperazone (2 g) was infused over 30 min before surgery and every 8 h for three postoperative doses. Simultaneous samples of serum and sternomastoid muscle were collected in 18 patients at 135 to 480 min after infusion. Mean cefoperazone concentrations in muscle tissue were 17.1% of those in simultaneously collected serum. Steady-state wound drainage concentrations after the fourth dose of cefoperazone averaged 55.2 micrograms/ml at 1 to 2 h and 62.1 micrograms/ml at 2 to 3 h. Simultaneous steady-state serum and wound fluid samples were obtained at regular intervals in six patients. In all patients, the peak level in wound fluid exceeded 25 micrograms/ml. Thus, cefoperazone reaches interstitial fluid concentration in soft tissue that exceeds the MICs required to inhibit the usual pathogens found at the site of wound infection after head and neck surgery.

Cefoperazone↗
PubMed1986

Comparative study of cefoperazone and spectinomycin for treatment of uncomplicated gonorrhea in men.

Beta-lactamase-negative Neisseria gonorrhoeae infections were treated with single-dose cefoperazone (0.5 or 1.0 g) or spectinomycin (2.0 g). Anogenital infections were cured in 36 (83%) of 43 volunteers given 0.5 g of cefoperazone, 61 of 61 volunteers given 1.0 g of cefoperazone, and 99 of 100 volunteers given spectinomycin. The cefoperazone geometric mean MIC for 242 isolates was 0.028 microgram/ml. Cefoperazone (1.0 g) and spectinomycin (2.0 g) are comparable for the therapy of anogenital gonorrhea in men.

Adolescent↗
PubMed1985

Pharmacokinetics of multiple-dose cefoperazone in hemodialysis patients.

We studied the pharmacokinetics of cefoperazone 2 g i.v. every 12 h for 7 days in 12 patients on hemodialysis with normal hepatic function. The half-life of indocyanine green was determined in each patient via ear oximetry. Serum levels of cefoperazone during dialysis were well described by a two-compartment multidose infusion model. From this model we determined the steady state volume of distribution (Vdss), elimination phase half-life during dialysis T1/2D) and off hemodialysis (T1/2), and the corresponding elimination rate constants (KeD and Ke). Multiple correlations between pharmacokinetic parameters, liver function, and physical characteristics of the patients were evaluated. The T1/2 of cefoperazone was 2.9 h off compared to 2.3 h during hemodialysis. The corresponding elimination rate constants were Ke = 0.45/h versus KeD = 0.80/h. Cefoperazone clearances were 78 ml/min off dialysis compared to 140 ml/min during hemodialysis. Vdss was 0.20 liters/kg. The indocyanine green half-life ranged from 1.8 to 4.6 min with a mean of 2.7 min. The ages of the patients correlated with the beta phase half-life (r = 0.68, p = 0.015). We found no significant correlations among the other parameters including hepatic enzymes and indocyanine green half-life. Thus, hemodialysis approximately doubles the elimination rate constant (clearance), but, assuming drug redistribution kinetics remain unchanged, only shortens half-life by about 20%. Scheduling of a 12-hour dosing regimen to coincide with the end of hemodialysis should obviate any need for alteration of dose. Cefoperazone is thus unique among cephalosporins, since the half-life does not change appreciably with end-stage renal disease or dialysis.(ABSTRACT TRUNCATED AT 250 WORDS)

Adult↗
PubMed1981

Activity and specific beta-lactamase susceptibility of cefoperazone and moxalactam. Comparison with other cephalosporins.

Comparison of the activity of cefoperazone, cefamandole, cefotaxime, cephalothin and moxalactam against Enterobacteriaceae showed cefoperazone to be twofold (Escherichia coli, Klebsiella) to eigthfold (Enterobacter) more active than cefamandole. The lowes MIC values were found for cefotaxime (0.03 - 0.25 microgram/ml) followed by moxalactam (0.06 - 0.25 microgram/ml). Cefoperazone stood out in activity against Pseudomonas aeruginosa (MIC50 4 microgram/ml). Cephalothin resistance affected the MIC values of cefoperazone and moxalactam only to a small degree. From beta-lactamase susceptibility studies it was concluded that cefoperazone may be hydrolyzed by TEM type beta-lactamases, but that the cephalosporinases (class I) and the chromosomal broad-spectrum beta-lactamases (class IV) only have little effect on this antibiotic. Moxalactam was not degraded by any of the beta-lactamase preparations tested.

Bacteria↗
PubMed1986

Therapeutic efficacy of cefpiramide and cefoperazone alone and in combination with gentamicin against pseudomonal infections in neutropenic mice.

Cefpiramide and cefoperazone alone and in combination with gentamicin were compared for therapeutic efficacy against pseudomonal infections in normal mice and in mice made neutropenic by administration of cyclophosphamide. Neutropenic mice were more susceptible to infection with Pseudomonas aeruginosa than normal mice. At all challenge doses, combination therapy with either cefpiramide-gentamicin or cefoperazone-gentamicin was more effective than that with a single agent. Therapy with the cefpiramide-gentamicin combination was significantly more active than that with the cefoperazone-gentamicin combination in protecting mice from fatal bacteremia. Pharmacokinetic studies in mice showed that cefpiramide attained a peak serum concentration of 12 micrograms/ml and a serum half-life of 40 min, which are higher than attained by cefoperazone with values of 4 micrograms/ml and 18 min. These factors may have caused the combined cefpiramide-gentamicin therapy to result in significantly improved survival rates in mice as well as in higher bactericidal titers than the cefoperazone-gentamicin combination. The results show that cefpiramide when combined with gentamicin is effective in treating serious infections with P. aeruginosa in neutropenic mice.

Animals↗
PubMed1983

Cefoperazone (Cefobid, Pfizer).

Cefoperazone is a new beta-lactam antibiotic that possesses a broad spectrum of activity against gram-positive and gram-negative organisms. Cefoperazone differs from all previous cephalosporins in that it has exceptional activity against P. aeruginosa. The other distinguishing feature of cefoperazone is its high rate of biliary excretion, which will allow for treatment of biliary tract infections. Renal elimination accounts for only 20 percent of the agent's elimination; dosage modification is not necessary in decreased renal function. The clinical response rate of infections to cefoperazone is similar to that of moxalactam, cefotaxime, or the cephalosporins in general. The overall incidence of side effects was 14 percent in U.S. trials, with skin rash, fever, or urticaria occurring in 1 percent; phlebitis and injection-site pain in 2 percent; and diarrhea in 5 percent. As with the other third-generation cephalosporins, cefoperazone requires close scrutiny because of its expected high cost and the lack of comparative trials with standard antibiotic regimens.

Bacterial Infections↗