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PubMed1985

Comparison of Escherichia coli susceptibility to cephalothin, cefazolin, ceforanide, and cefamandole.

Twenty-seven Escherichia coli test strains that were not susceptible to cephalothin were tested for susceptibility to cefazolin, cefamandole, and ceforanide. By zone-size criteria (greater than or equal to 18 mm), 67% of E coli were susceptible to cefazolin and cefamandole, and 93% were susceptible to ceforanide. By microtiter assay (MIC less than or equal to 8 micrograms/ml), 88% were susceptible to cefazolin and cefamandole, and 94% were susceptible to ceforanide. The results support susceptibility testing of E coli with specific first- or second-generation cephalosporins rather than with class agents.

Cefamandole↗

PubMed1985

Controlled, comparative study of moxalactam and cefazolin for prophylaxis of abdominal hysterectomy.

Moxalactam was compared with cefazolin and a control group to determine the efficacy and value of a third generation cephalosporin in abdominal hysterectomy antibiotic prophylaxis. One hundred patients were prospectively randomized in a double-blind manner between moxalactam and cefazolin. An additional 50 patients who were either allergic to penicillin or refused participation in this study were simultaneously observed to establish a base line level of infection on our service during this time period. Dosage for both antibiotic groups was 1 gram given intravenously or intramuscularly on call to the operating room followed by two 1 gram doses at six and 12 hours after the first dose. Standard febrile morbidity was 36, 30 and 42 per cent for moxalactam, cefazolin and control groups, respectively. Postoperative surgical infection requiring antibiotic treatment occurred in 8, 6 and 4 per cent, respectively; urinary tract infection or symptomatic findings, or both, requiring treatment occurred in 8, 10 and 10 per cent, respectively. No pelvic abscesses occurred in this series. In every statistical evaluation of postoperative morbidity, there were no differences noted among the three groups. Our results suggest no benefit from the use of prophylactic antibiotics in abdominal hysterectomy in terms of standard febrile or infectious morbidity or urinary tract pathologic findings. In addition, there was no difference between the two antibiotic groups.

Adolescent↗

PubMed1986

Pharmacokinetics of probenecid and the effect of oral probenecid administration on the pharmacokinetics of cefazolin in mares.

The pharmacokinetics and bioavailability of probenecid given IV and orally at the dosage level of 10 mg/kg of body weight to mares were investigated. Probenecid given IV was characterized by a rapid disposition phase with a mean half-life of 14.0 minutes and a subsequent slower elimination phase with a mean half-life of 87.8 minutes in 5 of 6 mares. In the remaining mare, a rapid disposition phase was not observed, and the half-life of the elimination phase was slower (172 minutes). The mean residence time of probenecid averaged 116 minutes for all 6 mares and 89.2 minutes for the 5 mares with biphasic disposition. The total plasma clearance of probenecid averaged 1.18 +/- 0.49 ml/min/kg, whereas renal clearance accounted for 42.6 +/- 9.3% of the total clearance. The steady-state volume of distribution of probenecid averaged 116 +/- 28.2 ml/kg. Plasma protein binding of probenecid was extensive, with 99.9% of the drug bound at plasma probenecid concentrations of 10 micrograms/ml. The maximum plasma probenecid concentration after 10 mg/kg orally averaged nearly 30 micrograms/ml. The half-life of probenecid after oral administration was approximately 120 minutes. Oral bioavailability was good with greater than 90% of the dose absorbed. The effect of probenecid on tubular secretion of organic anions was evaluated by determining the pharmacokinetics of IV cefazolin (11 mg/kg) administered alone and 15 minutes after probenecid (10 mg/kg orally). Treatment with probenecid did not affect pharmacokinetic values of cefazolin. This failure of probenecid to alter the pharmacokinetics of cefazolin may be caused by insufficient plasma probenecid concentrations after the oral dose.

Administration, Oral↗

PubMed1977

Unsuccessful treatment of staphylococcal endocarditis with cefazolin.

Two patients with staphylococcal endocarditis were treated unsuccessfully with cefazolin sodium. One patient relapsed after 52 days of therapy. The second patient had concomitant central nervous system infection and failed to respond to cefazolin therapy. Both patients recovered with methicillin sodium or nafcillin sodium therapy. Other studies report unsuccessful therapy of staphylococcal endocarditis with cefazolin.

Adult↗

PubMed1979

Clinical pharmacology phase I of cefazedone, a new cephalosporin, in healthy volunteers. I. Tolerance in comparison with cefazolin.

In conjunction with pharmacokinetic investigations, the tolerance of (6R,7R)-7-(2-[3,5-dichloro-4-oxo-1 (4H)-pyridyl]-acetamido)-3-([(5-methyl-1,34-thiadiazol-2-yl)-thio]methyl)-8-oxo-5-thia-1-azabicyclo[4,2,0]oct-2-ene-2-carboxylic acid (cefazedone, Refosporen), a new semisynthetic cephalosporin, was compared with that of cefazolin in two consecutive cross-over studies conducted on 10 healthy male volunteers each. The systemic tolerance of cefazedone after 1 X 500 mg and 1 X 1000 mg i.v., and 1 X 500 mg i.m. injections was very good and comparable with that of cefazolin. The same holds true for the local tolerance after i.v. administration. The local tolerance of i.m. administered cefazedone can also be classified as good when compared with that of cefazolin.

Adult↗

PubMed1984

Antibiotic prophylaxis in high-risk biliary operations: multicenter trial of single preoperative ceftriaxone versus multidose cefazolin.

A prospective, double-blind trial of a single preoperative dose of ceftriaxone, a new long-acting cephalosporin, versus one preoperative and three postoperative doses of cefazolin was carried out in 81 patients at high risk of infection after biliary surgery. Indications for antibiotic prophylaxis included recent or ongoing cholecystitis (52 patients), common duct stones (14 patients), common duct obstruction (3 patients), and age greater than 70 years (22 patients). Intraoperative bile cultures were positive in 7 of 41 patients (17.1 percent) given ceftriaxone and 12 of 40 patients (30 percent) given cefazolin, but there were no wound infections in either group. Neither regimen was associated with significant antibiotic resistance. Side effects, such as proteinuria and elevated liver transaminases and alkaline phosphatase levels, were transient and not definitely related to the antibiotics. We conclude that a single preoperative dose of ceftriaxone is as effective as multiple perioperative doses of cefazolin in the prophylaxis of infection associated with biliary tract surgery.

Adolescent↗

PubMed1984

Comparison of ceftriaxone and cefazolin prophylaxis against infection in open heart surgery.

One hundred four patients undergoing elective open heart surgery were enrolled in a prospective, double-blind trial comparing prophylaxis against infection using a single 1 g dose of ceftriaxone and seven doses of cefazolin. Patients in both groups had similar risk factors for infection. The likelihood of achieving a tissue concentration in excess of the minimal inhibitory concentration for Staph. aureus was significantly greater with ceftriaxone in atrial appendage (p less than 0.001), muscle (p less than 0.01), and bone (p less than 0.01) than with cefazolin. The serum half-life of ceftriaxone was approximately 15.7 hours. All 49 serum samples obtained 18 to 24 hours after delivery of ceftriaxone and 26 of 33 samples obtained 40 to 48 hours after delivery had drug concentrations in excess of 3.1 micrograms/ml, the mean minimal inhibitory concentration for isolates of Staph. aureus. Early and late infectious complications were infrequent and occurred at similar rates in both groups. Neither drug was associated with significant toxicity. A single 1 g dose of ceftriaxone was as effective and safe as multiple doses of cefazolin and demonstrated superior tissue penetration.

Aged↗

PubMed1980

Cefazolin experimental epilepsy: the effects of diazepam on the interictal ECoG.

Diazepam i.v. injected at the dose of 5 mg/Kg on a group of 14 Rhode-Island-Red chicks was able to antagonize and prevent the interictal EEG pattern induced by cefazolin i.v. Since cefazolin epilepsy is most probably dependent on a receptorial antagonism with GABA, these data seem to confirm the GABA-ergic nature of cefazolin epilepsy.

Animals↗

PubMed1982

Antibiotic prophylaxis in genitourinary surgery: a comparison of cefotaxime and cefazolin.

In a prospective, single-blind study, the efficacy of cefotaxime and cefazolin in the prevention of postoperative infection was compared in 133 patients admitted for elective genitourinary surgery (over half of whom were undergoing transurethral resection). In regimen 1, cefotaxime was given perioperatively (before, during, and up to two hours after surgery); in regimen 2, cefotaxime was given perioperatively and for 24 hours postoperatively; and in regimen 3, cefazolin was given perioperatively and for 24 hours postoperatively. All doses equaled 1 gm and were given either intramuscularly or by intravenous bolus. All patients had negative urine cultures preoperatively. The criterion for absence of infection was a negative urine culture (less than 10(5) organisms/ml) after surgery. At the final evaluation, 113 of the 133 patients (85%) were free of infection--39 of 45 (86.7%) on regimen 1, 40 of 45 (88.9%) on regimen 2, and 34 of 43 (79.1%) on regimen 3. All 20 patients who had postoperative infections had been catheterized for at least three days. Only 12 patients had temperatures greater than or equal to 101 F two days after surgery, and none had been clinically septic. No side effects other than a mild rash and itching in one patient on regimen 2 were reported. Both cefotaxime regimens were slightly more effective, bacteriologically and clinically, than the standard prophylactic cefazolin regimen. It is concluded that cefotaxime given perioperatively (up to two hours postoperatively) and/or up to 24 hours postoperatively effectively prevents postoperative complications associated with genitourinary surgery.

Adolescent↗

PubMed1984

Ceforanide compared with cefazolin in skin and soft tissue infections.

The response of serious skin and skin structure infections to ceforanide 1 gm every twelve hours or cefazolin 1 gm every eight hours was evaluated in ninety-six patients hospitalized for treatment. Most of the patients had decubitus ulcers; predominant pathogens were Staphylococcus aureus, Escherichia coli, and Proteus mirabilis. Ceforanide produced a satisfactory clinical response in 89 percent (forty-eight of fifty-four) of the patients evaluated and eradicated 90 percent (seventy-four of eighty-two) of the pathogens. Although the clinical response of forty-two cefazolin-treated patients was similar (satisfactory response in 86 percent, thirty-six patients), only 81 percent (forty-eight of fifty-nine) of the pathogens were eradicated. Both ceforanide and cefazolin were very well tolerated systemically and locally.

Adult↗

PubMed1981

Effects of cefazolin and moxalactam on serum chemistry values determined by autoanalyzer.

A study was undertaken to determine if cefazolin or moxalactam (LY127935), a new 1-oxa-beta-lactam antibiotic, would falsely elevate serum creatinine (determined by the Jaffé reaction) and other commonly determined serum chemistry values when performed by an automated method (Technicon SMAC System). In a balanced crossover study, each of six normal volunteers received a 30-minute infusion of 10 mg/kg of cefazolin, followed in two days by the same dose of moxalactam. The mean SMAC results for 10 common tests, including creatinine, determined from serum obtained immediately after each infusion exhibited no significant differences from the respective baseline values. Cefazolin and moxalactam did not falsely elevate any of the tests examined, including serum creatinine, and should not cause confusion in the assessment of the renal function of patients receiving these agents.

Adult↗

PubMed1983

Comparison of six methods for preparing cefazolin sodium for intermittent injection.

The time and cost of preparing i.v. piggyback doses of cefazolin sodium using automated and manual methods were compared. One-gram doses of cefazolin sodium were prepared in batches of 100 using each of six methods. Total equipment process times were recorded during five trials with each method. Personnel time and total materials costs were determined. Bulk-vial reconstitution methods, including a manual syringe and three automated fluid-delivery devices (Burron Multi-Ad syringe pump, Unispense peristaltic pump, and Valleylab heart-valve cassette pump), were compared. Two prefilled container systems (Faspak flexible plastic bags with Physio-Control peristaltic pump, and glass piggyback bottles with the Multi-Ad pump) were compared with each other and with the bulk-reconstitution methods. Of the bulk-vial methods, total process times were significantly shorter for the Multi-Ad and Unispense systems. Of the prefilled container systems, total process time and personnel time were significantly shorter for the Faspak method than for the manufacturer's piggyback bottle method. Materials costs were similar for all bulk-vial methods and were significantly lower for both prefilled container systems. Overall costs were lower for prefilled systems; the cost per dose was $3.63 for the manufacturer's piggyback bottle system and $4.26 for the Faspak system. Total personnel time required by the Faspak method was 21.5 minutes per batch, approximately one third the time required by any other method. In terms of personnel time and materials costs for preparation of i.v. cefazolin sodium doses, manufacturers' prefilled container systems have advantages over bulk-reconstitution methods.

Cefazolin↗

PubMed1983

Effects of certain antiepileptics on cephaloridine- and cefazolin-induced seizures in rats.

Effects of phenobarbital, phenytoin and diazepam on cephaloridine-induced spiking activity (focal seizure) and cefazolin-induced violent seizure appearing repeatedly in EEG and general behavior (repeated generalized seizure) were studied in rats with chronically implanted electrodes. Phenobarbital, phenytoin and diazepam showed remarkable inhibition on cephaloridine-induced focal seizure and the ED50 values were 4.52 mg/kg, 9.41 mg/kg and 0.86 mg/kg, respectively. Phenobarbital and diazepam also inhibited cefazolin-induced repeated generalized seizure. The ED50s to inhibit seizure pattern in EEG were 30.5 mg/kg and 3.4 mg/kg, respectively and the ED50 values to suppress seizure behavior were 49.0 mg/kg and 4.7 mg/kg. However, phenytoin did not suppress repeated generalized seizure even at 100 mg/kg. From these results, cephaloridine-induced focal seizure and cefazolin-induced generalized seizure are thought to be useful models for evaluating the inhibitory effect of test compounds on cortical seizure and status epilepticus, respectively.

Animals↗

PubMed1983

Pharmacokinetics of intravitreal carbenicillin, cefazolin, and gentamicin in rhesus monkeys.

Although intravitreal injection of antibiotics is being used more widely in treatment of bacterial endophthalmitis, the pharmacokinetic principles that underlie such therapy have been derived exclusively from experiments in the rabbit. Therefore, we studied several representative antibiotics in normal eyes of rhesus monkeys. Carbenicillin (1,000 micrograms), cefazolin (1,000 micrograms), or gentamicin (100 micrograms) was injected intravitreally. Vitreous and aqueous humors were aspirated at intervals up to 96 hours after injection. The half-life values in the vitreous humor were: carbenicillin 10 hours, cefazolin 7 hours, and gentamicin 33 hours. Concomitant intraperitoneal administration of probenecid prolonged the vitreal half-life of carbenicillin to 20 hours and of cefazolin to 30 hours. The estimated vitreous volumes in these monkeys were approximately 3.0-4.0 ml. These results are consistent with the hypothesis that, in primates as in rabbits, beta-lactam antibiotics are eliminated via the retinal route and the aminoglycoside via the anterior route. This supports the applicability of the rabbit model to the treatment of endophthalmitis in humans.

Animals↗

PubMed1980

Antagonism by classical antiepileptics and sodium valproate of cefazolin in induced experimental epilepsy in rats.

The effects of cefazolin, a semisynthetic cephalosporin, on rat behavior, electrocortical activity and on electrocortical spectrum power were evaluated. In addition, the possible antagonism by some antiepileptic agents was studied. Cegazolin, given intravenously in rats, produced generalized convulsions, electrocortical high-voltage spikes and other electrocortical abnormalities similar to those described to occur in human epilepsy. Power spectrum analysis of the electrocortical activity revealed a significant increase in total voltage output during electrocortical epileptogenic discharges. In addition high-voltage spikes induced by cefazolin were easily counted and lasted approximately 90 min. Classical antiepileptic drugs (diphenylhydantoin, phenobarbital and clonazepam as well as sodium valproate were able to counteract electroclinical disorders induced by cefazolin.

Animals↗

PubMed1981

Complicated urinary tract infections treated with cefuroxime or cefazolin: a comparative study.

In a prospective, randomized study, 58 men with complicated urinary tract infections were divided into two groups and treated intramuscularly with either cefuroxime (0.75 gm) or cefazolin (1 gm) every eight hours for five to ten days. Both groups were comparable in age, weight, and underlying disease of the urinary tract. Patients with creatinine clearance below 25 ml/min were excluded from the study. All infecting microorganisms were sensitive to both drugs, as determined by disk sensitivity testing. One day after treatment, 97% of the urine cultures were negative in both the cefuroxime and cefazolin groups. One week after treatment, 62% and 63% of the cultures were negative in the two groups, respectively. Thus no differences were found in the therapeutic effects of the two drugs. No significant differences were observed in the complete blood count or chemistry evaluations carried out before and after treatment in both groups, nor were any allergic reactions encountered. We concluded that cefuroxime and cefazolin are equally effective and safe in the treatment of complicated urinary tract infections.

Adult↗

PubMed1982

Prevention of wound infection: the comparative effectiveness of topical and systemic cefazolin and povidone-iodine.

From studies in mice, the irrigation of a contaminated surgical wound saline alone proved of little benefit. The addition of cefazolin to the irrigating solution favorably influenced the rate of infection. The most effective way to administer antibiotics topically was by the application of the antibiotic powder to the wound. Topical cefazolin administered in this way was equally as effective as systemic administration in preventing wound sepsis. Irrigation of a contamined wound with a solution of povidone-iodine was no more effective than the use of cefazolin powder but may be associated with significant toxicity.

Administration, Topical↗

PubMed1982

Analog computer simulation of maternal - fetal transfer of cefazolin.

Cefazolin concentration-time data after normal vaginal delivery were obtained for maternal serum, placenta, umbilical cord blood, and amniotic fluid. After normalizing of the data, concentration-time profiles were generated for each sampling compartment. A pharmacokinetic model for analog computer simulation was developed. Multiple dosing simulation suggests a higher accumulation of cefazolin in fetal than in maternal blood, and a slow accumulation in amniotic fluid, which acts as a depot or storage. The drug is transferred diaplacentally; paraplacental transfer seems to be absent for cefazolin.

Amniotic Fluid↗