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PubMed1982

Neuromuscular blocking effects of tobramycin, gentamicin, and cefazolin.

Forty patients (A.S.A. class I or II), 18 to 75 years of age, who were undergoing elective surgery were studied to determine the clinical and subclinical neuromuscular blocking effects of two antibiotics, tobramycin and gentamicin and to compare these effects with those produced by cefazolin, an aminoglycoside not known to produce paralysis. Patients were prospectively and randomly assigned in approximately equal numbers to one of four groups: group A received 1 mg/kg of tobramycin; group B, 1 mg/kg of gentamicin; group C, 500 mg of cefazolin; or group D, control (no antibiotic). Antibiotics were administered intravenously 45 minutes immediately preceding the study. The ulnar nerve was stimulated supramaximally and neuromuscular function was measured electromyographically. Anesthesia was induced with thiopental, 4 mg/kg IV, and maintained with endotracheal enflurane 1.0% to 1.5% (inspired) and N2O-O2 (2 L:1 L) after intubation. Succinylcholine (1 mg/kg) was administered after induction of anesthesia and the magnitude and duration of neuromuscular block monitored. d-Tubocurarine (0.1 mg/kg) was given 5 to 10 minutes after full recovery from succinylcholine and repeated as required. At the end of the operation, atropine, 0.02 mg/kg, and neostigmine, 0.4 mg/kg, were used to reverse the block. Base line neuromuscular data, duration of block of succinylcholine, and potency, duration of block, recovery rate, train-of-four fade, tetanic trend, response to double stimuli, post-tetanic effect, and reversibility of the subsequent d--tubocurarine-induced neuromuscular block were not significantly different (p less than 0.01) between any two groups. Tobramycin, gentamicin, and cefazolin, in recommended single doses, lack clinical neuromuscular blocking and subclinical relaxant-potentiating effects.

Adolescent↗
PubMed1980

Stability of cefazolin sodium admixtures in plastic bags after thawing by microwave radiation.

The effect on antibiotic stability of thawing, with microwave radiation, cefazolin sodium admixtures frozen in polyvinyl chloride minibags was studied. Two brands of cefazolin sodium (Ancef and Kefzol) were reconstituted and placed in 50-, 100- and 250-ml polyvinyl chloride minibags of 5% dextrose in water or 0.9% sodium chloride. The resulting solutions were assayed for antibiotic stability, using an agar disk diffusion technique, and for pH. The solutions were then stored at -20 degrees C for 48 hours, thawed to room temperature in a microwave oven, and kept at room temperature for four hours, after which they were reassayed for potency and pH. The results indicated that after the freeze-thaw process, the cefazolin sodium minibag admixtures retained at least 90% of their initial antimicrobial activity. The minimal pH changes could not be related to changes in antimicrobial activity, and no color changes could be detected visually. Using a microwave oven can greatly reduce thawing time of antibiotic admixtures. To maintain solution stability and prevent accidents, it is important to calibrate the oven, avoid solution overheating, and observe full precautions in oven operation.

Biological Assay↗
PubMed1994

[Evaluation of the effectiveness of cefazolin++ (Kefzol) in preventing infections in patients after abdominal surgery].

The purpose of the work as an assessment of the effectiveness of cefazolin (Kefzol) in preventing infections in patients after abdominal surgery. The prospective studies included 200 patients, out of whom in 100 patients in the studied group Kefzol was administered prior to and for 24 hours after operation, while in 100 patients in the control group no prevention was used. The percent of infections in the studied group was lower in comparison to the control group (9% vs 25%, p < 0.01). A statistically significant reduction was obtained of wound infection per cent from 19% in the control group to 7% in the studied group, including a reduction from 14.3% to 3.1% after operations on the gall bladder and bile ducts, and from 18.2% to 11.1% after gastroduodenal operations. The per cent of wound infections after appendectomy was 5.9% in the patients from the studied group receiving prophylactically Kefzol with metronidazole, and 20.6% in the patients from the control group. Bacteriological investigations, demonstrated that 87.5% bacterial strains were susceptible to cefazolin. In the authors' opinion cefazolin (Kefzol) is effective in the prevention of purulent complications, and the reduction of the per cent of infections causes lowering of treatment cost.

Abdomen↗
PubMed1976

Stability of frozen solutions of cefazolin sodium.

The stability of frozen solutions of cefazolin sodium was investigated in nine commonly used diluents at concentrations of 1 g with 2.5 ml, 500 mg with 100 ml and 10 g with 45 ml in both glass and polyvinylchloride plastic containers. The diluents were: Water for Injection USP; 0.9% Sodium Chloride Injection USP; 5% Dextrose Injection USP (D5W); D5W with 0.02% sodium bicarbonate; D5W in Lactated Ringer's Injection USP; Lactated Ringer's Injection USP; Ionosol B in D5W; Normasol M in D5W; and Plasmalyte in D5W. Frozen cefazolin sodium solutions, containing Water for Injection USP, 5% Dextrose Inection USP or 0.9% Sodium Chloride Injection USP as the diluents, retained more than 90% of labeled potency for up to 26 weeks when frozen within one hour after reconstitution and held at -10 C or -20 C. Frozen cefazolin sodium solutions, made with other diluents, were stable for up to four weeks when frozen within one hour after reconstitution and held at -10 C.

Animals↗
PubMedDate not supplied

[Correlation between crystalline structure and biological properties of sodium cefazolin].

Antimicrobial activity and toxicity of four polymorphic forms of sodium cefazolin were studied in comparison to those of the initial cefazolin. The observed changes reflecting a broader antimicrobial spectrum and low toxicity of one of the forms as compared with those of the initial cefazolin could serve as a prerequisite to successful screening of more active crystalline forms of the antibiotic aimed at designing the drug with better therapeutic properties.

Animals↗
PubMed1977

The influence of biliary disease on the excretion of cefazolin in human bile.

Forty-five patients with varying biliary pathology were injected with one gram of intramuscular cefazolin sodium prior to surgery. Serum, gallbladder bile, and common duct bile levels were measured. The type of biliary disease did not influence serum levels (mean, 29 mug per milliliter) which reached a peak one hour after injection. Mean common duct bile levels were reduced from 52 mug per milliliter in nonjaundiced patients to 4 mug per milliliter in those with jaundice (p less than 0.001). Patients with radiologically functioning gallbladders had significantly higher mean gallbladder bile levels (21 mug per milliliter; p less than 0.005). Surprisingly, the mean gallbladder bile level in acute cholecystitis was 25 mug per milliliter. As the minimum inhibitory concentration of cefazolin for organisms commonly found in the bile is 0.5 to 6 mug per milliliter, we suggest that cefazolin sodium may be of value in the treatment of biliary disease, particularly acute cholecystitis.

Bile↗
PubMed1977

Convulsions associated with sodium cefazolin: a case report.

Our patient was severely injured, and had a prolonged period of hypotension. After operation she received moderate doses of cefazolin, intravenously, in the face of acute renal failure. Seizures associated with a serum cefazolin level of 455 mg/ml were observed. Although a cause and effect relationship between high cefazolin levels and neurotoxicity cannot be proven conclusively, the implication of this relationship exists. The clinician should be aware of the potential neurotoxicity of this commonly used drug. The importance of adjusting the dose in patients with renal failure is re-emphasized.

Acute Kidney Injury↗
PubMed1977

The penetration characteristics of cefazolin, cephalothin, and cephradine into bone in patients undergoing total hip replacement.

Preoperatively, to prevent infection, seventy-one patients who were to have total hip arthroplasty were given one gram of cephalothin, cephradine, or cefazolin intravenously. Simultaneous samples of bone and serum were obtained after various time intervals and assayed for cephalosporin concentration to correlate the antibiotic concentrations in these sites with time. Of the cephalosporins tested, cefazolin achieved the highest total peak levels in bone (thirty micrograms per gram), followed in descending order by cephradine (twenty-three micrograms per gram) and cephalothin (2.8 micrograms per gram). These peak levels in bone, reached twenty-five to forty minutes after injection, were sixty, 6.7, and fifteen times higher than the usual mean minimum inhibitory concentrations of cefazolin, cephradine, and cephalothin, respectively, for penicillin-resistant staphylococci. The half-lives of the antibiotics in bone were forty-two, forty, and thirty minutes, respectively.

Aged↗
PubMed1975

Pulmonary infections in elderly patients: treatment with cefazolin.

The effects of cefazolin were studied in 15 hospital patients (average age, 67) with respiratory-tract infections. The infections were chiefly bronchopneumonia caused by organisms such as D. pneumoniae, Staph. aureus, or E. coli. In 13 of the 15 patients the results were excellent to good (eradication of the primary pathogen and clinical improvement); in the other 2 patients the response was fair. Intramuscular injection was well tolerated and only one patient complained of pain at the site of injection; no other adverse clinical effects were observed. In the laboratory determinations, including liver and kidney function tests, the only abnormalities were 2 cases in which the Coombs' test gave positive results without hemolysis. Cefazolin seems to be a safe and effective antibiotic for the treatment of respiratory-tract infections caused by cefazolin-susceptible organisms.

Adult↗
PubMed1973

Pharmacodynamics of cefazolin in the presence of normal and impaired renal function.

The excretion of cefazolin, a new cephalosporin antibiotic, was studied in subjects with normal and impaired renal function. Twelve subjects with creatinine clearances ranging from 0 to 144 ml per min per 1.73 m(2) were given a single 500-mg intramuscular dose of cefazolin. Serum and urine levels were determined at intervals by agar diffusion. Peak serum levels in normals ranged from 44 to 70 mug/ml and occurred 30 to 60 min after injection. The mean serum half-life in normals was 1.6 h, and this was prolonged from 20 to 40% by simultaneous administration of probenecid. The total elimination constant varied linearly with the creatinine clearance in patients with renal impairment. The serum half-life in anephric patients was about 42 h. The fractional clearance of the drug varied directly with the serum level. Peak urine levels ranged from 60 to over 2,000 mug/ml, and more than 90% of the dose was recovered in the urine of normals during the first 24 h. The data suggest that cefazolin is cleared primarily by the glomerulus, with tubular and biliary secretion playing a secondary role.

Cephalosporins↗
PubMed1986

Cefazolin vs moxalactam? A double-blind randomized trial of cephalosporins in head and neck surgery.

Cefazolin and moxalactam were compared in a prospective randomized double-blind trial of 118 patients undergoing oncologic head and neck surgery. Both antibiotics were given 2 g every four hours for four doses. Five infections were encountered in the cefazolin group (8.5%) and two infections in the moxalactam group (3.4%); this difference was not statistically significant. This assessment does not indicate, however, that the two regimens are equally efficacious.

Cefazolin↗
PubMed1979

Cefazolin vs penicillin. Treatment of uncomplicated pneumococcal pneumonia.

Cefazolin sodium, 500 mg intramuscularly twice daily, was compared with penicillin G procaine, 600,000 units intramuscularly twice daily, in the treatment of 82 patients with pneumococcal pneumonia. Patients were randomly assigned except when there was a history of penicillin allergy. The patients received treatment for five days or until they were afebrile for 48 hours. No patients experienced side effects or allergic reactions. All patients recovered satisfactorily without relapses. Cefazolin in the previously described dosage is as effective as penicillin in the treatment of pneumococcal pneumonia.

Cefazolin↗
PubMed1998

Incidence of postpartum endomyometritis following single-dose antibiotic prophylaxis with either ampicillin/sulbactam, cefazolin, or cefotetan in high-risk cesarean section patients.

OBJECTIVE: To assess the efficacy of single-dose antibiotic prophylaxis against postpartum endomyometritis in high-risk cesarean section patients. DESIGN: Patients were administered one of three single-dose antibiotic regimens following umbilical cord clamping after cesarean section delivery. SETTING: Prospective randomized trial at a university-based hospital. PATIENTS: The study evaluated 293 consenting women undergoing cesarean section who had either experienced labor for a duration of > or = 6 hr or rupture of amniotic membranes. MAIN OUTCOME MEASURES: Development of postpartum endomyometritis. RESULTS: The incidence of postpartum endomyometritis was 7/95 (7.4%) following the ampicillin/sulbactam regimen, 14/98 (14.3%) after the cefazolin regimen, and 11/99 (11.1%) after the cefotetan regimen. There was no significant difference in postpartum infection among the three study arms. In addition, the incidence of endomyometritis in the three single-dose study arms was not higher than previously noted in studies where three doses of antibiotic were administered. CONCLUSION: Single-dose antibiotic prophylaxis should replace the standard triple-dose therapy for uninfected women undergoing cesarean section who are at risk for postoperative endomyometritis. Ampicillin/sulbactam, cefazolin, and cefotetan are all reasonable antibiotic choices for single-dose therapy.

Adult↗
PubMed1999

Prophylactic cefazolin in amnioinfusions administered for meconium-stained amniotic fluid.

OBJECTIVE: To determine if amnioinfusion with an antibiotic solution decreased the rate of clinical chorioamnionitis and puerperal endometritis in patients with meconium-stained amniotic fluid. METHODS: Patients in labor at 36 weeks of gestation or greater with singleton pregnancies and meconium-stained amniotic fluid were randomized to receive either cefazolin, 1 g/1,000 mL, of normal saline (n = 90) or normal saline (n = 93) amnioinfusion. Rates of clinically diagnosed chorioamnionitis and endometritis and of suspected and culture-proven neonatal infection were determined. RESULTS: Between the study and control groups, the incidences of clinical chorioamnionitis (7.8% vs. 8.6%), endometritis (2.4% vs. 3.5%), aggregate intrauterine infection (10.0% vs. 11.8%), suspected neonatal infection (17.8% vs. 21.5%), and proven neonatal infection (0.0% vs. 2.2%) were not significantly different. CONCLUSIONS: Prophylactic use of cefazolin in amnioinfusions did not significantly reduce rates of maternal or neonatal infection in patients with meconium-stained amniotic fluid.

Adult↗
PubMed1979

One-dose antibiotic prophylaxis against wound infection after appendicectomy: a randomized trial of clindamycin, cefazolin sodium and a placebo.

Two hundred and fifty patients were admitted to a prospective randomized trial of single dosage prophylaxis against wound infection after appendicectomy. There were 12 exclusions, 72 patients received placebo, 81 received 600 mg i.m. clindamycin phosphate and 85 received 1 1 g i.m. cefazolin sodium, the agent being given in the anaesthetic room. Clindamycin produced a significant reduction in the overall rate of wound infection from 33 per cent in the controls to 17 per cent. In cases with a gangrenous or perforated appendix the infection rate in controls was 78 per cent; this was reduced to 44 per cent by a single dose of clindamycin. Cefazolin significantly reduced the number of aerobic organisms isolated from wound infections, but did not significantly reduce the incidence of wound infection. We conclude that anaerobic organisms are more important than faecal aerobic organisms in the pathogenesis of wound infection after appendicectomy.

Adult↗
PubMed1976

Pharmacokinetics and hemodialyzability of cefazolin in uremic patients.

Cefazolin may be used in azotemic patients at reduced dosage as suggested by others. Although hemodialysis removes some of the drug, therapeutic levels are maintained throughout dialysis after a single intravenous dose of 500 mg. Imperfect transport from blood to dialysate is related to protein binding but varies with the degree of azotemia. Small amounts of cefazolin may be administered to patients during dialysis by addition to dialysate.

Adult↗
PubMed2003

Strategies for the determination of cefazolin in plasma and microdialysis samples by short-end capillary zone electrophoresis.

Capillary zone electrophoresis was employed to determine cefazolin, a first-generation cephalosporin antibiotic, in plasma and microdialysis samples from patients. To shorten the analysis, the samples were injected from the short end of the capillary, resulting in a separation time of < 3 min. Due to a high ionic strength of the biological matrices it was necessary to optimize the stacking conditions. For microdialysis samples a 1:10 dilution with water before injection was sufficient to obtain good peak shape. For plasma samples a protein removal step was required to obtain clean electropherograms and a good peak shape. Acetonitrile was used as precipitant resulting in an enhanced sample stacking in comparison to water dilution. The disadvantage of using acetonitrile was severe evaporation loss making quantitation impossible. A self-sealing film was used to seal each individual sample vial to suppress evaporation during long-term sequences. The calibration curves for spiked plasma and cefazolin in Ringer's solutions were linear in the range from 2-500 and 2.5-100 microg/mL, respectively. Limits of detection were 1.0 and 2.0 microg/mL in plasma and microdialysis samples, respectively. The assay was successfully applied to plasma and microdialysis samples obtained in vivo from the interstial space fluid of subcutaneous adipose and muscle tissue of patients undergoing cardiac surgery.

Acetonitriles↗