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PubMed1986

Pharmacokinetics and protein binding of cefazolin and cephalothin in patients with cirrhosis.

The effects of liver disease on the pharmacokinetics and protein binding of cefazolin and cephalothin were studied in patients with cirrhosis, chronic active hepatitis or normal liver function. The T1/2 and mean residence time of cefazolin were significantly shorter in cirrhosis. Cephalothin clearance was decreased by cirrhosis. Plasma protein binding of cefazolin, but not cephalothin was significantly reduced in cirrhosis. It is suggested that no dose reduction is necessary for either drug in severe hepatic impairment.

Adult↗
PubMed2007

Protein binding of cefazolin is saturable in vivo both between and within patients.

AIMS: The aims of the study were a) to determine if there is evidence of saturable protein binding of cefazolin in plasma across the range of concentrations achieved clinically (between patient variability) and b) to investigate whether saturable protein binding is also evident from trough and peak concentrations in the same patient (within patient variability). METHODS: Unbound and total plasma concentrations were measured in patients who were treated with cefazolin intravenously by continuous infusion or intermittent injection. In study (i) single random samples were taken from one series of patients. In study (ii) paired samples (troughs and peaks) were taken from a second series of patients. RESULTS: Thirty-one patients were included in study (i). Linear regression analysis of the percentage unbound vs. unbound plasma concentrations revealed a slope significantly different from zero, suggesting saturable protein binding. Mean values for percentage unbound ranged from 9% at low concentrations (8.5 mg l(-1)) to 51% at high concentrations (140 mg l(-1)). Twelve patients were investigated in study (ii). Values for protein binding ranged from 85% at low concentrations (2.7 mg l(-1)) to 52% at high concentrations (200.3 mg l(-1)). The percentage unbound was significantly higher (P < 0.0001) at high (peak) concentrations than at lower (trough) concentrations, confirming saturable protein binding. CONCLUSIONS: The protein binding of cefazolin is saturable in vivo in humans, both between and within patients.

Adult↗
PubMed1996

Long-term stability of cefuroxime and cefazolin sodium in intravenous infusions.

Cefazolin and cefuroxime sodium are often used as antibiotic infusions for hospitalized patients. Because advance preparation of these intravenous solutions is efficient, the stability of both antibiotics stored at 4 degrees C in polyvinyl chloride (PVC) bags was studied. Five bags of solutions containing either 1 g of cefazolin sodium or 1.5 g of cefuroxime sodium per 100 ml of 5% dextrose were studied for 1 month by high-performance liquid chromatography (HPLC), visual inspection and pH measurement. No colour change or precipitation was observed. The pH values of both drugs increased significantly over the period of study. Based on a shelf-life of 90% residual potency, the cefuroxime sodium concentration was stable for 13 days when stored at 4 degrees C, and the cefazolin sodium concentration was stable for at least 30 days at 4 degrees C. Within these limits, both antibiotics may be prepared in advance by a centralized intravenous admixture service.

Cefazolin↗
PubMed1980

The prevention of post-appendicectomy sepsis by metronidazole and cefazolin: a controlled double blind trial.

A double blind, randomized, controlled trial was carried out at two hospitals to try the effect of metronidazole, which is effective against most anaerobes, and cefazolin, which is effective against many aerobic organisms, singly and in combination, on the incidence of wound sepsis following appendicectomy. Patients were placed at random into one of four groups; to receive metronidazole and placebo, cefazolin and placebo, metronidazole and cefazolin, or double placebo. Patients with generalized peritonitis were excluded for ethical reasons. Treatment was started before operation and continued eight-hourly for twenty-four hours. All patients in the trial were followed up at about two weeks after discharge from hospital and their wounds inspected. Two hundred and seventy-one patients were assessed. Sepsis rates at the two hospitals were similar. On the untreated controls, 30% discharged pus from their wounds, and in the groups receiving one drug only, about 20%. In those receiving both drugs the infection rate was 3%, a highly significant difference from that in the other three groups.

Adolescent↗
PubMed1991

[Formation of biofilm by slime producing Staphylococcus epidermidis and bactericidal activity of cefazolin].

Slime production was studied in a total of 598 strains of Staphylococcus aureus and 11 species of coagulase negative staphylococci and the relationship of the slime production and biofilm formation was investigated. The high slime production was obtained in 42 of 263 strains (16%) of S. epidermidis only. The adherence of S. epidermidis to biomedical silicone discs (S discs) and biofilm formation were investigated in vitro in high slime producing and non-producing strains. The adherence rates of S. epidermidis to the S discs ranged from 2.3 to 14.8%. There was no relationship between slime production by S. epidermidis and the adherence rates. Biofilm was formed only in slime producing strains with cell growth on the S discs when they were incubated. The process of the biofilm formation was obtained by scanning electron microscopy; there were many projections, probably slime secreted from the cells, on the cell surface, and picture showing agglutination of cell by crosslinking. The bactericidal activity of cefazolin, cefmetazole and flumoxef against S. epidermidis after formation of the biofilm decreased more markedly than that before formation. Cefazolin reduced the number of S. epidermidis and eliminated the formed biofilm in an in vitro simulation model of serum concentration in human after drip infusion of 2 g of cefazolin.

Cefazolin↗
PubMed1976

Synergism of cefazolin-gentamicin against enterococci.

A miniaturized technique for detecting antibiotic synergy by using microliter volumes was perfected. With this microtiter serial dilution method, the effect of the previously untried combination of cefazolin and gentamicin on 10 strains of enterococci was evaluated. At clinically achievable concentrations, the combination of cefazolin and gentamicin was found to be synergistic against all 10 strains when the data were plotted in the form of an isobologram. These results were compared with the conventional method of detecting synergy in vitro, namely, the determination of the rate of killing of the microorganisms with the antibiotics, singly and in combination. Similar results were also observed. These findings indicate that the microtiter serial dilution technique is a useful method for the routine determination of drug synergy. Moreover, in a patient with penicillin hypersensitivity and enterococcal infection, the combination of cefazolin and gentamicin should be considered for possible therapy.

Cefazolin↗
PubMed1978

HR 756, a highly active cephalosporin: comparison with cefazolin and carbenicillin.

HR 756, a new parenteral cephalosporin, was compared with cefazolin and carbenicillin for activity against a total of 264 strains of Pseudomonas aeruginosa, Escherichia coli, Klebsiella spp., Proteus mirabilis, Proteus spp. (indole positive), Enterobacter spp., Salmonella typhi, Serratia marcescens, Providencia stuartii, and Staphylococcus aureus. In every comparison, except that with the last organism, HR 756 was clearly more active than cefazolin and carbenicillin. All three compounds had similar activity against penicillin-susceptible staphylococci; against penicillin-resistant strains, HR 756 and cefazolin were equally active and superior to carbenicillin. HR 756 was compared with penicillin for activity against strains of Streptococcus pyogenes, Lancefield group D streptococci, and Neisseria gonorrhoeae; with ampicillin against Haemophilus influenzae; and with cefoxitin against Bacteriodes fragilis. HR 756 was clearly more active than the respective reference compounds in all of these comparisons, except those involving the streptococci. HR 756 and penicillin were essentially equally active against S. pyogenes; against Lancefield group D, penicillin was 32 times as active as HR 756. HR 756 not only compared favorably with the reference compounds with respect to relative activity, but also effected growth inhibition of essentially all test organisms (P. aeruginosa and group D streptococci excepted) at remarkably low concentrations ranging from 0.015 to 2.0 mug/ml. A series of seven transfers of selected strains of E. coli, Klebsiella spp., S. aureus, and P. aeruginosa through medium containing HR 756 led to emergence of strains with significant levels of resistance to the agent. Resistance to HR 756 was retained for at least seven transfers through plain medium.

Bacteria↗
PubMed1979

Clinical pharmacokinetics and safety of high doses of ceforanide (BL-S786R) and cefazolin.

The pharmacokinetics and safety of ceforanide and cefazolin were compared in normal subjects after 30-min intravenous infusions of 2-, 3-, and 4-g single doses and 4-g twice-daily doses for 10 days. No significant differences were observed in plasma-renal pharmacokinetic parameters between single and multiple doses of ceforanide. Half-life (t((1/2)), 2.8 h), plasma clearance (Cl(p), 48 ml/min per 1.73 m(2)), and renal clearance (Cl(0-12h) (r), 47 ml/min per 1.73 m(2); tubular secretion, 44%, and glomerular filtration, 56%) did not change with increased dose or on multiple dosing. No significant change was observed in t((1/2)) (1.9 h), area under the plasma concentration-time curve, Cl(r) (60 ml/min per 1.73 m(2); tubular secretion, 80%, and glomerular filtration, 20%), or Cl(p) (75 ml/min per 1.73 m(2)) for 4-g single doses compared with twice-daily administration of cefazolin. A small increase in cefazolin clearance was observed when plasma concentrations were greater than 100 mug/ml, when the single dose was increased from 2 to 4 g; this was a result of the decrease in percentage of plasma protein binding and increased renal clearance due to increased glomerular filtration. The increase in renal clearance resulted in a lack of linear proportionality of the plasma area under the curve with dose over a range of 2 to 4 for both cephalosporins, although this effect was much less marked with ceforanide. Both compounds were well tolerated both locally and systemically. There was no evidence of any change in renal function based on clearances of drug, p-aminohippuric acid, or creatinine, and other standard clinical parameters.

Adult↗
PubMed1980

Comparative pharmacokinetics of ceforanide (BL-S786R) and cefazolin in laboratory animals and humans.

Ceforanide (BL-S786R) is a new, broad-spectrum, parenteral cephalosporin. Pharmacokinetic properties were determined in rats (100 mg/kg), rabbits (30 mg/kg), dogs (25 mg/kg), and humans (2 g or 30 mg/kg) and compared with equivalent single doses of cefazolin. Plasma half-lives for ceforanide and cefazolin were 1.1 and 0.5 h in the rat, 5 and 0.3 h in the rabbit, 1 and 0.8 h in the dog, and 2.6 and 2 h in humans, respectively. The slower elimination of ceforanide, as reflected by longer plasma half-life, larger area under the curve, and peak plasma concentrations, was due to slower body and renal clearances. The apparent volumes of distribution of ceforanide and cefazolin were comparable. Rats, dogs, and humans excreted 80 to 100% of the ceforanide dose in the 0- to 24-h urine; rabbits excreted only 50%. Tubular secretion constituted 50% of ceforanide renal excretion in rabbits, dogs, and humans and 90% in rats; the remainder was excreted by glomerular filtration. There was no apparent correlation between the extent of tubular secretion and degree of plasma protein binding in different species. There was no significant pharmacokinetic interaction between ceforanide and amikacin in the rat. The slower elimination kinetics of ceforanide are indicative of the potential for a longer dosing interval and more effective antibiotic therapy as compared with available cephalosporins.

Adult↗
PubMed1980

Carbenicillin plus cefazolin with or without mecillinam as an early treatment of bacteremia caused by gram-negative organisms: randomized double-blind study.

Mecillinam or a placebo was added to a combination of cefazolin and carbenicillin as an early therapy of septicemia caused by gram-negative organisms in patients with serious underlying diseases, none of whom was neutropenic, however. Patients in whom infection was caused by pathogens against which mecillinam and cefazolin or mecillinam and carbenicillin were synergistic might have responded more often than patients treated with nonsynergistic combinations. However, overall results did not show any benefit from combining mecillinam with cefazolin and carbenicillin. This study suggests that in nonneutropenic patients with septicemia caused by gram-negative organisms, there is no need to intensify antimicrobial therapy beyond a certain point of efficacy. The measurement of the bactericidal activity in the serum of treated patients might serve as guide for adequate therapy.

Amdinocillin↗
PubMed1980

Therapeutic effects of cefotiam and cefazolin on experimental pneumonia caused by Klebsiella pneumoniae DT-S in mice.

The efficacies of several dosage schedules, productive of plasma levels of cefotiam and cefazolin of short and long duration and starting at three levels of cefotiam and cefazolin of short and long duration and starting at three different times (3, 18, and 30h) after infection, were examined in experimental pneumonia caused by Klebsiella pneumoniae DT-S in mice. With each of the multiday regimens there was a large segment of the day when plasma levels fell below assayable concentrations. In all cases, cefotiam proved about eight times as active as cefazolin, indicating that the potent in vitro antibacterial activity of cefotiam was well reflected in the therapeutic effect in this model infection. As judged by the total dose administered, the regimen of cefotiam producing a low but sustained plasma level gave better therapeutic effects than that exhibiting a high but transient plasma level. The cefotiam levels in the plasma of mice that received the regimen effective when initiated at 18 h after infection were less than the expected levels in humans after intravenous infusion of the usual clinical dose.

Animals↗
PubMed1981

Moxalactam and cefazolin: comparative pharmacokinetics in normal subjects.

Moxalactam, a new beta-lactam antibiotic with a wide in vitro spectrum of activity, was compared with cefazolin after intravenous and intramuscular administration of 1.0 g in a double-blind crossover design in 21 adult male subjects with normal renal function. Serum samples were obtained at 0.5, 1, 2, 3, 4, 6, 8, and 12 h, and urine was collected at 0 to 2, 2 to 4, 4 to 6, 6 to 8, and 8 to 12 h after dosing. Intravenous kinetics were described by a linear two-compartment model. For moxalactam, the drug clearance and volume of distribution were larger (115.2 versus 75.9 ml/min per 70 kg, P = 0.001, and 0.44 versus 0.19 liter/kg, P less than 0.001, respectively), and the t1/2beta was longer (3.47 versus 2.18 h, P = 0.01), with correspondingly smaller area under the curve (151 versus 236 h x mg/ml, P = 0.003) and lower serum concentration at 30 min (62 versus 106 micrograms/ml, P = 0.003) than cefazolin. Intramuscular kinetics were similar and were well described by a single-compartment model. Urinary recovery was essentially identical for both drugs: 55 to 75% in 8 h. Consistent departures from the two-compartment model for moxalactam (not noted for cefazolin) suggested enterohepatic recirculation of moxalactam. Both drugs were well tolerated, and no adverse reactions were noted.

Adult↗
PubMed1981

Ceforanide and cefazolin therapy of pneumonia: comparative clinical trial.

Ceforanide is a new (parenteral) long-acting cephalosporin with antimicrobial activity comparable to those of other second-generation cephalosporins. In a randomized prospective study, patients with community-acquired bacterial pneumonia were treated with ceforanide at 0.5 g every 12 h (28 cases) or with cefazolin at 1.0 g every 8 h (26 cases). The study groups were comparable in clinical and laboratory findings, including etiological diagnosis. Streptococcus pneumoniae was isolated from the sputum of 38 patients, of whom 8 (21%) were bacteremic. Mean peak and trough serum levels of ceforanide drawn 1 and 11.5 h after the 0.5-g intravenous dose were 39.6 and 2.5 microgram/ml, respectively. Of the 50 patients evaluable for efficacy, all responded clinically with no serious adverse reactions. In spite of clinical improvement and in vitro susceptibility, Haemophilus influenzae persisted in the sputum of five of the eight cefazolin-treated patients and four of the five patients treated with ceforanide. Ceforanide appears to be as safe and effective as cefazolin for the therapy of pneumonia caused by S. pneumoniae or H. influenzae, but neither drug was effective in clearing H. influenzae from the sputum.

Adult↗
PubMed1982

Comparative in vitro activities of temocillin and cefazolin against Klebsiella pneumoniae.

Temocillin (BRL 17421) a new penicillin, was compared with cefazolin against 20 strains of Klebsiella. The in vitro minimal bactericidal concentration of cefazolin was twice as active as that of temocillin. Serum bactericidal levels obtained in volunteers treated with temocillin were consistently higher than those levels reached after the administration of cefazolin at the 6-h sampling.

Cefazolin↗
PubMed1985

Comparison of moxalactam and cefazolin as prophylactic antibiotics during cesarean section.

Prophylactic antibiotics have been shown to be effective in decreasing the incidence of febrile morbidity associated with cesarean section after labor. However, the relative effectiveness of different single antibiotics has been studied infrequently, and these investigations have been limited by small patient samples. Several new, broad-spectrum antibiotics are now available, and any further benefit from more traditional antibiotics for surgical prophylaxis remains untested. A randomized prospective double-blind therapeutic trial was therefore undertaken to compare the value of a first-generation cephalosporin (cefazolin) with a new third-generation cephalosporin (moxalactam). Between July 1981 and June 1983, 254 qualifying women who underwent primary cesarean section after labor were randomly chosen for either of the two treatment groups. Although not statistically significant, the rates of febrile morbidity, wound infection, and endometritis were less for those treated with cefazolin (4.0, 3.2, and 0.8%, respectively) than for those treated with moxalactam (9.2, 7.7, and 1.6%, respectively). No serious adverse effects were apparent in the mother and newborn infant from short-term exposure to either drug. Although the newer, more expensive, and broader-spectrum cephalosporin, moxalactam, was associated with a low postoperative febrile morbidity rate and short postpartum hospitalization, it was no more beneficial than cefazolin.

Anti-Bacterial Agents↗
PubMed1985

Relevance of serum protein binding of cefoxitin and cefazolin to their activities against Klebsiella pneumoniae pneumonia in rats.

An experimental Klebsiella pneumoniae pneumonia in rats was used to study the effect of protein binding of cefoxitin and cefazolin on their therapeutic activity. Both cephalosporins were similar with respect to their antimicrobial activity against the K. pneumoniae in vitro, but they differed in their degree of protein binding, being 34% for cefoxitin and 89 to 93% for cefazolin in uninfected rats and 24 and 71 to 83%, respectively, in infected rats. Various doses of these agents were administered by continuous infusion, which started 5 h after bacterial inoculation and continued for 65 h. Antimicrobial response was evaluated with respect to the numbers of bacteria recovered from lung and blood at the end of treatment. An inhibitory effect of protein binding on the in vivo antimicrobial activity was demonstrated. Cefoxitin was therapeutically effective at a constant plasma level that reached the MIC. To obtain a similar effect with cefazolin the plasma level of that drug had to be increased to a concentration more than three times the MIC.

Animals↗
PubMed1986

Comparative in vitro evaluation of cefonicid, cefazolin, and penicillin against viridans group streptococci isolated from blood.

The in vitro activity of cefonicid against 60 strains of viridans group streptococci isolated from blood of patients with bacteremia and infective endocarditis was compared with those of cefazolin and penicillin. Cefonicid was less active than cefazolin, and both cephalosporins were less active than penicillin. The MIC50 and MIC90 for the strains tested were 0.06 and 1 microgram/ml for penicillin, 0.125 and 8 micrograms/ml for cefazolin, and 4 and 32 micrograms/ml for cefonicid.

Cefamandole↗
PubMed1987

Activity of cefazolin and two beta-lactamase inhibitors, clavulanic acid and sulbactam, against Bacteroides fragilis.

One hundred clinical isolates of the Bacteroides fragilis group of bacteria were tested by agar dilution for susceptibility to cefazolin alone or in combination with clavulanic acid or sulbactam. For cefazolin, the MIC for 50% of the isolates (MIC50) was 32 micrograms/ml, the breakpoint for susceptibility. With the addition of 0.5 micrograms of clavulanic acid per ml, the MIC for 90% of the isolates (MIC90) was 8 micrograms/ml, well within the achievable range of concentrations in serum or tissue. Similarly, with the addition of 0.5 micrograms of sulbactam per ml, the MIC90 was 16 micrograms/ml. The addition of a higher concentration (4.0 micrograms/ml) of clavulanic acid or sulbactam resulted in MIC90S which were fourfold lower than those with 0.5 micrograms/ml. A fixed ratio of cefazolin-beta-lactamase inhibitor of 4:1 resulted in an MIC50 and MIC90 which were intermediate between the 0.5- and 4.0-micrograms/ml fixed concentration of beta-lactamase inhibitor.

Bacteroides fragilis↗