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At least 19 recordsLinked to original sources

PubMed1984

The action of beta-lactamases on desacetyl-cefotaxime and cefotaxime.

Desacetyl-cefotaxime is the main cefotaxime metabolite. Its antibacterial activity is less than that of the parent molecule, but the combination of cefotaxime and desacetyl-cefotaxime is often synergistic. We analysed the hydrolysis of desacetyl-cefotaxime, in comparison with cefotaxime, by 10 beta-lactamases, mostly cephalosporinases, isolated from various Gram-negative species. From partially purified beta-lactamase preparations of high specific activity, we determined the maximum rates of hydrolysis (Vm) and the Michaelis constants (Ki and Km when possible). It appeared for 7 beta-lactamases the rate of desacetyl-cefotaxime hydrolysis was 2.1 times greater than that of cefotaxime, in terms of geometrical mean value, but with 3 enzymes no hydrolysis was shown for one compound. For 8 enzymes, the Ki, and sometimes Km, of desacetyl cefotaxime are 39 times higher than those of cefotaxime (geometric mean value), which corresponds to a lower affinity.

Cefotaxime↗

PubMed1985

Cefotaxime and desacetyl cefotaxime kinetics in renal impairment.

Cefotaxime and desacetyl cefotaxime kinetics after a single, 1 gm intravenous dose were evaluated in five groups of subjects: group I, normal creatinine clearance (CLCR greater than 90 ml/min); group II, mild renal insufficiency (CLCR 30 to 89 ml/min); group III, moderate renal insufficiency (CLCR 16 to 29 ml/min); group IV, severe renal insufficiency (CLCR 4 to 15 ml/min); and group V, end-stage renal disease requiring maintenance hemodialysis (CLCR less than 6 ml/min). The steady-state volume of distribution (Vss) ranged from 10% to 55% of body weight but was not related to CLCR. The terminal t1/2 values of cefotaxime and desacetyl cefotaxime were 0.79 and 0.70, 1.09 and 3.95, 1.55 and 5.65, 2.54 and 14.23, and 1.63 and 23.15 hours in groups I to V, respectively. There were no significant changes in Vss or t1/2 after multiple dosing, but there were significant correlations between CLCR and cefotaxime total body clearance, cefotaxime and desacetyl cefotaxime renal clearance, and cefotaxime nonrenal clearance. Dosage regimens for the use of cefotaxime in patients with renal impairment are proposed.

Acute Kidney Injury↗

PubMed1983

Elimination kinetics of cefotaxime and desacetyl cefotaxime in patients with renal insufficiency and during hemodialysis.

The pharmacokinetics of cefotaxime, a new semi-synthetic cephalosporin for injection, was studied in 30 subjects with various degrees of renal function after a single 1-gram intramuscular injection. Serum and urinary concentrations of cefotaxime and desacetyl cefotaxime were determined by high pressure liquid chromatography. The pharmacokinetic parameters of cefotaxime were obtained using a one-compartment open model. The mean serum half-life of the parent compound (cefotaxime), 0.87 h in normal subjects, was prolonged to 2.35 h in hemodialysis patients. There was a significant linear correlation between the elimination rate constant of cefotaxime and creatinine clearance. The mean cumulative urinary recovery of the administered dose in the 24-hour urine was 51.7% as cefotaxime and 25.6% as desacetyl cefotaxime in normal subjects.

Adult↗

PubMed1993

Effectiveness of single dose prophylaxis with cefotaxime and metronidazole compared with three doses of cefotaxime alone in elective colorectal surgery.

OBJECTIVE: To compare three doses of cefotaxime alone with a single dose of cefotaxime and metronidazole for the prophylaxis of infection after elective colorectal operations. DESIGN: Prospective random control trial. SETTING: Hillerød and Frederiksberg Hospitals, Copenhagen, Denmark. SUBJECTS: 660 consecutive patients who were to undergo elective colorectal operations during a 48 month period (January 1987-January 1991); 93 (14%) were withdrawn after randomisation leaving 567 for assessment. INTERVENTIONS: Mechanical bowel preparation, and then either cefotaxime (Claforan) 2 g intravenously at induction of anaestesia and 3 and 9 hours later (n = 280) or a single dose of cefotaxime 2 g plus metronidazole (Flagyl) 1.5 g intravenously at induction of anaestesia (n = 287). RESULTS: 44 patients in the cefotaxime group developed wound infection (16%) compared with 19 (7%) in the combined group (p < 0.001). In the cefotaxime group 22 of the 241 patients who had an anastomosis developed leaks (9%) compared with 8 of the 239 in the cefotaxime/metronidazole group (3%). There were no differences in the incidence of intra-abdominal abscesses or burst abdomens. The most common organisms isolated from wounds were Escherichia coli and Bacteriodes fragilis. CONCLUSION: One dose of cefotaxime and metronidazole is active against a wide range of organisms and resulted in significantly fewer wound infections than three doses of cefotaxime alone.

Adult↗

PubMed1984

Pharmacokinetics of cefotaxime and desacetyl-cefotaxime in neonates.

Cefotaxime was given to neonates as treatment of infection in a dose of 25 mg/kg 12 hourly by intravenous injection. Blood samples taken by heel-prick were specially treated to minimize any effect of haemolysis on the hydrolysis of cefotaxime. The mean peak plasma concentrations of cefotaxime on the first, second and third days of therapy were 43, 40 and 52 mg/l, respectively, with mean plasma half lives of 4.0, 2.7 and 3.2 h. The mean peak concentrations of desacetyl-cefotaxime were about a quarter of those of cefotaxime, which is in good agreement with adult studies, but much lower than those previously published in studies with neonates. These results emphasize the care that is necessary in the assay of body fluids and tissues for cefotaxime and desacetyl-cefotaxime if accurate results are to be obtained.

Cefotaxime↗

PubMed1987

A prospective randomised comparison of cefotaxime vs. netilmicin vs. cefotaxime plus netilmicin in the treatment of hospitalised patients with serious sepsis.

93 patients were enrolled into a prospective randomised study to determine the efficacy and safety of netilmicin, cefotaxime or their combination in the treatment of sepsis caused by susceptible strains of Enterobacteriaceae or staphylococci. 83 patients were evaluable for safety, 74 for clinical efficacy and 63 for microbiological response including 36 patients (57%) with positive blood cultures. There were significantly more clinical failures with cefotaxime than with netilmicin even when urinary tract sepsis was excluded. Microbiological failures occurred more frequently in the cefotaxime arm and were associated with Klebsiella and Enterobacter spp. Four cefotaxime failures were subsequently successfully treated with netilmicin. More mixed infections were however enrolled by chance into the cefotaxime arm. The statistical difference between netilmicin and cefotaxime is not significant if mixed infections are excluded. There was no difference in efficacy between the netilmicin and combination groups although superinfection was seen in the latter group. The incidence of nephrotoxicity was greater in the netilmicin group but not significantly so. Only one minor case of ototoxicity was detected in the 41 patients receiving netilmicin who had serial audiograms. The results suggest that netilmicin is a more effective agent than cefotaxime for treating life-threatening infections with susceptible Enterobacteriaceae or staphylococci particularly with infections in non-urinary tract sites. If dosage of netilmicin is closely monitored by measuring serum concentrations, toxicity is minimal.

Adolescent↗

PubMedDate not supplied

[Prophylactic and therapeutic action of ceftazidime in comparison to that of cefotaxime and combined use of cefotaxime with other antibiotics in experimental plague of albino mice].

In a model of experimental plague of albino mice the prophylactic and therapeutic action of ceftazidime by comparison with that of cefotaxime and the combined action of cefotaxime with other antibiotics were studied. The studies showed that the drugs had a high prophylactic and therapeutic action when used in doses of 200 to 400 mg/kg (ceftazidime) and 400 to 800 mg/kg (cefotaxime). The survival of the animals amounted to 80-100 per cent. The therapeutic effect was defined by the drug dose and the treatment term. When the treatment term was decreased to 3 days, ceftazidime proved to be more advantageous than cefotaxime. When the antibiotic dose was insufficient, the treatment efficacy was shown to depend on the infective dose. The use of cefotaxime in combination with aminoglycosides (gentamicin or sisomicin), rifampicin or doxycycline significantly increased the percentage of the animal survival in comparison to the use of the drugs alone and promoted a rapid elimination of the pathogens in the animals. The combined use of cefotaxime and gentamicin or sisomicin as well as cefotaxime and rifampicin had a synergistic action.

Animals↗

PubMed1991

Ascitic fluid and serum cefotaxime and desacetyl cefotaxime levels in patients treated for bacterial peritonitis.

Forty-one episodes of ascitic fluid infection were treated with cefotaxime 2 g intravenously every 8 hr, and ascitic fluid and serum were sampled 6, 12, 24, 48, and 96 hr after the first dose of antibiotic. Concentrations of cefotaxime and desacetyl cefotaxime were measured in ascitic fluid and serum by high-performance liquid chromatography. There was essentially 100% penetration of cefotaxime and metabolite from serum into ascitic fluid at all time points. Ascitic fluid was sterilized in 94% of episodes after the first dose of antibiotic. The ascitic fluid concentration of cefotaxime 6 hr after the first dose of antibiotic was greater than 20 times the minimal inhibitory concentration of the drug for 90% of the isolated flora. This rapid ascitic fluid penetration of cefotaxime in high concentration explains the rapid sterilization of ascitic fluid by the drug in the setting of bacterial peritonitis and obviates the need to give a loading dose or intraperitoneal injection.

Adult↗

PubMed1982

The cooperation of cefotaxime and desacetyl-cefotaxime with respect to antibacterial activity and beta-lactamase stability.

Desacetyl-cefotaxime, the main metabolite of cefotaxime, possesses a broad antibacterial spectrum. Its activity is lower than that of cefotaxime, but significantly surpasses that of cefazolin against gram-negative bacteria. The beta-lactamase stability of desacetyl-cefotaxime is higher than that of the parent compound. This beta-lactamase stability might be responsible for the synergistic effects of cefotaxime and desacetyl-cefotaxime occasionally seen in in vitro combination studies.

Bacteria↗

PubMed1995

Criteria for testing the susceptibility of Streptococcus pneumoniae to cefotaxime and its desacetyl metabolite using 1 microgram or 30 micrograms cefotaxime disks.

In vitro susceptibility tests were performed with 350 selected strains of Streptococcus pneumoniae to evaluate disk diffusion tests with 30 micrograms and 1 microgram cefotaxime disks. Zones were compared to MICs of cefotaxime with and without its desacetyl metabolite. Cefotaxime was two to eight times more active than desacetyl cefotaxime, but the two compounds were additive when combined in vitro. For 30 micrograms disks, zone size breakpoints were < or = 27 mm, 28-30 mm and > or = 31 mm for resistant, intermediate and susceptible, respectively. For 1 microgram disks, those zone size criteria were reduced to < or = 13 mm, 14-16 mm and > or = 17 mm. The 30 micrograms disk that is currently available for testing other species can be used for testing pneumococci; however, the 1 microgram disk has some important advantages.

Cefotaxime↗

PubMed1990

Antibiotic prophylaxis with cefotaxime in endoscopic extraction of upper urinary tract stones: a randomized study. The Cefotaxime Cooperative Group.

This French multicentre, placebo-controlled, double-blind study investigated the efficacy of a single dose of cefotaxime 1 g iv in the prophylaxis of patients undergoing endoscopic extraction of urinary tract stones. Postoperative fever occurred in 12 patients in the placebo group and in nine in the cefotaxime group (no significant difference). The incidence of postoperative bacteriuria, between the first and third postoperative day, was significantly higher in the placebo group (15/60, 25%) than in the cefotaxime group (5/60, 8.5%). This controlled study clearly demonstrates the efficacy of antibiotic prophylaxis in endourological procedures. Cefotaxime significantly reduced the incidence of early postoperative bacteriuria without causing any significant side effects.

Adult↗

PubMed1987

Antimicrobial activity of ceftriaxone, cefotaxime, desacetylcefotaxime, and cefotaxime-desacetylcefotaxime in the presence of human serum.

Eighty-seven organisms were tested against ceftriaxone, cefotaxime, desacetylcefotaxime, and the combination of cefotaxime and desacetylcefotaxime (1:1 ratio) in broth containing 0, 25, or 50% human serum. In the presence of human serum, ceftriaxone MICs were four- to eightfold higher than those obtained in broth, changing 98% of Staphylococcus aureus strains from the susceptible to the moderately susceptible category and 53% of selected gram-negative strains to a more resistant category. The MICs of cefotaxime, desacetylcefotaxime, and cefotaxime plus desacetylcefotaxime were not adversely affected by human serum; in fact, the bactericidal activity was slightly improved.

Bacteria↗

PubMed1990

Antibacterial activity of combined cefotaxime and desacetyl-cefotaxime against aerobic and anaerobic gram-negative bacilli.

Synergy between cefotaxime and desacetyl-cefotaxime was evaluated against 12 strains (9 Enterobacteriaceae and 3 Bacteroides fragilis) by the chequerboard technique. A 1:1 combination of cefotaxime and desacetyl-cefotaxime was synergistic against two-thirds of the 12 strains tested. The in vitro activity of the combination was compared with that of four other beta-lactam antibiotics against 96 recent clinical isolates: 78 Enterobacteriaceae, 8 Haemophilus influenzae, 10 B. fragilis. The MICs of the combination for Gram-negative bacilli were similar to those of ceftazidime. Cefotaxime/desacetyl-cefotaxime was more active than cefotetan, cefonicid and piperacillin against Enterobacteriaceae and H. influenzae.

Bacteroides fragilis↗

PubMed1986

The sustained release of cefotaxim from a fibrin-cefotaxim compound in treatment of osteitis. Pharmacokinetic study and clinical results.

Following a survey of the literature regarding clinical examinations and experimental studies of local absorbable carrier for an antibiotic in treatment of osteitis, a study is presented concerning clinical experience with 46 patients treated with a cefotaxim-loaded fibrin sealant. In connection with simultaneous focal sanitation the clinical results were satisfying. When autogenous cancellous bone was added at the same time, only one surgical operation was necessary in some cases to show results equivalent to other methods. Postoperatively, the cefotaxim levels in the blood and in the wound drainage fluid were measured. The serum cefotaxim concentrations were low and only identifiable for a period of 36h, whereas the wound drainage fluid contained very highly effective antibacterial concentrations over a measured period of 3.5 days. The best results were seen in cases of hematogenic osteomyelitis. The disadvantage of this system is the quick release of the antibiotic by diffusion. Therefore, high concentrations can be obtained only for a short period of several days.

Administration, Topical↗

PubMedDate not supplied

Study of cefotaxime twice daily for the therapy of postoperative pneumonia. The German Cefotaxime Study Group.

A total of 548 patients with postoperative pneumonia were treated with 1 or 2 g cefotaxime twice daily. Of the 88 patients without serious underlying diseases who received the 1-g 12-h dosage regimen, all were considered to be clinically cured, and all 54 isolated pathogens were eradicated or presumed to be eradicated. In the group with severe infection or severe underlying disease receiving 2 g 12-h cefotaxime, the overall clinical success rate (cured plus improved) was 98.4%. Results from this study support the use of cefotaxime as an alternative to empiric monotherapy for nosocomial pneumonia in surgical-service patients who are not neutropenic or on long-term artificial ventilation.

Aged↗

PubMed1984

Cefotaxime and desacetyl-cefotaxime blood levels in hepatic dysfunction.

Serum levels of cefotaxime and desacetyl-cefotaxime were studied in 18 patients with hepatic cirrhosis after an intravenous bolus injection of 2 g of cefotaxime. Blood levels were independent of the degree of hepatic dysfunction and did not differ from those reported in normal individuals.

Adult↗

PubMed1981

Comparative determination of cefotaxime and desacetyl cefotaxime in serum and bile by bioassay and high-performance liquid chromatography.

In rat serum as well as in human serum and bile after injection of cefotaxime (CTX), the parent compound and the active metabolite desacetyl cefotaxime (dCTX) have been demonstrated by quantitative analysis with high-performance liquid chromatography (HPLC). Simultaneous determination of CTX by bioassay using test organisms sensitive to both CTX and dCTX resulted in spuriously high concentration readings of CTX. Using dCTX insensitive test organisms concentrations of cefotaxime obtained by agar diffusion test and by assay with HPLC were highly correlated. In human serum and bile after i.v. injection of 2 g CTX, as may be administered therapeutically, high concentrations of dCTX were observed. dCTX has a longer elimination half-life than the parent molecule. It is concluded that the measurement of CTX in biological fluids should be performed by HPLC or by bioassay with a selective test organism in order to obtain correct pharmacokinetic parameters.

Adult↗

PubMed1982

[Therapy with cefotaxime-cefotaxime/ticarcillin for bronchopulmonary infections in patients under intensive care. (author's transl)].

55 intensive care patients with an internal underlying disease were treated with cefotaxime, and 12 patients with bronchopulmonary infections were treated with the combination cefotaxime/ticarcillin. The following aspects were evaluated: clinical success, antimicrobial activity of bacteria in evidence before and after therapy, persistence of pathogens, and resistance. Renal function was monitored continuously in 21 patients over a period of 20 days in order to demonstrate nephrotoxic side-effects of cefotaxime when administered simultaneously with furosemide (in doses of mre than 1 g/day). In view of the clinical results and of the fact that the cefotaxime/ticarcillin combination is well tolerated by the kidneys, the possibility of efficient chemotherapy without aminoglycosides is being discussed for treatment of bronchopulmonary infections in patients under intensive care.

Aged↗