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At least 19 recordsLinked to original sources

PubMed1976

[The liver concentration of cephradin and cephacetril and their elimination in the bile].

Liver biopsies and serum samples were collected after intravenous application of 2 g cephradin (n = 13) or 2 g cephacetril (n = 11) during surgery. There was no difference in the serum levels of cephradin and cephacetril. 30 min. after i.v. application of cephradin the liver tissue concentration was 72.62 mcg/g. 30 min. after i.v. cephacetril the liver tissue concentration was 5.83 mcg/g. The quotient of liver tissue concentration to serum concentration for cephradin was between 0.36 and 0.83, and for cephacetril between 0.02 and 0.16. The excretion of cephradin and cephacetril in human bile was studied by collecting bile samples from the common bile duct via T-tube drainage (n = 17). Cholecystomized patients were given 2 g of antibiotics intravenously. Serum levels of cephradin were 263 mcg/ml 5 min after application, and 22 mcg/ml after 240 min. Serum levels of cephradin were 263 mcg/ml 5 min after application, and 22 mcg/ml after 240 min. Serum levels of cephacetril were 193 mcg/ml 5 min after application, and 27 mcg/ml after 240 min. The highest levels of cephradin in the bile were found 75 min after injection at a concentration of 86.4 mcg/ml; the highest level for cephacetril was 21.8 mcg/ml at 15 min. In patients with hyperbilirubinaemia cephradin reached a mean maximum concentration of 29.6 mcg/ml in bile samples, in comparison to 117.4 mcg/ml in normal patients, while no difference was seen with cephacetril. After intravenous administration of 2 g cephradin biliary concentration are achieved which may be sufficiently high to be effective not only against the very sensitive gram-positive organisms, but also against most strains of E. coli, Klebsiella and indol-negative Proteus. Cephradin is effective in the treatment of cholangitis and intrahepatic abscesses, as was observed in 18 patients. A free bile-flow is essential.

Bile↗

PubMed1976

Metabolic fate of cephacetrile after parenteral administration in rats and rabbits.

1. The metabolic fate of 14C-cephacetrile was studied in rats and rabbits. The plasma level of intravenously injected cephacetrile decreased with half-lives of 17 and 22 minutes in rats and rabbits respectively, this decline being associated with a rapid appearance of the active metabolite, desacetylcephacetrile. Intramuscularly injected cephacetrile was rapidly absorbed by rats with a maximum plasma level at 20 minutes and a half-life of 16 minutes. Cephacetrile and desacetylcephacetrile did not enter erythrocytes. Cephacetrile was weakly bound to the plasma protein in the rat, rabbit and man. 2. Both in rats and rabbits, almost all of the injected radioactivity was excreted in the urine within 72 hours as the intact antibiotic and desacetylcephacetrile, only small amounts appearing in feces via bile. Neither the gamma-lactone of desacetyl-7-cyanacetamidocephalosporanic acid nor the violet-reddish pigment (CGP-695) produced from cephacetrile were detectable in the plasma or urine of the animals. 3. In rats given the labeled antibiotic intravenously, the radioactivity was widely distributed with concentrations being high in the kidney, plasma and liver, and lowest in the brain. The radioactivity crossed the rat placenta and appeared in the fetus. Radioactivity in these tissues disappeared as the plasma level declined. 4. During daily intramuscular injection of 14C-cephacetrile to rat, no significant changes were observed in the peak level of the plasma radioactivity or in the half-lives. In addition, dosing of the labeled antibiotic for 7 days caused no increase in tissue levels of radioactivity.

Animals↗

PubMed1974

Double-blind comparison of cephacetrile with cephalothin-cephaloridine.

Under double-blind protocol, a controlled comparison was made between a new cephalosporin, cephacetrile, and cephalothin or cephaloridine. The patient's primary physician determined the indications for treatment, and the dosage was uniform for each route of administration. Infecting strains of staphylococci and Proteus mirabilis had a lower median inhibitory concentration for cephalothin than cephacetrile; the opposite was true for Escherichia coli and Klebsiella species. The average peak serum level 1 h after a dose of 2 g intravenously was 74.9 +/- 21 and 21.5 +/- 8.7 mug/ml for cephacetrile and cephalothin, respectively; 6 h after the dose, the respective levels were 12.4 +/- 4.3 and 3.7 +/- 0.9 mug/ml. Renal clearances were similar and the plasma clearance was proportional to the serum levels. In the urine, the concentration of cephacetrile was three times higher than that of cephalothin. Based on a percentage of therapeutic potential, success in the treatment of infections with susceptible organisms was 42 and 44% for the two different drug regimens. Initial bacterial resistance was found in about one-fifth of infections, and concomitant therapy with other drugs was practiced in one-half of the treatment courses. Intravenous use of cephacetrile was discontinued prematurely more often than was use of cephalothin, suggesting less tolerance. Although there was no overt toxicity, more than 75% of patients on either regimen had some form of unwanted response to treatment, the most common being superinfection. From this limited but controlled experience, cephacetrile can be considered comparable to cephalothin in antimicrobial treatment and overall side reactions.

Acetamides↗

PubMed1979

Lack of penetration of cephacetril into the cerebro-spinal fluid of patients without meningitis.

Six neurosurgical patients were given 2-4 g cephacetril intravenously at six hourly intervals. Serum and cerebrospinal fluid (CSF) concentrations were determined. Cephacetril activity was not detectable in the CSF when the blood-CSF barrier was intact. In two patients with increased CSF cell counts cephacetril was found in the CSF in low concentrations (0.1-0.8 mcg/ml). Our investigations show that cephacetril does not penetrate into the CSF unless there is an inflammation or other impairment of the blood-CSF barrier. Thus we could not confirm the results of some authors who found cephacetril in therapeutically effective concentrations in the CSF of healthy persons.

Adolescent↗

PubMed1976

Cephacetrile--application of pharmacokinetic data to dosage determination.

This pharmacokinetic investigation was based on the determination of serum and urinary levles of cephacetrile in 50 subjects given single intramuscular or intravenous doses of 0.5 or 1 gm of the antibiotic; 30 normal subjects, 10 patients with renal insufficiency, and 10 patients with chronic nephritis undergoing maintenance haemodialysis were included in this study. In normal subjects, mean serum half-life was 1.09 hours (Ke = 0.6337) after intramuscular injection of 0.5 gm cephacetrile, 1.31 hours (Ke = 0.5276) after intramuscular injection of 1 gm, and 0.89 hours (Ke = 0.7806) after intravenous injection of 1 gm. Absorption half-life was 0.45 hours after intramuscular injection of 1 gm cephacetrile. The urinary elimination of cephacetrile over the first 6 hours after injection was on the average 72.7% of the administered dose. After intravenous injection of 1 gm of the antibiotic, the plasma clearance of cephacetrile was 407 ml/min., and its renal clearance 313 ml/min. A linear correlation was found between the values of overall elimination rate constant (Ke) and creatinine clearance in the subjects under investigation (Ke = 0.0080 + 0.0061 ClCr). The established pharmacokinetic characteristics were used to calculate the maintenance and loading doses as well as the intervals between injections adjusted to creatinine clearance. These data constitute true dosage schemes adapted to the particular case of each patient according to his kidney function.

Cephacetrile↗

PubMed1973

Renal handling and lymph concentration of two cephalosporin analogues, cephacetrile and cephaloridine: an experimental study in dogs.

Cephacetrile (CIBA 36' 278-Ba) and cephaloridine (both cephalosporin derivatives) were compared in dogs with regard to their possible nephrotoxicity, renal handling, and concentration in the renal lymph. No adverse acute effect of either drug on the glomerular filtration rate and effective renal plasma flow was found at very high concentrations in the plasma, with or without concomitant administration of a potent diuretic (furosemide). Cephaloridine was filtered only by the kidney, whereas there was evidence that cephacetrile was also excreted by tubular secretion at low concentrations. The renal lymph concentration of the two antibiotics (in the hilar as well as the capsular lymph vessels) was found to be significantly lower than the simultaneous arterial plasma concentrations. When concentrations in the plasma were high, the relative lymph concentrations of cephaloridine and cephacetrile were in the same range as those of iothalamate (70 to 90% of the arterial plasma level), whereas at low plasma concentrations the lymph concentration of cephacetrile was markedly lower, a finding possibly explained by the active tubular secretion of cephacetrile.

Animals↗

PubMed1975

Cephacetrile, a new cephalosporin: in vitro, pharmacological and clinical evaluation.

Cephacetrile, a parenteral cephalosporin, was evaluated for in vitro antibacterial activity, clinical pharmacology and effectiveness in the treatment of severe infections. The antibacterial activity against 187 isolates was determined by an agar-dilution technique. The MICs were 0.06 to 0.5 mug/ml for Group A Streptococcus, D. pneumoniae, and Staph. aureus, 4-6 mug/ml for E. coli and Klebsiella-Enterobacter 8-32 mug/ml for Pr. mirabilis and more than 500 mug/ml for Ps. aeruginosa. A few strains of Klebsiella and E. coli had MICs of more than 125 mcg/ml. Serum levels after 0.5 and 1 g of i.m. cephacetrile were respectively 14.6 and 18.6 mug/ml after 1 hr, and 1.5 and 2.5 mug/ml after 6 hr. Serum levels after i.v. infusion of 0.5 and 1 g were respectively 16 and 25 mug/ml after 1 hr., and 1 and 2 mug/ml after 6 hr. Urine levels after 0.5 and 1 g i.m. cephacetrile were respectively 500 and 650 mug/ml in the 0-3 hr period, and 250 and 300 mug/ml in the 3-6 hr period. Renal clearance was 166 +/- 5 ml/min/1.73 m2; renal excretion was about 20% of the dose 6 hr after i.m. injection. Cephacetrile was well tolerated when administered i.m. with lidocaine. Mild phlebitis occurred sometimes after i.v. infusions. The clinical response, evaluated in 36 patients with severe systemic, respiratory and urinary infections, was good in all but two cases.

Bacteria↗

PubMed1973

Cephacetrile: clinical evaluation in 27 patients.

Cephacetrile, a new derivative of 7-aminocephalosporanic acid, was evaluated in 27 patients. Soft tissue infections due primarily to gram-positive cocci were treated in 16 patients; 12 had bacteriological and clinical cure, and 4 improved but the lesions resolved incompletely or cultures remained positive. Seven of eight patients with respiratory tract infections were cured, including three with pneumococcal pneumonia; the eighth proved to have a noninfectious process and failed to respond. Two patients with acute urinary tract infections due to Escherichia coli had prompt clinical and bacteriological improvement, but follow-up was incomplete. One patient with sepsis due to Staphylococcus aureus expired. Laboratory abnormalities observed during cephacetrile therapy included mild eosinophilia in four patients, thrombocytosis in nine, direct Coombs' test positivity in four, and an elevated serum glutamic pyruvic transaminase in eight patients. No evidence of nephrotoxicity was detected. Severe superinfection due to Enterobacter species was observed in one patient. Mean peak serum concentrations of cephacetrile were 22, 69, and 104 mug/ml after 1 g intramuscularly, 1 g intravenously, and 1.5 g intravenously, respectively. Thus, in early studies cephacetrile was efficacious for selected bacterial infections, but determination of its comparative value within the cephalosporin group of antibiotics requires further clinical investigation.

Bacterial Infections↗

PubMed1976

Cephacetrile in the treatment of female pelvic inflammatory disease.

The efficacy and tolerability of cephacetrile administered by the intravenous or intramuscular route was evaluated in an open-label study of 55 hospitalized females diagnosed as having mild to severe pelvic inflammatory disease. Rapid improvement was observed in most patients. All patients were classified as clinically cured or significantly improved. Pain was absent or mild in 86% of the patients who received cephacetrile by intramuscular injection. Seventy-two percent of the patients given the drug intravenously experienced no localized pain. Phlebitis occurred in 6 of the 53 patients (11%) who received intravenous cephacetrile and thrombosis was present in 3 (6%). Rash and puritus was reported in 1 patient. Results of this study suggest that cephacetrile is an important and useful drug in the treatment of pelvic inflammatory disease.

Adolescent↗

PubMed1979

Pharmacokinetics of cephacetrile in patients undergoing haemodialysis.

The pharmacokinetics of cephacetrile were studied after its administration as a single i.v. bolus injection of 15 mg/kg body weight to 11 patients with terminal renal inpairment undergoing haemodialysis for 6 h. A two-compartment kinetic model was used to describe the biphasic decrease in plasma concentration. The quantities of antibiotic in the central and peripheral compartments, and the amounts eliminated, were calculated for different times. During haemodialysis sessions, the average pharmacokinetic parameters of cephacetrile determined at the dialyser input were: a = 5.03 h-1, beta = 0.458 h-1, K12 = 2.337 h-1, K21 = 1.996 h-1 K13 = 1.154 h-1, Vc = 5.5081, Vp = 6.4481, Vdss = 11.9561. As a function of the pharmacokinetic parameters of cephacetrile, a regimen of multiple doses was established for patients with terminal renal impairment, which will guarantee safe and effective concentrations of the antibiotic.

Adolescent↗

PubMed1986

Effects of cephacetrile on reproduction cycle.

The research of possible effects of cephacetrile (Celospor) on the reproductive function was carried out on two animal species, rats and rabbits. The animals were divided into experimental groups, each treated subcutaneously with different amounts of cephacetrile (50, 100 and 500 mg/kg/die), control group receiving physiological solution. Effects of the preparation on fertility and post-natal growth in rats were analyzed, and trials were performed to test perinatal toxicity and teratogenesis in rabbits. From the observation of the experimental data collected it can be assumed that cephacetrile, administered subcutaneously in the given doses--1, 2 and 10 times, respectively, higher than the maximum therapeutic dose advisable--does not alter fertility, gestation and post-natal development of term foetuses of rats and fertility and gestation of rabbits.

Animals↗

PubMed1979

High-performance liquid chromatographic determination of cephacetrile.

A rapid and accurate quantitative determination of cephacetrile in finished bulk and dosage forms is reported. The high-performance liquid chromatographic method is free of interference by acetyl hydrolysis products and synthesis by-products. The assay can be performed in about 15 min, affording less than 0.7% coefficients of variation within and between days. The chromatographic results are in good agreement with the microbiological assay requested by the "Code of Federal Regulations" for certification of cephacetrile sodium.

Cephacetrile↗

PubMed1977

Studies on serum and cerebrospinal fluid levels of cephacetrile in neonates.

The serum half-life of cephacetrile and its penetration from the serum into the cerebrospinal fluid (CSF) was determined in 33 premature and full-term neonates. On an average the serum half-life was 3.6 hours in children with a birth weight above 1,500 g; in children with a birth weight below 1,500 g it was 5.1 hours. The penetration volume of cephacetrile into CSF was higher and the rate of penetration faster in neonates with meningeal infections than in those without. The highest CSF concentrations were reached 2-4 hours after drug application (2.6-25.8 mcg/ml in infants with bacterial meningitis and 1.8-15.2 mcg/ml in infants without).

Birth Weight↗

PubMed1976

[In vitro effect of cephacetril and colistin combinations on Klebsiella pneumoniae and Proteus Strains (author's transl)].

In 14 out of 43 Klebsiella pneumoniae strains (33%) the combination cephacetril-colistin showed a synergistic, in 11 strains (25%) an additive effect. In Proteus strains no synergistic action was found. The combination was more likely to be synergistic or additive in strains requiring higher minimal inhibitory concentrations of cephacetril and colistin. Most highly resistant Klebsiella pneumoniae strains were synergistically inhibited by concentrations of both drugs, which can easily be obtained in serum by usual clinical doses.

Cephacetrile↗

PubMed1982

In vitro evaluation of pyridine-2-azo-p-dimethylaniline cephalosporin, a new diagnostic chromogenic reagent, and comparison with nitrocefin, cephacetrile, and other beta-lactam compounds.

Pyridine-2-azo-p-dimethylanaline cephalosporin (PADAC), a chromogenic reagent which is purple and changes to yellow upon cleavage of its beta-lactam ring, was evaluated in comparison with other chromogenic cephalosporins. PADAC exhibited little antimicrobial activity against gram-negative bacteria, but did have good activity (minimum inhibitory concentration, 0.12 to 0.5 microgram/ml) against Staphylococcus aureus, a quality comparable to nitrocefin. Nitrocefin, however, demonstrated an unexpected and uniquely potent activity against Streptococcus faecalis (minimum inhibitory concentration, less than or equal to 0.06 to 0.12 microgram/ml) The relative hydrolysis rate of PADAC when subjected to six different beta-lactamases was substantially greater than that of cephacetrile, but less than that of nitrocefin. The relative hydrolysis rates of PADAC and nitrocefin were comparable with type IIIa beta lactamase and the derived from Bacillus cereus. The inhibition of beta-lactamase hydrolysis of the chromogenic cephalosporin substrates by six enzyme-stable inhibitors was generally greater with PADAC than with nitrocefin. Unlike nitrocefin, PADAC mixed with 50% human serum or various broth culture media showed no evidence of color change or degradation over several hours. The subsequent enzyme hydrolysis rates of such mixtures were the same as in phosphate buffer. Beta-lactamase-containing bacterial suspensions and clinical specimens containing such bacteria produced positive visual and spectrophotometric color changes when mixed with PADAC or nitrocefin. Although color changes occurred more slowly with PADAC than with nitrocefin, PADAC was not adversely influenced (non-enzyme-related color change) by the protein content of specimens. PADAC appears to be a promising alternative for beta-lactamase diagnostic testing in the clinical and research microbiology laboratory.

Bacteria↗

PubMed1976

[Fundamental studies on combination of antibiotics; especially on pharmacokinetics. I. Combination of gentamicin with sulbenicillin or cephacetrile (author's transl)].

1. When gentamicin (GM) and sulbenicillin (SBPC) or cephacetrile (CEC), in combination with pre- or post-treatment, were injected intravenously to the rat, their pharmacokinetics were investigated. 2. The antibiotics in the samples were separated by paper electrophoretic technique and their concentrations were determined by cup thin layer plate method using Bacillus subtilis as the test organism. 3. The biological half-life of SBPC in the serum was shortened in pretreatment with GM and prolonged in posttreatment with GM, while that of GM did not vary in pre- or post-treatment with SBPC. 4. The half-life of CEC was prolonged in treatment with GM, while that of GM did not vary. 5. These phenomena may be considered to be produced as the results of a concentration ratio of SBPC and GM or of CEC and GM, and protein binding of these antibiotics, as far as plasma initial levels, tissue distribution, urinary excretion and protein binding of these antibiotics are concerned.

Animals↗

PubMed1976

Reversible encephalopathy following cephacetril therapy in high doses in a patient on chronic intermittent hemodialysis.

A patient on chronic intermittent hemodialysis at home showed signs of acute encephalopathy after an 8-day's treatment with a total dose of 78 g cephacetril (Celospor). Features included papilledema, loss of visual fields, severe generalized EEG changes and bilateral occipital abnormalities on a brain scintigram. Psychopathological findings consisted of a severe psychosis. The visual fields defects were the last sign of the encephalopathy to disappear.

Abscess↗

PubMed1980

A comparison of the activity in vitro of different cephalosporins: cephalothin, cephradine, cephacetrile, cefaclor, cefuroxime and cefotaxime.

6-cephalosporins (cephalothin, cephradine, cephacetrile, cefaclor, cefuroxime, cefotaxime) has been tested in vitro against 212 gram negative bacteria and 60 Staphylococci. Cefuroxime and especially Cefotaxime showed the highest activity against the gram negative bacteria, with a very low MIC. Cefotaxime also acted fairly well against several strains of Pseudomonas. Of the six cephalosporins tested, cephalothin gave the best results against the Staphylococci.

Cefaclor↗