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PubMed1974

Comparative serum levels and protective activity of parenterally administered cephalosporins in experimental animals.

Six cephalosporin antibiotics were administered subcutaneously to mice at a level of 20 mg/kg. The serum levels of each were determined at five time intervals ranging from 5 to 120 min after dosing. Urinary recovery and the presence of active metabolites in mouse urine were determined. The peak serum levels and serum half-lives in mice were found to be positively correlated with the mean effective dose values obtained after lethal challenge with Escherichia coli. The administration of cefazolin and cephanone resulted in the highest serum level and the best protection. Good protection was obtained with cephaloridine despite somewhat lower serum levels. The cephalosporins with the acetoxy side chain (cephalothin, cephapirin, and cephacetrile) showed lower serum levels and the poorest protection. Cefazolin, cephaloridine, and cephalothin serum levels were also determined in dogs, squirrel monkeys, and rabbits. A mixed response was obtained in these species, with cefazolin peak serum levels being highest in rabbits and cephaloridine peak highest in dogs.

Animals↗
PubMed1976

Relative morphological effects induced by cefoxitin and other beta-lactam antibiotics in vitro.

Cefoxitin, a new semisynthetic cephamycin antibiotic, induced filament formation at subinhibitory concentrations with a beta-lactamaseless strain of Enterobacter cloacae (HSC 18410 M66). The extent of filament induction by cefoxitin was similar to that seen with cephalothin, cefazolin, and benzylpenicillin. Filament induction by cefoxitin was markedly less than that seen with cephalexin, carbenicillin, ticarcillin, cephradine, and cephapirin. Antibiotics which failed to induce filaments at any level tested included cephaloridine, cephacetrile, cephalosporin C, the cephamycins, 6-aminopenicillanic acid, 7-aminocephalosporanic acid, A16884, A16886, and FL-1060. Those antimicrobial agents tested which lacked an aromatic substituent in the 7-position (for cephems) or in the 6-position (for penams) did not induce filaments. These observations suggest a possible relationship between filament induction of the test organism and the molecular nature of constituents in the 7- or 6-position of beta-lactams.

Anti-Bacterial Agents↗
PubMed1974

Comparative activity of ampicillin and seven cephalosporins against group D streptococci.

Minimum inhibitory concentrations have been determined for ampicillin and seven cephalosporins against 93 strains of group D streptococci isolated recently from clinical material. Ampicillin was much the most active compound (modal MIC = 1.6 mug/ml); cephaloridine, cephacetrile, and cefazolin had a modal MIC of 25 mug/ml, while corresponding figures for cephalothin, cephradine, cephalexin, and cefoxitin were 50, 100, 200, and 800 mug/ml, respectively. Thus, none of the newer cephalosporins is an improvement in respect to activity against enterococci over existing compounds, and ampicillin remains overwhelmingly the beta-lactam antibiotic of choice for the treatment of infections by such organisms. Pharmacokinetic considerations, however, indicate that certain cephalosporins, for instance, cephaloridine, cefazolin, and cephanone, may be worthy of further study in view of possible synergy with aminoglycoside antibiotics.

Aminoglycosides↗
PubMed1987

Pharmacokinetic properties of the cephalosporins.

Most cephalosporins can only be administered parenterally. Among agents that are absorbed from the gastrointestinal tract, those with bioavailabilities of 85 to 90% include cefroxadine, cefadroxil, cefsumide, cephalexin, cephradine, cephacetrile, and cefazaflur. Most cephalosporins are eliminated rapidly, with serum half-lives (t1/2s) of 1 to 2 hours. Exceptions are cefonicid with a t1/2 of 4.4 hours, cefpiramide with a t1/2 of 5.0 hours, and cefotetan with a t1/2 of 3.5 hours. The longest half-life is shown by ceftriaxone with a t1/2 of 8.5 hours. Cephalosporins are eliminated mostly by the kidneys, some with a substantial contribution from active tubular secretion, which is blocked by probenecid. The degree of metabolism varies. Only a few cephalosporins have a high biliary elimination. For example, with intravenously administered cefoperazone, about 70% appears in bile. High biliary elimination is also observed with cefmenoxime, ceftriaxone, cefbuperazone, and latamoxef (moxalactam). Because these are not appreciably absorbed from the gastrointestinal tract, the consequence is high intraintestinal concentrations of the drugs and a marked ensuing depression of the normal microflora with simultaneous emergence of resistant bacteria. The untoward ecological impact may even lead to Clostridium difficile-associated enterocolitis.

Animals↗
PubMed2001

Relationship among plasmids recovered from Staphylococcus aureus, milk leukocytes, and antimicrobial resistance.

The efficacy and efficiency of mastitis control schemes in reducing the incidence of Staphylococcus aureus mastitis could be improved if the different strains of Staph. aureus were characterized by their pathogenicity. Plasmid finger printing of Staph. aureus strains could be a rather simple and efficient method to characterize the strains and their interaction with host cellular immune defenses. The aim of this study was to investigate the presence and distribution of plasmids in strains of Staph. aureus isolated from bovine mastitis and their relationship with mammary gland immune defenses and antimicrobial resistance. Overall, nine different plasmids were identified by their molecular weight. One or more plasmids were isolated from 293 strains (96.4%), and only 11 strains did not show the presence of any plasmid. A significant difference in polymorphonuclear neutrophil proportions was observed in association with 23-kb, 9416-bp, 2027-bp, or 1353-bp plasmids, and for macrophage proportions, significant differences were observed for 9416-bp, 6557-bp, or 1353-bp plasmids. Penicillin G minimum inhibitory concentration values showed significant differences when 6557-bp, 4361-bp, 2322-bp, or 2027-bp plasmids were present, and weak or no differences were observed for cephacetrile, rifamycin, and norfloxacin. The presence of 2027-bp plasmid was associated with a reduced neutrophil response and an increased resistance against beta-lactam antimicrobials; therefore, the strains carrying this plasmid have a higher probability to invade and colonize mammary gland, to survive to antimicrobial therapy, and to remain undetected. Results confirmed that plasmid fingerprinting is a simple and effective way to characterize Staph. aureus strains.

Animals↗
PubMed1981

IgE antibodies for penicillins and cephalosporins in rats. I. Characteristics of the IgE antibodies for penicillins and cephalosporins in rats.

Rats immunized with sulbenicillin-ovalbumin (SBPC-OvA) in combination with aluminum hydroxide (alum) and thimerosal-killed Bordetella pertussis produced high levels of anti-SBPC antibodies. Anti-SBPC antibodies were first detected on day 8, reaching the maximum titer on day 12 and rapidly declined thereafter. Anti-SBPC sera obtained on day 13 were sulfhydryl-labile and heat-labile. The optimal latent period in the passive cutaneous anaphylaxis (PCA) reaction was 60 approximately 72 hours. These results indicate that anti-SBPC antibodies were IgE antibodies. Sprague-Dawley (SD), Wister and F344 rats were equally productive of anti-SBPC antibodies, while SD rats were more productive of anti-cephaloridine (CER) antibodies than Wister and F344 rats did. In SD rats, the IgE antibodies for penicillin G (PCG), ampicillin (ABPC) and SBPC were more easily produced than the IgE antibodies for CER, cefazolin (CEZ) and cephacetrile (CEC).

Animals↗
PubMed1976

The effect of storage at 4 degrees C on antibiotic residues in kidney and meat tissues of dairy cows.

A method is described for the quantitative assay of antibiotic residues in the body of slaughtered farm animals by means of 3 types of agar media and 3 test organisms. With the help of programmed calculation procedures, data from large-scale tests for antibiotic residues could be analyzed accurately and rapidly. The concentrations of penicillin G, ampicillin, amoxycillin, cloxacillin, cephapirin, cephacetrile, neomycin, kanamycin, and oxytetracycline in the kidney, and also of tylosin in meat from the diaphragm muscle of cattle treated parenterally with these antibiotics were measured periodically in samples kept at 4 degrees C for up to 7 days after slaughter. The concentrations of penicillin G, ampicillin, amoxycillin and the cephalosporins in the kidney decreased rapidly upon storage whereas the levels of the other antibiotics remained essentially unchanged. Antibiotic stability in the meat was considerably greater than in the kidney upon storage for 4 days, and neomycin meat tissue levels were not reduced during storage for up to 144 hours. Results are discussed in relation to the conduct of the official qualitative Sarcina lutea Kidney Test and the most desirable procedure for preparing meat samples for assay.

Animals↗
PubMed1975

Comparison of absorption and excretion of cefazolin with cephalothin and cephapirin.

Since the discovery of cephalothin in 1962, many semi-synthetic cephalosporins have appeared. To choose the most suitable drug for the clinical treatment of infections, the characteristics of these antibiotics must be sufficiently understood. When cephalosporins which are or will be commercially available are divided into two categories, one consists of cephaloridine, cefazolin and cephalexin which are comparatively stable in the living body; and the other cephalothin, cephaloglycin, cephapirin and cephacetrile which are metabolized into desacetyl compounds with low antibacterial activity. In this study, the author compared the absorption, excretion and some other properties of cefazolin and cephalothin, (widely used clinically), and cephapirin (still under study in Japan).

Animals↗
PubMed1991

Pharmacologic enhancement or suppression of phagocytosis by bovine neutrophils.

Sixty-three drugs, belonging to 10 chemical classes, were tested in vitro to determine effects on phagocytosis of 32P-labeled Staphylococcus aureus by neutrophils isolated from milk. Within each class, the number of antibiotics tested were: nonsteroidal anti-inflammatory drugs (NSAID; 8), peptolids (2), aminoglycosides (8), tetracyclines and fusidic acid (4), beta-lactam antibiotics (25), secretolytic agents (2), macrolides (5), polypeptides (2), and antibacterial quinolones (8). Percentage of phagocytosis was determined after incubating (2 hours at 37 C) 12.5 x 10(6) viable neutrophils, 200 x 10(6) 32P-labeled S aureus with antibiotics and 5% skimmed milk. Concentrations of antibiotics tested were 1,000, 500, and 10 micrograms/ml of incubation media. When compared with nonantibiotic controls at the highest drug concentration, the NSAID acetylsalicylic acid and centrophenoxine increased phagocytosis 23.2 and 8.8%, respectively, and benzydamine, indomethacin, phenylbutazone, ibuprofen, and acetominophen decreased phagocytosis 22.8, 14.2, 9.8, 27.0, and 18.2%, respectively. The peptolids novobiocin and pristinamycin decreased phagocytosis 24.5 and 22.0%, respectively. The aminoglycosides tobramycin, amikacin, and gentamicin decreased phagocytosis 21.1, 15.4, and 19.2%, respectively. For the tetracyclines and fusidic acid, minocycline and doxycycline decreased phagocytosis 39.8 and 54.2%, respectively. The beta-lactam antibiotics carfecillin, cephapirin sodium, and cephacetrile sodium decreased phagocytosis 11.2, 12.8, and 23.8%, respectively. The secretolytic agent, bromhexin, increased phagocytosis 10.8%. These data indicate that the potential for enhanced phagocytosis exists through use of some NSAID, and for depressed phagocytosis through use of aminoglycosides, peptolids, tetracyclines, and beta-lactams, as well as certain other NSAID.

Animals↗
PubMed1979

Investigations on the effectiveness of cefazedone in experimental E. coli pyelonephritis.

The therapeutic effectiveness of (6R,7R)-7-(2-[3,5-dichloro-4-oxo-1(4H)-pyridyl]-acetamido)-3-([(5-methyl-1,3,4-thiadiazol-2-yl)-thio]methyl)-8-oxo-5-thia-1-azabicyclo[4,2,0]oct-2-ene-2-carboxylic acid (cefazedone, Refosporen), cephazolin, cephacetrile and cephalothin was compared in the test model of estradiol-induced E. coli pyelonephritis in the rat. Cefazedone and cephazolin were similar in effect. The relations between results of treatment and microbiological and pharmacokinetic characteristics of the cephalosporins tested are discussed.

Animals↗
PubMed1979

Tubular-toxic effects of aminoglycosides and their combinations with cephalosporins.

Cephalosporins have a distinctly different effect from that of aminoglycosides on membranes of the proximal tubule of the human kidney as measured by urinary AAP concentrations. Except for a slight influence by cephacetrile, cephalosporins showed no effect on the proximal tubule. In contrast, after three days of administration, the aminoglycosides caused a cumulative increase in membrane proteins of the proximal tubule to be excreted in the urine. Tobramycin appears to have the least and amikacin the greatest effect on the brush border membranes of the proximal tubule of the normal human kidney. The combination of cephalosporins with aminoglycosides increases the potential toxic effect on the proximal tubule.

Adolescent↗
PubMed1984

[Evaluation of the biliary passage of beta-lactam antibiotics].

The present study is devoted to the biliary excretion of some beta-lactam antibiotics (6 derived from the penicillin group: Penicillin G, Ampicillin, Metampicillin, Carbenicillin, Mezlocillin, Apalcillin and 9 from the cephalosporin group: Cephalothin, Cephaloridine, Cephacetrile, Cefalexin, Cefazolin, Cefamandole, Cefuroxime, Cefaclor and Ceftizoxime). The biliary excretion of these antibiotics was assessed by 4 different procedures: 1) experimental study of their biliary elimination by a perfused isolated rabbit liver; 2) in humans, by evaluation of their passage: a) in aspirated duodenal fluid, b) in bile collected by external biliary drainage, c) and in bile obtained by puncture of the main bile duct and the gall bladder during surgery. The results of these different investigations were concordant and showed that the biliary excretion of Metampicillin, Apalcillin and Mezlocillin was definitely higher than that of the other studied beta-lactams; on account of their suitable antibacterial spectrum, these 3 derivatives should be used in preference for the treatment of biliary infection.

Animals↗
PubMed1980

[Yersinia enterocolitica: the influence of incubation temperature on antibiotic susceptibility, beta-lactamase activity and growth characteristics (author's transl)].

The influence of incubation temperature (37, 30 and 22 degrees C) on antibiotic susceptibility, beta-lactamase activity and growth characteristics was studied on 43 unselected strains of Y. enterocolitica (Serovar O:3 and O:9) freshly isolated from cliical specimens. Antibiotic susceptibility was measured by the disc diffusion technique and by a broth dilution test (MIC). Beta-lactamase activity was detected with chromogenic cephacetrile using standard curves prepared for 37, 30 and 22 degrees C. Continuous increase of beta-lactamase activity was found when incubation temperatures were lowered. All strains were found to be resistant by ampicillin and cephalothin at the three temperatues tested. Some strains showed an intermediate susceptibility to carbenicillin in the disc diffusion test. A temperature reduction of 37 to 30 degrees C significantly decreased the inhibitory zone diameters for the beta-lactam antibiotics ampicillin, carbenicillin and cephalothin, but also for other substances like tetracycline, chloramphenicole and cotrimoxazole. This suggests, that the observed decrease is caused by a better growth of Y. enterocolitica at 30 degrees C rather than increased beta-lactamase production. From 30 to 22 degrees C a further decrease in inhibitory zone diameters was only seen with ampicillin and carbenicillin. This seems to be mainly due to the increased B-lactamase activity observed at 22 degrees C. In contrast the resistance to cephalothin was apparently not influenced by this additional beta-lactamase activity. Resistance to cephalothin therefore depends probably more on other, not beta-lactamase-related, factors such as permeability variations of the outer membrane or modifications of binding proteins involved in the peptidolycan biosynthesis. The correlation between beta-lactamase activity at various incubation temperatures and resistance to beta-lactam antibiotics was less pronounced when the broth dilution test (MIC) was applied. Only carbenicillin showed significantly increasing MIC values from 30 to 22 degrees C. All the Y.e. strains investigated could be divided into two groups with respect to their beta-lactamase production characteristics. The first group showed continuously increasing beta-lactamase values at lower incubation temperatures. In the second group generally lower amounts of beta-lactamase values were found and temperature dependence was not observed. On the other hand variations in cell wall permeability, resulting in a diminished accessability of the cell wall bound enzymes must also be considered.

Anti-Bacterial Agents↗
PubMed1982

[A study on penetration of antibiotics into the cerebrospinal fluid after the ventriculo-peritoneal shunt (author's transl)].

Neurological surgeon must select the effective antibiotics to bacterium, that which penetrated enough to the intracranial organ through the blood-brain barrier. In this study, we measured the concentration of cefotiam (CTM), cephalothin (CET), cephacetrile (CEC) and sulbenicillin (SBPC) into the cerebrospinal fluid in the non inflammatory cases with V-P shunt. 1. Antibiotic concentrations in CSF and CSF/serum ratio (%) were evaluated at 2 hours after an intravenous administration of antibiotics. CTM; 0.543 microgram/ml (3.66%), CET; 1.84 micrograms/ml (7.45%), CEC; 1.77 micrograms/ml (7.5%), SBPC, 6.15 micrograms/ml (5.58%). 2. The peak of antibiotic concentration in CSF appeared from 2 hours after administration and gradually decreased. In cellular tumor cases, the penetration of antibiotics into CSF showed similar levels as the cerebrovascular disease cases. 3. Concentration of CTM in CSF was higher than MIC of CTM to S. pyogenes and E. coli.

Adult↗
PubMed1980

Availability and usage of new antibacterial drugs in Europe.

The present-day availability and usage of established and new antibacterial drugs approved for clinical and therapeutic purposes in food-producing animals and poultry in the United States and Europe were compared. Presently, 42 such drugs are approved in Europe, 13 of which were approved since Dec 31, 1974. In the United States, 17 such drugs are currently approved, only four were approved since Dec 31, 1974. Most drug products approved in Europe contain two or more antibacterial agents, whereas most of the products approved in the United States are single drug entities. Drugs approved in Europe but not in the United States include sulfonamide and trimethoprim combinations, nafcillin, oxacillin, metampicillin, cephoxazole, cephalonium, cephacetrile, cephalexin, gentamicin, rifamycin SV, nifuroquine, tiamulin, chloramphenicol, colistin, and polymyxin B. Pharmacologic and clinical features of several of these drugs are briefly described.

Animal Diseases↗
PubMed1981

[Antibiotic prophylaxis with cephalosporins in heart surgery].

60 minutes after i.v. injection tissue levels of 7 different cephalosporins were obtained using biological assay. The following concentrations were measured: cephalothn 1.4 micrograms/g; cepharin 4.7 micrograms/g; cephacetrile 11.2 micrograms/g; cephradine 15.4 micrograms/g; cefazedone 26.9 micrograms/g; cefamandole 40.3 micrograms/g, and finally cefoxitin 43 micrograms/g. The high tissue levels of cefamandole and cefoxitin are especially remarkable as i.v. doses of both antibiotics had been 50 mg/kg body weight ( doses of all other cephalosporins 100 mg/kg body weight). Except cephalothin, all cephalosporins tested were suitable for antibiotic prophylaxis in cardiac surgery.

Cardiac Surgical Procedures↗
PubMed1979

[Diffusion of cefamandole into the prostatic tissue (author's transl)].

From 21 patients with prostatic adenoma with an average age of 69 years, serum and prostatic tissue concentrations after a single i.v. dose of 2 grams of cefamandole were estimated. The mean serum concentrations 30 minutes after the infusion was completed, were measured with 104.8 and after 60 minutes with 51 microgram/ml. The corresponding concentrations in the prostatic adenoma tissue were after 30 minutes 32.87 and after 60 minutes 17.1 microgram/g. These data are compared with earlier findings with other caphalosporine antibiotics (cephradine, cephapirine, cephacetrile, cephalothin) in the same tissue materials at the same time points. The estimated concentrations of cefamandole in serum and prostatic tissue are suited for the treatment of infections caused by cefamandole sensitive microorganisms.

Aged↗