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Comparison of cefadroxil and cephalothin disk susceptibility test results.

Diffusion susceptibility tests with 30-micrograms cefadroxil disks and 30-micrograms cephalothin disks were evaluated. For both agents, the same zone size interpretive criteria were recommended (less than or equal to 14 mm for resistance and greater than or equal to 18 mm for susceptibility). Tests were performed with 904 bacterial isolates, and the data were examined to determine whether the two cephalosporins might be used interchangeably for purposes of in vitro susceptibility testing. When Haemophilus influenzae, Listeria monocytogenes, and methicillin-resistant staphylococci were evaluated, the two agents differed significantly. For testing other species, a cephalothin disk or cephalothin MIC could be used for predicting susceptibility or resistance to cefadroxil.

Bacteria↗

Acute renal failure associated with combined gentamicin and cephalothin therapy.

Three patients with normal renal function developed acute renal failure between the ninth and twenty-seventh days of combined gentamicin and cephalothin therapy. The dose of gentamicin (4-6 mg/kg/day) was in the normal range, but that of cephalothin (180 mg/kg/day) was abnormally high. The nephropathy was of the tubular-interstitial type and the clinical picture similar to that seen in acute drug-induced nephropathies. Frusemide was given only after the onset of renal failure. In these three patients the high intravenous doses of cephalothin combined with gentamicin were probably nephrotoxic.

Acute Kidney Injury↗

Sensitivity of penicillinase-forming strains of Staphylococcus aureus and of their penicillinase-negative variants to cephaloridine, cephalothin, methicillin, and benzylpenicillin.

Twenty-eight penicillinase-forming cultures of Staphylococcus aureus and their penicillinase-negative variants were examined for resistance to benzylpenicillin, methicillin, cephalothin, and cephaloridine. The results supported the view that cephaloridine was more easily destroyed by staphylococcal penicillinase than was cephalothin. In our tube-dilution tests, the minimum inhibitory concentration (M.I.C.) of cephaloridine for methicillin-sensitive cultures was never as high as some of the values reported by other workers who used apparently comparable methods. This was probably due to small differences in technique. The M.I.C. is an unsatisfactory measure of the antibiotic sensitivity of an organism which produces an enzyme which destroys the antibiotic.Methicillin-resistant strains of Staph. aureus have an intrinsic resistance of ;heterogenous' type also to benzylpenicillin, cephalothin, and cephaloridine.

Cephaloridine↗

Relationships between in vitro susceptibility and efficacy in experimental mouse infection-protection assay of cefazolin and cephalothin using Escherichia coli strains.

The disc sensitivity and minimal inhibitory concentrations (MIC) of cefazolin and cephalothin were compared against a series of Escherichia coli isolates. These data were correlated with the mouse protective doses of the 2 cephalosporins in animals infected with E. coli strains selected according to their various degrees of in vitro sensitivity to the 2 cephalosporins. The overwhelming majority of E. coli strains showed a significantly higher degree of susceptibility and lower MIC values for cefazolin than for cephalothin. There has been found a good correlation between the inhibition zones and especially the MIC values and the ED50 results for both cephalosporins. Using E. coli clinical isolates, cefazolin was found to be superior to cephalothin not only in vitro experiments but also more potent in protecting the experimentally infected mice.

Animals↗

Augmentation effect of clavulanic acid with penicillin, cephalothin and ticarcillin against Bacteroides fragilis.

The effect of clavulanic acid on the in vitro activity of beta-lactam antibiotics against Bacteroides fragilis (154 strains) was tested. The MIC90 on 154 strains of B. fragilis tested was greater than 64 micrograms/ml for penicillin and cephalothin, and greater than 128 for ticarcillin alone. 32 strains of B. fragilis relatively resistant to the test beta-lactam antibiotics (most of them beta-lactamase producers) were retested with the addition of clavulanic acid. 90% of the strains were then inhibited by less than or equal to 8 micrograms/ml of penicillin and cephalothin, and by 32 micrograms/ml of ticarcillin. The strongest beta-lactamase producers were the most susceptible, and this was not influenced by change in pH of the diluent for clavulanic acid from 6.0 to 7.4. Both penicillin and cephalothin when combined with clavulanic acid were highly effective against B. fragilis but the therapeutic relevance of these combinations remains to be evaluated.

Bacteroides fragilis↗

Cephalothin induced neutropenia during the treatment of bacterial endocarditis.

The occurrence of cephalothin induced neutropenia in 3 patients with infective endocarditis is described. In each patient, withdrawal of cephalothin was followed by rapid haematological recovery. It is apparent that granulocytopenia may frequently occur in patients receiving prolonged, high dose, intravenous cephalothin for the treatment of bacterial endocarditis.

Adult↗

Cephalothin and penicillin G polymers as elicitors of rat PCA mediated by mouse IgE antibodies.

PCA-eliciting activities of cephalothin- and penicillin G-polymers were examined in rats sensitized with homologous IgE antibodies of mouse origin. Cephalothin-polymers elicited PCA regardless of the source of antibodies and the methods to raise them, the minimal effective dose being 2 to 20 micrograms/animal. Penicillin G-polymers provoked PCA only when anti-benzylpenicilloyl IgE antibody of C57BL/6J mouse raised early after immunization was used. The minimal effective dose in this case was 5 micrograms/animal, being comparable to that of cephalothin polymers.

Animals↗

Variable in vitro activity of cefaclor, cephalothin and cefadroxil against Escherichia coli, Klebsiella pneumoniae and Proteus mirabilis.

The in vitro activity of cefaclor, cephalothin and cefadroxil to 50 Escherichia coli, 23 Klebsiella pneumoniae and 20 Proteus mirabilis strains was tested with the disc diffusion and microdilution plate techniques. Cefaclor was more active than cefadroxil, while cephalothin was intermediate. The differences seriously affected the classification into the routine SIR system. For susceptibility testing we question the use of cephalothin as a class representative of oral cephalosporins.

Cefaclor↗

BL-S786, a new parenteral cephalosporin. I. A collaborative in vitro susceptibility comparison to cephalothin against 5,762 clinical bacterial isolates.

The in vitro activity of Compound BL-S786 was compared with that of cephalothin against 5,762 clinical isolates by the microdilution broth method. BL-S786 demonstrated a broader spectrum and a significantly lower MIC against the Enterobacteriaceae. Although greater susceptibility to BL-S786 than to cephalothin was exhibited by Serratia marcescens, Proteus morganii and Proteus vulgaris, these three species were generally resistant to both drugs. By contrast, the staphylococci were significantly more susceptible to cephalothin than to BL-S786. Resistance to both drugs was demonstrated by Pseudomonas aeruginosa and other pseudomonads, enterococci and Bacteroides fragilis.

Anaerobiosis↗

Cephalothin and cephaloridine therapy for bacterial meningitis.

The efficacy of cephalothin and cephaloridine in the treatment of bacterial meningitis was evaluated from a review of 106 cases reported in the literature. Fifty-nine percent of 34 patients treated with intravenous cephalothin responded suboptimally; those receiving daily doses of 12 g or more fared significantly better (P less than 0.025). In contrast, 74% of 72 patients treated with cephaloridine responded favorably; those who received concomitant intrathecal cephaloridine responded significantly better (P less than 0.005). These findings indicate that cephalosporin therapy for bacterial meningitis, without concomitant intrathecal medication, is unreliable and that this is probably due to inadequate penetration of the antibiotics into cerebrospinal fluid. In penicillin-allergic patients with pneumococcal, meningococcal, and hemophilus meningitis, chloramphenicol is the agent of choice. For staphylococcal meningitis, intravenous cephalothin at doses of 12 g/day with additional intrathecal cephaloridine at doses of 12.5 to 50 mg/day should be administered concomitantly.

Bacterial Infections↗

[The serum and uterine muscle concentrations of Cephradin and Cephalothin].

On the day of operation 2 grams of Cephradin was given intravenously to 33 patient and 2 grams of Cephalothin was given intravenously to 31 patients. At various time intervals, uterine tissue and serum was removed. The mean serum concentrations of Cephradin were 3 times higher and the mean tissue concentrations of Cephradin were 7-8 times higher than the corresponding concentrations of Cephalothin. Because of the difference in protein binding of the examined cephalosporins (Cephradin 6%, Cephalothin 60-65%) the difference for the antimicrobially active portion (Protein free portion) is even more favorable for Cephradin. The significance of these pharmacokinetic differences for the treatment are obvious.

Adult↗

Nephrotoxicity associated with cephalothin administration.

Variable degrees of acute renal failure developed in three patients receiving therapy with cephalothin sodium. The course and findings were consistent with acute tubular necrosis of the oliguric and nonoliguric types. One patient had protracted oliguria, a second experienced transient oliguria, and one had normal urine output. All had urinary sediment changes consistent with tubular necrosis, and the two oliguric patients had elevated urine sodium concentrations. No other causes for renal failure could be detected, and all recovered after discontinuation of cephalothin therapy, although peritoneal dialysis was required in one patient. These observations indicate that cephalothin is capable of inducing renal damage in man.

Acute Kidney Injury↗

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↗

[Penetration of cephaloridine and cephalothin into the cerebrospinal fluid-clinical study (author's transl)].

There were 35 cases, treated with Cephaloridine or Cephalothin after neurosurgical operation. Neurological surgeon always troubled with passage of blood-brain barrier when drug was given. Antibiotics was not exceptionally, therefore we, neurological surgeon, must select the effective drug to bacterium, that which penetrated enough to the intracranial organ through the blood-brain barrier. In this paper, we measured the concentration of Cephaloridine and Cephalothin into cerebrospinal fluid in the cases with non inflammatory meninges. We collected the cerebrospinal fluid from continued ventricle tap and serum, then measured the concentration of the drug with bioassay. Cephaloridie treated cases. 22 cases. 1) 1 g intramuscular injection. 4 cases. Serum level got to highest value, 64 mug/ml (mean value) 1 hour after injection. CSF level got to maximum concentration 46.8 mug/ml. (mean value) serum mean level 21.5 mug/ml. CSF mean level 0.73 mug/ml. 2) 1 g 3 minutes-intravenous injection 5 cases. Serum level got to highest value 67.5 mug/ml. CSF maximum level was 5.25 mug/ml. Serum mean level 19.74 mug/ml. CSF mean level 0.61 mug/ml. 3) 1 g 1 hour-intravenous drip. 9 cases. Serum maximum level 121.0 mug/ml. CSF maximum level 2.30 mug/ml. Serum mean level 20.08 mug/ml. CSF mean level 0.67 mug/ml. 4) 1 g 8 hours-intravenous drip. 3 cases. Serum maximum level 61.0 mug/ml. CSF maximum level 1.36 mug/ml. Serum mean level 14.78 mug/ml. CSF mean level 0.47 mug/ml. Cephalothin treated cases, 12 cases. 1) 1 g 8 hours-intravenous drip, 4 cases. In fact we could detect the drug only in one case, in CSF, and we could not in other three cases. In KF - 4 case, serum maximum concentration was 26.0 mug/ml, CSF maximum concentration was 0.07 mug/ml. Serum mean level 16.97 mug/ml. CSF mean level 0.01 mug/ml 2) 2 g 1 hour-intravenous drip, 9 cases. Serum maximum level 690.0 mug/ml. CSF maximum level 2.03 mug/ml. Serum mean level 29.59 mug/ml. CSF mean level 0.06 mug/ml. In cephaloridine cases, the tendency was observed, that which, as concentration of the drug in CSF increased, cell count and protein decreased, and, as concentration of the drug decreased, cell count and protein increased. CSF/serum concentration ratio of Cephaloridine increased, when time passed, in intramuscular, 3 minutes intravenous, and 1 hour-intravenous drip group. Then only in 8-hours-intravenous prip group. Then only in 8-hours-intravenous drip group, concentration ratio decreased. In Cephaloridine group, mean value of CSF/serum ratio showed. 1 g i.m. 0.084 1 g 3 minutes-i.v. 0.098 1 g 1 hour-i.v. 0.194 1 g 8 hours-i.v. 0.044.

Adolescent↗

Cephalothin prophylaxis assay during cardiopulmonary bypass.

Efficient use of prophylactic antibiotics in surgery demands their presence in adequate serum concentration at the time of maximal potential contamination. This cover should extend from the moment of incision until at least the time of removal of large tubes and intravenous connulas. Critical cardiac contamination may occur during the bypass procedure while the operation within the cardiac chambers is being done. This is a special danger in valve replacement with prostheses. The antibiotic regimen of the Cardiothoracic Unit was studied in 12 consecutive patients and was generally found to provide adequate antibiotic coverage throughout the surgical procedure, including the bypass procedure. In all patients, a reinforcing cephalothin dose on completion of bypass ensured adequate circulating cephalothin levels for the completion of surgery. Clearance of the cephalothin from the blood of patients was found to decrease markedly during cardiopulmonary bypass.

Adolescent↗

[The in vitro effect of a combination of sulbactam with cephalothin and cefazolin on strains of Escherichia coli and Proteus mirabilis which produce beta lactamase].

The effect of the combination of sulbactam, cephalothin, and cephazolin was studied in vitro on 88 strains of E. coli and 11 strains of P. mirabilis producing beta-lactamases. Quantitative susceptibility of the tested strains to cephalothin was examined by the disk dilution method and the effect of the combinations with sulbactam by the micromethod. The production of beta-lactamases was determined by the qualitative test with the chromogenic substrate PODAC. Of the total number of 160 E. coli strains beta-lactamases were established in 53.3% of the strains. Of the 47 P. mirabilis strains 23.4% were found to produce beta-lactamases. The effect of the combinations with sulbactam was assessed as synergistic, additive, indifferent or antagonistic. In the combination of sulbactam in the concentration of 16.0 mg/l with cephalothin and cephazolin a higher rate of synergistic and additive effect was recorded on both strains. In none of the combinations did sulbactam exert an antagonistic effect.

Cefazolin↗

Endocarditis due to Citrobacter diversus developing resistance to cephalothin.

A 43-year-old man was admitted with acute bacterial endocarditis. Citrobacter diversus susceptible to cephalothin was isolated from blood cultures. Citrobacter diversus was later isolated from the aortic valve cusps at surgery, but this isolate was resistant to cephalothin. Laboratory testing showed that the Citrobacter diversus recovered from blood cultures was capable of producing mutants highly resistant to cephalothin.

Adult↗

[Urinary enzyme excretion in cephalothin therapy in adults and children].

A damage of the kidney, particularly of proximal tubular cells, can be indicated by an increased concentration of definite enzymes in urine. After gynecological operation the repeated application of 8 g cephalothin daily provokes an higher increase of enzyme concentrations in urine than the application of ampicillin under the same conditions. These results show that cephalothin produces a slight alteration of tubular cells, probably without practical importance. In contrast to this, in children a total dose of 1.5 up to 6 g cephalothin, administered after an operative correction of vesikoureterale reflux, provokes no marked changes in urinary enzyme excretion. Probably, in these children the determination of urinary enzyme excretion is not a suitable parameter to demonstrate a slight tubulotoxic damage.

Adult↗