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PubMed1979

Pharmacokinetics of cephalothin: accumulation of its deacetylated metabolite in uremic patients.

The pharmacokinetics of cephalothin and its deacetyl metabolite were studied with use of a chemical assay involving high-pressure liquid chromatography. In seven patients with normal renal function, the half-life of cephalothin was about 28 min and concentrations of deacetylcephalothin in serum were low. In five patients with uremia, the half-life of cephalothin averaged 221 min and there was a continuous accumulation of the deacetyl metabolite in serum during treatment. Recovery of the drug in urine was quantitative when renal function was normal, whereas the amount of drug excreted was very low in cases of uremia. The results offer some explanation of the complex pharmacokinetics of cephalothin seen with microbiological tests and illustrate the usefulness of specific chemical assays, especially in the monitoring of serum concentrations of mixtures of antibiotic compounds that differ in antibacterial activity.

Cephalothin↗
PubMed1980

Direct stimulation of lymphokine production by cephalothin.

Cephalothin significantly suppressed in vitro DNA and total protein synthesis in human peripheral blood lymphocytes stimulated by antigens or mitogens. However, similar concentrations of this antibiotic enhanced streptokinase-streptodornase-stimulated production of the lymphokine leukocyte-migration-inhibition factor (LMIF) and directly stimulated production of this lymphokine by otherwise unstimulated lymphocytes from 10 of 12 normal human subjects. Penicillin did not appear to produce these effects. Cephalothin did not interfere directly with neutrophil migration or the interaction of preformed LMIF with neutrophils. Stimulation of LMIF production by cephalothin required viable lymphocytes and was inhibited by puromycin. These results suggest that cephalothin is capable of inducing lymphokine production by human lymphocytes in a manner that appears to be nonspecific in nature. This type of effect could be the basis of some apparently immunologic reactions to this antibiotic.

Cephalothin↗
PubMed1983

Intraphagocytic killing of Salmonella typhimurium by liposome-encapsulated cephalothin.

Multilamellar liposomes (lipid bilayer vesicles) composed of phosphatidylcholine, cholesterol, and phosphatidylserine (molar ratio, 6:3:1) were produced and then made to entrap an aqueous solution of cephalothin. Resident murine peritoneal macrophages were shown to be capable of interiorizing the liposome-antibiotic complex; this event resulted in a relatively high intracellular concentration of cephalothin. In macrophages infected in vitro with Salmonella typhimurium, intracellular killing of the bacteria was maximal at 60 min of incubation; at this time, 60% of the interiorized organisms had been killed. Treatment of infected macrophages with liposome-encapsulated cephalothin enhanced the intraphagocytic killing of S typhimurium over that by macrophages treated with free cephalothin. These results demonstrate the superiority of liposome-encapsulated antibiotics to free antibiotics in effecting the elimination of a facultative intracellular bacterium from its intracellular site. This type of complex may find application in the treatment of diseases caused by this group of microorganisms.

Animals↗
PubMed1997

A prospective, randomized trial of two antibiotic regimens in the treatment of peritonitis in CAPD patients: teicoplanin plus tobramycin versus cephalothin plus tobramycin.

A multicentre, comparative, randomized study was performed to compare the efficacy and tolerability of two antibiotic regimens in the treatment of peritonitis in continuous ambulatory peritoneal dialysis (CAPD) patients: teicoplanin plus tobramycin versus cephalothin plus tobramycin. After informed consent had been obtained, 68 patients were randomized prospectively to receive either teicoplanin plus tobramycin or cephalothin plus tobramycin. Patients were followed throughout the study and for up to 4 weeks after the end of treatment, when clinical and microbiological parameters were assessed again. The incidence of clinical failure was 4.6 times higher in the cephalothin plus tobramycin group than in the teicoplanin plus tobramycin group (7/28 versus 2/37; P < 0.05). There was no significant difference in bacterial eradication between the two groups. Local and systemic tolerability were good for both regimens. The study shows that teicoplanin plus tobramycin is more effective than cephalothin plus tobramycin and might become a 'first-line' treatment for peritonitis in CAPD patients.

Aged↗
PubMed1984

Resistance types in Citrobacter freundii. Occurrence and resistance to ampicillin, carbenicillin, cephalothin and mecillinam. Transfer of ampicillin resistance.

The resistance types of Citrobacter freundii were investigated. The strains were divided into three groups according to susceptibility to penicillin derivatives. Group 1, comprising the ampicillin-carbenicillin sensitive strains (A-s/Ca-s), constituted 22%. Group 2 (ampicillin-resistant (A-r)/Ca-s) constituted 45% and group 3 (A-r/Ca-r) 32%. Two strains (1%) were recorded as A-s/Ca-r. Group 3 contained a higher proportion of multi-resistant strains than groups 1 and 2. The log2IC50 with ampicillin, carbenicillin, cephalothin and mecillinam in the tube-dilution method were determined for 32 strains. Groups 1 and 2 differed only as regards cephalothin resistance. The strains of group 3 were more A-r than the group 2 ones. The mecillinam susceptibility did not differ between the three groups. No strains in group 2 could transfer A-resistance. In group 3 ten out of 16 strains were able to transfer A-resistance. Resistance to sulphonamide, tetracycline, and streptomycin was also transferred, but with low frequency. The A-r/Ca-r strains could be divided into two subgroups, probably reflecting different modes of developing beta-lactam resistance. One group was very A- and Ca-r, less cephalothin-r, more mecillinam-r and could transfer A-resistance. The other group had very high cephalothin-resistance and could not transfer A-resistance. Citrobacter freundii and Enterobacter cloacae are very similar as regards resistance conditions.

Ampicillin↗
PubMed1988

Studies on clinical isolates of coagulase-negative staphylococci resistant to methicillin. Evidence of cross-resistance between methicillin and cephalothin.

The in vitro susceptibility to cephalothin and cefuroxime of 195 isolates of methicillin-resistant coagulase-negative staphylococci was determined by the agar-diffusion test, using 7.5% NaCl-supplemented agar. The distribution of the inhibition zone diameters for isolates of S. epidermidis (S. biotype 1) as well as for S. haemolyticus (S. biotype 4) was trimodal. While 4% of the isolates were found susceptible to cefuroxime, 39% of the S. epidermidis/S. hominis (S. biotype 1) isolates and 34% of the S. haemolyticus (S. biotype 4) isolates were found susceptible to cephalothin by this method. Eight of these isolates (six S. epidermidis, two S. haemolyticus) were selected for susceptibility testing by the tube-dilution method, together with four isolates (three S. haemolyticus, one S. epidermidis) found resistant to cephalothin by the agar-diffusion test. The first-mentioned isolates were all found susceptible to cephalothin with MICs less than or equal to 2 micrograms/l, while the last-named all were resistant with MICs greater than or equal to 16 micrograms/ml. Population analyses revealed sub-populations of highly resistant bacteria in all methicillin-resistant isolates of S. epidermidis (S. biotype 1), as well as in all isolates of S. haemolyticus (S. biotype 4). We thus concluded that methicillin-resistance in isolates of coagulase-negative staphylococci implies resistance to cephalosporins and that the difference between S. epidermidis and S. haemolyticus as regards cephalosporin-susceptibility is quantitative and not qualitative. Eighty-nine per cent of the 195 methicillin-resistant isolates in this study were resistant to penicillin and at least one more antibiotic. We therefore think that resistance to penicillin and one or more non-beta-lactam antibiotics strongly suggests methicillin-resistance and that such isolates should be further tested on hypertonic media.

Anti-Bacterial Agents↗
PubMed1978

Quantitation of antibiotics by high-pressure liquid chromatography: cephalothin.

A technique for quantitative determination of cephalothin and desacetylcephalothin in serum using a method based on high-pressure liquid chromatography is described. Both compounds were quantitatively extracted from serum by using dimethylformamide. After separation of the drugs by reverse-phase chromatography and detection by ultraviolet light absorption at 254 nm, serum concentrations of cephalothin and desacetylcephalothin as low as 1.0 mug/ml were measured. No interfering absorption was found in extracts of serum samples from normal humans or patients receiving a variety of other drugs, including other antimicrobial agents. Serum specimens obtained after an intravenous infusion of cephalothin to two human subjects and three dogs were assayed by the chemical and microbiological assays. When values, as determined by the chemical method and the microbiological assay in samples from human subjects, were compared, the correlation coefficient (r) was 0.96, whereas, in the dogs, the r value was 0.79. The chemical procedure described in this report for determination of cephalothin and desacetylcephalothin permits future pharmacokinetic investigations of these compounds. This assay is sensitive, specific, accurate, and rapid (approximately 30 min), and appears suitable for routine clinical use.

Animals↗
PubMed1982

Excretion of cephalothin and cefamandole by the normal pancreas and in acute pancreatitis in dogs.

Nine mongrel dogs were studied to evaluate the excretion of cefamandole (five dogs) and cephalothin (four dogs) in the pancreatic fluid. Each dog was studied before and after the induction of pancreatitis, with 2 weeks between studies. After intravenous administration of a 25-mg/kg dose of either cephalosporin, serum and pancreatic fluid concentrations were monitored for 6 h. Both cephalothin and cefamandole were excreted in bactericidal concentrations in the normal pancreas and in acute pancreatitis. Clearance of cefamandole (290 ml/min) and cephalothin (348 ml/min) were similar pre- and postinduction of pancreatitis. Serum albumin concentration was less during the post-pancreatitis phase compared with the prepancreatitis phase. Penetration of cephalothin was reduced in pancreatitis, whereas cefamandole penetration increased in pancreatitis.

Acute Disease↗
PubMed1984

Correlation of in vitro activities of cephalothin and ceftazidime with their efficacies in the treatment of Staphylococcus aureus endocarditis in rabbits.

Rabbits with Staphylococcus aureus endocarditis were treated with cephalothin or ceftazidime to determine whether differences in in vitro activity would result in differences in in vivo efficacy. Antibiotics were administered in doses equivalent to maximum recommended human doses, and results of laboratory tests to predict antimicrobial efficacy were determined during treatment. Cephalothin and ceftazidime MICs for the challenge strain were 0.5 and 8 micrograms/ml, respectively. MBCs were 32 and greater than 128 micrograms/ml, respectively. With peak sera, laboratory results (means) for cephalothin and ceftazidime were as follows: ratios of concentration in serum to MIC, 300 and 16; ratios of concentration in serum to MBC, 4.8 and less than 1; bacteriostatic antibacterial activity titers in serum, 1:256 and 1:16; and bactericidal antibacterial activity titers in serum, 1:16 and 1:4, respectively. Trough sera contained little or no measurable antibiotic and had no antibacterial activity. Both cephalothin and ceftazidime were efficacious in the treatment of infected rabbits. There were no statistically significant differences in efficacy as defined by survival, eradication of bacteremia, or sterilization of cardiac vegetations. Results of laboratory tests which quantitated antimicrobial activity did not correlate with efficacy, either independent of antibiotic or adjusted for antibiotic. Despite their lesser in vitro activities, the new cephalosporins may be equivalent to the older cephalosporins for treating staphylococcal infections in humans, when administered in maximum recommended doses.

Animals↗
PubMed1974

Biliary tract excretion of cefazolin, cephalothin, and cephaloridine in the presence of biliary tract disease.

The biliary tract excretion of three cephalosporins, cefazolin, cephaloridine, and cephalothin, was compared in patients with biliary tract disease. In the absence of obstruction, mean antibiotic levels in bile from gall bladder and common duct in patients undergoing cholecystectomy were highest for cefazolin (17 and 31 mug/ml, respectively) than either cephaloridine (7 and 9 mug/ml) or cephalothin (1 and 4 mug/ml). Biliary tract levels generally paralleled serum levels. In no patient with cystic duct obstruction were any of the cephalosporins detectable in appreciable amounts in gall bladder bile. In patients with T-tube drainage given each of the three different cephalosporins on separate days, concentrations of cefazolin in bile were many-fold higher than either cephaloridine or cephalothin. Peak levels of cefazolin in T-tube bile averaged 51 mug/ml after intravenous and 26 mug/ml after intramuscular administration, whereas mean peak levels of cephalothin and cephaloridine were only 6 and 16 mug/ml, respectively. Here, too, T-tube levels reflected serum concentrations and obstruction to biliary flow impaired excretion of each of the drugs.

Biliary Tract↗
PubMed1975

Effect of diuretics on urinary excretion of cephalothin in humans.

Diuretics and antibiotics are frequently used concomitantly. The possibility of drug interactions led us to study the effects of several diuretics on the renal elimination of cephalothin. Five healthy volunteers received a constant infusion of 500 mg of sodium cephalothin per h for 9 h on 4 consecutive days. Each day, after the third hour of infusion, the subjects were given one of the following in varying order: (i) furosemide (1 mg/kg, intravenous), (ii) mercaptomerin (250 mg, intramuscular), (iii) mannitol (25 g, intravenous), or (iv) no diuretic (control day). Fluid losses were replaced hourly. Serum and complete urine collections were obtained each hour and assayed for creatinine and cephalothin (bioassay). Clearances (milliliter per minute) and urinary excretions (milligram per hour) of cephalothin did not differ either when the diuretic day values were compared with control day, or when pre- and postdiuretic results on the same day were compared. Creatinine clearances were not affected by diuretics except for a transient rise after furosemide.

Adult↗
PubMed1965

Inactivation of cephalothin and cephaloridine by Staphylococcus aureus.

Benner, Ernest J. (University of Washington School of Medicine, Seattle), John V. Bennett, Jean L. Brodie, and William M. M. Kirby. Inactivation of cephalothin and cephaloridine by Staphylococcus aureus. J. Bacteriol. 90:1599-1604. 1965.-Marked differences were observed in the susceptibility of penicillinase-producing staphylococci to cephalothin and cephaloridine. All of 100 strains of penicillin G-resistant Staphylococcus aureus, with the use of a large inoculum, were found to be susceptible to 2 mug/ml of cephalothin, whereas only 50% were susceptible to this concentration of cephaloridine, and 15% required 15 mug/ml or more for inhibition. In contrast, penicillin G-sensitive strains were more susceptible to cephaloridine and did not show the marked inoculum effect observed with the cephaloridine-resistant strains. These differences were due to a much greater destruction of cephaloridine than of cephalothin by staphylococcal penicillinase. Cephaloridine-resistant staphyloccoci were stronger penicillinase producers than were susceptible strains, and the resistant strains were found to inactivate cephaloridine by hydrolysis of the beta-lactam ring. In population studies, cephaloridine-resistant cells differed from methicillin-resistant cells in that they decreased in numbers as the drug concentration was increased, and the survivors in higher drug concentrations were no more resistant than was the parent strain. Treatment with acriflavine eliminated resistance of the cells to both penicillin G and cephaloridine. It was concluded that cephaloridine resistance was due to hydrolysis by penicillinase, and that this was related to the pyridine ring substitution in the cephalosporanic acid nucleus.

Anti-Bacterial Agents↗
PubMed1979

Renal tubular necrosis following cephalothin.

Renal tubular necrosis was observed following intramuscular injections of cephalothin into rats. Lesions were consistently produced with 5.0g/kg and were maximal in severity at the 2nd and 3rd days following injection. Renal tubular necrosis following cephalothin was similar in morphology to that produced by nephrotoxic doses (2.0 g/kg) of cephaloridine. The nephrotoxic potential of cephalothin has been demonstrated in the rat model and caution is urged in using large doses of cephalothin.

Acute Kidney Injury↗
PubMed1976

Cephalothin-induced immune hemolytic anemia.

A patient with renal disease developed Coombs-positive hemolytic anemia while receiving cephalothin therapy. An anti-cephalothin IgG antibody was detected in the patient's serum and in the eluates from her erythrocytes. In addition, nonimmunologic binding of normal and patient's serum proteins to her own and cephalothin-coated normal red cells was demonstrated. Skin tests and in vitro lymphocyte stimulation revealed that the patient was sensitized to cephalothin and also to ampicillin. Careful investigation of drug-induced hemolytic anemias reveals the complexity of the immune mechanisms involved.

Anemia, Hemolytic↗
PubMed1977

Pharmacokinetics of ampicillin, cephalothin and doxycycline in various tissues of the rat.

To study the behavior of antibiotics in the tissues, rats were sacrificed repeatedly in groups of six, after the injection of 25 mg/kg ampicillin, 100 mg/kg cephalothin or 10 mg/kg doxycycline. These antibiotics were bioassayed in ten different organs. Standards were established for each organ by using identical organs, thus avoiding errors caused by tissue binding or inhibition. Penetration into the tissue is very fast. Compared to serum levels, lung, muscle, heart, testicle and spleen, levels are higher for doycycline, lower for ampicillin and variable for cephalothin: for example, lung/serum ratio at 1 h is 2.2, 0.5 and 1.1, respectively; muscle/serum is 2.3, 0.2 and 0.18. The decrease in tissue levels parrallels that in the serum for doxycycline, but is slower for ampicillin. The hepatic penetration of cephalothin is less than that of doxycycline or ampicillin. Levels are higher in the renal cortex than in the medulla for doxycycline, lower for cephalothin, and similar for ampicillin. The data enabled calculation of tissular pharmacokinetics. They have practical implications in the selection of antibiotics.

Ampicillin↗
PubMed1981

A comparison of the in vitro activity of cefoxitin and cephalothin against 7,312 clinical isolates.

The antibacterial activity of cefoxitin and cephalothin was tested against 7,312 clinical isolates of aerobic pathogens. Cefoxitin was found to have a broad spectrum of activity. Among the gram-positive cocci, 99.1% of Staphylococcus aureus, 94.4% of Staphylococcus epidermidis and 98.1% of streptococci group B had a minimal inhibitory concentration of 16 microgram/ml or less, while only 4.6% of enterococci were sensitive to this concentration of cefoxitin. Among the gram-negative rods 94.4% of Escherichia coli, 89.3% of Klebsiella spp., 97.3% of Proteus mirabilis, 97.4% of Proteus vulgaris and 79.3% of Proteus morganii were sensitive to 16 microgram/ml of cefoxitin or less. The effect of Pseudomonas spp. and Acinetobacter calcoaceticus was negligible. Cefoxitin was less active than cephalothin against gram-positive cocci, the difference being most pronounced against enterococci. Cephalothin was also found to be more active than cefoxitin against P. mirabilis, while cefoxitin was superior to cephalothin against E. coli, Klebsiella spp., Enterobacter spp., P. vulgaris and P. morganii.

Bacteria↗
PubMed1983

In vitro protection of group A beta-hemolytic streptococci from penicillin and cephalothin by Bacteroides fragilis.

beta-Lactamase produced by Bacteroides fragilis could protect from antibiotics group A beta-hemolytic streptococci (GABHS), penicillin-susceptible pathogens frequently isolated from acute tonsillitis in children. To test this hypothesis we determined the minimal bactericidal concentration (MBC) to penicillin and cephalothin of GABHS alone and in mixed culture with eleven beta-lactamase-producing strains of B. fragilis. B. fragilis strains with MBC values less than or equal to 32 micrograms/ml to penicillin and less than or equal to 64 micrograms/ml to cephalothin did not provide any protection for GABHS. However, strains with MBC greater than or equal to 128 micrograms/ml to penicillin and greater than or equal to 256 micrograms/ml to cephalothin provided protection by increasing the MBC of GABHS at least 8,534 times for penicillin and 2,048 times for cephalothin. This phenomenon was most marked in 5% CO2. B. fragilis provided no protection against clindamycin. These results may explain the inability of penicillin therapy to completely eradicate GABHS from cases of recurrently infected tonsils.

Bacteroides fragilis↗
PubMed1989

Antimicrobial activities and susceptibility testing considerations of ampicillin, cephalothin, cefaclor, and cefuroxime against invasive isolates of Haemophilus influenzae.

The activities of ampicillin, cefaclor, cephalothin, and cefuroxime against invasive clinical isolates of Haemophilus infleunzae were studied to determine the correlation between resistance and beta-lactamase production. Approaches to in vitro susceptibility testing of cephalosporins in the clinical laboratory were also assessed. Three hundred and eight isolates of H. influenzae were tested for ampicillin susceptibility, and those which required for inhibition greater than or equal to 1.0 micrograms/ml of ampicillin were tested for beta-lactamase production with a chromogenic cephalosporin. Twenty-two percent of isolates produced beta-lactamase and 85% were serotype b. All isolates considered resistant (MIC greater than or equal to 2.0 micrograms/ml) to ampicillin produced beta-lactamase. A single beta-lactamase-producing isolate was identified, but was inhibited by 1.0 microgram/ml of ampicillin, and a zone diameter of 20 mm was produced by disk diffusion testing. One hundred and ninety-seven isolates were tested for susceptibility to cefaclor, cefuroxime, and cephalothin. Chloramphenicol susceptibility testing by disk diffusion was also performed on these isolates. General agreement and interchangeable results were found among these three cephalosporins by both agar dilution and disk diffusion methods. We conclude that ampicillin-resistant H. influenzae not producing beta-lactamase is rare among these isolates of H. influenzae responsible for invasive disease. Susceptibility testing results of cephalothin, cefaclor, or cefuroxime appear to be interchangeable, although results of cephalothin testing would tend to underestimate the activities of cefaclor or cefuroxime.

Ampicillin↗