Search PubMed⌕ Search

SEARCH · Search PubMed

Results for “Cephaloridine”

Search indexed PubMed citations on genomics, clinical trials, systematic reviews and public health. Explore titles, authors and supplied subject terms, then open the PubMed record.

Quote a phrase for an exact phrase match. Source license links do not imply unrestricted reuse.

At least 73 records · Page 4Linked to original sources
PubMed1979

Cephaloridine and the rat kidney lysosomes stability in vitro.

Two methods employing lysosomal enzyme release and light scattering measurements have shown that Cephaloridine Stabilises rat kidney lysosomes in vitro against beta-Progesterone and lysolecithin, the two well known agents to labilise lysosomal membranes. Treatment of the isolated lysosomes suspended in 0.25 M-sucrose-EDTA (0.34 mM) pH 7.4 with cephaloridine (100mcM) at 37 degrees C for 10 min. and subsequent incubation of the mixture with progesterone (0.25mM) at the same temperature for varying periods of time up to 50 min. resulted in no significant changes from the normal values in the release of acid phosphatase activity obtained from the supernatant fraction after centrifugation of the incubated mixture at 33,000g. for 5 min. at 4 degrees C. When lysosomes were mixed with cephaloridine before treatment with progesterone or lysolecithin, and then subjected to light scattering measurements, lysosomal swelling was considerably decreased, indicating that cephaloridine could exert a stabilising effect on rat kidney lysosomal membrane and thereby limit the release of lysosomal acid hydrolases.

Acid Phosphatase↗
PubMed1983

Effect of cephaloridine on the transport of organic ions in dog kidney plasma membrane vesicles.

The cephalosporin antibiotics cephaloridine and cefazolin were examined for their effects on the transport of a prototype anion, [3H]p-aminohippurate (PAH) and a prototype cation, N1-[3H] methylnicotinamide (NMN) in basolateral membrane vesicles and brush border membrane vesicles (BBMV). Cefazolin inhibited transport of 50 microM PAH in both membranes and had no effect on transport of 50 microM NMN transport. Under identical conditions, cephaloridine, a zwitterion, inhibited PAH transport in both membranes and NMN transport in BBMV but not in basolateral membrane vesicles. Cephaloridine was less effective than cefazolin in inhibiting PAH transport in BBMV. The results demonstrate the organic transport systems in the basolateral membrane vesicles differ from those in the BBMV. Furthermore, a zwitterionic drug can interact with both systems in the BBMV. An explanation for the intracellular accumulation of cephaloridine is presented.

Aminohippuric Acids↗
PubMed1978

[Experimental studies on the passage of antibiotics into cerebrospinal fluid in staphylococcal meningitis in rabbits. II. Cephaloridine, cephalothin and cefazolin (author's transl)].

Passage of cephaloridine, cephalothin and cefazolin into cerebrospinal fluid (CSF) was evaluated in Staphylococcus aureus meningitis in rabbits and the following results were obtained. 1. Concentration in CSF (microgram/ml) [CSF/serum ratio (%)] was determined 1/2, 1 and 2 hours after a single intravenous injection of 100 mg/kg of each antibiotic, respectively; cephaloridine-7.5 [8.9], 9.7 [13.8], 9.1 [22.6]; cephalothin-0.42 [3.6], 0.23 [6.4], not detectable [0]; cefazolin-7.5 [11.8], 5.2 [19.3], 2.0 [17.5]. 2. When results with cefazolin after an intravenous injection 100 mg/kg and 200 mg/kg were compared, a definite dose response was noted in blood concentration but not in CSF concentration. 3. A standard error of CSF concentrations of each antibiotic was larger than that of penicillins, and "Unpredictability" of their passage into CSF was considered to be one of the characteristics common to these three drugs in respect of their passage into CSF. 4. There was no significant difference noted in antibiotic passage into CSF between cephaloridine of low protein binding rate and cefazolin of very high binding rate. Cephalothin, of which binding rate was intermediate, showed a remarkably lower passage into CSF. These results indicate that a correlation does not always exist between protein binding rate of the antibiotics and their passage into CSF. 5. Based on the above results, a review of the literature was made on clinical applicability of these three antibiotics in the treatment of bacterial meningitis. Low transport rate of cephalothin into CSF and nephrotoxicity of cephaloridine make them to be unsuitable for bacterial meningitis. Cefazolin is considered to be suitable in the treatment of ampicillin-resistant Escherichia coli meningitis and Gram-positive coccal meningitis in which penicillins are not applicable.

Animals↗
PubMed1976

Renal effects of gentamicin and cephaloridine. Evaluation by renal enzyme excretion studies in rats and comparison with other antibiotics.

The renal effects of gentamicin and cephaloridine were investigated by determining the changes in renal enzyme excretion. Both drugs provoked significant elevations or urinary AP-, LAP-, or LDH-activities. This result permits the conclusion that both drugs take influence on the kidney. The exact pathomechanism leading to this increased renal enzyme excretion was not elucidated. The fact that gentamicin in the applied dosage (about 30% of LD50) provoked more pronounced changes than cephaloridine (about 20% of LD50) could be explained by an in-vitro interference of cephaloridine with the enzymatic activities investigated in this study. In the discussion, the changes elicited in the same model by other antibacterial compounds were compared with the data obtained with gentamicin and cephaloridine. In closing, implications, restrictions, and validity of renal enzyme excretion studies in rats for screening nephrotoxic properties of a drug for human use are briefly discussed.

Alkaline Phosphatase↗
PubMed1988

Zero-crossing derivative spectrophotometry for the determination of mixtures of cephaloridine and cephalothin in pure and dosage forms.

First- and second-derivative spectrophotometry, with a zero-crossing technique of measurement, has been used for the quantitation of two-component mixtures of cephaloridine and cephalothin Na, which are cephalosporins with closely overlapping spectral bands. Beer's Law is followed for up to 28 and 36 micrograms/mL of cephaloridine in the first- and second-derivative modes, respectively, and up to 36 micrograms/mL of cephalothin Na in both modes. Detection limits at the 0.05 level of significance were calculated to be 0.13 and 0.37 micrograms/mL of cephaloridine and cephalothin Na, respectively, in the first-derivative mode, and 0.25 and 0.29 micrograms/mL, respectively, in the second-derivative mode. The recovery of these antibiotics in mixtures of injectable dosage forms is also reported.

Cephaloridine↗
PubMed1975

Convulsion following intrathecal cephaloridine.

Following therapeutic intrathecal administration of cephaloridine to an 11-day-old premature infant with suspected meningitis, a generalized tonic convulsion was observed. Symptoms continued to subside over the next six hours, followed by postictal sleep. That convulsion and other symptoms were due to cephaloridine was confirmed when the second intrathecal administration produced the same symptom. Because of its possible damaging effect on CNS, it is strongly suggested that cephaloridine should not be administered directly into the cerebrospinal fluid space.

Cephaloridine↗
PubMed1982

Further studies on the in vivo effect of cephaloridine on the stability of rat kidney lysosomes.

The stabilizing effect of cephaloridine, an antibiotic, on rat kidney lysosomal membranes was tested by a single subcutaneous injection. The release of two lyososomal enzymes, acid phosphatase and muramidase, was used as an index of lysosome membrane integrity. The levels of these enzymes in the kidney extracts as well as in the isolated kidney lysosome fractions were found to be raised considerably, compared to the controls. In rats treated with cephaloridine, the supernatant fraction obtained from the kidney homogenates, after centrifugation at 15,000 gav, contained lower enzyme activities than were found in the control animals. It is suggested that cephaloridine may inhibit the release of acid phosphatase and muramidase from rat kidney lysosomes and, therefore, may exert a stabilizing effect on the lysosomal membrane system. The possible mechanism of interaction of this antibiotic with rat kidney lysosomal membranes is proposed.

Acid Phosphatase↗
PubMed1988

Specific alterations of rat renal microsomal proteins induced by cephaloridine.

In order to elucidate the molecular mechanisms of cephaloridine (CPH) nephrotoxicity, the effect of cephaloridine treatment on the protein composition of different subcellular fractions from rat kidney cortex was investigated. After intravenous treatment of male Wistar rats with 250-1200 mg/kg/d CPH for 1-3 days, kidneys were removed and the homogenate from renal cortex was separated into lysosomal, cytosolic and microsomal fractions. The polypeptide composition of the different subfractions was analyzed by one-dimensional SDS-gel electrophoresis and quantified by densitometry. Significant differences in the polypeptide composition between treated and non-treated animals were seen in the microsomal fraction. CPH-treatment induced a polypeptide with an apparent molecular weight of 44,000 and decreased the content of cytochrome P-450 isoenzymes in the microsomal fraction. Solubilization experiments showed that the CPH-induced microsomal polypeptide of molecular weight 44,000 is a peripheral membrane protein rather than an integral membrane protein. The induction of this protein by CPH was dose- and time-dependent. Preliminary experiments using the kidney slice technique indicate that the induction of this polypeptide correlates with the nephrotoxicity measured as decrease in renal cortical accumulation of organic ions. Thus, the results of the present study indicate that treatment of rats with CPH resulted in the induction of a microsomal polypeptide of molecular weight 44,000 which could be a sensitive parameter of cephaloridine nephrotoxicity.

Animals↗
PubMed1979

The effect of cephaloridine on the stability of rat kidney lysosomes.

The administration of cephaloridine to rats caused a decrease in the excretion of acid phosphatase into the urine. The antibiotic itself had no effect on urinary acid phosphatase and inhibitors or proteolytic enzymes were not present in the urine from treated rats. Cephaloridine may therefore be stabilizing the lysosomal membrane in vivo and experiments with isolated lysosomes confirm this hypothesis. The lysosomal integrity was followed by measuring the acid phosphatase activity and the light scattering properties of the particles. A good correlation was obtained between these parameters in the case of thermal disruption and progesterone induced lysis of the lysosomes and low concentrations of cephaloridine (0.1-1.0 mmol/1) protected the lysosomes against this form of damage.

Acid Phosphatase↗
PubMed1988

In vitro assessment of cephaloridine nephrotoxicity: comparison of renal cortical slice and renal tubule fragment techniques.

Renal cortical slices and a suspension of renal tubule fragments were prepared from male Wistar rats that had received a single s.c. dose of either cephaloridine (100 mg/kg) or normal saline (1 ml/kg) 48 h previously. The comparative sensitivity of these tissue preparations as in vitro models to assess nephrotoxin-induced changes in renal function was investigated by measuring the ability of the preparations to undertake the active accumulation of [3H]para-aminohippuric acid and to undertake gluconeogenesis from sodium pyruvate. Through the use of the cortical slice technique, [3H]para-aminohippuric acid tissue accumulation and glucose production in the cephaloridine-treated group were not significantly different from control. In contrast, using the tubule fragment technique, significant (p less than 0.05) reductions in the accumulation of [3H]para-aminohippuric acid and in the production of glucose via gluconeogenesis, between cephaloridine and normal saline control treatments were observed. Control values in the tubule fragment technique, for para-aminohippuric acid transport and glucose production via gluconeogenesis, were observed to be much greater than control values obtained from the cortical slice technique. It is suggested that the tubule fragment technique may be a more valuable in vitro preparation to assess the effects of potential nephrotoxins on tubule transport function than the still widely used cortical slice technique. The use of specific metabolic substrates, such as acetate, that will stimulate cellular metabolism and substrate transport, will also enhance the value of the technique.

Aminohippuric Acids↗
PubMed1984

The reversible deactivation of beta-lactamase from Staphylococcus aureus by quinacillin and cephaloridine and its modification by antibodies.

The effect of antibody on the reversible deactivation of the beta-lactamase (penicillin amino-beta-lactamhydrolase, EC 3.5.2.6) from Staphylococcus aureus has been studied using quinacillin and cephaloridine as substrates. The latter has been shown to exhibit the characteristics of an A-type substrate Citri, N., Samuni, A. and Zyk, N. (1976) Proc. Natl. Acad. Sci. U.S.A. 73, 1048-1052) and reversibly to lower the activity of the enzyme towards benzylpenicillin in a manner analogous to quinacillin. Both divalent and monovalent antibodies reduce the activity of the lactamase to 60% of the native value in the absence of substrate. The reduction by monovalent antibody is slow (t1/2 approximately equal to 25 min). Both divalent and monovalent antibodies modify the time-course of reversible deactivation independently of being added before or subsequent to deactivation by substrate. The full recovery of activity is delayed in the case of quinacillin and accelerated for cephaloridine. The activity against benzylpenicillin in the deactivated states is unaffected. These effects are shown to reflect the changed rates of hydrolysis of the two substrates in the presence of antibody. The effect of antibody is mediated by minor conformational change. Continuous assays for following the hydrolysis of quinacillin and cephaloridine by optical rotation are reported.

Cephaloridine↗
PubMed1975

A controlled trial of intraperitoneal cephaloridine administration in peritonitis.

From a controlled therapeutic trial extending for more than 2 yr and involving 69 patients with appendicitis and peritonitis a clear-cut statistically significant result emerged. There was a major reduction in the incidence of intraperitoneal abscesses using cephaloridine by the intraperitoneal as opposed to the systemic route. After randomized selection into treatment and control groups, cephaloridine, 25 mg/kg was given by injection every 6 hr for 48 hr to the treatment group by i.p. installation and to the control group by systemic injection. Both groups received initial intraoperative peritoneal lavage with normal saline and also continued systemic injections of cephaloridine on postoperative days 3, 4, and 5. Only one out of 36 patients in the treatment group developed a residual intraperitoneal abscess, as opposed to six abscesses developing in 33 patients in the control group. Technical problems and complications of the method were trivial and have not prevented us from continuing and extending the applications of the method.

Administration, Oral↗
PubMed1997

Magnesium lithospermate B ameliorates cephaloridine-induced renal injury.

To determine whether magnesium lithospermate B ameliorates renal injury induced by cephaloridine, the effect of cephaloridine was investigated in rats given magnesium lithospermate B for 20 days preceding cephaloridine administration and in control rats given no magnesium lithospermate B. In the control rats, blood and urinary parameters and the activity of radical-eliminating enzymes in the renal tissue deviated from the normal range, indicating damage to the kidneys. In contrast, rats given magnesium lithospermate B showed decreased urine volume, increased urinary osmotic pressure, and decreased urinary levels of glucose, protein, sodium and potassium, denoting less damage to the kidney. In this group, the urinary nitrite/nitrate ratio, and the activities of superoxide dismutase and catalase in the renal tissue were increased, while the malondialdehyde levels were decreased, suggesting the involvement of radicals in the normalizing of kidney function. The increased levels of urea nitrogen in the blood of rats with induced renal failure were also lowered by administering magnesium lithospermate B.

Animals↗
PubMed1975

Peptidoglycan synthesis in Bacillus licheniformis. The inhibition of cross-linking by benzylpenicillin and cephaloridine in vivo accompanied by the formation of soluble peptidoglycan.

The synthesis of peptidoglycan by an autolysin-deficient beta-lactamase-negative mutant of Bacillus licheniformis was studied in vivo in the absence of protein synthesis. Benzylpenicillin and cephaloridine inhibited the formation of cross-bridges between newly synthesized peptidoglycan and the pre-existing cell wall. This inhibition, detected by measurement of the incorporation of N-acetyl[14C]glucosamine into the glycan fraction of the cell wall, was reversed by treatment with beta-lactamase and washing. Inhibition of D-alanine carboxypeptidase by benzylpenicillin was not reversed under similar conditions. Cells in which the initial penicillin inhibition of transpeptidation had been reversed showed an increased sensitivity to a subsequent addition of the antibiotic. Chemical analysis of peptidoglycan synthesized after reversal of penicillin inhibition revealed the presence of excess of alanine resulting from the continued inhibition of D-alanine carboxypeptidase. When the cell walls were digested to yield muropeptides so that the degree of cross-linking could be measured, the product after reversal of penicillin inhibition contained fewer cross-links than did the control preparation. Cultures treated with benzylpenicillin and cephaloridine continued to synthesize uncross-linked soluble peptidoglycan, which accumulated in the medium. This soluble material was all newly synthesized peptidoglycan and did not result from autolysis of the bacteria. The average chain lengths of the glycan synthesized in vivo and released as soluble peptidoglycan in the presence of both benzylpenicillin and cephaloridine were similar to those found previously in this organism.

Acetylglucosamine↗
PubMed1975

Inactivation of cefazolin, cephaloridine, and cephalothin by methicillin-sensitive and methicillin-resistant strains of Staphylococcus aureus.

Cefazolin was more susceptible than cephaloridine and cephalothin to in vitro inactivation by coagulase-positive, penicillinase-producing strains of Staphylococcus aureus. Inactivation (which was greater with methicillin-resistant than with methicillin-sensitive strains) was demonstrated by assay of the antibiotics in broth cultures with simultaneous colony counts and by exposure of the antibiotics to penicillinase powders extracted from S. aureus. Cefazolin was destroyed to a greater extent than was cephaloridine, whereas cephalothin underwent little, if any, destruction. The clinical implications of this degradation, thought by some to be of importance for cephaloridine, might also apply to cefazolin.

Cefazolin↗
PubMed1979

Cephaloridine prophylaxis in resection of the large intestine.

A controlled prospective clinical trial of cephaloridine chemoprophylaxis in resection of the large intestine was undertaken between 1974 and 1978. Data were available on 159 of 177 unselected patients. All were operated on by one surgeon. Three groups were studied: intraabdominal resection and anastomosis (102 patients); pullthrough resection and anastomosis (30 patients): and resection, with colostomy or ileostomy, without anastomosis (27 patients). In the total patient series cephaloridine reduced wound infection from 38.3% to 15.4% (P less than 0.003). There was no significant decrease in intraabdominal infection. In the group of patients undergoing intraabdominal resection and anastomosis the would infection rate was reduced from 40.0% to 14.9% (P less than 0.01). Cephaloridine reduced wound infection from 50.0% to 21.4% (P = 0.05) in those patients in whom drainage tubes were inserted. A decrease in the incidence of faecal fistula from 10.9% to 4.3% was not significant. Wound infections were not reduced significantly after pullthrough excisions or resections without anastomosis. The results support the routine prophylactic use of cephalosporins in patients undergoing intraabdominal resection of the large intestine with anastomosis.

Cephaloridine↗
PubMed1978

Microcalorimetric study of the effects of cephalexin and cephaloridin on Escherichia coli and Staphylococcus aureus.

The kinetics of the antibacterial actions of cephalexin and cephaloridin against a strain of Escherichia coli and a strain of Staphylococcus aureus were studied by a flow microcalorimeter. The heat production was related to the number of viable organisms (CFU ml-1), the pH, the optical density of the culture medium (OD540), and the morphology of the antibiotic-exposed bacteria. No heat effects could be registered when the number of CFU was below 10(4) ml-1. The addition of cephalexin, 2.5 microgram ml-1 (5 x MIC), to cultures of S. aureus caused a decrease in the heat production which was only roughly correlated with the number of CFU ml-1. This was also the case when 9.0 microgram ml-1 (2 x MIC) of this drug were added to cultures of E. coli. Two to three hours after the drugs had been added, no heat effects could be registered for the following 6--8 hours, after which an increase in the heat production again occurred. The MIC and MBC of the organisms isolated during this late heat increase were 8--40 times higher than those of the parent test organisms. A direct relation between drug concentration and response, i.e. heat effects produced, was found when increasing concentrations of cephalexin, i.e. 1.0 up to 50 micrograms ml-1 (2--100 x MIC) were added in the logarithmic growth phase to cultures of S. aureus. In ampoule calorimetric experiments, E. coli was cultured in a non-aerated, sealed growth vessel in the presence of cephalexin or cephaloridin in concentrations corresponding to 1/2 x MIC. The thermograms did not differ in shape, although the heat effects occurred somewhat later in the culture containing cephaloridin.

Calorimetry↗
PubMed1977

Penetration of cefazolin, cephaloridine, and cefamandole into interstitial fluid in rabbits.

We compared the penetration of three cephalosporins into interstitial fluid. Interstitial fluid was obtained in rabbits from Silastic tissue cages. Cefazolin, cephaloridine, and cefamandole were administered by the intramuscular route (30 mg/kg per injection). Peak blood levels and interstitial concentrations were studied after a single injection. Interstitial levels were also compared in a three-injection study (one injection every 12 h) and in a cumulative effect study (six injections), in which the interval between injections was established for each drug on the basis of its common therapeutic use. After a single injection, cephaloridine activity was detected more rapidly and attained higher levels than the other two drugs within the first 4 h. However, 2 h after the third injection, cefazolin levels in tissue fluid were higher than with cephaloridine. Cefamandole consistently gave the lowest interstitial levels. With all three drugs, detectable concentrations were present in interstitial fluid at a time when no detectable antibiotic was found in serum. In the six-injection study, the interstitial levels obtained with cefazolin were significantly higher than those observed with the other drugs. Our data suggest that cefazolin is a drug of choice due to its high extravascular levels.

Animals↗