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PubMed1982

Peroperative cephradine concentrations in the gall bladder wall and bile.

Cephradine levels were assayed in serum, gall bladder wall and bile sampled from the gall bladder and common bile duct in 24 patients undergoing elective cholecystectomy. Cephradine was administered either as 1 g given intravenously at the time of anaesthetic induction, or as three 6-hourly doses of 0.5 g taken orally during the pre-operation day followed by 1 g intramuscularly with the premedication. Adequate antibacterial levels of cephradine were achieved in all serum samples, 8 of 9 samples of choledochal bile, 6 of 12 samples of cholecystic bile and all 12 samples of gall bladder wall in the group receiving a single intravenous dose, compared to only 4 of 12 serum samples, 6 of 11 choledochal bile samples, 6 of 10 cholecystic bile samples, and only 3 of 12 samples of gall bladder wall in the group receiving oral cephradine. Therefore, cephradine given as a 1 g bolus intravenously with anaesthetic induction provides satisfactory concentrations for antibacterial prophylaxis during gall bladder surgery but a regimen of oral and intramuscular dosage was found to be unsatisfactory.

Adult↗
PubMed1979

Comparison of pivmecillinam and cephradine in bacteriuria in pregnancy and in acute urinary tract infection.

48 non-pregnant domiciliary patients referred by general practitioners and 50 pregnant women were treated for bacteriuria with either 500 mg cephradine or 400 mg pivmecillinam every 6 h for 7 days. In the pregnant women, cure rates were over 90% after 2 weeks for both compounds, and after 6 weeks were 86% for cephradine and 78% for pivmecillinam. Cure rates in the non-pregnant were 83% for cephradine and 95% for pivmecillinam at 6 weeks. Seven patients (3 given cephradine, 4 given pivmecillinam) stopped treatment due to side-effects. Overall, side-effects (many of which were trivial) were more common in patients treated with cephradine (51%) than in those receiving pivmecillinam (33%). It is concluded that both drugs are highly effective in these two common types of urinary infection.

Adult↗
PubMed2005

Synthesis and antibacterial activity of cephradine metal complexes : part II complexes with cobalt, copper, zinc and cadmium.

Cephradine, the first generation cephalosporin, is active against a wide range of Gram-positive and Gram-negative bacteria including penicillinase-producing Staphylococci. Since the presence of complexing ligand may affect the bioavailability of a metal in the blood or tissues, therefore, in order to study the probable interaction of cephradine with essential and trace elements present in human body, cephradine has been reacted with cobalt, copper, zinc and cadmium metal halides in L:M ratio of 2:1 in methanol and the products recrystallized from suitable solvents to pure crystals of consistent melting points. Infrared and ultraviolet studies of these complexes were carried out and compared with ligand. Magnetic susceptibility studies of these complexes were also carried out showing their paramagnetic behavior. From the infra red studies and elemental analysis of the complexes, it has been shown that the drug molecule serves as a bidentate ligand coordinating through both its carboxylate at C-3 and beta-lactam nitrogen and the metal having a square planar or octahedral geometry. To evaluate the changes in microbiological activity of cephradine after complexation, antibacterial studies were carried out by observing the changes in MIC (minimum inhibitory concentration) of the complexes and compared with the parent drug by measuring the zone of inhibition of complexes and compared with the parent cephalosporin against both Gram-positive and Gram-negative organisms. For MIC observation, serial dilution method was employed and zone series were determined by disk diffusion method. Our investigations reveal that formation of complexes results in decrease in antibacterial activity of cephradine and MIC values are increased.

Anti-Bacterial Agents↗
PubMed1989

Effect of various chemical modifiers on H+ coupled transport of cephradine via dipeptide carriers in rabbit intestinal brush-border membranes: role of histidine residues.

We examined the effect of diethylpyrocarbonate (DEPC), a histidine specific reagent, on H+ coupled transport of cephradine via dipeptide carriers in the intestinal brush-border membranes, in comparison with the effects of other chemical modifiers. Pretreatment of membrane vesicles with DEPC resulted in the inhibition of cephradine transport in the presence or absence of an inward H+ gradient. This inhibition was reversed by subsequent treatment with hydroxylamine, but not with dithiothreitol. The inactivation by DEPC pretreatment was abolished by the presence of cephradine or glycylsarcosine. In the DEPC-pretreated membranes, the V(max) value of cephradine uptake was decreased without any change in the Km value. In contrast, cephradine uptake was not changed by the pretreatment with N-acetylimidazole, a tyrosine specific reagent, or p-chloromercuribenzene sulfonate, a sulfhydryl reagent. These results suggest that histidine residues in the carriers are essential for H+ coupled transport of amiocephalosporins.

Animals↗
PubMed1973

Comparison of the chemotherapeutic and pharmacodynamic activities of cephradine, cephalothin, and cephaloridine in mice.

Cephradine, a new semisynthetic cephalosporin derivative, is 7[d(-)-2-amino-2-(1,4-cyclohexadien-1-yl) acetamido]-3-methyl-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid hydrate. The compound has a broad spectrum of antimicrobial activity in vitro. When given subcutaneously to mice, cephradine was appreciably more effective than cephalothin against infections induced by penicillinase-producing Staphylococcus, Escherichia coli, Klebsiella pneumoniae, or Enterobacter cloacae strains. Cephradine and cephaloridine possessed equivalent activity in treating infections caused by these same three gram-negative bacteria. The mean total bioactivity of cephradine in the serum of mice peaked within 30 min (59 mug/ml) after parenteral administration and was approximately threefold that of cephalothin (20 mug/ml), but less than that of cephaloridine (83 mug/ml). Nearly all of the administered cephradine (84%) and cephaloridine (70%) were excreted in the urine as the parent compounds. In contrast, only 47% (total bioactivity) of administered cephalothin was recovered, an amount that represented only 15 to 20% of the parent substance.

Animals↗
PubMed1975

[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↗
PubMed2003

Synthesis and antibacterial activity of cephradine metal complexes: part I complexes with magnesium, calcium, chromium and manganese.

Cephradine is included among the first generation cephalosporins, which is active against a wide range of Gram-positive and Gram-negative bacteria including penicillinase-producing Staphylococci. Since the presence of complexing ligand may affect the bioavailability of a metal in the blood or tissues, therefore, in order to study the probable interaction of cephradine with essential and trace elements present in human body, cephradine has been reacted with cobalt, copper, zinc and cadmium metal halides in L:M ratio of 2:1 in methanol and the products recrystallized from suitable solvents to pure crystals of consistent melting points. Infrared and ultraviolet studies of these complexes were carried out and compared with ligand. Magnetic susceptibility studies of these complexes were also carried out showing their paramagnetic behavior. From the infra red studies and elemental analysis of the complexes it has been shown that the drug molecule serves as a bidentate ligand coordinating through both its carboxylate at C-3 and beta -lactam nitrogen and the metal having a square planar or octahedral geometry. To evaluate the changes in microbiological activity of cephradine after complexation, antibacterial studies were carried out by observing the changes in MIC (minimum inhibitory concentration) of the complexes and compared with the parent drug by measuring the zone of inhibition of complexes against both Gram-positive and Gram-negative organisms. For MIC observation, serial dilution method was employed and zone series were determined by disk diffusion method. Our investigations reveal that formation of complexes results in decrease in antibacterial activity of cephradine and MIC values are increased.

Journal Article↗
PubMed1976

Cephradine excretion in humans with pH-altered urine.

In a random crossover study, ten healthy men were pretreated with ammonium chloride or sodium bicarbonate to alter urinary pH, and then were given a single 1-Gm dose of cephradine, either orally or intravenously. No significant changes were found in the terminal phase rate constant nor in the time or magnitude of peak concentration. Total recovery was greater than 90 per cent whenever degradation of cephradine did not occur. An unexplained but significant reduction in area under curve was present in data for prealkalinized subjects and for all subjects who took cephradine orally. Trapping of cephradine was not significant in the excretory pathway.

Administration, Oral↗
PubMed1978

[Interference of the tissue concentration of antibiotics with a salidiuretic. Behaviour of cephradine and cephalothin in brain tissue after additional administration of furosemide (author's transl)].

Serum and brain tissue concentrations were determined after i.v. administration of 4 g cephradine to 11 patients of whom 6 were additionally receiving 40 mg furosemide t.i.d. peroral. Five further patients were given 4 g cephalothin i.v. All patients were undergoing a brain operation at the time of antibiotic administration. Between 60 and 100 min after dosage, cephradine decreased in the serum from 104.9 mcg/ml to 56.7 mcg/ml and in the brain tissue from 13.02 mcg/g to 8.37 mcg/g in the mean. Cephradine concentrations in serum were higher and in brain tissue lower when furosemide was given as well. These differences are statistically significant (p less than 0.01). Serum concentrations of cephalothin over the same period and in the absence of furosemide were very low with 32.2 mcg/ml at 60 to 70 min, and extremely low in the brain tissue (0.55 mcg/g in the mean) so that a trial with furosemide was not performed. Neither antibiotic was detectable in the cerebrospinal fluid. The differences in serum and brain tissue concentrations of cephradine in the presence and absence of furosemide demonstrate that special care must be taken when administering more than one drug.

Brain Chemistry↗
PubMed1988

Evaluation of roxithromycin (RU-965) versus cephradine in pneumococcal pneumonia.

One hundred and sixty black South African gold miners with acute pneumococcal pneumonia were enrolled in a prospective randomized double-blind trial comparing roxithromycin (150 mg 2 X day) with cephradine (1.0 g 2 X day). Ninety patients with pneumonia caused by Streptococcus pneumoniae were treated for 5-10 days. Forty-three of 46 (93.4%) of the roxithromycin and all 44 (100%) of the cephradine treated groups had satisfactory clinical responses. In eight of the 46 (17%) roxithromycin treated patients and 10 of the 44 (23%) cephradine treated patients, Streptococcus pneumoniae was not eradicated from sputum cultures by the tenth day. Side effects in 18 patients (20%) were mild and were usually manifested by elevation of the transaminases; these were more common in the cephradine group (12) than in the roxithromycin group (5). Roxithromycin appears to be a safe and effective oral antibiotic for treatment of patients with mild to moderate pneumococcal pneumonia.

Adult↗
PubMed1987

Qualitative and quantitative analysis of cephradine in biological materials by high performance liquid chromatography.

A reversed phase high performance liquid chromatographic method was developed for the determination of cephradine, one of the commonly used antibiotics, in biological materials. Mimic samples for stomach contents, miso soup, were applied to high performance liquid chromatography (HPLC) after centrifugation and purification by Sep-Pak C18 cartridge treatment. Serum samples deproteinized or urine samples diluted were directly injected into the HPLC. The recoveries of cephradine from these materials were 95-97% and the detection limit was 0.01 microgram/injection. This method was applied to the analysis of cephradine in stomach contents obtained by autopsy. After purification by the cartridge treatment, cephradine in the sample was identified and determined by HPLC and further confirmed by thin-layer chromatography (TLC) and mass spectrometry (MS).

Adult↗
PubMed2005

Preparation and characterization of uniform nanosized cephradine by combination of reactive precipitation and liquid anti-solvent precipitation under high gravity environment.

In this work, a novel direct method, which was combined with reactive precipitation and liquid anti-solvent precipitation under high gravity environment, had been developed to prepare nanosized cephradine with narrow particle size distribution. Compared with commercial crude cephradine, the prepared cephradine showed a significant decrease in particle size, a significant increase in the specific surface area and shorter dissolving time when used for injection. The characteristic particle size was between 200-400 nm. The specific surface area increased from 2.95 to 10.87 m2/g after micronization. When the amount of L-arginin decreased from 0.25 to 0.18 g, the mixture of nanosized cephradine and L-arginine could still dissolve in 1 min. The X-ray diffraction (XRD) and Fourier transform infrared spectroscopy (FT-IR) analysis indicated that the physical characteristics and molecular states remained unchanged after the recrystallization process. This method had potential application in industrial fields because of its low cost, efficient processing and the ease of scaling-up.

Cephalosporins↗
PubMed1983

Double-blind study to compare the selection of antibiotic resistance by amoxycillin or cephradine in the commensal flora.

Elderly patients with acute urinary infections were treated in a double-blind study with either amoxycillin or cephradine. In 52 patients who had received amoxycillin for one week about a third of all intestinal Escherichia coli were highly resistant to amoxycillin, and many were resistant to tetracycline, trimethoprim, or chloramphenicol. Cephradine selected less resistance. At a week after completion of chemotherapy, cephradine-resistant E coli were replaced by sensitive cultures at a greater frequency than were amoxycillin-resistant E coli. Neither antibiotic altered the skin flora. Amoxycillin, but not cephradine, selected for Enterobacteriaceae in the saliva. The propensity of amoxycillin to select resistance in E coli will limit its usefulness in treating urinary infections.

Acute Disease↗
PubMed1978

Probenecid and the antibacterial activity of cephradine in vivo.

The influence of probenecid on the concentrations in blood and antibacterial efficacy of cephradine was studied in experimentally infected mice. An infection was induced by injection of 5 X 10(6) Escherichia coli into the thighs of irradiated, granulocytopenic mice. Probenecid was given 1 hr later, just before the administration of cephradine. The control animals received only the vehicle. Concentrations of cephradine in blood were determined for 2 hr; the antibacterial activity was estimated from bacterial counts made in the homogenized individual thighs. The blood concentrations of cephradine were 1.77 times higher in the probenecid-treated animals than in the controls. The potency ratio for doses was 2.41, the potency ratio for the areas under the drug concentration in blood vs. time curves was 1.34, and that for the peak blood concentrations was 1.43.

Animals↗
PubMed1985

Treatment of neutropenic infection: a randomized trial comparing latamoxef (moxalactam) with cephradine plus tobramycin.

Sixty neutropenic patients with infection were studied in a randomized trial comparing treatment with latamoxef (moxalactam) alone or with cephradine and tobramycin. The two treatment groups were comparable in respect to their clinical sites of infection, degree of neutropenia underlying malignancy, and organisms. Forty-two bacterial isolates were obtained from various clinically infected sites. All but two of these isolates were sensitive to latamoxef (30 highly sensitive, ten moderately sensitive). In contrast 29 of the isolates were resistant to cephradine and eight were resistant to both cephradine and tobramycin. Control of infection was achieved in 72% of patients treated with latamoxef and 55% treated with cephradine plus tobramycin. Latamoxef appears to be an effective antibiotic for the treatment of neutropenic patients with infection.

Adult↗
PubMed1989

Determination of serum and bone concentrations of cephradine and cefuroxime by HPLC in patients undergoing hip and knee joint replacement surgery.

Bone and serum concentrations of cephradine and cefuroxime were measured by HPLC in 21 patients undergoing hip and knee joint replacement surgery. An intravenous dose of 750 mg of each cephalosporin was given to patients at induction of anaesthesia. The serum and bone concentrations of both compounds were similar in individual patients although there was considerable interpatient variation. The mean concentrations in the femoral head bone supernatant in hip replacements were 7.2 mg/kg of cephradine and 8.0 mg/kg of cefuroxime. In knee replacement the femoral condyle bone concentrations were 5.1 mg/kg of cephradine and 4.2 mg/kg of cefuroxime, and for tibial bone 5.6 and 4.6 mg/kg respectively. Both cephradine and cefuroxime diffuse well into bone giving bone concentrations effective against common pathogens such as Staphylococcus aureus and S. epidermidis.

Adult↗
PubMed1981

Pharmacokinetics of cephradine given intravenously with and without probenecid.

1 In the light of questions raised by an earlier oral study (Welling, Dean, Selen, Kendall & Wise, 1979) the influence of probenecid on the pharmacokinetics of intravenously administered cephradine has been investigated. 2 Intravenous administration of cephradine resulted in a bi-exponential curve and the level of antibiotic after 15 min was significantly greater when subjects received probenecid than when they did not. The influence of probenecid on urinary excretion of cephradine was similar to that observed previously. 3 The increase in serum of cephradine due to probenecid could be accounted for by the decrease in the elimination rate of the antibiotic. These results are discussed in the light of other observations.

Adult↗
PubMed1977

Cephradine penetration into cerebrospinal fluid and effects of its administration into the cerebral ventricles of cats.

In cats that had high, sustained serum concentrations of cephradine, penetration of the drug into the cerebrospinal fluid (CSF) was poor. Serum cephradine levels were, on the average, 100-fold higher than the CSF levels. On the other hand, the direct injection of cephradine into the lateral cerebral ventricles of cats yielded high CSF cephradine concentrations without evidence of central nervous system toxicity.

Animals↗