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PubMed1977

Comparison of in vitro antibacterial activity of three oral cephalosporins: cefaclor, cephalexin, and cephradine.

Cefaclor, a new oral cephalosporin, was compared in vitro with cephalexin and cephradine against 233 organisms. Evaluations were performed in Mueller-Hinton and nutrient broth and agar using two inoculum sizes. In agar, cefaclor had greater antibacterial activity than either cephalexin or cephradine against isolates of Escherichia coli, Proteus mirabilis, Staphylococcus aureus, Klebsiella pneumoniae, and Salmonella typhi. All three drugs were relatively inactive against isolates of enterococci, Enterobacter species, and indole-positive Proteus. Cefaclor, however, did exhibit the greatest activity of the three antibiotics against these organisms. Although there was wide variability with respect to test parameters, the broth results generally paralleled the agar results. In nutrient broth a clear separation of the results with these three cephalosporins was seen with K. pneumoniae, E. coli, and S. typhi. Cefaclor was the most active, cephalexin had intermediate activity, and cephradine was the least active. From the data obtained in this in vitro study, it can be concluded that cefaclor, which has a substituted chloro group attached to the molecule, had increased antibacterial activity over cephalexin and cephradine. Comparative clinical trials with cefaclor will determine whether the differences outlined above are of clinical significance.

Cephalexin↗

PubMed1990

Comparative study of cephradine and amoxicillin-clavulanate in the treatment of recurrent urinary tract infections.

Eighty-eight female patients with a history of recurrent urinary tract infections were treated according to a randomization scheme with either 1 g of cephradine every 12 h (47 patients) or 375 mg of amoxicillin-clavulanate every 8 h (41 patients) for 7 days. The treatments were equally effective (cure rates of 89% for cephradine and 88% for amoxicillin-clavulanate) and showed similar relapse rates (cephradine, 14%; amoxicillin-clavulanate, 11%). Adverse effects were similar in both groups (cephradine, 23%; amoxicillin-clavulanate, 22%).

Amoxicillin↗

PubMed1984

Pharmacokinetics of oral cephradine in continuous ambulatory peritoneal dialysis patients.

Parenteral cephalosporins are widely used to treat peritonitis associated with continuous ambulatory peritoneal dialysis (CAPD). Few data exist on oral antibiotics in treating this disease. This study examined the pharmacokinetics of oral cephradine in noninfected patients on CAPD. Assays for cephradine in dialysate and urine were performed by high-performance liquid chromatography. Following a 500-mg dose, the peak dialysate cephradine concentration was 8.7 +/- 1.4 micrograms/ml. The peak urinary concentration was 201 +/- 119 micrograms/ml. The maximum peritoneal clearance was 4.3 +/- 0.3 ml/min/1.73 m2. Dialysate cephradine concentrations were inadequate against Staphylococcus epidermidis and most gram-negative bacteria found in CAPD-associated peritonitis, but may be adequate for most strains of other gram-positive organisms causing this disease.

Administration, Oral↗

PubMed1980

Tissue levels of cephradine in ischaemic limbs following a single intravenous injection.

A single dose of 2g cephradine was administered intravenously at the time of anaesthetic induction to 20 patients with occlusive arterial disease. Concentrations of cephradine were measured in serum, subcutaneous fat from the groins of 10 patients underdoing arterial reconstruction and in the subcutaneous fat and skeletal muscle of 10 legs amputated for severe arterial ischaemia. Concentrations of cephradine were adequate for antibacterial prophylaxis at the time of operation in all serum samples, 9 out of 10 samples of subcutaneous fat from reconstruction cases, all muscle and 8 of 10 fat samples from the level of section of amputated limbs, and in 8 of 10 muscle and fat samples from the distal parts of amputated limbs. These results confirm that a single intravenous dose of 2 g cephradine given with anaesthetic provides adequate serum and tissue concentrations for antibacterial prophylaxis during vascular surgery.

Aged↗

PubMed1981

The importance of cephradine in hip surgery.

Effective concentrations of antibiotic in the fluid bathing implanted hip prostheses are essential to prevent infection by micro-organisms. Twenty patients undergoing total hip replacement were given one gram of Cephradine intramuscularly one hour before operation and one other received a single bolus of Cephradine intravenously before operation and one other received a single bolus of Cephradine intravenously before operation. The concentrations of antibiotic were greater and persisted longer in the tissue fluid than in the blood. The antibiotic was sufficient to inhibit most micro-organisms causing contamination. We recommend that Cephradine is given intramuscularly one hour before operation and at six-hourly intervals after operation until the drainage tubes and intravenous lines have been removed.

Bacterial Infections↗

PubMedDate not supplied

Treatment of acute maxillary sinusitis. IV. Ampicillin, cephradine and erythromycinestolate with and without irrigation.

Six groups, each containing 50 patients with acute maxillary sinusitis, were treated with ampicillin plus nasal decongestant, ampicillin plus irrigation, cephradine plus nasal decongestant, cephradine plus irrigation, erythromycinestolate plus nasal decongestant, erythromycinestolate plus irrigation. The diagnosis was radiologically established and the healing likewise radiologically assessed on the fifth, tenth and fifteenth day. Treatment was given for 10 days. All groups demonstrated a similar radiological healing except cephradine plus nasal decongestant which was inferior to the others. Contrarily, side effects were least frequent in the cephradine groups and most frequent in patients cured with ampicillin. The difficulty in choosing the best treatment is discussed in relation to such factors as therapeutic results, side effects, long-term consequences of antibiotic treatment, establishment of any bacterial etiology and penetration characteristics of antibiotics into the diseased sinus.

Acute Disease↗

PubMed2000

[Prospective, randomized, comparative study of the efficacy, safety and cost of cefuroxime versus cephradine in acute pyelonephritis during pregnancy].

BACKGROUND: Second generation cephalosporins (CFPs) are more active in the treatment of acute pyelonephritis during pregnancy but their cost is considerably higher than their predecessors. Cefuroxime, a second generation CFP with oral and parenteral presentations, might offer significant advantages and become a first choice antimicrobial in this setting. AIM: To compare the efficacy, safety and cost of cefuroxime and cephradine in the treatment of acute pyelonephritis in pregnancy. PATIENTS AND METHODS: Hospitalized women with 12 to 34 weeks of pregnancy, with clinical and bacteriological diagnosis of acute pyelonephritis, were randomly assigned to receive cefuroxime (Curocef(r), Glaxo Wellcome) 750 mg t.i.d, i.v. or cephradine 1 g q.i.d., i.v. If the isolated organism was resistant to the assigned drug the patient was excluded. Once patients were afebrile, they were switched to an oral form of the same antimicrobial. They were discharged according to the clinical status and treated for a total of 14 days. laboratory tests, including urine culture were requested during controls and at the end of follow-up at 28 days. RESULTS: One hundred and one patients were randomized: 49 to receive cephradine and 52 to receive cefuroxime. Patients in the cefuroxime group hed fewer febrile days (mean 1.7 vs 2.2, p < 0.05), faster clinical recovery (mean 2.7 vs 3.1 days, p < 0.05), a higher rate of bacteriological cure at 28 days (78.8% and 59.2%, p < 0.05) and lower rate of failure (21.2% vs 40.8% p < 0.05). The rate of resistance of isolated uropathogens was 14% to cephradine and 1% to cefuroxime. CONCLUSIONS: Cefuroxime can be considered as a first choice option in the treatment of acute pyelonephritis during pregnancy due to its tolerance, microbiological activity and efficacy.

Acute Disease↗

PubMed1979

[Comparative study of cephalexin and cephradine distribution in the body of rats].

Distribution regularities of cephalexin and cephradine, 2 semisynthetic cephalospor in antibiotics for oral use were studied on rats. It was found that the cephalosporins had a capacity for satisfactory penetration through the histochematological barriers. The drugs were rather rapidly absorbed from the gastrointestinal tract of the rats into the blood. Their maximum blood levels were determined 1 hour after the administration. The highest cephalosporin concentrations were detected in the kidneys and liver. Still, the level of cephradine in the kidneys was lower and that in the liver was higher than the levels of cephalexin. The lowest concentrations were found in the skeletal muscles. The character of cephradine distribution in the lungs, heart and spleen differed from that of cephalexin; the maximum concentrations of cephradine in these organs were achieved 1 hour after its administration, while those of cephalexin were achieved in 30 minutes. The antibiotics were not detected in the brain tissue. No increase in the concentration gradient with time was observed.

Administration, Oral↗

PubMed1984

Comparison of bone levels after intramuscular administration of cephradine ('Velosef') or flucloxacillin/ampicillin in hip replacement.

Serum and bone levels of antibiotics were measured after the intramuscular injection of either 1 g cephradine or 500 mg flucloxacillin plus 500 mg ampicillin in 48 patients undergoing total hip replacement. The results showed that both regimens produced adequate blood levels, but that the levels after cephradine were higher and more prolonged. Bone levels of cephradine were significantly higher than for flucloxacillin or ampicillin. In half of the patients studied, flucloxacillin bone levels were below the limit of detection in both cancellous and cortical bone samples. In all 24 patients, cortical levels of cephradine were satisfactory for anti-staphylococcal activity although cancellous levels were unsatisfactory in 4 patients. The penetration of the antibiotics was greater into cortical bone than into cancellous bone.

Aged↗

PubMed1982

[A study of the disc sensitivity test for cephradine].

Susceptibilities of 189 strains of 28 bacterial species to cephradine were determined by the 2-fold agar dilution method in parallel with the diameter of inhibition zone by the single-disc method, under the experimental condition established by Kanazawa. The experiments demonstrated significant correlation between MIC by the dilution method and diameter of inhibition zone in each of conventional assay of the over-night (about 16 hours) incubation, delayed assay (about 24 hours incubation), and rapid assay (after 3-4 or 5-6 hours incubation), thus confirming applicability of the single-disc assay for cephradine. Analysis of the data obtained by using cephradine disc containing 30 micrograms revealed the primary regression equation to be: D (diameter, mm) = 28.5-11.2 log MIC (microgram/ml) in conventional assay, D = 35.1-14.6 log MIC (microgram/ml) in delayed assay, D = 18.0-5.41 log MIC (microgram/ml) in 3-4 hours rapid assay and D = 23.2-8.33 log MIC (microgram/ml) in 5-6 6 hours rapid assay, respectively. The range of variations in MICs estimated from the diameter of of inhibition zone by the disc test was then calculated in comparison with that in MIC determined by the 2-fold agar dilution assays, as reference for the experimental errors which may be involved in the estimation of MIC of cephradine by the single-disc assay.

Bacteria↗

PubMedDate not supplied

Evaluation of cephradine-chemoprophylaxis in Cesarean section.

The clinical efficacy of the prophylactic use of cephradine was evaluated prospectively in 118 women who underwent cesarean section. The patients of the cephradine group had a significantly lower (p less than 0.01) postoperative morbidity rate (17.79%) as compared with the control group (51.06%). The mean hospitalization time was also significantly shorter (p less than 0.01) in the cephradine group (7.2 +/- 0.13) than in the control group (10.9 +/- 0.23). Cephradine was proved to be an effective antimicrobial agent for chemoprophylaxis, due to its wide antimicrobial spectrum, beta-lactamase resistance, low percentage protein binding, large volume of distribution and non metabolic degradation.

Cephalosporins↗

PubMed1994

Noncompetitive inhibition of cephradine uptake by enalapril in rabbit intestinal brush-border membrane vesicles: an enalapril specific inhibitory binding site on the peptide carrier.

ACE inhibitors, as well as aminocephalosporins with peptide-like structures, are transported by the intestinal peptide carrier. We investigated the transport mechanism using intestinal brush-border membrane vesicles from rabbits and observed that enalapril, an angiotensin converting enzyme inhibitor and substrate of the peptide carrier, noncompetitively inhibited the uptake of cephradine, an aminocephalosporin and substrate of the peptide carrier, with an inhibition constant (Ki) of 2.6 mM when it was present on the cis side (outside) of the vesicles. By contrast, enalaprilat, cefadroxil and GlyPro competitively inhibited cephradine transport with Ki values of 5.4, 3.8 and 5.1, respectively. These results suggest the presence of an enalapril-specific inhibitory binding site on the peptide carrier. In addition, enalapril on the trans side (inside) of the vesicles inhibited the uptake of cephradine, suggesting an apparent reduction of carrier availability by a trapping mechanism. On the other hand, cefadroxil stimulated the uptake of cephradine in the trans experiment, consistent with the concept of countertransport. These findings reveal the uniqueness of enalapril regarding its mode of interaction with the peptide carrier(s) which has been of increasing interest regarding its role in the intestinal absorption of peptide-type drugs.

Animals↗

PubMed1981

Cephradine levels in human aqueous humor.

In an attempt to investigate penetration of cephradine into the primary aqueous humor in man, we administered 500-mg and 1-g doses of cephradine orally to 27 patients about to undergo elective cataract extraction. A mean peak aqueous humor level of 0.87 microgram/mL was obtained at about three hours after the 500-mg dose. The mean peak aqueous humor level after the 1-g dose also occurred at three hours and was 1.99 microgram/mL, with a range from 0.91 to 3.25 microgram/mL. This concentration was greater than the median minimum inhibitory concentration (MIC) of cephradine for Streptococcus pneumoniae, Str pyogenes, and Staphylococcus aureus (when tested in nutrient agar) but was greater than the MIC for 90% of isolates only with Str pyogenes.

Administration, Oral↗

PubMed1975

Sex differences in the intramuscular absorption and bioavailability of cephradine.

Six male and six female volunteers each received a single intramuscular injection of cephradine, a new cephalosporin antibiotic, once weekly for 3 consecutive weeks. The drug was injected into the gluteus maximus, vastus lateralis, or deltoid muscle groups. Injection sites were rotated each week so that each subject received an injection into each muscle. Pharmacokinetic evaluation of serum concentrations and urinary excretion data indicated a sex difference with respect to the rate and extent of cephradine absorption from the three injection sites. Smaller areas under the curve and absorption rate constants were observed for females after injection into each muscle group. The most striking difference was observed when cephradine was injected into the gluteus maximus muscle, where the exponential function describing the alpha phase was observed to be 1.16 +/- 0.17 hr(-1) for females and 2.70 +/- 0.34 hr(-1) for males. Total area under the mean serum concentration-time curves, mean time to peak, and peak height parameters consistent with the slower rate of absorption and lesser bioavailability in females were observed. These results show that the vastus lateralis or deltoid muscle groups are preferable to the gluteus maximus as injection sites because of the more rapid rates of drug absorption from those muscles.

Absorption↗

PubMed1976

Iodmetric and spectrophotometric assays for cephradine after its hydrolysis with a beta-lactamase.

Iodmetric and spectrophotometric methods were developed for the analysis of the new antibiotic cephradine. The procedures are modifications of known methods but are novel in employing a specific beta-lactamase for hydrolysis of the beta-lactam ring of the cephalosporin molecule. The iodometric method is rapid, precise, and accurate, but it requires fairly large amounts of cephradine. The spectrophotometric method, using differential UV absorption at 260 nm, is more rapid and more sensitive than the iodometric method but somewhat less accurate. Both methods proved useful for the routine assay of cephradine in certain formulations.

Alkalies↗

PubMed1987

Bone levels of cephradine and cefuroxime after intravenous administration in patients undergoing total hip replacement.

A randomised, comparative study is reported of single intravenous doses of cephradine 2 g or cefuroxime 1.5 g given as prophylactic cover for total hip replacements in 40 patients. The serum and bone levels of cephalosporin achieved were higher in the cephradine treated group in proportion to the higher dose employed. Both agents provided adequate bone levels on average, cephradine 25.34 mcg/g, cefuroxime 17.39 mcg/g, although bone penetration was more variable with cefuroxime.

Adult↗

PubMed1987

Recurrent urinary infections in women: clinical trial of cephradine as a prophylactic agent.

Cephradine 250 mg at night for 12 months was given as a prophylactic measure to 33 female patients of mean age 41.6 years, who had a history in the preceding 12 months of between three and 24 (median = 7) episodes of frequency and/or dysuria. When on such treatment the mean period between symptomatic attacks was 300 days, while before treatment attacks occurred at a mean frequency of 60.3 days. Thus, prophylactic cephradine increased the interval between attacks five-fold. In a total of 9002 patient-days of treatment, only five bacteriuric breakthrough infections occurred. 27% of the patients reported adverse effects "probably" or "possibly" related to treatment. Hence, cephradine appears to be as effective and better tolerated than macrocrystalline nitrofurantoin, presently the drug of choice for the prophylaxis of recurrent urinary infections.

Adult↗

PubMed1991

A randomized prospective study to compare ceftizoxime with cephradine as single dose prophylaxis in elective cholecystectomy.

This study compares the efficacy of ceftizoxime with that of cephradine as single agent prophylaxis in elective cholecystectomy. The incidence of purulent wound infection was low in both groups (ceftizoxime 1/99; cephradine 2/92). No adverse reactions to the trial antibiotics occurred in either group. Ceftizoxime is a safe, effective, convenient and well-tolerated antibiotic for use as single agent prophylaxis in elective cholecystectomy. However, because it has no demonstrable advantage over cephradine and is three times as expensive, its routine use is not justified.

Ceftizoxime↗