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PubMed1979

The pharmacokinetics of the oral cephalosporins cefaclor, cephradine and cephalexin.

The pharmacokinetics of the oral cephalosporins cefaclor, cephradine, and cephalexin were examined following single 500 mg oral doses to fasted, healthy volunteers. Absorption of the three compounds was rapid following a brief lag period and peak serum levels were obtained in 1-1.5 hours. Serum levels of cefaclor tended to be lower than those of cephradine and cephalexin during the 2-5 hour postdosing period and cefaclor was eliminated more rapidly than other cephalosporins from serum. No difference was observed in the overall bioavailability of the three antibiotics based on comparable FD/V values. Urine levels of the three cephalosporins greatly exceeded the minimum inhibitory concentrations of susceptible organisms during 0-6 hours postdosing, but were considerably reduced during the 6-12 hour collection period. Total urinary recovery of antibiotic activity accounted for almost 90 percent of dosed cephradine and cephalexin compared to 55 percent of dosed cefaclor. Lower serum levels and reduced urinary recovery of intact cefaclor are probably due primarily to its chemical instability. The reduced levels of cefaclor may be compensated for therapeutically by its greater in vitro antibacterial activity.

Adolescent↗
PubMed1983

The effect of cephradine prophylaxis on wound infection after arterial surgery through a groin incision.

Cephradine administered prophylactically to a group of 35 patients undergoing reversed saphenous vein femoro-popliteal bypass, iliofemoral endarterectomy or profundaplasty through a groin incision, resulted in a significant reduction in the incidence of wound infection (P = 0.025; exact probability test). One gram of cephradine was given at induction of anaesthesia, followed by three postoperative doses of one gram at 6 hourly intervals. The overall wound infection rate at 7 days, as assessed by frank purulent discharge, was 15%. After cephradine prophylaxis, no infections were noted as judged on this basis, but erythema of the suture line was seen in equal numbers (40% of each group). Where the indication for operative intervention was rest pain or gangrene, the incidence of wound infection was very much increased, 80% of the infected cases being from this group.

Aged↗
PubMed1980

A lower dose regimen for cephradine capsules in the treatment of urinary tract infections.

In this double-blind, randomized, multicenter trial, an oral dosing regimen of 500 mg twice daily (BID) of cephradine was evaluated for the treatment of acute uncomplicated urinary tract infections due to susceptible pathogens. This dose was compared to the already established cephradine regimen of 1,000 mg BID. Of the 218 cases entered into the study, 130 were evaluable for efficacy, 64 in the 500-mg BID group and 66 in the 1,000-mg BID group. There was no statistically significant difference between the two dosage regimens regarding rapidity of clinical improvement, eradication of the pathogens, and overall therapeutic outcome. Successful responses were obtained in 89.1% of the 500-mg BID cases and in 87.9% of the 1,000-mg BID cases. These results demonstrate the safety and efficacy of a 500-mg BID dosing regimen of cephradine for this use. This regimen offers the advantages of convenience, potentially improved compliance, and cost economy.

Adolescent↗
PubMed1980

Five-day therapy with cephradine capsules, 500 mg BID, for the treatment of acute, uncomplicated urinary tract infections.

This double-blind, randomized multi-center study compared the efficacy and safety of a five-day treatment regimen with that of a ten-day treatment regimen for acute, uncomplicated urinary tract infections. All patients received cephradine capsules, 500 mg BID. Efficacy was evaluated in 71 patients (38 with five days of treatment; 33 with ten days of treatment). All but one patient in each group had a rapid resolution of symptoms. At the completion of treatment, cephradine eradicated the causative pathogen in 97.4% and 96.9% of patients in the two groups, respectively. One week after therapy, 86.8% of patients in the five-day treatment group and 84.8% of those in the ten-day treatment group maintained both complete resolution of symptoms and bacterial eradication. The incidence of side effects was equally low in the two groups. Thus a five-day regimen of cephradine, 500 mg BID, offers the potential advantages of cost-efficiency and improved patient compliance, while maintaining clinical efficacy in treating acute, uncomplicated urinary tract infections.

Acute Disease↗
PubMed1979

Cephradine-induced interstitial nephritis.

A patient developed acute interstitial nephritis following cephradine administration. The clinical illness preceding the interstitial nephritis and the eosinophilia in peripheral blood suggested an allergic reaction. Immunological studies demonstrated an allergy to cephradine and penicillins which was IgG2-mediated. It is probable, therefore, that allergy to cephradine caused the renal lesion from which there was full clinical and biochemical recovery.

Adult↗
PubMed1977

The penetration characteristics of cefazolin, cephalothin, and cephradine into bone in patients undergoing total hip replacement.

Preoperatively, to prevent infection, seventy-one patients who were to have total hip arthroplasty were given one gram of cephalothin, cephradine, or cefazolin intravenously. Simultaneous samples of bone and serum were obtained after various time intervals and assayed for cephalosporin concentration to correlate the antibiotic concentrations in these sites with time. Of the cephalosporins tested, cefazolin achieved the highest total peak levels in bone (thirty micrograms per gram), followed in descending order by cephradine (twenty-three micrograms per gram) and cephalothin (2.8 micrograms per gram). These peak levels in bone, reached twenty-five to forty minutes after injection, were sixty, 6.7, and fifteen times higher than the usual mean minimum inhibitory concentrations of cefazolin, cephradine, and cephalothin, respectively, for penicillin-resistant staphylococci. The half-lives of the antibiotics in bone were forty-two, forty, and thirty minutes, respectively.

Aged↗
PubMedDate not supplied

Simultaneous liquid chromatographic analysis of the beta-lactam antibiotics cefazolin, cefadroxil, cephalexin, ampicillin, and cephradine in solution.

A liquid chromatographic method was developed for the determination of nanogram quantities of 5 broad-spectrum structurally related beta-lactam antibiotics (cefazolin, cefadroxil, cephalexin, cephradine, and ampicillin) in solution. The method uses a C18 reversed-phase column, UV absorption (240 nm) detection, and an aqueous mobile phase containing isopropyl alcohol and acetic acid. Relative resolution between the antibiotic peaks ranged from 1.7 to 5.9 for all peaks. Chromatographic retention times were 2.97, 3.92, 4.57, 5.37, and 6.56 min for cefazolin, cefadroxil, cephalexin, ampicillin, and cephradine, respectively. Accuracy, precision, linearity, and long term analytical reproducibility were determined by statistical analysis. Use of the proposed method to evaluate the degradation of cephradine solutions stored at room temperature illustrated its potential as a stability-indicating assay.

Anti-Bacterial Agents↗
PubMed1979

Wound sepsis following gastrointestinal surgery: a comparison of topical and two-dose systemic cephradine.

A prospective study of the effect of the route of administration of prophylactic antibiotic on the wound infection rate following gastrointestinal surgery was performed. Patients were randomly allocated to one of three groups: group 1 received no form of antibiotic prophylaxis; group 2 received 1 g of cephradine applied topically to the wound at closure; group 3 received 1 g of cephradine intravenously at induction of anaesthesia and a further intravenous dose of 500 mg 4 h later. Wound infections occurred in 12 of 83 patients in the control group (14.5 per cent), in 6 of the 83 patients in the group who received topical antibiotic (7.2 per cent) and in 3 of the 82 patients who received systemic antibiotics (3.6 per cent). Only the group who received systemic antibiotic showed a statistically significant reduction in the incidence of wound infections compared with the control group (P = 0.03).

Administration, Topical↗
PubMed1978

Quantitative determination of cephalexin in cephradine by NMR spectroscopy.

An NMR method to determine quantitatively the presence of cephalexin in cephradine was developed. The method is applicable to the chemical itself as well as to capsules and oral suspension formulations. The determination is based on the NMR signal arising from the five aromatic protons of the cephalexin molecule. Integration of this signal relative to a signal from cephradine provides the data necessary to determine the percentage of cephalexin present. The precision at the 2% cephalexin levels is +/- 0.18%. The time required to carry out a single analysis is about 10 min, and five analyses can be done in about 0.5 hr.

Capsules↗
PubMed1978

Cefazolin and cephradine: relationship between serum concentrations and tissue contents in mice.

The relationship between serum concentrations and tissue levels of various doses of cefazolin and cephradine was determined in experimentally infected mice. An infection was induced by injection of 5 X 10(6) Escherichia coli into the right hind leg, antibiotics were administered 1 h later. At 15-minute intervals mice were killed by exsanguination after a blood sample was taken, and the infected thigh was taken out and homogenized. The total amount of antibiotic per gram thigh muscle tissue was calculated on the basis of the concentration in the supernatant of the homogenate. From the parallel course between blood concentrations and total tissue contents it may be concluded that the thigh was easily accessible for both cephalosporins. The ratio between the total tissue content and the free serum concentrations was the same for both antibiotics despite the difference in protein binding between cefazolin and cephradine in mouse serum. This implies that the discrepancy between the relative antibacterial activity of the cephalosporins in vitro and in vivo found in earlier experiments cannot be explained by differences in accessibility of the tissue.

Animals↗
PubMed2006

Crystal form of cephradine.

Four crystal forms of cephradine were isolated by recrystallization and characterized by powder X-ray diffractometry, differential scanning calorimetry, and thermogravimetric analysis. The dissolution patterns of four crystal forms of cephradine were studied in water at 37 +/- 0.5 degrees C, 90 rpm for 120 min. The amount dissolved at 120 min was highest for Form I (100%), followed by Form 3 (98.9%), Form 4 (77.83%), and Form 2 (75.55%). After storage for two months at 0% RH (silica gel, 20 degrees C), 52% RH (saturated solution of Na2Cr2O7 x 2H2O/ 20 degrees C), and 95% RH (saturated solution of Na2HPO4/20 degrees C), none of the crystal forms showed transformation.

Anti-Bacterial Agents↗
PubMed1988

Short-term cephradine prophylaxis in elective transurethral prostatectomy.

A prospective randomized trial was conducted to assess the value of short-term antibiotic prophylaxis in elective transurethral resection of the prostate. Two hundred patients were randomized to receive 1.5g cephradine intramuscularly preoperatively and 1g cephradine orally before removal of the urethral catheter or to receive no antibiotic prophylaxis. Fifty-eight patients were excluded because of occult neoplasm or protocol violation. There was no difference in time to removal of catheter, incidence of pyrexial episodes, length of hospital stay or minor complication rate between the two groups. We conclude that a short-term antibiotic regime is of no value in the elective patient with sterile urine.

Cephalosporins↗
PubMed1989

Cephradine penetration of mandibular bone.

The concentration of cephradine in serum and mandibular bone was assayed in 22 patients undergoing third molar surgery following a single 1-g intramuscular injection. Serum and cortical bone samples taken simultaneously contained mean cephradine concentrations of 12.41 micrograms/mL and 1.25 micrograms/g, respectively. These results, when compared with those reported for other bony sites, including femoral head and knee, show a reduced bone penetration with a bone-to-serum ratio of approximately 0.10:1.

Adult↗
PubMed2000

Determination of the cephalosporin antibiotic cephradine in human plasma by high-performance liquid chromatography with ultraviolet detection.

A simple and sensitive high-performance liquid chromatographic method, for the determination of cephradine in human plasma samples has been developed and validated. Cephradine and cephaloridine (internal standard) were extracted from human plasma by perchloric acid protein precipitation followed by centrifugation. Aliquots of the extracts were analysed by reversed-phase high-performance liquid chromatography (HPLC) utilising a polymeric reversed-phase PLRP-S column, followed by ultraviolet detection at 260 nm. The method has a working dynamic range from 0.2 to 30.0 microg/ml from 200 microl human plasma. The precision of the method at 0.2 microg/ml was 4.9% (intra-assay) and negligible (inter-assay) as calculated by one-way analysis of variance and the accuracy of the method at 0.2 microg/ml was -4.1% in terms of percentage bias. This method has been successfully applied to clinical studies including an oral bioequivalence study comparing the pharmacokinetics of 500 mg tablets of Kefdrin with 500 mg tablets of Velosef in healthy human volunteers.

Calibration↗
PubMed1990

Cephradine (Velosef) penetration of mandibular bone.

The concentration of cephradine in serum and mandibular bone was assayed in 28 patients undergoing 3rd molar surgery following a single 1 g intravenous injection. Serum and cortical bone samples taken simultaneously, contained mean cephradine concentrations of 42.11 micrograms/ml and 2.61 micrograms/g respectively. These results, when compared with those reported for other bony sites including the femoral head and knee, show a reduced bone penetration with a bone-to-serum ratio of approximately 0.06:1.

Adult↗
PubMed1979

In vitro combination of mecillinam with cephradine or amoxycillin for organisms resistant to single agents.

Of 36 multi-resistant Gram-negative bacilli isolated from different cases of urinary tract infection, 18 strains of Escherichia coli, klebsiella, enterobacter, proteus, providencia and serratia with the exception of Acinetobacter species showed synergy when mecillinam was combined with cephradine or amoxycillin in the ratio of 1:1. Combination with cephradine was synergistic on sixteen occasions and amoxycillin on six. Synergy, which might have clinical relevance, was demonstrated only when the test organism was either fully or moderately sensitive to one of the two antibiotics combined but not when resistant to both.

Amdinocillin↗
PubMed1976

Serum and lung tissue levels of cephradine in thoracic surgery.

Serum and lung tissue levels in fifteen patients who underwent thoracic surgery were determined by the agar-diffusion plate method after i.m. administration of cephradine (500 mg). The mean value of the serum level 30 to 120 min after administration was 6.5 mug/ml, the mean lung tissue level was 2.6 mug/g. The lung tissue levels reached 40% of the simultaneous serum level. Four patients received cephradine for the treatment of post-operative chest infections. This antibiotic has an important therapeutic role in cases of thoracic-surgical infections.

Adult↗