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PubMed1997

Spectrophotometric methods for the determination of cephradine or ceftazidine in human urine using batch and flow-injection procedures.

Sensitive and fast spectrophotometric methods for the determination of cephradine or ceftazidine in human urine, based on the formation of compounds between these drugs and Pd(II), are described. In the batch procedures the calibration graphs resulting from the measurement of the absorbance at 330 nm is linear over the range 5.0-60.0 micrograms. ml-1 for cephradine and 3.0-60.0 micrograms ml-1 for ceftazidine. The methods were successfully adapted to FI-systems, the peak heights being proportional to cephalosporin concentration over the range 5.0-60.0 micrograms ml-1 for cephradine and 3.0-60.0 micrograms ml-1 for ceftazidine. The sampling frequency was 60 h-1 with a sample injection of 72 microliters.

Ceftazidime↗

PubMed1993

Peptide carrier-mediated transport in intestinal brush border membrane vesicles of rats and rabbits: cephradine uptake and inhibition.

The uptake kinetics of cephradine, an amino-beta-lactam antibiotic, were studied in rat and rabbit intestinal brush border membrane vesicles preparations using both the Ca2+ and the Mg2+ methods of preparation, in the presence of an inward proton gradient. The Ca2+ method demonstrated greater uptake of cephradine in intestinal brush border vesicles prepared from both rat and rabbit and was used for these studies. The transport was observed to be of Michaelis-Menten carrier-mediated type with a passive transport component. The kinetic parameters obtained were as follows: for rat and rabbit, respectively, Km, 1.6 and 1.9 mM; Jmax', 1.7 and 20.7 nmol/mg/min; Pc' (= Jmax'/Km), 1.1 and 10.9 microL/mg/min; and Pm', 0.4 and 0.8 microL/mg/min. The kinetic parameters for the rat vesicles are consistent with those from our previous perfusion study using a conversion factor of 0.71 cm2/mg protein. The rabbit vesicles exhibited a similar Michaelis constant and a 10-fold larger maximal transport velocity, suggesting a quantitative advantage for the study of carrier-mediated transport in the rabbit compared to rat vesicles from the intestine. Cephradine uptake was inhibited by phenylpropionylproline, a proline derivative, and enalapril, an ACE inhibitor, which do not have an alpha-amino group, as well as dipeptides, tripeptides, and amino-beta-lactam antibiotics in both rat and rabbit vesicles. These results support the suggestion that they share the same peptide carrier pathway for oral absorption and that the vesicles may be a useful tool in developing orally effective peptide-type drugs.

Alkaline Phosphatase↗

PubMed1993

A comparative study of cephradine, amoxycillin and phenoxymethylpenicillin in the treatment of acute dentoalveolar infection.

A comparative double blind trial was undertaken of the efficacy of cephradine, amoxycillin and phenoxymethylpenicillin in the treatment of acute dentoalveolar abscesses. Patients were admitted to the trial with acute dentoalveolar abscesses with systemic involvement and assessments were made of pain, swelling, temperature and lymphadenopathy. After admission to the trial appropriate surgical therapy was undertaken. The patients were then given either phenoxymethylpenicillin 250 mg four times daily, cephradine 500 mg twice daily or amoxycillin 250 mg three times daily, all for 5 days. The patients were assessed after 2 days and 5 days. All the patients recovered with those taking cephradine showing the best recovery in the first two days of treatment.

Actinomyces↗

PubMed1992

A rapid first-derivative spectrophotometric analysis of cephalexin and cephradine in human urine.

A rapid, simple, and accurate first-derivative spectrophotometric method has been established for the determination of either cephalexin or cephradine in urine. Quantitative analysis of each antibiotic was achieved by measuring the peak amplitude at 268 nm. The relative and absolute recoveries ranged from 98.90 to 104.00% for cephalexin and from 97.85 to 105.10% for cephradine. The within-day coefficient of variation varied from 3.27 to 6.45%. The applicability of the method for the determination of the cumulative amount of either cephalexin or cephradine excreted unchanged in urine, following an oral dose containing 500 mg of the drug to a human male volunteer, is demonstrated.

Adult↗

PubMed1980

48-hour cephradine and post-prostatectomy bacteriuria.

In a randomised, controlled trial of intramuscular cephradine given in a dose of 1 g 6-hourly for 48 h, there was a significant reduction in the incidence of significant bacteriuria after transurethral resection. In contrast, the incidence of significant bacteriuria after open prostatectomy was unchanged. Post-operative complications were reduced in patients who received cephradine. The use of short-term cephradine would appear to be justified.

Aged↗

PubMed1988

Cephradine prophylaxis in transurethral procedures for carcinoma of the bladder.

The value of cephradine prophylaxis in reducing urinary infection was assessed in 243 patients undergoing endoscopy for bladder carcinoma. Patients were randomised either to receive 3 peri-operative doses of cephradine or to receive no antibiotic. Urine specimens taken on the fifth post-operative day showed a significantly lower urinary infection rate in those patients receiving cephradine prophylaxis.

Adult↗

PubMed1984

The transfer of cephradine across the placenta.

The transfer of maternally administered cephradine (1 g given intravenously) to the fetal circulation and amniotic fluid was investigated in 2 pregnant patients undergoing fetoscopy. Cephradine was detected in fetal serum between 23 and 72 minutes after injection and was present in therapeutic concentrations. Fetal serum levels appeared to peak at approximately 40-50 min. Amniotic fluid levels were rising during the sampling period of 97 min. Cephradine is transferred across the placenta and appears to be a suitable antibiotic for use in selected obstetric patients when penetration of the fetal compartment is desirable.

Amniotic Fluid↗

PubMed1996

Interactions of cephradine and cefaclor with the intestinal absorption of D-galactose.

Oral cephalosporins are frequently prescribed beta-lactam antibiotics. Although it has been well established that cephalosporins compete with dipeptides for absorption in the intestine, using the same transport mechanism, little is known about the action of the drugs on the absorption of other nutrients. In this work the effect of cephradine and cefaclor on the absorption of D-galactose has been studied. Intestinal sugar uptake was measured in-vitro in pieces of intestine (50 mg) and brush-border membrane vesicles, and in-vivo in intestinal loops. Galactose uptake was inhibited by cephalosporins in a dose-related, time-dependent manner. In-vivo the inhibition appeared when the antibiotics were on the luminal side of the enterocyte and when they reached the gut from the basolateral side. Only the active transport of the sugar was modified; passive transfer did not change in the presence of cephalosporins. In brush-border membrane vesicles, cephradine and cefaclor did not alter sugar uptake in either sodium or potassium gradients. Both antibiotics non-competitively inhibited basolateral Na+,K(+)-ATPase activity. These findings show that cephradine and cefaclor inhibit the active-transport component of galactose absorption because they reduce the activity of the basolateral Na+,K(+)-ATPase.

Animals↗

PubMed1978

Materno-fetal cephradine transfer in pregnancy.

Cephradine, a semisynthetic cephalosporin, has widespread use. There is, however, a paucity of data on the transfer of this antibiotic in pregnancy. Studies were undertaken after an intravenous dose of 2 g of cephradine was given in two elective situations: (i) therapeutic abortion in the first trimester and (ii) elective cesarean section in late pregnancy. Blood and tissue levels of cephradine obtained showed that the antibiotic is rapidly transferred to the feto-placental unit throughout pregnancy after intravenous administration to the mother.

Abortion, Therapeutic↗

PubMed1979

Pharmacokinetics of cephradine suspension infants and children.

The pharmacokinetics of cephradine suspension were studied in 16 infants and children who were 13 months to 8 years and 3 months of age (means age, 3.5 years). Mean peak concentrations of 21.3 and 9.9 mug/ml were achieved at 30 min after administration of 60-mg/kg doses to fasting and nonfasting patients. The area under the serum concentration-time curve was 26% larger in fasting than in fed subjects. The half-life of cephradine in serum was 0.8 and 1.0 h in fasting and fed groups, respectively. Antimicrobial activity was detected in 49% of all salivary samples; in 75% of specimens, the concentrations were less than the 50% minimum inhibitory concentration for most pneumococci and group A streptococci. Urinary concentrations of cephradine ranged from 28 to 8,760 mug/ml and were independent of feeding status.

Administration, Oral↗

PubMed1975

Clinical and laboratory evaluation of the effect of cephradine on patients with ear, nose and throat infections.

27 patients with ear, nose and throat infections have been treated with cephradine orally. Ten patients received 250 mg and 17 patients 500 mg every 6 h during 10 days. 26 patients were cured. One patient failed to respond to treatment but reinfection could not be excluded. Determination of plasma concentrations showed that cephradine was well absorbed. The drug showed no severe adverse effects. Cephradine is a good replacement in patients with allergy to penicillins. It is also suitable when broad-spectrum therapy is needed.

Administration, Oral↗

PubMed2002

Prolonged intestinal absorption of cephradine with chitosan-coated ethylcellulose microparticles in rats.

Cephradine-containing ethylcellulose microparticles (MPC) were prepared by the solvent evaporation method. Chitosan-coated MPC (Chi-MPC) were prepared by doping MPC with viscous chitosan solution and subsequently drying. When fluorescein isothiocyanate (FITC)-labeled chitosan-coated ethylcellulose microparticles without drug were administered intraduodenally, they moved slowly in the intestine, that is, most of them were retained at the upper and middle parts of the small intestine for more than 8 h, which is considered due to mucoadhesive properties of coated chitosan. When MPC and Chi-MPC was incubated at 37 degrees C in the JP 14 second fluid, pH 6.8, both released the drug slowly with similar release rates. Cephradine solution and suspension, MPC and Chi-MPC were administered intraduodenally to investigate intestinal drug absorption. Only Chi-MPC suppressed the initial plasma level and maintained the plasma concentration for a long time up to 24 h, suggesting Chi-MPC would be useful for prolonged intestinal absorption of cephradine.

Animals↗

PubMed1986

Cefadroxil. A review of its antibacterial, pharmacokinetic and therapeutic properties in comparison with cephalexin and cephradine.

Cefadroxil is an oral cephalosporin which is similar to cephalexin and cephradine in structure and spectrum of antibacterial activity, but has different pharmacokinetic properties. Not only does cefadroxil exhibit a longer serum half-life, and thus a prolonged duration of activity, but it is virtually unaffected by simultaneous food intake. The concentrations of cefadroxil attained in body tissues and fluids are also higher and more sustained than those of cephalexin and cephradine. These characteristics permit the administration of cefadroxil during meals on a once-daily or twice-daily basis, thus encouraging patient compliance which often determines the successful management of out-patient infections. Many studies have established the efficacy of the administration of once- or twice-daily cefadroxil, compared with regimens of cephalexin or cephradine given 4 times daily, in the management of infections in the respiratory tract, urinary tract, skin and soft tissues, and bones and joints.

Cefadroxil↗

PubMed1976

[Application of parenteral cephradine in urinary tract infections (author's transl)].

A new antibiotic cephradine was administered intravenously for 3 approximately 7 days at daily doses of 1.0 approximately 2.0 g to 56 patients, including 39 cases of acute urinary tract infections, 13 of chronic urinary tract infections and 4 for postoperative prophylaxis. Of 39 cases with acute urinary infections, definite response was seen in 35 cases and no definite response in 4 cases. Of 13 cases with chronic urinary tract infections, definite response was seen in 7 cases and no definite response in 6 cases. Good results were obtained clinically in 4 cases for prophylaxis of postoperative infections. No side effect was observed with cephradine with cephradine throughout the experiment.

Acute Disease↗

PubMedDate not supplied

Intraperitoneal ciprofloxacin and rifampicin versus cephradine as initial treatment of (C)APD-related peritonitis: a prospective randomized multicenter comparison (CIPPER trial).

OBJECTIVE: The initial treatment of peritonitis has evolved from single-agent to combination regimens. The initial response rates improved with these newer regimens but relapsing peritonitis continues to occur. For biofilm-embedded or intracellularly sequestrated bacteria, a combination of intracellularly- and biofilm-active agents such as ciprofloxacin and rifampicin might be beneficial. Many Dutch centers continue to use cephradine as initial treatment, claiming clinically adequate responses with this regimen. We compared the impact of these two regimens on outcome in patients who developed a new episode of peritonitis. DESIGN: Prospective randomized open trial. SETTING: Multicenter study including 14 Dutch dialysis units. PATIENTS AND INTERVENTIONS: From October 1996 to October 1999, 367 patients from 14 centers were randomized to be treated with ciprofloxacin + rifampicin (CR; each 50 mg/L) or cephradine (C; 250 mg/L) in case of peritonitis. Of these 367 patients, 98 developed peritonitis, 44 of whom were treated with CR and 54 with C. MAIN OUTCOME MEASURES: Clinical response, divided into early (during the 2 weeks of therapy) and late (including the following 4 weeks) response. Success was defined as disappearance of all signs and symptoms by days 4-6, through day 42. Bacteriological response was either success (eradication) or failure (persistence, superinfection, or eradication with relapse/reinfection). RESULTS: The groups were comparable for age, sex, duration of continuous ambulatory/automated peritoneal dialysis, and occurrence of diabetes. Bacteriological cultures in both groups revealed predominantly gram-positive micro-organisms. Initial and late clinical successes were obtained in 27/54 and 20/54 episodes (50% and 37%) in the C group, and 33/44 and 28/44 episodes (75% and 63.6%) in the CR group (p = 0.021 and p = 0.019). Bacteriological success occurred in 29.6% in the C group, and in 59.1% in the CR group (p= 0.026), with failure in 46.3% and 18.2%, respectively. Peritonitis episodes were bacteriologically not evaluable in 24.1% of episodes in the C group and 22.7% of episodes in the CR group, due mostly to no growth in the initial culture. CONCLUSION: The CIPPER Trial showed ciprofloxacin + rifampicin to be superior to cephradine as empiric treatment of peritonitis.

Anti-Infective Agents↗

PubMed1998

[Enzymatic synthesis of cephradine].

Cephradine was synthesized by gamma-alumina-immobilized form of the penicillin G acylase of Bacillus megaterium with D-phenyglycine methylester hydrochloride (CH DGME.HCl) as acyl donor and 7-aminodeacetoxycephalosporanic acid (7-ADCA) as acyl acceptor. 0.1 g of 7-ADCA was dissolved by adding 2.5 ml of distilled water and about 0.25 ml of 2 mol/L NaOH in a 25 ml flask. To the solution, after 0.25 g of CHDGME.HCl was added, 0.1 mol/L phosphate-0.05 mol/L citric acid buffer, pH 7.5 was added to result in a volume of 5 ml with pH 7.5 Then 1 g(220 IU) of immobilized enzyme was added. The flask was shaken on a rotary shaker at 110 r/min and 25 degrees C for 5 h. The conversion rate of 7-ADCA was 81%. In an expanded experiment in 500 ml of reactive volume, 11.8 g of cephradine was obtained from 10 g of 7-ADCA. The conversion rate of 7-ADCA was 80% with about 87% yield of cephradine. Enzymatic synthesis was inhibited in varying degrees by phenylacetic acid, phenoxyacetic acid and cephalosporin G.

Bacillus megaterium↗

PubMed1989

Controlled trial of cephradine versus cefuroxime in vascular surgery.

Two hundred and three consecutive patients undergoing acute or elective vascular reconstructions (N = 162) or amputations (N = 41) were randomized to receive either a single dose of cephradine 2 g intravenously or cefuroxime 1.5 g intravenously at induction of anaesthesia. Infective morbidity in both groups was assessed post-operatively as was therapeutic antibiotic prescribing. No significant differences in septic complications were found between patients receiving cefuroxime or cephradine. In addition, tissue penetration of each antibiotic was assessed by assay of serum and tissue specimens. Serum levels of cefuroxime were significantly less than cephradine 10 min after injection (median concentrations 115 micrograms/ml versus 182 micrograms/ml, p less than 0.01 Wilcoxon), but there were no differences in tissue penetration.

Amputation, Surgical↗

PubMed1978

Biophotometric investigations on the influence of cephradine and related cephalosporins on the growth of beta-lactamase-producing staphylococi.

Biophotometric growth studies were conducted with clinical isolates of beta-lactamase-producing staphylococi in the presence and absence of cephradine, cephalexin, cefazolin and cephacetrile. Of the four antibiotics, cephradine was the most effective in prolonging the suppression of bacterial growth resulting from antibiotic action while cefazolin was the least effective. Cephalexin and cephacetrile were intermediate in effect. The superiority of cephradine over cephalexin was shown to be related to the more rapid destruction of cephalexin by beta-lactamase. On comparing the results of these studies with clinical experience it was concluded that biophotometric studies have clinical relevance and consequently should be used for evaluating the efficacy of beta-lactam antibiotics against pathogenic staphylococi.

Cephalosporinase↗