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At least 19 recordsLinked to original sources

PubMed1977

[Cephradine in open heart serugery. Concentrations of cephradine in pericardial exudate and serum after cardiac surgery (author's transl)].

The diffusion of cephradine into the pericardial exudate was measured in 19 patients undergoing heart surgery. Every patient received 2 grams of cephradine (=30 mg/kg) during a 20 minute infusion period, before, during, and after the operation, and than at intervals of 6 hours, together 8 grams per day. The highest mean serum level, 10 minutes after the end of the first injection was 150 microgram/ml and after repeated dosages 102.5 microgram/ml, and at the end of the infusion interval 3.2 microgram/ml in the mean. At the time of opening the pericardium the concentration of the substance in the pericardial exudate, 15, 30, 45 and 60 minutes after finishing the first injection, varied from 4.1 to 38.6 microgram/ml in the average. The postoperative maximum levels were higher than 50 microgram/ml and 6 hours after the respective administrations the levels varied between 12.83 and 15.77 microgram/ml in each case. These high concentrations of cephradine in the pericardial exudate could not be attributed to seepage of blood into the pericardium.-At specific "check points" bacteriological materials were taken. Out of 1168 specimens only 6.7% were bacteriological positive. Drains in wounds, the pleura or the pericardium were sterile in most cases. Intravenous catheters were contaminated only in 1%. However the contamination rate rises with period of storage. The results show that cephradine exhibits good diffusion into the exudate of pericardium. With the chosen dosage the concentrations of the antibiotic in the pericardial exudate are higher than the MIC values of most pathogen bacteria.

Bacterial Infections↗

PubMed1976

[The liver concentration of cephradin and cephacetril and their elimination in the bile].

Liver biopsies and serum samples were collected after intravenous application of 2 g cephradin (n = 13) or 2 g cephacetril (n = 11) during surgery. There was no difference in the serum levels of cephradin and cephacetril. 30 min. after i.v. application of cephradin the liver tissue concentration was 72.62 mcg/g. 30 min. after i.v. cephacetril the liver tissue concentration was 5.83 mcg/g. The quotient of liver tissue concentration to serum concentration for cephradin was between 0.36 and 0.83, and for cephacetril between 0.02 and 0.16. The excretion of cephradin and cephacetril in human bile was studied by collecting bile samples from the common bile duct via T-tube drainage (n = 17). Cholecystomized patients were given 2 g of antibiotics intravenously. Serum levels of cephradin were 263 mcg/ml 5 min after application, and 22 mcg/ml after 240 min. Serum levels of cephradin were 263 mcg/ml 5 min after application, and 22 mcg/ml after 240 min. Serum levels of cephacetril were 193 mcg/ml 5 min after application, and 27 mcg/ml after 240 min. The highest levels of cephradin in the bile were found 75 min after injection at a concentration of 86.4 mcg/ml; the highest level for cephacetril was 21.8 mcg/ml at 15 min. In patients with hyperbilirubinaemia cephradin reached a mean maximum concentration of 29.6 mcg/ml in bile samples, in comparison to 117.4 mcg/ml in normal patients, while no difference was seen with cephacetril. After intravenous administration of 2 g cephradin biliary concentration are achieved which may be sufficiently high to be effective not only against the very sensitive gram-positive organisms, but also against most strains of E. coli, Klebsiella and indol-negative Proteus. Cephradin is effective in the treatment of cholangitis and intrahepatic abscesses, as was observed in 18 patients. A free bile-flow is essential.

Bile↗

PubMed1990

Pharmacokinetics of cephradine administered intravenously and orally to young and elderly subjects.

The pharmacokinetics of IV and oral cephradine in healthy young male and female volunteers (ages 19 to 25, n = 10) were compared to those of older individuals (ages 65 to 81, n = 9). Subjects received 1 gram of cephradine by a 5-minute intravenous (IV) infusion followed the next day by a 1-gram oral dose. Serial serum and urine samples collected over a period of 12 hours after the dose were analyzed for cephradine concentration by a microbiologic assay. After IV administration, mean serum cephradine concentrations in the elderly group were significantly higher at both 6 hours (1.52 +/- 0.41 mcg/mL) and 8 hours (0.73 +/- 0.22 mcg/mL) than in the young group at 6 hours (0.43 +/- 0.11 mcg/mL). Total systemic clearance was significantly lower (2.64 +/- 0.34 vs. 4.81 +/- 0.59 ml/min/kg) and the elimination half-life was significantly longer (1.71 +/- 0.20 vs 1.12 +/- 0.13 hours) in the elderly group (P = .0001). Systemic cephradine clearance correlated positively with creatinine clearance (r2 = 0.34, P = .0110) and negatively with age (r2 = 0.79, P = .0052). The mean volume of distribution was not significantly different between the two groups. Mean renal clearance was significantly lower in the elderly group (P = .0001), but more than 80% of the dose was excreted in the urine within 6 hours in both groups. After oral administration, the mean peak concentration and time to peak concentration did not differ between groups. The relative oral bioavailability was approximately 94% in both groups. The mean serum concentrations in the elderly were higher at both 6 and 8 hours than in the young group at 6 hours. There were no differences in pharmacokinetic parameters between male and female subjects. Because of reduced cephradine clearance secondary to an age-related decline in renal function, administration of cephradine every 8 hours, rather than every 6 hours, may be sufficient in elderly patients.

Administration, Oral↗

PubMed1985

CAPD peritonitis: a prospective randomized trial of oral versus intraperitoneal treatment with cephradine.

In a prospective randomized clinical trial 84 peritonitis episodes were treated with cephradine, either orally or intraperitoneally. No difference in treatment outcome between both groups could be demonstrated. In episodes caused by susceptible micro-organisms a good response was seen in 82% in the oral and 82% in the intraperitoneal groups. These clinical findings were supported by the demonstration of adequate cephradine concentrations in serum and dialysate after oral as well as after intraperitoneal administration. Altogether cephradine was given orally or intraperitoneally in 88 episodes of peritonitis as drug of first choice. In 52 a complete cure was obtained, in 36 another antibiotic was subsequently needed as soon as bacterial susceptibility was known. No patient deteriorated appreciably during the delay between the start of cephradine and the switch to another antibiotic. Of the 36 episodes 14, caused by methicillin-resistant Staphylococcus epidermidis, responded well initially to cephradine but relapsed later. Change to another antibiotic effected a complete recovery in all 14 cases. Of the remaining 22 episodes, 14 were cured by the other antibiotic, in eight the catheter had to be removed. Aminoglycosides could be avoided except for ten of the episodes. During peritonitis CAPD was continued, in 71% of the cases on an outpatient basis. Mortality due to peritonitis was absent. We conclude that oral cephradine can be used as drug of first choice in the initial treatment of CAPD peritonitis, because a good initial response was obtained in 66 (52 + 14) i.e. 75% of 88 episodes. However, complete cure by cephradine alone was achieved in only 60%.(ABSTRACT TRUNCATED AT 250 WORDS)

Administration, Oral↗

PubMedDate not supplied

Cephradine in the treatment of infective endocarditis.

Ten patients with a mean age of 34.1 years with infective endocarditis (55% of cases due to Staphylococcus aureus) were treated with cephradine. The peak serum levels of cephradine (8-42 microgram/ml) were 3- to 17-fold higher than the minimum inhibitory concentrations of cephradine against pathogenic strains of S aureus (1.2-4 microgram/ml). Patients treated with cephradine became afebrile in 2 to 13 days of therapy, and their white blood cell count returned to a normal level in 3 to 30 days. Cephradine therapy was well tolerated without any incidence of phlebitis. The drug could be administered by three different routes. Cephradine is a useful cephalosporin for treatment of nonenterococcal gram-positive endocarditis in young heroin addicts.

Adult↗

PubMed1988

Cost-benefit analysis of cephradine and mezlocillin prophylaxis for abdominal and vaginal hysterectomy.

Four hundred patients (300 abdominal and 100 vaginal hysterectomies) were randomized to receive a single, pre-operative intravenous injection of saline (placebo), 2 g cephradine or 5 g mezlocillin. The frequency of wound and pelvic infections was significantly reduced (P less than 0.05, chi 2- or Fisher's exact test) in the abdominal hysterectomy patients who received cephradine (16% vs 23% mezlocillin, 29% placebo) and in the vaginal hysterectomy patients who received cephradine or mezlocillin (0% mezlocillin, 6% cephradine vs 27% placebo). These results are similar to those of previous studies and suggest that prophylaxis is more effective for vaginal than for abdominal hysterectomy. However, a cost-benefit analysis supported the opposite conclusion. Cephradine prophylaxis for abdominal hysterectomy resulted in cost savings to the hospital and the community health services with measurable benefits to the patient. In contrast, cephradine or mezlocillin prophylaxis for vaginal hysterectomy resulted in increased costs to the hospital, no savings to community services and no significant benefit to the patient. We conclude that cost-benefit analysis provided valuable additional information to the conventional, statistical analysis of wound or pelvic infection rates.

Adult↗

PubMed1987

Comparison of the pharmacokinetics of cephradine and cefazolin in pregnant and non-pregnant women.

The pharmacokinetics of cephradine, a cephalosporin with a low degree of protein binding, was studied in 12 women after oral and intravenous administration of the drug during and after pregnancy. Six of the 12 women also received a cephalosporin with a high degree of protein binding, cefazolin, intravenously during and after pregnancy. For both drugs most pharmacokinetic parameters were altered in pregnancy. The area under the plasma concentration-time curve (AUC) following intravenous administration was smaller for both drugs during as compared to after pregnancy (mean change 39% for cephradine and 31% for cefazolin). Half-lives of both drugs were significantly shorter during compared with after pregnancy (mean change 26% for cephradine and 35% for cefazolin). Consequently, total body clearance was increased during pregnancy. A significant negative correlation between length of gestation and total clearance per kg bodyweight was seen for cephradine. The bioavailability of oral cephradine did not differ significantly during compared with after pregnancy. It is concluded that the dosage of both cefazolin and cephradine should be increased when treating infections in pregnant women in order to obtain the same antibacterial effect as when treating non-pregnant women.

Absorption↗

PubMed1988

H+ coupled transport of p.o. cephalosporins via dipeptide carriers in rabbit intestinal brush-border membranes: difference of transport characteristics between cefixime and cephradine.

We demonstrated previously that aminocephalosporins, such as cephradine, possessing a alpha-amino group and a carboxyl group, are transported via H+/dipeptide carrier system in the intestinal brush-border membranes. The present study examined the transport characteristics of cefixime, a new p.o. cephalosporin with two carboxyl groups, by the rabbit intestinal brush-border membrane vesicles in comparison with those of cephradine. With an intravesicular pH of 7.5, apparent optimum extravesicular pH was 6.0 for cephradine uptake and more acidic (pH 4.5-5.0) for cefixime uptake. An inward H+ gradient [( pH]i = 7.5, [pH]o = 5.0) induced overshoot uptake of cefixime, and this uptake was reduced in the presence of carbonyl cyanide p-trifluoromethoxyphenylhydrazone, a protonophore. Cefixime uptake at pH 5.0 was trans-stimulated (countertransport effect) and cis-inhibited by dipeptides and aminocephalosporins but not at pH 7.5. Cephradine uptake at pH 7.5 was stimulated by the countertransport effect of dipeptide but not by cefixime. Cefixime and cephradine uptake at pH 5.0 was greatly inhibited by 4,4'-diisothiocyano-2,2'-disulfonic stilbene. These findings indicate that cefixime is transported by an inward H+ gradient via dipeptide carrier only in an acidic pH region, whereas cephradine is transported via dipeptide carrier in both neutral and acidic pH regions, suggesting the existence of multiple transport systems for dipeptides; a neutral pH preferring system (Type I) and an acidic pH preferring system (Type II).

4,4'-Diisothiocyanostilbene-2,2'-Disulfonic Acid↗

PubMed1975

[The plasma-protein-binding of Clindamycin Cephazolin and Cephradin in neonates and adults (author's transl)].

In pooled serum of 12 healthy adults and 12 neonates (blood taken from the umbilical cord) the free and protein-bound parts of Cephazolin, Cephradin and Clindamycin were tested by equilibrium dialysis in relation to the concentration of the antibiotic. In the serum of adults at a concentration of 36 mcg/ml the free part of Cephazolin amounted to 16%, at a concentration of 35 mcg/ml the free Cephradin was 87%, at a concentration of 97 mcg/ml the free Clindamycin was 16%. The binding constant k of Cephazolin was 12.0 (rise-constant 0.58), of Cephradin 0.26 and of Clindamycin 15.8 (rise-constant 0.58). When concentration of antibiotics rose, the free part of Clindamycin and Cephazolin increased more than with Cephradin. At a concentration of 30--42 mcg/ml the differences between the sera of adults and neonates were 26.4% with Cephazolin, 3.7% with Cephradin and 3.1% with Clindamycin (concentration 92--97 mcg/ml). In neonates the free part of Cephazolin was 43%, of Clindamycin 19% and of Cephradin 90%. The lower ablumin content in serum of neonates (3.7 g%) does not altogether explain the reduced protein-binding. In neonates a different affinity for binding has to be assumed.

Adult↗

PubMed1976

Fluorometric determination of cephradine in plasma.

A fluorometric method was developed for the determination of cephradine in plasma. A fluorescent product is formed when samples of deproteinized plasma containing cephradine are heated for 3 hr at 100 degrees and pH 1. The fluorescence is determined in sodium hydroxide solution (pH 13.5) at excitation and emission wavelengths of 350 and 445 nm, respectively. Only 0.1 ml of plasma is required, and concentrations of cephradine as small as 0.1 mug/ml may be determined. In plasma samples from a dog taken over a 10-hr period after an intramuscular injection of 250 mg of cephradine, essentially similar concentrations of cephradine were obtained by the fluorometric method and a standard microbiological bioassay.

Animals↗

PubMed1987

One and two doses of cephradine in the prophylaxis of experimental streptococcal endocarditis.

The efficacy of cephradine in the prophylaxis of rabbit Streptococcus sanguis endocarditis was investigated. Three days after cardiac catheterization and prior to challenge with S. sanguis, rabbits received either 1000 mg/kg (ten animals) or 500 mg/kg cephradine intramuscularly. Infective endocarditis was prevented in only 30% of the animals. The addition of a second dose of cephradine (100 mg/kg) 8 h after an initial dose of 400 mg/kg did not prevent streptococcal endocarditis in 80% of animals tested. In one or two dose regimens cephradine was found to be inferior to a single 400 mg/kg prophylactic dose of amoxycillin. Cephradine is not recommended for prophylaxis against streptococcal endocarditis.

Amoxicillin↗

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↗

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↗

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↗

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↗