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.

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.

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.

Comparative pharmacokinetics of cefamandole, cefuroxime and cephradine during total hip replacement.

Serum, bone and tissue levels of the three cephalosporins, cefamandole, cefuroxime and cephradine were determined in 60 patients given a single 1 g dose intravenously before total hip surgery and two similar doses at 8 h intervals. The levels achieved were comparable for all three antibiotics, hence the choice of prophylactic antibiotic for total hip replacement should be guided by the pathogens causing infection and cost of the antibiotic.

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.

[Clinical evaluation of cefroxadine dry syrup in children (author's transl)].

Clinical efficacy of cefroxadine dry syrup, a new oral cephalosporin antibiotic, was evaluated in children, and the following results were obtained. 1. Three children were given a single oral dose of about 10 mg/kg of the drug when fasting, and its blood concentrations were determined. Blood concentrations were maximum at 30 approximately 60 minutes, i.e., 16.9 approximately 18.2 microgram/ml, and markedly low at 4 hours. 2. Thirty-six patients with the following diseases were tested with 23.1 approximately 44.4 mg/kg/day of the drug in 3 to 4 divided doses; 21 patients with lacunar tonsillitis, 2 with tonsillitis, 1 with scarlet fever, 4 with bronchitis and tonsillitis, 2 with cystitis, 4 with pyelonephritis, 1 with impetigo and 1 with probable Mycoplasma pneumonia. An overall efficacy rate in 35 patients excluding the last mentioned case was 91.4%, i.e., excellent in 20, good in 12 and poor in 3, and an eradication rate of the causative organisms was 88.9%. 3. Adverse reactions noted were diarrhea in 1 patient, eruption and diarrhea in 1 transient neutropenia in 1, eosinophilia in 3 and an elevation of GOT and GPT in 1. None were significant. 4. Taste and flavor of the drug was considered to be well palatable to children. 5. Taking into consideration of the results of fundamental evaluation of the drug, cefroxadine dry syrup is considered to be a potent new antibiotic in children, and the recommended dose will be 10 mg/kg 3 to 4 times a day.

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.

[Concentrations of cefradine in renal tissue (author's transl)]. / Konzentrationen von Cefradin im Nierengewebe.

After a single bolus injection of two grams of cefradine the concentrations of antibiotic in serum and renal tissues of 21 patients were estimated. After 30 minutes the mean serum concentrations were 159 microgram/ml, after 60 mins 62 microgram/ml and after 95 mins 22 microgram/ml. The tissue concentrations in normal renal tissue (group I) after 30 minutes were 348 microgram/ml and with tissue of chronically inflamed kidneys (group II) 118 microgram/ml in the same period. After 90 minutes the concentrations of group I were 214 microgram/g, and in group II 28 microgram/g, e.g. 8 times lower. The estimated cefradine concentrations in serum and in normal and impaired renal tissue within the time interval of 10 to 90 minutes are above the minimal inhibition concentrations for most cefradine sensitive pathogens.

[Human lung tissue and serum concentrations of cefradin (author's transl)]. / Etude, chez l'homme, des concentrations pulmonaires et sériques de la céfradine.

This work was performed on samples from 30 patients requiring lung removal. One dose of 2 g of cefradin was injected intravenously before operation. Titrations of the antibiotic was performed simultaneously on large pieces of the excised lung and on the serum.

[Cephradine in open heart serugery. Concentrations of cephradine in pericardial exudate and serum after cardiac surgery (author's transl)]. / Cefradin in der offenen Herzchirurgie. Cefradin-Konzentrationen im Perkardexsudat und Serum nach Herzoperationen.

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.

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.