[in Japanese]

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Cefadroxil was administered orally at a daily dose of 30-40mg/kg to 8 cases of the infection of upper respiratory tract mainly due to β-hemolytic Streptococcus, and efficacy was obtained in 7 cases, this rate being considered to be satisfactory, though the cases were too few to reach a conclusion. As to pathogens of bacterial infection of upper respiratory tract, β-hemolytic Streptococcus and Staphylococcus aureus were encountered especially frequently, and in view of antibacterial activity against these 2 bacteria, our results could be approved.
Further investigations should be performed carefully, however, to determine if cefadroxil may be a drug of first choice in the treatment of severe bacterial pneumonia and pyothorax.
No side effects were observed throughout our treatment, though digestive tract disorders, especially diarrhea, are most frequent in literatures.
As to pharmacokinetical characteristic of cefadroxil, almost the same results were obtained to other reports, though our data are insufficient as our experience was limited in only 1 case. Serum levels were determined after 35.7mg/kg of cefadroxil were administered once orally, and a peak of about 38 mcg/ml appeared 2hours later, and a high level of about 30mcg/ml was maintained at 5hours, though an oral dose was high. Efficacy for large area of bacterial infections may be expected from these serum levels. From urine collected simultaneously, about 74% of cefadroxil was recovered within more than 4hours. This showed that cefadroxil was well absorbed from digestive tract, and a major part was excreted rapidly through kidney.
From the results of our experiment, characteristics of cefadroxil may be summarized as follows. Cefadroxil is absorbed well after oral administration, antibacterial action is fully expected from serum level, a major part is excreted through kidney, and clearance is good. Cefadroxil will be recommended especially for bacterial infections of upper respiratory tract due to β-hemolytic Streptococcus and Staphylococcus aureus.

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Cefadroxil was administered to 16 pediatric patients at dose levels ranging from 27 to 56mg/kg daily for 5-9 consecutive days. Of 16 patients, 9 had urinary tract infections including 5 cases with nephrotic syndromes, 4 had respiratory tract infections including 2 cases with nephrotic syndromes, 3 had skin infections including 2 cases of pyoderma and 1 case of suppurative gingivitis, including 1 case with nephrotic syndrome.
Clinical results obtained were 9 excellent, 4 effective and eineffective showing an efficacy ratio of 81%. Of 9 urinary tract infections, 5 patients exhibited bacteriuria and 3 had original pathogens persisting after treatment. In respiratory tract, skin and gingival infections, cefadroxil was eithereexcellent for effective in all 7 patients. The above results demonstrate a distinctive feature of cefadroxil that attains a good cutaneous distribution after oral administration. The absorption of the drug was not adversely affected by a food intake.
No significant side effects were observed in all 16 patients.
Judging from our clinical results, cefadroxil is considered one of the valuable cephalosporin antibiotics in the treatment of pediatric infections.

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Cefadroxil was administered at a daily dose of 50mg/kg in 113 children including acute respiratory tract infections suspected to be a bacterial infection and other febrile diseases.
Among 41 cases in which pharyngeal culture was made twice before and after administration or urine and feces cultures were made,. 20 cases (48.8%) were good bacteriologically, 5 cases (12.2%) were poor, and 16 cases (39.0%) were unknown. Clinical efficacy was obtained in 105 cases (92.9%) out of 113 cases.
Microbial substitution was noticed in 12 cases (29.3%) out of the cases of which pharyngeal culture was made after cefadroxil administration. Haemophilus influenzae was detected newly after the administration in 7 cases (58.3%) out of these 12 cases. Bacteriological efficacy was obtained in 5 cases of acute respiratory tract infection of which pathogen was considered to be Haemophilus influenzae. No microbial substitution was noticed in these 5 cases. As to the side effects of cefadroxil administration, only a slight diarrhea was observed in 2 cases.

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(1) Cefadroxil powder for syrup was administered in 24 cases of respiratory tract infection and urinary tract infection, and the efficacy was obtained in 21 cases, effective ratio being 87.5%.
(2) Clinical effect could be obtained satisfactorily at a daily dose of 10-15mg/kg divided into 3 times after each meal.
(3) As to the side effect, GOT and GPT rose in 1 case, and stomatitis in 1 case, though the patients returned to normal after discontinuation of the drug.
(4) Haemophilus appeared by pharyngeal culture after administration of the drug, and attention should be paid on an alteration of pharyngeal flora.

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Clinical investigations were performed on clinical effects of cefadroxil, and the following results were obtained.
1. Cefadroxil was administered at a daily dose of 30mg/kg divided into 3 times in 24 cases of acute tonsillitis and pharyngitis, and clinical results were obtained; remarkably excellent in 8 cases, good in 13 cases, and poor in 3 cases.
2. It was suggested, though the case numbers were limited, that higher efficacy may be obtained in urinary tract infection.
3. No noteworthy side effect was observed throughout all 29 cases, and cefadroxil will be expected to be administered safely in pediatric field.

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Clinical effects were investigated on cefadroxil powder for syrup (containing 100 mg of cefadroxil per 1g) for acute bacterial infections (mostly scarlet fever) in the field of pediatrics, and the results were obtained as follows.
Cefadroxil was applied in 100 cases of scarlet fever. Among 49 cases administered 30-39 mg/kg/day, the results were excellent in 34 cases and good in 15 cases, efficacy ratio being thus 100%. Among 38 cases administered 40-49mg/kg/day, the results were excellent in 33 cases, and good in 5 cases, efficacy ratio being thus 100%.
Out of 4 cases administered 20-29mg/kg/day, the results were excellent in 3 cases and good in 1 case, while out of 9 cases administered 50-59mg/kg/day, excellent in 4 cases and good in 5 cases. Among 78 cases of scarlet fever from which β-hemolytic Streptococcus was proven from swab liquid of palatal tonsil, 67 cases received cefadroxil at a daily dose of 30-49mg/kg, and the bacteria turned to negative the next day of administration in 72 cases, 2 days later in 6 cases. Cefadroxil was administered at a daily dose of 46mg/kg for 7 days in 1 case of SSS syndrome of which Staphylococcus aureus was proven from skin lesion, and local bacteria turned to negative, as well as clinical effect was excellent. No pathogen was proven in 1 case of acute tonsillitis, maybe because ampicillin (ABPC) and cefazolin (CEZ) were administered before cefadroxil treatment, and yet a clinical efficacy was judged by administering cefadroxil at a daily dose of 46mg/kg, though no clinical improvement was observed with the prior antibiotics.
As to the side effects of cefadroxil in 102 cases, a slight vomiting was noticed in 6 cases, though the administration could be continued, and a slight rise of GOT or GPT was observed respectively in 3 cases and 1 case, all of which were recovered without abnormal clinical findings. Among the patients of scarlet fever, after β-hemolytic Streptococcus became negative, reelimination or recurrence was noticed in 2 cases, but these patients were cured completely by readministration of cefadroxil or administration of amoxicillin (AMPC).
Cefadroxil powder for syrup was absorbed quite well, its serum levels were maintained for long, and it was easily administered in children. Considering from its superior antibacterial activity, cefadroxil may be expected to be useful for a remedy in slight or middle infections of children.

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MIC of cefadroxil (CDX) against A group β-Streptococcuswas distributed between 0.05-0.2μg/ml, that is, more susceptible than cephalexin (CEX) and cefaclor (CCL), and susceptible to tetracycline (TC), erythromycin (EM), lincomycin (LCM) resistant strains. Serum level was higher than CCL administered orally at the same dose, and urinary excretion ratio after oral administration was good similarly to CEX and CCL.
Patients treated were mostly scarlet fever and upper respiratory tract infections as acute tonsillitis and lacunar tonsillitis. They responded well to CDX at a daily dose of 30 mg/kg divided into 3-4 times. All cases of scarlet fever became normal temperature within 2 days. Among 14 cases in which A group, β-hemolytic Streptococcus was detected by pharyngeal sputum culture at admission, 11 cases became negative on the 1st day. This result was superior to CEX, when this drug was administered orally at a daily dose of 40-60 mg/kg, bacteria became negative at the ratio of 73.3% on the 2 nd day. CDX was effective for acute tonsillitis, lacunar tonsillitis, acute bronchitis, impetigo and maxillary lymphadenitis in which numerous A group β-Streptococcus, Staphylococcus aureusandHaemophilus influenzaewere proven, as well as for acute urinary tract infection due to Escherichia coli. Clinical results of CDX in totalling 69 cases were excellent in 63 cases, good in 6 cases, efficacy ratio being 100%.
No local nor systemic side effects were observed in 69 cases including maximum 11 days' treatment, as well as no effect was noticed on hepatic and renal functions.
From the above results, it was concluded that satisfactory treatment results may be obtained with CDX dry syrup for children at a daily dose of 20-50 mg/kg divided into 3-4 times in acute infections due to CDX susceptible pathogens.

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I studied on absorption and excretion of cephaloridine. Cephaloridine was administered intravenously to 5 healthy volunteers weighing 65 kg to 83 kg, and the blood levels were measured. A cross over test subjecting 2 grams intravenous drip infused for 1 hour against the same dose for 2 hours was performed after 1 week interval.
The disposition of cephaloridine was estimated by applying one-compartment model which was scaled from YOKOKAWA HULET PACKARD'S disc top computer.
Pharmacokinetic parameters are as followings:
1 hour d.i.v.: Kel 1.410 (hr-1), Vd 9.629 (L), T1/2 30.290 (min.)
2 hours d.i.v.: Kel 0.876 (hr-1), Vd 21.106 (L), T1/2 49.372 (min.)

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[in Japanese]

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Cephalothin antimicrobial activities were studied against selected bacteria with special reference to the time of exposure of microbes to the drug assessed in broth medium. The minimal concentration of this drug producing 10⁰-10¹ reduction of colony forming unit (CFU) per ml after given exposure times an approximation to the theoretical bacteriostatic concentration inhibiting increase or decrease of CFU-was designated as minimally reducing concentration (MRC). The concentration was determined after 6h, 18h and 42h of incubation and designated as 6-h, 18-h and 42-h MRC, respectively. Conventional minimal inhibitory concentration (MIC) with 18h exposure time was also studied. The minimal concentration of the drug yielding 99.9% reduction of CFU after an exposure to the drug was determined and designated as minimal lethal concentration (MLC). The determinations were made at 6h, 18h and 42h of incubation and designated as 6-h, 18-h and 42-h MLC, respectively. The data indicated that the bacteriostatic concentration for Escherichia coli and Klebsiella sp. with brief exposure time (6-h MRC) was 2-4 times lower than the MIC. If the exposure time was prolonged (18-42h), the bacteriostatic concentration increased and almost agreed with the MIC. A significant effect of inoculum size was observed on the MRC values for the Gram-negatives when the values were determined with the inoculum concentrations at 10⁶-10⁷ CFU/ml and 10³-10⁴ CFU/ml. In contrast to these Gramnegatives, the 6-h MRC for most strains of Staphylococcus aureus and Enterococcus roughly agreed with the MIC.
If the ratio of bacteriostatic to bactericidal concentrations was used as the criterion, the mode of action of cephalothin appeared to be bactericidal for most of the Gram-negatives. This drug was bacteriostatic for a number of the Gram-positive strains, in particular to those of Enterococcus, especially when microbes were exposed to the drug over a brief period of time.

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Group B Streptococcus was isolated from the clinical materials of the patients examined in the Kobe Central Municipal Hospital, in 1974 to 1979.
1. Clinical isolates were all resistant to bacitracin.
2. Serotypes of 19 isolates were type III in 12 strains, Ia in 3, Ic in 2 and untypable in 2.
3. The MICs were determined to 15 antibiotics, and the results showed that penicillin G was the best and in the order of decreasing potency, cefotaxime, ampicillin, ceftizoxime and cefoperazone.
4. Compared with group A Streptococcus, the sensitivity of group B Streptococcus to penicillin G and ampicillin was inferior by 2 to 3 tubes.
5. Based on the above results, the significance of the cephalosporin antibiotic of the third generation, particularly cefotaxime, was evaluated in the treatment of infectious diseases of the newborn infants.

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1. Serum and sputum concentrations of cefoxitin were measured at fixed intervals following a one hour drip infusion of 2g to a total of three patients with chronic respiratory tract diseases. The peak levels in serum were found to be 142.1-273.6μg/ml at the end of the infusiori and those in sputum were found to be 0.92-2.30μg/ml at 2 to 4 hours after initiation of the infusion.
2. Cefoxitin was administered to a total of five patients with chronic respiratory tract infections who had failed to respond to the previous treatments with conventional antibiotics. The results were that in one case the therapeutic effect was judged as excellent, in three cases as good, and in one case it was difficult to evaluate. In all cases, there was no significant abnormality indicative of side effects regarding clinical symptoms and laboratory tests of renal and hepatic functions.
In view of the findings stated above, it is considered that cefoxitin is a new antibiotic which can be used for the treatment of chronic respiratory tract infections.

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Pharmacokinetic differences between ampicillin and carbenicillin in the cerebrospinal fluid (CSF) were evaluated in experimental staphylococcal meningitis in rabbits after a single intravenous administration of 100 mg/kg dose of each drug. Half-lives (T1/2) in CSF and CSF/serum ratios of T1/2 were 52 minutes and 2.1 for ampicillin and 23 minutes and 1.3 for carbenicillin, respectively. These findings indicate that ampicillin is eliminated from CSF more slowly than carbenicillin. Penetration rates were calculated from CSF/serum ratios of area under the curve (AUC) and were 16.8% for ampicillin and 11.6% for carbenicillin, although the maximum concentration (C_max) of carbenicillin in CSF was twice as high as that of ampicillin. Thus the penetration rate appeared to be influenced more by T1/2 in CSF than by C_max. C_maxin CSF was obtained at 15 minutes for carbenicillin and 30 minutes for ampicillin. As to carbenicillin there were considerable individual variations in CSF levels. The above observations suggest that T1/2 and AUC in CSF are important parameters when evaluating the usefulness of an antibiotic in the treatment of bacterial meningitis.

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