[Fundamental and clinical studies of cefroxadine in pediatric field (author's transl)]

Fundamental and clinical studies on cefroxadine (CXD) were carried out, and we have obtained the following results. (1) Sensitivity distribution: As for the sensitivity distribution in S. aureus, the peak was within the ranges from 3.13 to 6.25 microgram/ml in the inoculum size of 10(9) CFU/ml, the distribution was less than or equal to 0.1 to 50 microgram/ml in the inoculum size of 10(6) CFU/ml, with the peak at 1.56 to 6.25 microgram/ml. In S. pyogenes, the sensitivity distribution ranged between less than 0.1 and 1.56 microgram/ml, with the peak at 0.1 microgram/ml in the inoculum size of 10(9) CFU/ml. In the inoculum size of 10(6) CFU/ml, however, the all strains were distributed within the ranges of 0.1 to 0.78 microgram/ml, and the growth of 49 out of 54 strains (91%) was inhibited at less than or equal to 0.1 microgram/ml. In E. coli, the sensitivity peak was at 25 to 50 microgram/ml in the inoculum size of 10(8) CFU/ml, and 5 strains (9.3%) were detected with greater than 100 microgram/ml. Of the 5 strains, 1 strain showed cross tolerance with CEX, the remaining 4 strains was at 50 microgram/ml and at 25 microgram/ml in 2 strains each. In the case of inoculum size of 10(6) CFU/ml, the sensitivity distribution was all within the ranges from 0.78 to 12.5 microgram/ml, except for 1 strain at 100 microgram/ml, with the peak being within the ranges from 3.13 to 12.5 microgram/ml. As for the above 100 microgram/ml-strain, it was showing cross tolerance with CEX. (2) Serum concentration: CXD was administered at a dose level of 10 mg/kg and 20 mg/kg between meals to 5 children, and CXD concentration in their serum was measured. In the group of the 10 mg/kg administration: average 30 minutes value; 8.7 microgram/ml, 1 hour value; 9.15 microgram/ml, 2 hours value; 7.4 microgram/ml, 3 hours value; 2.85 microgram/ml, 4 hours value; 1.0 microgram/ml and 6 hours value; 0.32 microgram/ml, with half-life of 0.88 hours. In the group of the 20 mg/kg administration: average 30 minutes value; 11.7 microgram/ml, 1 hour value; 16.8 microgram/ml, 2 hours value; 10.7 microgram/ml, 3 hours value; 8.15 microgram/ml, 4 hours value; 3.33 microgram/ml, 6 hours value; 1.22 microgram/ml, with half-life of 1.03 hours. A significant interrelation in dose response was observed between the 2 groups. (3) CLINICAL RESULTS: Clinical investigation were held in 29 cases (47 boys and 32 girls). Their diseases comprised of 2 acute pharyngitis, 28 acute purulent tonsillitis, 11 scarlet fever, 3 cervical purulent lymphadenitis, 14 acute bronchitis, 7 acute pneumonia, 11 urinary tract infection and 3 skin soft tissue infection. The drug was effective in 74 out of the 79 cases (93.7%). Causative organism was proved in 60 out of the 79 cases. Fifty-five cases (91.7%) were observed bacterial disappearance or reduction in the 60 cases. Side effects were observed in a total of 3 cases (3.8%), i.e. 2 cases of abnormal values in the laboratory findings (an eosinophilia and/or an elevation of the GPT readings) and 1 case of manifestation of exanthema.