FUNDAMENTAL AND CLINICAL STUDIES OF CEFROXADINE IN PEDIATRIC FIELD

Abstract

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 6.25μg/ml in the inoculum size of 10⁸ CFU/ml, the distribution was _??_0.1 to 50μg/ml in the inoculum size of 10⁶ CFU/ml, with the peak at 1.56 to 6.25μg/ml. In S. pyogenes, the sensitivity distribution ranged between _??_0.1 and 1.56μg/ml, with the peak at _??_0.1μg/ml in the inoculum size of 10⁶ CFU/ml, In the inoculum size of 10⁶CFU/ml, however, the all strains were distributed within the ranges of 0.1 to 0.78μg/ml, and the growth of 49 out of 54 strains (91%) was inhibited at _??_0.1μg/ml. In, E. coli, the sensitivity peak was at 25 to 50μg/ml in the inoculum size of 10⁶CFU/ml, and 5 strains (9.3%) were detected with _??_100μg/ml. Of the 5 strains, 1 strain showed cross tolerance with CEX, the remaining 4 strains was at 50μg/ml and at 25μg/ml in 2 strains each. In the case of inoculum size of 10⁶CFU/ml, the sensitivity distribution was all within the ranges from 0.78 to 12.5μg/ml, except for 1 strain at 100μg/ml, with the peak being within the ranges from 3.13 to 12.5μg/ml. As for the above 100μg/ml-strain, it was showing cross tolerance with CEX.
(2) Serum concentration:
CXD was administered at a dose level of 10mg/kg and 20mg/kg between meals to 5 children, and CXD concentration in their serum was measured. In the group of the 10mg/kg administration: average 30 minutes value; 8.7μg/ml, 1 hour value; 9.15μg/ml, 2 hours value; 7.4μg/ml, 3 hours value; 2.85μg/ml, 4 hours value; 1.0μg/ml and 6 hours value; 0.32μg/ml, with half-life of 0.88 hours. In the group of the 20mg/kg administration: average 30 minutes value; 11.7μg/ml, 1 hour value; 16.8μg/ml, 2 hours value; 10.7μg/ml, 3 hours value; 8.15μg/ml, 4 hours value; 3.33μg/ml, 6 hours value; 1.22μg/ml, with half-life of 1.03 hours. A significant interrelation in dose response was observed between the 2 groups.
(3) Clinical results:
Clinical investigations were held in 79 cases (47 boys and 32 girls). Their diseases comprised of 2 acute pharyngitis, 28 acute purulent tonsillitis, 11 scarlet fever, 3 carvical 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 atotal 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.