Antibacterial activities of cefatrizine (CFT), a new oral cephalosporine, and its therapeutic effect on various infections were studied and following results were obtained.
1) Antibacterial activities of CFT against gram-positive organisms were examined using clinically isolated 18 strains of Staphylococcus aureus, 3 of Staphylococcus epidermidis, 4 of Streptococcus β-hemolyticus, 3 of Streptococcus pneumoniae and 3 of enterococci. Minimal inhibitory concentration (MIC) was mostly 0.39 to 0.78μg/ml in Staphylococcus aureus, 0.39 μg/ml in Staphylococcus epidermidis and 6.251μg/ml in enterococci which is 1/4 to 1/2 times lower than that of cephalexin (CEX). MIC against Streptococcus β-hemolyticus and Streptococcus pneumoniae was not more than 0.19 μg/ml. Antibacterial activities against gram-negative organisms examined by the use of 20 strains of Escherichia coli, 12 of Klebsiella, 7 of Proteus mirabilis ranged mostly from 0.78 to 1.56 μg/ml, 0.78 to 6.25μg/ml and 0.78 to 1.56 μg/ml as MIC, respectively, and it is 1/8 to 1/4 times lower than that of CEX. No antibacterial activity was noted against Pseudomonas aeruginosa both in CFT and CEX.
2) Clinical trial with CFT was carried out in 260 patients suffering from various infections cornprizing 105 patients in internal medicine, 17 in pediatrics, 23 in surgery, 12 in orthopedics, 30 in urology, 15 in obstetrics and gynecology, 27 in otorhynolaryngology and 21 in ophthalmology. Daily dose of CFT was 1.0 to 2.0 grams (capsules) in adult patients and 40 mg per kg (dry syrup) in infantile patients. The result obtained was 36 cases of marked effectiveness and 164 effective cases, the effectiveness rate being 76.9%.
3) Side effects were seen in 20 (7.6%) out of 263 patients examined, 15 showing gastrointestinal disturbances (nausea, vomiting, a sensation of discomfort in stomach region, abdominal pain, soft feces and diarrhea) and 5, skin rash.
4) Influences of CFT on blood picture, liver and kidney functions were checked. Red blood cell and white blood cell counts were examined in 119 and 121 cases, respectively, and except one case showing the increase in white blood cell counts from 11, 200 to 16, 100, no abnormality was found. Slight elevation of SGOT up to 50-70 units was noted in 3 out of 114 cases and slight aggravation was noted in 2 cases who had had slight abnormal value before the medication. Slight elevation of SGPT up to 50-75 units was observed in 3 out of 114 cases and slight aggravation was found in 3 already slightly disordered cases. Alkaline phosphatase was checked in 91 case, but no abnormal finding was observed. Slight elevations of BUN and serum creatinine level were noted in 3 out of 98 and 1 out of 108, respectively, after CFT dosing. Coomb's test was performed in 31 cases but no positive case was noted.
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