Fundamental and clinical studies on PC-904, a new semisynthetic penicillin developed by Sumitomo Chemical Company Limited, were performed in 46 institutions in Japan and the results were presented at ...the 25th Congress of Chemotherapy (the annual meeting of Japan Society of Chemotherapy), New Drug Symposium, Gifu, 1977. The results are summarized as follows. 1) In vitro activity of PC-904 against Pseudomonas and other gram-negative bacteria was more potent than the other broad-spectrum penicillins. 2) When 2g of PC-904 were administered by drip infusion, the peak serum level was more than 100μg/ml and its urinary recovery within 6 hours was more than 30%. It was characteristic that 50-60% of administered dose was excreted in bile. 3) Clinical effects of PC-904 against various infections were analyzed by the results of 613 cases out of total 650 cases treated with PC-904. The effective rate in 335 cases of the field of internal medicine was 63. 6% and the effective rate in 275 cases in the field of surgery, urology, obstetrics and gynecology, otorhinolaryngology and ophthalmology was 72.4%, and the effective rate in total of 613 cases was 67.5%. 4) No severe side effects were observed while incidence of allergic reactions was comparatively high. Abnormalities in laboratory findings were observed in some cases, but they turned to normal immediately after discontinuing the drug.
1. Pneumonia as an opportunistic infection Pneumonia caused by gram negative bacilli (GNB) which belong to Enterobacteriaceae is found increasingly in recent years. It occurs in most cases ...nosocomially in patients with severe diseases such as malignant tumor, malignat lymphoma, leukemia, etc. and treated with anticancer drugs, immunosuppressive substances, radiation, adrnocortical steroids etc. Pneumonia caused by Pneumocystis carinii is also an opportunistic infections and occurs in patients treated with long-term, large dose steroids, immunosuppressive substances etc. for leukemia, malignant lymphoma, organ implantation etc. The causative protozoa, Pneumocystis carinii can be found by Gomori's methonamine silver stain in needle-puncture fluid and in needle- or pen biopsied specimen. Intramuscular or intravenous injection of pentamidine isothianate 4mg/kg/day for one to two weeks is effective in nearly the half of the cases. 2. Causative bacteria in pneumonia From a few reports in recent years it can be inferred that the causative bacteria in primary simple pneumonia (pneumonia in patients without severe complications) is still Str. pneumoniae or Hemophilus influenzae and both of them have few resistant strains against common antibiotics. 3. Causative bacteria in broncho-pulmonary infections The endeavour to find out or to determine the causative bacteria in pneumonia by many authors was tabulated and our method, the so-called Washculture method of sputum was introduced. 4. Experimental model for the study of pharmacokinetics of antibiotics The pharmacokinetics of antibiotisc in diseased organ tissue must be different from that of experimental healthy in these rabbit lung were introuduced and discussed.
Twenty patients with complicated urinary tract infections, two of them were dropped out of effect evaluation, were given biapenem (BIPM) at a daily dose of 0.6g (in 15 cases) or 0.9g (in 3 cases) by ...intravenous drip infusion for five days, and the following results were obtained. Clinical results were excellent in 4 cases, moderate in 10 and poor in 4. The overall clinical efficacy rate was 78%. As to the bacteriological response, 37 strains of total 40 were eliminated. Nine new organisms appeared after treatment. No extraordinary values of the clinical laboratory findings were observed in 20 patients treated by BIPM, except for two cases who showed eosinophilia and elevation of GPT and Al-P.
A newly developed cephalosporin antibiotic, CS-807, was administered to 13 patients with respiratory infection to determine its usefulness and safety. Two, six, one and four patients had pneumonia, ...acute bronchitis, chronic bronchitis and acute tonsillitis, respetively. The patients were six males and seven females aged 18-73 (mean age, 42), 12 being outpatients and one inpatient. CS-807 was given orally twice a day at 100 mg to seven patients and at 200 mg to six patients for 7-21 days (mean duration, 9 days). Total dose per patient ranged from 1.4-4.2g (mean total dose, 2.5g). Efficacy of CS-807 was excellent in 1 patient, good in 11, fair in 1. Thus, 92 % of the efficacy rate (12/13) consisted of excellent and good clinical results. As to dose efficacy, the rate was 86 % in the 100 mg group and 100 % in the 200 mg group. Causative organisms were identified in 4 of the 13 patients ; these were β-hemolytic group G Streptococcus, S. aureus, a yeast-like organism, S. pyogenes and E. coli, which were all eradicated by treatment with CS-807. As to safety, there were neither side-effects causing clinical problems not abnormal laboratory findings during or after treatment. These results indicate that CS-807 was sufficiently absorbed through the oral route and was effective when administered twice daily. We therefore consider CS-807 to be a highly useful and safe antibiotic with a wide spectrum against Gram-positive and-negative organisms, and a drug of first choice for the treatment of mild to moderate respiratory infections.
We clinically evaluated the efficacy and safety of RU 28965, a new macrolide antibiotic, in 14 cases of respiratory tract infection (acute upper respiratory infection 4, acute bronchitis 5, chronic ...bronchitis 3 and acute pneumonia 3). RU 28965 was administered at 300 mg daily for 5-14 days. Clinical response was excellent in 3 cases, good in 8 and fair in 2 one case dropped out. The efficacy rate was 84.6%. As to safety, neither side-effects nor abnormal laboratory findings were observed in any of the cases, including 2 with hepatic disease. From our results, we consider that RU 28965 is sufficiently effective at 300 mg/day in 2 doses, and very safe even in patients with hepatic disorders, where side-effects of existing macrolides present clinical problems.
Azthreonam (SQ 26, 776), a new monocyclic β-lactam (monobactam) antibiotic, was administered to 15 patients with infections in the field of internal medicine, and its effectiveness and safety were ...evaluated. Azthreonam was administered to a total of 15 patients consisting of 7 cases of respiratory tract infections, 6 cases of digestive tract infections and 2 cases of urinary tract infections. Organisms isolated were H. influenzae (1), K. pneumoniae (3), P. vulgaris (1), E. coli (2), S. epidermidis (1), Acinetobacter (1), Salmonella (1) and Normal flora. Clinical efficacy was evaluated as excellent or good in 5 cases (5/7) with respiratory tract infections, 5 cases (5/6) with digestive tract infections and 2 cases (2/2) with urinary tract infections. The overall efficacy rate was 80% (12/15). No serious side effects were observed. From these results it appears that Azthreonam was evaluated to be a effective and safe P-lactam antibiotic against infections in the field of internal medicine.
This study was carried out to evaluate the therapeutic efficacy and safety of cefixime (CFIX) in the field of internal medicine. CFIX was given orally to 13 patients in a dose of 100mg twice daily ...for 4-22 days (average: 11.7 days). The subjects consisted of 12 patients with respiratory tract infection and 1 with urinary tract infection; 3 with pharyngolaryngitis, 1 with tonsillitis, 2 with acute bronchitis, 2 with acute exacerbation of chronic bronchitis, 3 with pneumonia, 1 with infected lung cancer and 1 with acute cystitis. The overall effect of CFIX was “excellent” in 2, “good” in 8 and “fair” in 3, with an effectiveness rate of 76.9%. The causative organisms were identified as E. coli in 2 patients, which were eradicated after treatment with CFIX. No side effects or abnormal laboratory data were observed in any of the 13 patients. Considering its broad spectrum, prolonged serum level and clinical results, it was concluded that CFIX is an oral antibiotic of first choice which is highly useful for the treatment of infections in the field of internal medicine.
PDF
