L-105, a new semisynthetic cephalosporin, was intravenously administered at a dose of 1.0g to 11 patients with gallstones before operation. The concentrations of L-105 in serum, gallbladder tissue ...and bile were measured. The mean value of serum concentrations after 30 minutes and one hour were respectively 56.5 and 25.8μg/ml. The gallbladder tissue concentrations after 2 hours ranged widely from 3.20 to 1, 540μg/g and the mean value was 313μg/g. The cases with severe inflammation at their diseased parts showed low concentrations. The gallbladder bile concentrations after 2 hours ranged from 1.90 to 3, 900μg/mi and the mean value was 1, 440μg/ml. The cases with puruloid bile showed low concentrations. The common duct concentrations which were measured in only three cases after 2 hours ranged from 1, 180 to 2, 750μg/ml and the mean value was 1, 990μg/ml. As the result of the above mentioned, L-105 showed so high concentrations in both gallbladder tissue and bile. Therefore, it may be concluded that L-105 is very useful drug for treatment of biliary tract infections.
We carried out basic and clinical studies on fleroxacin, a new oral pyridonecarboxylic acid, and obtained the following results. The in vitro antibacterial activity of fleroxacin was tested against ...275 strains of clinical isolates of 15 species and compared with those of norfloxacin, ofloxacin, ciprofloxacin, enoxacin, cefixime, cefaclor, ampicillin and minocycline. Fleroxacin and other new pyridonecarboxylic acids were very active against Gram-negative bacilli. We administered fleroxacin to 12 patients with respiratory infections at a dose 200-300mg daily for 7-14 days. The clinical response obtained was excellent in 1 and good in 11 cases. The organisms isolated from two cases, one of Streptococcus pneumoniae and Escherichia coli, were eradicated. Neither side effects nor remarkable worsening of laboratory findings was observed.
We have treated surgically 7 patients with tracheal injury, 6 patients with tracheal stenosis caused by tracheostomy, and 20 patients with primary or secondary tracheal tumors in the past 20 years. ...Five of the 20 patients with tracheal tumors had resection of the carina. In 3 of the 5 patients, a new carina was created by anastomosing the trachea with the left main bronchus and the right intermediate trunk. In 4 patients, 9 rings or more the trachea were resected. All of the 33 patients were treated by primary anastomosis. Eight of the 33 patients died. In 3 of the death cases, the cause was unrelated to the surgery. Eight patients had complications.
Basic and clinical studeis on 7432-S, a new oral cephem antibiotic, were carried out and the following results obtained. The in vitro antibacterial activity of 7432-S was tested against 135 clinical ...isolates of 9 species and compared with that of cefaclor, T-2525, cefixime, ampicillin, imipenam, ofloxacin and minocycline. 7432-S was more effective against Gram-negative bacteria (Escherichia coli, Klebsiella pneum.oniae, Proteus vulgaris, Providencia rettgeri, Morganella morganii, Enterobacter cloacae, Serratia marcescens and Haemophilus influenzae) than any other antibiotic tested, but less active against Gram-positive cocci (Streptococcus pyogenes). We administered 7432-S to 6 patients with respiratory and 2 with urinary tract infection at a dose of 300-400mg daily in 2 or 3 divided doses for 7-15 days. The clinical efficacy rate was 71.4% in all 7 cases except one, which was unknown. The organisms isolated from 3 cases, 2 strains of Streptococcus agalactiae and 1 of Enterococcus faecalis, were eradicated except E. faecalis. There were no side effects or abnormal laboratory findings.
We carried out in vitro and in vivo studies on temafloxacin (TMFX), a newly-developed quinolone, and obtained the following results. The MICs of 488 clinical isolates of 25 species were compared with ...those of the other tested antibiotics, ciprofloxacin, ofloxacin, tosufloxacin, lomefloxacin, fleroxacin, sparfloxacin (SPFX), cefteram pivoxil (CFTM-PI), clavulanic acid/amoxicillin (CVA/AMPC) and minocycline (MINO). Against Gram-positive cocci, the antibacterial activity of TMFX was higher than or almost equal to those of the other antibacterial agents examined. Against Gram-negative rods and cocci, the MICs of TMFX were lower than those of SPFX, CFTM-PI, CVA/AMPC and MINO, and equal to those of the other new quinolones tested. In the clinical study, TMFX was given to 21 patients with respiratory infections and 4 with urinary tract infections. Clinical efficacy was excellent in 12, good in 12 and poor in 1, with an efficacy rate of 96.0%. Side effects observed were urticaria in 1 and vomiting in 1, which disappeared while the agent was continued. There were no newly-developed abnormal findings in laboratory examinations.
Cefotiam hexetil (CTM-HE), a new oral cephalosporin, is a pro-drug of cefotiam. The MICs of cefotiam for 260 strains of 13 species of clinical isolates were compared with those of other oral ...antibiotics: cefaclor (CCL), cephalexin (CEX), cefixime (CFIX), bacampicillin (BAPC), fosfomycin (FOM), and clavulanic acid/amoxicillin (CVA/AMPC). The MIC80 of cefotiam (CTM), was 0.78μg/ml for Staphylococcus aureus, 12.5μg/ml for penicillinase-producing Staphylococcus aureus, 25μg/ml for methicillin-resistant Staphylococcus aureus, 0.2μg/ml for Streptococcus pneumoniae, 0.39μg/ml for Escherichia coli, 0.78μg/ml for Klebsiella pneumoniae, 25μg/ml for Enterobacter cloacae, 100μg/ml for Citrobacter freundii, 0.39μg/ml for Proteus mirabilis, 0.78μg/ml for Morganella morganii, 6.25μg/ml for Providencia rettgeri, 100μg/ml for Proteus vulgaris, and 1.56μg/ml for Haemophilus influenzae. The drug proved to have the most potent antibacterial activity of all the antibiotics used in the study against S.aureus, penicillinase-producing S.aureus, E.coli, E.cloacae and M.morganii. Seven patients, 4 with respiratory and 3 with urinary tract infection, were administered 600mg daily of CTM-HE, for 1-13 days. The clinical efficacy was evaluable in 6: excellent 1, good 4, and poor 1. Nausea and vomiting were observed as adverse reactions in 1, but no abnormal laboratory data were found.
We carried out in vitro and in vivo studies of loracarbef (LCBF), a newly developed carbacephem, and obtained the following results.The MICs of 180 clinical isolates of 9 species were compared with ...those of cefaclor (CCL), amoxicillin, cefixime, cefteram and minocycline. Against gram-positive cocci other than Staphylococcus epidermidis, the antibacterial activity of LCBF was higher than or almost equal to that of CCL.Against gram-negative rods, the MICs of LCBF were lower than those of CCL. In the clinical study, LCBF was given to 15 patients with respiratory infections.The clinical efficacy was excellent in 4, good in 10 and fair in 1.The causative organisms, which included Staphylococcus aureus, Streptococcus agalactiae, Haemophilus influenzae and Klebsiella pneumoniae, were all eradicated. There were neither side effects nor newly developed abnormal findings in laboratory examinations.
BAY o 9867, a new quinoline carboxylic acid derivative, was evaluated that of clinical efficacy and safety in this study. BAY o 9867 was administered orally to 55 cases of infectious diseases.Daily ...doses ranged from 200 to 600 mg for 7 to 56 days. Among 31 cases of RTI, the efficacy rate was 44.4% on acute RTI, 52.6% on chronic RTI and 50.0% on total RTI. Among 22 cases of UTI, the efficacy rate was 100% on acute UTI, 80.0% on chronic UTI and 94.1% on total UTI. As for bacteriological effect, the eradicated rate was 78.3% and the MICs were excellent except one strain of S. marcescens (MIC: 12.5 μg/ml). No side effect was observed except for one case with slight abdominal pain and borborygmus.Laboratory findings revealed 3 cases (8.3%), showed slight elevation of serum GOT, GPT and Al-P in each one case. From these results, BAY o 9867 is considered to be useful and safe antimicrobial agent in the field of internal infections.
BASIC AND CLINICAL STUDIES ON ME 1207 Ohishi, Akira; Sakauchi, Michihiro; Nakamura, Hidetoshi ...
CHEMOTHERAPY,
1992, Letnik:
40, Številka:
Supplement2
Journal Article
Odprti dostop
We performed basic and clinical studies on ME 1207, a new oral cephalosporin, and obtained the following results. The in vitro antibacterial activity of ME 1206, an active metabolite of ME 1207, ...against 285 clinical isolates from 17 species was compared with that of cefpodoxime, ceftibuten, cefdinir, cefprozil, ofloxacin, clavulanic acid/amoxicillin, cefixime and cefteram. ME 1206 was more effective against gram-positive bacteria than other cephalosporins except cefdinir, and the MICs of ME 1206 against gram-negative bacteria were equal to that of cefteram. In clinical studies, ME 1207 was administered to 11 patients with respiratory infections; the clinical response was excellent in 3 cases, good in 6, poor in 1 and unknown in 1. Side effects and abnormal laboratory findings were observed in 2 cases.
We carried out basic and clinical studies on cefdinir (CFDN), a newly developed oral cefhalosporin antibiotic, and obtained the following results. The in vitro antibacterial activity of CFDN against ...477 clinical isolates of 19 species was studied and compared with that of cefteram (CFTM), cefixime (CFIX), cefaclor (CCL), minocycline (MINO), ofloxacin (OFLX) and clavulanic acid/amoxicillin (CVA/AMPC). CFDN showed more effective activity against Gram- negative bacteria (Eschcrichia coli, Klehsiella pneumonkze, Pros mirabilis, Haoophilus influcnzae, Branhamella catarrhalis) than any other antibiotic. It was also more effective against Gram-positive bacteria (methicillin sensitive Staphylococcus aureus, Stephylococcus epidermidis, Streptococcus pneumoniae) than any other antibiotic. We administered CFDN to 21 patients with respiratory and 3 with urinary tract infections at a dose of 300-600mg daily and 3 times a day for 4 16 days. The clinical efficacy rate was 78.3% in all 23 cases. The organisms isolated from 5 cases were 2 strains of H. influenzae, 1 of S. pneumoniae, 1 of K. pneumonia, 1 of S. epidermidis and 1 of E. coli. All were eradicated. There were a few side-effects (diarrhea, 2 cases) and one abnormal laboratory finding (elevated GOT and GPT, 1 case).
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