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1.
Jpn J Antibiot ; 36(1): 1-15, 1983 Jan.
Article in Japanese | MEDLINE | ID: mdl-6221127

ABSTRACT

Latamoxef (LMOX) is a new antibiotic synthesized by Shionogi Research Laboratory. Chemically LMOX is especially unique with a sulfur atom replacing the oxygen atom in the 1 position of the conventional cephalosporin nucleus, and in addition, this antibiotic has a cephamycin-like structure. The antibacterial activity of LMOX shows high potency against Gram-negative bacteria, but tends to be weak against Gram-positive bacteria. The tissue levels of LMOX in humans after intravenous injection of 1 g were examined. The levels in uterine and adnexa uteri tissue at 1 hour after administration were 25.4 and 27.4 micrograms/g respectively. LMOX was administered to 147 cases in infections of obstetric and gynecological field. The clinical effect according to disease was 94.6% for intrauterine infections, 95.0% for adnexitis, 87.0% intrapelvic infections, and 100% for external genital organ infections, making a total of 92.5%. The rate of occurrence of side effects or abnormal laboratory findings was similar to or slightly less than that seen with other beta-lactam antibiotics.


Subject(s)
Bacterial Infections/drug therapy , Cephalosporins/therapeutic use , Cephamycins/therapeutic use , Genital Diseases, Female/drug therapy , Adult , Aged , Cephamycins/administration & dosage , Cephamycins/metabolism , Drug Evaluation , Exudates and Transudates/metabolism , Female , Genitalia, Female/metabolism , Humans , Middle Aged , Moxalactam , Pregnancy
3.
Jpn J Antibiot ; 35(6): 1585-609, 1982 Jun.
Article in Japanese | MEDLINE | ID: mdl-6290708

ABSTRACT

The study group was organized to evaluate the usefulness of cefmenoxime (CMX) injection, a new synthetic cephalosporin, for the treatment of infections in the field of obstetrics and gynecology. Fundamental and clinical studies were made by the society and the following results were obtained. 1. The peak distribution of CMX's MIC for E. coli, Klebsiella sp., Enterobacter sp., Bacteroides sp. and Peptococcus sp. isolated from obstetrical and gynecological infections with relatively high frequencies area 0.1, less than or equal to 0.05, 0.2, 3.13, 1.56 micrograms/ml, respectively, with an inoculation of 10(6) cells/ml. 2. When 1 g of CMX is administered by intravenous drip infusion for 1 hour, the maximum concentrations in various tissues of female genital organs were as follows: 14.2 and 13.2 micrograms/g in ovary and oviduct, respectively, at 1.20 hours after the start of administration, and 16.9 and 26.3 micrograms/g in corpus uteri and cervix uteri, respectively, after 1 hour. As for the transfer to the exudate in the pelvic dead cavity, the peak concentration was 15.6 micrograms/ml after 2.13 hours. 3. In the clinical studies, CMX was given to 258 cases with female genital organ infections and others. As for the clinical effects, with exclusion of 3 cases in which other antibiotics are concomitantly used, responses were excellent in 76 cases, good in 162 cases and poor in 17 cases, among 255 cases in total. The efficacy rate was 93.3%. The efficacy rates by diseases were 97.1% (68/70) for intrauterine infections, 88.8% (79/89) for intrapelvic infections, 98.4% (62/63) for adnexitis, and 100% (23/23) for infections of external genital organs. As for the clinical effects on causative bacteria, the efficacy rates were 100% (19/19) for single infections due to Gram-positive bacteria, 94.8% (55/58) for single infections due to Gram-negative bacteria, and 88.2% (15/17) for single infections due to anaerobic bacteria. And its efficacy rates were 89.6% (69/77) for mixed infection cases. Side effects were observed in 2 cases (0.8%); 1 case with eruption, and 1 case with diarrhea and vomiting. As for abnormal laboratory findings, lower white blood cell count was observed in 2 cases and elevation of the values regarding hepatic functions in 9 cases. All cases were returned to the normal after the completion of the administration. Cefmenoxime showed a satisfactory clinical efficacy and a potent bacteriological effect in treatment of the infections in the field of obstetrics and gynecology, and it has been concluded that cefmenoxime will be useful addition to the antibiotics for the therapy of these infections.


Subject(s)
Bacterial Infections/drug therapy , Cefotaxime/analogs & derivatives , Genital Diseases, Female/drug therapy , Adolescent , Adult , Aged , Bacteria/drug effects , Bacterial Infections/microbiology , Cefmenoxime , Cefotaxime/metabolism , Cefotaxime/pharmacology , Cefotaxime/therapeutic use , Child , Clinical Trials as Topic , Drug Resistance, Microbial , Exudates and Transudates/metabolism , Female , Genital Diseases, Female/microbiology , Genitalia, Female/metabolism , Humans , Middle Aged
4.
Jpn J Antibiot ; 34(4): 521-31, 1981 Apr.
Article in Japanese | MEDLINE | ID: mdl-6270401

ABSTRACT

UNLABELLED: Fundamental and clinical studies were made on cefotaxime (CTX), a new cephalosporin antibiotic. The following results were obtained: 1. Antibacterial activity: At a concentration of 3.13 mcg/ml, CTX inhibited the growth of 90.2% of 92 strains of Gram-negative rods and 80.0% of 15 strains of Gram-positive cocci. 2. Concentrations of CTX in body fluids and genital organs after 2 g i.v.: (1) CTX level in pus reached the peak (5.6mcg/ml) at 2 hours after administration. (2) Mean CTX levels in the pelvic space exudate reached the peak (28.0 mcg/ml) at 2 hours after administration. (3) CTX levels in the uterine appendages and uterus reached the peak (8.9 and 4.5 mcg/g, respectively) at 100 to 280 minutes after administration. 3. CLINICAL RESULTS: CTX was excellent in 7 of 13 cases and good in the remaining 6 cases. The response rate to CTX was 100%. 4. The bacteriological effect: The bacteriological effect of CTX was also 100%. Bacteria were eradicated in 7 of the 10 cases where organisms were demonstrated before CTX treatment. Partial reduction bacteria was observed in the remaining 3 cases. 5. No side effect attributable to CTX was observed.


Subject(s)
Bacterial Infections/drug therapy , Cefotaxime/therapeutic use , Genital Diseases, Female/drug therapy , Adult , Aged , Bacteria/drug effects , Body Fluids/metabolism , Cefotaxime/metabolism , Cefotaxime/pharmacology , Drug Evaluation , Drug Resistance, Microbial , Female , Genitalia, Female/metabolism , Humans , Middle Aged
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