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Biomedical subjects

M Kanao

Publications and source records attributed to M Kanao.

54 records · Page 3Linked to original sources

[Evaluation of cefotetan in obstetrics and gynecology].

Fundamental and clinical studies on gynecological use of cefotetan (CTT), a new cephamycin antibiotic, were performed with following results. Following the intravenous administration of 2.0 g of CTT, T 1/2 beta in serum was 3.1 hours and longer than the previous cephamycin antibiotics. The yields of CTT from serum to various uterine tissues and discharge from retroperitoneum were about 30 approximately 50%. In clinical use, 14 patients with gynecological infections were administrated CTT, and it showed excellent or good efficacy in all patients. No side effects were noted except 1 transient disturbance in liver function.

Adult↗

[Fundamental and clinical studies on T-1982 (cefbuperazone) in the field of obstetrics and gynecology].

Fundamental and clinical studies were carried out on T-1982 (cefbuperazone) a new cephamycin antibiotic, with the following result. Following a single intravenous administration of 1.0 g of T-1982, the transfer of T-1982 to the internal genital organs was found to be good. The transfer of T-1982 to retroperitoneal fluid was also good. In clinical trial, T-1982 was administered to 10 patients with obstetrical and gynecological infection. Efficacy was excellent in 4 cases and good in 6 cases. No side effects were observed. In laboratory findings, a transient elevation of alkaline phosphatase was noted in 1 case.

Adult↗

[Experimental and clinical studies on latamoxef during the perinatal period].

Fundamental and clinical studies on the perinatal use of latamoxef (LMOX) were performed, with the following results. Concentration of LMOX was examined in maternal serum, umbilical cord serum and amniotic fluid after intravenous administration of 2 g dose. Data were analyzed by the simulation curves using the two-compartment model. The peak level of LMOX in maternal serum was 218.4 micrograms/ml and half-life of the beta-phase was 1.9 hours. The peak levels of LMOX in umbilical cord serum and amniotic fluid were 37.4 micrograms/ml (1.4 hours) and 27.5 micrograms/ml (8.9 hours) after administration. The concentration of LMOX in amniotic fluid decreased in amount after the peak, but it still remained 21.9 micrograms/ml (16 hours) after administration. Above these results, it was concluded that the transfer of LMOX to umbilical cord serum and to amniotic fluid was sufficient. In clinical use, LMOX was administered to 30 pregnant patients with premature rupture of membrane. It showed excellent efficacy in preventing perinatal infection. Seven patients with perinatal infections were treated with LMOX and all of them had excellent efficacy. No side effects were observed in any of the cases studied.

Adult↗

Spasmolytic agents. 2. 1,2,3,4-Tetrahydro-2-naphthylamine derivatives.

N-[(Benzoyloxy)alkyl]-1,2,3,4-tetrahydro-2-naphthylamine derivatives were synthesized from 1,2,3,4-tetrahydro-2-naphthylamines and evaluated for their spasmolytic. Some of these compounds showed a nerve-selective effect on colon rather than stomach in anesthetized dogs and were found to be equal to or more active than the reference drug (mebeverine). The biological data have indicated some structure-activity relationships. Among these compounds, N-ethyl-N-[6-(3,4-dimethoxybenzoyl)oxy]hexyl]-1,2,3,4-tetrahydro-6-methoxy-2- napththylamine hydrochloride (63) was found to be the most active spasmolytic agent.

Animals↗

[Fundamental and clinical studies on piperacillin in the field of obstetrics and gynecology].

We conducted a study on the utility in the obstetric and gynecological field of piperacillin (PIPC) which is a broad spectrum penicillin developed here in Japan. After administration of PIPC by intravenous one shot injection or intravenous dripping infusion the yield of PIPC to the various uterine tissues was a favorable 30 approximately 40% in comparison with the serum concentration and the discharge from retroperitoneum was about 100% to 300% in 4 hours. Thus it is thought to be useful in the treatment of infections of the retroperitoneum. During a clinical trial PIPC was administered to 16 patients with obstetrical and gynecological infections and it proved to be excellent in 4 patients, good in 10 patients and ineffective in 2 patients. Thus an overall efficacy rate of 87.5% was obtained. The only side effects observed was a slight transitory abnormality of liver function in 2 patients. Thus in the overall evaluation, this drug was considered to be useful in the treatment of infections in the obstetric and gynecological field.

Adult↗

[Experimental and clinical studies of cefmenoxime in the field of obstetrics and gynecology].

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.

Adolescent↗

[Fundamental and clinical studies on cefotaxime in the perinatal period].

Fundamental and clinical studies on the perinatal use of cefotaxime (CTX, HR-756), a new cephalosporin antibiotic, were done, with the following results. 1. Following intravenous administration of 2 g of CTX, transport of CTX from maternal serum to umbilical cord serum and to amniotic fluid was found to be good. CTX was not transferred into mother's milk. 2. In clinical use, CTX was given to 16 pregnant patients with premature rupture of the membrane. It showed excellent efficacy in preventing perinatal infection. Five patients with perinatal infections were administered CTX, and in 4 patients CTX had good efficacy. No side effects were noted in any cases.

Amniotic Fluid↗

[Fundamental and clinical studies on cefotaxime in the field of obstetrics and gynecology (author's transl)].

Fundamental and clinical studies were made on cefotaxime (HR-756, CTX), a new cephalosporin antibiotic, with the following results. 1. Cefotaxime was given to 22 patients. Efficacy was excellent in 3 cases, good in 17 cases and poor in 2 cases. No side effects were observed in any cases. 2. Following a single intravenous injection of 1.0 or 2.0 g, the transfer of CTX to the internal genital organs was found to be good. The transfer of CTX to exudate of the dead space of pelvis was also good. 3. The above data demonstrated that CTX is a safe and effective drug.

Adult↗

[Clinical studies on cefoperazone in gynecological and obstetrical field (author's transl)].

Fourteen patients suffering from female genital organ infections including mastitis and urinary tract infections were treated with cefoperazone (CPZ). CPZ was administered intravenously or by drip infusion at a dose of 2.0-4.0 g/day for 3-7 days. Clinical results obtained were as follows: Of 8 patients with genital organ infections, excellent responses were seen in 2 patients, good responses in 5 patients. Of 3 patients with mastitis, good responses were seen in all the patients. Of 3 patients with pyelonephritis, excellent and good responses were seen in all the patients. No adverse effects and abnormal laboratory findings were observed. From the above results, we concluded that CPZ was an effective and safe antibiotic against infections in the field of obstetrics and gynecology.

Adolescent↗

A novel pharmacokinetic method for analysis of placental transfer of latamoxef in humans.

A novel pharmacokinetic method was developed for analysing the behaviour of a drug in tissues. The absolute transfer ratio of a drug to a tissue was defined using the pharmacokinetic parameters obtained by this method. Composite data of latamoxef (moxalactam) concentration in maternal blood, umbilical cord blood and amniotic fluid following a 2g intravenous injection to pregnant women at delivery were analysed by this method to study the drug behaviour in pregnant women, fetuses and amniotic fluid. Latamoxef kinetics in pregnant women at full term were generally similar to that in previously reported healthy subjects. The concentration of latamoxef in umbilical cord blood peaked about 2 hours after dosing then decreased in parallel with the maternal blood concentration. The amniotic fluid concentration peaked about 7 hours after administration, then decreased slowly. The absolute transfer ratios to fetus and amniotic fluid were calculated to be about 2.5 and 0.37% respectively.

Amniotic Fluid↗

Identification of DP-1904 and its ester glucuronide in human urine and determination of their enantiomeric compositions by high-performance liquid chromatography with optical activity and ultraviolet detection.

The parent compound and one metabolite have been isolated from urine of five healthy male volunteers who received a single 200 mg oral dose of DP-1904. These compounds were extracted by using a Sep-Pak C18 cartridge and purified by the preparative HPLC method. On the basis of proton magnetic resonance and mass spectral data, unchanged drug and its ester glucuronide have been identified in human urine. DP-1904 has one asymmetric carbon and is used as a racemate in the current clinical trial. The enantiomeric compositions of unchanged DP-1904 and aglycon of DP-1904 glucuronide were determined by HPLC with optical activity and ultraviolet detection. The (R)-(+)-enantiomer percentages in unchanged DP-1904 and aglycon of its ester glucuronide in human urine collected at 0-4 hr after oral dosing were 60 +/- 1.3% and 38 +/- 1.4% (mean +/- SE, n = 5), respectively. The 0-4 hr urine collection represented approximately 80% of the given dose. These studies demonstrate that DP-1904 undergoes stereoselective disposition in humans. However, the difference in urinary excretion between DP-1904 enantiomers was rather small.

Chromatography, High Pressure Liquid↗