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Biomedical subjects

H Okada

Publications and source records attributed to H Okada.

At least 1,027 records · Page 57Linked to original sources
PubMed1986

[Study on tissue transfer of ceftizoxime suppository in the field of obstetrics and gynecology].

A pharmacokinetic study on ceftizoxime suppository (CZX-S), a new rectal suppository of ceftizoxime (CZX), was carried out in the field of obstetrics and gynecology. Concentrations of CZX after single rectal administrations of a 500 mg dose in peripheral venous serum, uterine arterial serum and internal genital organs of 15 patients who received simple panhysterectomy were examined. Peak levels of CZX in peripheral venous serum were 7.26 to 8.88 micrograms/ml at 30 minutes after the administration. Concentrations of CZX in internal genital organs reached 2.12 to 8.96 micrograms/g at 30 minutes after the administration and then decreased slowly, but still remained at 0.37-3.12 micrograms/g after 4 hours.

Adult↗
PubMed1986

[Fundamental and clinical studies on imipenem/cilastatin sodium in the field of obstetrics and gynecology].

Fundamental and clinical studies on imipenem/cilastatin sodium (MK-0787/MK-0791), a new carbapenem antibiotic, were performed and the following results were obtained. Concentrations of MK-0787 and MK-0791 in serum, internal genital organs and retroperitoneal fluid were determined after a 30 minutes drip infusion of 500 mg/500 mg dose. Venous serum levels of MK-0787 and MK-0791 were 47.3 to 67.5 micrograms/ml and 44.2 to 61.4 micrograms/ml, respectively, at the end of the administration. Sufficient transfer of MK-0787 and MK-0791 to internal genital organs and retroperitoneal fluid was demonstrated. In clinical trials, MK-0787/MK-0791 was given to 18 cases with obstetrical and gynecological infections, such as endometritis, puerperal fever, pelvic peritonitis, parametritis and lymphocystitis. The clinical efficacy was evaluated as excellent in 1 case, good in 14 and poor in 3. The efficacy rate was 83.3%. In a bacteriological study, 43 strains were isolated from 16 cases and the eradication rate was 61.1%. No side effects were observed in any of the cases. In laboratory findings, a transient elevation of GOT, GPT was noted in 1 case. From the above results, it was concluded that MK-0787/MK-0791 was useful drug for infections in the field of obstetrics and gynecology.

Adult↗
PubMed1986

[Pharmacokinetic and clinical studies of cefotiam in the perinatal period].

Pharmacokinetic and clinical studies on cefotiam (CTM) in the perinatal period were performed and results obtained are summarized below. Concentrations of CTM in maternal serum, umbilical cord serum and amniotic fluid were examined after a bolus intravenous administration at a dose of 1 g. Data were analyzed using simulation curves drawn by the two- or three-compartment open model. The peak level of CTM in maternal serum was 86.6 micrograms/ml and the half-life of the beta-phase was 0.91 hour. Peak levels of CTM in umbilical cord serum and amniotic fluid were 20.8 micrograms/ml at 0.1 hour and 9.2 micrograms/ml at 3.2 hours after the administration, respectively. The concentration of CTM in amniotic fluid decreased after reaching the peak, but it was still as high as 1.6 micrograms/ml even at 12.0 hours after the administration. These results clearly demonstrated that the transfer of CTM to umbilical cord serum and to amniotic fluid was efficient in protection of perinatal infections. In a clinical trial, CTM was given to 11 patients with perinatal infections. Clinical efficacies were evaluated as excellent in 2 patients, good in 8 patients and poor in 1 patient. No adverse effects were observed in any of the patients studied. In conclusion, CTM was useful and safe antibiotic for the treatment of infections in the perinatal period.

Amniotic Fluid↗
PubMed1986

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

Fundamental and clinical studies were carried out on ceftazidime (CAZ) in the perinatal period, and the results obtained were summarized below. Following bolus intravenous injection of CAZ 2 g, maternal serum concentrations of CAZ were as high as 145.3 +/- 17.2 micrograms/ml (mean +/- S.D.) at about 10 minutes, and then gradually decreased to 46.7 micrograms/ml at 2 hours, 5.31 micrograms/ml at 5 hours and 4 minutes, and 1.54 micrograms/ml at 11 hours and 10 minutes. The CAZ was detected in umbilical cord serum immediately after the administration, and concentrations were 31.0 +/- 1.54 micrograms/ml at about 10 minutes. Although the concentrations gradually decreased thereafter, they were higher than those in maternal serum at 3 hours and later and was 3.00 micrograms/ml at 11 hours and 10 minutes. The CAZ was detected in amniotic fluid a little later than in umbilical cord serum, and concentrations of CAZ in amniotic fluid were as low as 1.50 +/- 0.67 micrograms/ml at about 10 minutes after the administration. Concentrations then gradually increased to 12.8 micrograms/ml at 2 hours and 26.5 micrograms/ml at 5 hours and 4 minutes, and even at 11 hours and 10 minutes, they were as high as 14.2 micrograms/ml. The above results demonstrated that the transfer of CAZ through placental barrier was very rapid and satisfactory. Also, CAZ showed good transfer into amniotic fluid, as well as sufficient retention, and was considered to be an effective antibiotic for prophylaxis of both fetal infections and amniotic fluid infections.(ABSTRACT TRUNCATED AT 250 WORDS)

Adult↗
PubMed1986

Comparison of the subacute effects of a new glucocorticoid, deflazacort, and prednisone on the hypothalamic-pituitary-adrenal axis of normal subjects.

The effects of deflazacort (DFL), a new oxazoline derivative of prednisolone, were compared with those of prednisone (Pd) by measuring plasma cortisol (F) levels as an index of the function of the hypothalamic-pituitary-adrenal (HPA) axis. Twelve normal volunteers received each glucocorticoid for 16 to 24 days in a double-blind cross-over trial with random allocation of subjects to treatment with DFL (24 mg/day) and Pd (20 mg/day) in clinically equivalent doses, with a washout period from 20 to 45 days between administration of the glucocorticoids. The following tests were performed in a randomized sequence: cortisol (F) circadian rhythm, insulin tolerance test (ITT), lysine-vasopressin (LVP) and B1-24 ACTH stimulation. Despite basal F suppression by DFL, the relative maximum F response (maximum F increment above basal/basal x 100) was significantly greater than control for the ITT and ACTH tests and was similar to the control after intramuscular injection of LVP, suggesting that the responses were appropriate for the basal F levels, with the HPA being reset at a lower level. After Pd, despite higher basal F levels, the F diurnal rhythm disappeared and there was no significant response to ITT, LVP or ACTH, indicating that the limiting factor in the HPA response was the reduced adrenal F production independent of the effects on the steroid-sensitive tissues of the brain including the pituitary.

Adult↗
PubMed1986

Steroid receptors in uterine cervical cancers.

In cervical cancers, the estrogen receptor (ER) and progestin receptor (PR) were characterized in the cytosol protein. Receptor levels were determined in cytosol, nuclear KCl extract, and nuclear KCl unextractable fraction in various cervical cancer tissues. The androgen receptor (AR) was also similarly characterized. In the cytosol, the estrogen (E2)-ER complex and the promegesterone (R5020)-PR complex were sedimented at approximately the 5S and 8S or the 4S and 8S regions, respectively, by 5-20% linear sucrose gradient centrifugation. A steroid specificity study showed the presence of an estrogen-specific and a progestin-specific binder. The dissociation constant of the specific binder for estrogen (ER), progestin (PR), or androgen (AR) was approximately 10(-10) to 10(-9)M in cytosol, nuclear KCl, and nuclear KCl unextractable fraction in detected cases. Levels were determined by Scatchard analyses, using the dextran-coated charcoal (DCC) adsorption method for the former two and the washing method for the latter one. ER, PR, or AR was detected in some cases of determined cervical cancers (27 cases of squamous cell carcinoma, and 7 cases of adenocarcinoma); regardless of the histological types, ER was detected in almost all cases. PR was not detected in the given cases of cervical adenocarcinoma. It is suggested that estrogen stimulation of PR synthesis in cervical adenocarcinoma may be damaged.

Adenocarcinoma↗
PubMed1986

[Relations between neonatal heart rate variability and the behavioral state].

In sixty healthy newborn infants the relations between the neonatal heart rate variability (NHRV) and the behavioral state were investigated. The infants were divided to subsequent two subgroups according to the mode of delivery. One was normal vaginal delivery (N = 47), and the other was elective cesarean section (N = 13). R-R intervals less than 280 msec and more than 700 msec were excluded. The maximum difference in successive R-R intervals accepted was 60 msec. The standard deviation of R-R intervals as LTV index and the mean of absolute beat to beat difference as STV index were calculated with a minicomputer. The behavioral states were classified according to Prechtl's criteria. The LTV in state 2 and state 4 increased progressively and reached its maximum level on the third day after birth. The change of STV was neither consistent nor significant. In state 5, both the STV and the LTV were very low. The discriminant function gave percentages of correct classification of 85-100% for the active quiet states. The NHRV was similar in state 1 and state 3, and in state 2 and state 4 respectively. There was an increase in the LTV during the 24 hours after birth in the CS group. Thus, neonatal adaptation of CS differs from that of normal labor.

Adaptation, Biological↗
PubMed1986

Cellular existence of estrogen receptor in C3H mouse mammary tumor.

Estrogen receptor (ER) in the C3H mouse mammary tumor was characterized in the cytosol and determined in the nuclear KCl extract and the nuclear KCl unextractable fraction (non-extract). In the cytosol, the estradiol (E2)-ER complex was sedimented in the 8S region by 5-20% linear sucrose gradient centrifugation. A steroid specificity study showed the presence of estrogen-specific binder with a dissociation constant (Kd) of approximately 2 nM. ER levels in the cytosol, the nuclear KCl extract, and the suspension of nuclear KCl unextractable fraction were determined by Scatchard analyses, using the dextran-coated charcoal (DCC) adsorption method for the former two and the sedimentation method for the latter. Although ER was present in the nuclear fractions, it seems more plausible that cytosol ER contributes to nuclear translocation of the estrogen-ER complex. The results suggest the presence of an intranuclear mechanism for the estrogen action.

Animals↗
PubMed1986

[A case of leiomyosarcoma of the kidney].

Leiomyosarcoma of the left kidney seen in a 58-year-old man is reported. On April 10, 1982, he complained of left flank pain. He visited our hospital and left solitary renal cyst was suspected. He had been treated as an outpatient, but left flank pain became exacervated. On May 18, he was admitted to our hospital. On June 7, radical nephrectomy was done under the diagnosis of left renal cell carcinoma. At operation, the tumor invased directory to the psoas muscle and abdominal wall, and could not be completely resected. Pathological diagnosis was renal cell carcinoma with sarcomatoid change. On July 1, he was discharged from the hospital. In December, left flank distention appeared and back pain became exacervated. On February 8, 1983, he was readmitted to our hospital. Low density area was found in left psoas muscle by CT scanning and recurrence of renal cell carcinoma was suspected. alpha-Interferon therapy had been done, but tumor increased remarkably and caused ileus. He died on June 14, 1983. The autopsy revealed a child head-sized cystic tumor in the upper retroperitoneal space, a 5 X 5 X 5 cm metastasis of the left lobe of the liver, a 3 X 3 X 4 cm tumor to the left upper lobe with cavity formation and direct invasion into the spleen, diaphragma and gastric serosa. These metastatic lesions were leiomyosarcoma. Retrospectively, the primary tumor of kidney revealed primary leiomyosarcoma of kidney.

Diagnosis, Differential↗
PubMed1985

[The relationship between changes of the steroid receptor and synchronization in human adenocarcinoma cells in vitro of the endometrium].

We investigated the G1 and S phases of synchronization using sodium n-butyrate, MTX and excess thymidine. The flow cytometry system was employed for cell cycle analysis while the receptor assay was adopted dextran coated charcoal (DCC) and the wash method. The results were as follows: S phase synchronization by MTX was 138% (control 100%) and by excess thymidine in the block and release method 210%. G1 phase synchronization by sodium n-butyrate was 140%. The progesterone receptor level, by E2 priming increased to 1.45 fmol/ug DNA being more than five times that of the control PR. The estrogen receptor level increased to 18.29 fmol/ug DNA in the G1 phase synchronization, seven times that of the control ER. From this study, the functional increase of the steroid receptor was most significant in the G1 phase.

Adenocarcinoma↗
PubMed1985

Synthesis of poly(ethylene glycol)-bound NADP by selective modification at the 6-amino group of NADP.

The N-1 position of the adenine ring of NADP was selectively alkylated by the reaction of 2',3'-cyclic NADP with 3-propiolactone to yield 2',3'-cyclic 1-(2-carboxyethyl)-NADP (I). Derivative I was converted to a mixture of the isomers of N6-(2-carboxyethyl)-NADP with their phosphate groups at the 2' or 3' position (IIa and IIb) by chemical reduction, alkaline rearrangement and chemical reoxidation. Carbodiimide coupling of the mixture of IIa and IIb to alpha, omega-diaminopoly(ethylene glycol) gave the 2', 3'-cyclic derivative of poly(ethylene glycol)-bound NADP (III), which was enzymically hydrolyzed to yield poly(ethylene glycol)-bound NADP (PEG-NADP). PEG-NADP has good cofactor activity (16-100% of that of NADP) for NADP-specific and NAD(P)-specific dehydrogenases except isocitrate and glucose dehydrogenases. For NAD-specific enzymes, PEG-NADP has higher cofactor activity than NADP: for horse liver alcohol dehydrogenase, the cofactor activity of PEG-NADP is 40 times that of NADP and 14% of that of NAD. Kinetic studies show that for most of enzymes tested, Km values for PEG-NADP are larger than those for NADP and V values for PEG-NADP are similar to those for NADP. PEG-NADP proved to be applicable in a continuous enzyme reactor, in which reactions of glutamate dehydrogenase and glucose-6-phosphate dehydrogenase were coupled by the recycling of PEG-NADP.

Alkylation↗
PubMed1985

Preparation and characterization of NADP derivatives alkylated at 2'-phosphate and 6-amino groups.

Reaction of NADP with 3-propiolactone at pH 6 gave new NADP derivatives carboxyethylated at the 2'-phosphate or 6-amino group, or both: 2'-O-(2-carboxyethyl)phosphono-NAD (I), N6-(2-carboxyethyl)-NADP (II), and 2'-O-(2-carboxyethyl)phosphono-N6-(2-carboxyethyl)-NAD (III). Their structures were assigned on the basis of ultraviolet, 1H-NMR and 31P-NMR spectra, and also treatment with nucleotide pyrophosphatase or alkaline phosphatase. Carbodiimide-promoted reaction of derivative I with 1,2-diaminoethane gave 2'-O-[N-(2-aminoethyl)carbamoylethyl]phosphono-NAD (IV); derivative III gave 2'-O-[N-(2-aminoethyl)carbamoylethyl]phosphono-N6-[N-(2-aminoethyl ) carbamoylethyl]-NAD (IV). The same reaction of derivative II, on the other hand, gave a mixture of N6-[N-(2-aminoethyl)carbamoylethyl]-NADP (Va) and its 3'-phosphate isomer (Vb). The mixture was converted to Va via the 2',3'-cyclic derivative (Vc). Their structures were assigned on the basis of ultraviolet and 1H-NMR spectra, and also treatment with alkaline phosphatase or 3'-nucleotidase. All the NADP derivatives obtained in this work could be reduced with yeast glucose-6-phosphate dehydrogenase.

Alkylating Agents↗
PubMed1985

Coenzymic activity of NADP derivatives alkylated at 2'-phosphate and 6-amino groups.

Coenzymic activities of the following NADP derivatives were investigated: 2'-O-(2-carboxyethyl)phosphono-NAD (I), N6-(2-carboxyethyl)-NADP (II), 2'-O-(2-carboxyethyl)phosphono-N6-(2-carboxyethyl)-NAD (III), 2'-O-[N-(2-aminoethyl)carbamoylethyl]phosphono-NAD (IV), N6-[N-(2-aminoethyl)carbamoylethyl]-NADP (Va), 2',3'-cyclic NADP, and 3'-NADP. Derivatives I and IV show the effects of modification at the 2'-phosphate group, and derivatives II and Va show those at the 6-amino group of NADP. As for enzymes, alcohol, isocitrate, 6-phosphogluconate, glucose, glucose-6-phosphate, and glutamate dehydrogenases were used. These enzymes were grouped on the basis of the ratio of the activities for NAD and NADP into NADP-specific enzymes (ratio less than 0.01), NAD(P)-specific enzymes (0.01 less than ratio less than 100), and NAD-specific enzymes (ratio greater than 100). For NADP-specific enzymes, modifications at the 2'-phosphate group of NADP caused great loss of cofactor activity. The relative cofactor activities (NADP = 100%) of derivatives I and IV for these enzymes were 0.5-20 and 0.01-0.5%, respectively. On the other hand, NAD(P)-specific enzymes showed several types of responses to the NADP derivatives. The relative cofactor activities of I and IV for Leuconostoc mesenteroides and Bacillus stearothermophilus glucose-6-phosphate dehydrogenases and beef liver glutamate dehydrogenase were 60-200%; whereas, for B. megaterium glucose dehydrogenase and L. mesenteroides alcohol dehydrogenase, the values were 0.8-8%. For NAD-specific enzymes, these values were 20-50%. The relative cofactor activities of 2',3'-cyclic NADP and 3'-NADP were very low (less than 0.2%) except for beef liver glutamate dehydrogenase, B. stearothermophilus glucose-6-phosphate dehydrogenase, and horse liver alcohol dehydrogenase. Kinetic studies showed that the losses of the cofactor activity of NADP by these modifications were mainly due to the increase of the Km value. The mechanisms of coenzyme specificity of dehydrogenases are discussed. Unlike the 2'-phosphate group, the 6-amino group is common to NAD and NADP, and the effects of modification at the 6-amino group were independent of the coenzyme specificity of enzymes used for the assay. Derivatives II and Va had high relative cofactor activities (65-130%) for most of the enzymes except for isocitrate and glucose dehydrogenases (less than 1%) and L. mesenteroides alcohol dehydrogenase (20-60%). The cofactor activity of derivative III was generally lower than those of I and II.

Alkylation↗
PubMed1985

Aromatization of androstenedione by normal and neoplastic endometrium of the uterus.

The ability of human uterine endometrium to aromatize androstenedione to estrogens was investigated using 10 normal and neoplastic tissues. Normal and neoplastic endometrial homogenates were incubated with [6,7-3H]androstenedione (A) and NADPH. Estrone (E1) and estradiol (E2) were subsequently isolated in amounts ranging from 0-17600 fmol/h/g and 0-377 fmol/h/g, respectively, from the incubates after purifications by using Bio-Rad AG1-X2 column, thin layer chromatographies and co-crystallization. The conversion of A to E1 and E2 was significantly higher in neoplastic tissues.

Adult↗