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Biomedical subjects

S Usuki

Publications and source records attributed to S Usuki.

102 records · Page 6Linked to original sources

Metabolic fate of the new cardiotonic denopamine in animals. 2nd communication: tissue accumulation in the rat after consecutive oral administration of 14C-denopamine.

Accumulation characteristics of (-)-(R)-1-(p-hydroxyphenyl)-2-[(3,4-dimethoxyphenethyl)amino]ethanol (denopamine, TA-064) in organs and tissues were investigated after oral administration of 14C-denopamine to rats once a day (5 mg/kg/d) for 1, 6 and 10 days. The levels of radioactivity in each organ and tissue were measured at various time intervals after the final dose. The levels of radioactivity at 15 min after administration were generally higher in the consecutive-dose groups than in the single-dose group. However, the levels were equilibrated within 6 days of administration. Radioactivity at 24 h after administration decreased to about the detection limit in each group. In addition, half-lives of disappearance of radioactivity from the body were not significantly affected by the consecutive doses. About 100% of the dose was recovered from the urine and feces during consecutive administration periods. Consequently, it was considered that the drug hardly showed retention and accumulation characteristics in the body.

Administration, Oral↗

[Clinical studies on aztreonam in various infections in obstetrics and gynecology].

Aztreonam (AZT) was administered to 10 patients with obstetric and gynecologic infections to evaluate its clinical effect. Two-four grams of AZT per day (b.i.d.) were administered for the treatment for 4-15 days by intravenous drip infusion or intravenous injection. AZT was effective for 3 cases of pelvic peritonitis, 1 case of pyoovarium and 2 cases of Bartholin's abscess. For 2 cases of intrauterine infection, AZT was effective for 1 case, and the other case could not be judged. For 2 cases of local infection, AZT was effective for 1 case and ineffective for 1 case. Efficacy rate was 89% for the 9 cases excluding the 1 unevaluable case. Microbiological effect was determined for 4 out of 10 cases. Two strains of Haemophilus influenzae and one each of Escherichia coli, Bacteroides fragilis and Streptococcus intermedius were isolated, but all of them were eliminated for a elimination rate of 100%. Neither abnormal laboratory findings in hepatic or renal functions, etc. nor side effects were recognized.

Adult↗

[Application of cefpimizole in obstetrics and gynecology].

We made fundamental and clinical studies of a new cephalosporin derivative, cefpimizole (AC-1370). AC-1370 was relatively efficiently transferred into the uterine adnexa; in other words, it was as well transferred into the tissues as the other cephalosporin derivatives. There seemed to be no specific relation between its blood level and its level in any tissue. In 1 patient treated with AC-1370 for postoperative infection, clinical findings, WBC and CRP improved: the drug was evaluated as effective. Neither hepatic nor renal function was impaired in the patients treated with AC-1370 in the fundamental and clinical studies of the drug.

Adult↗

Metabolism of afloqualone, a new centrally acting muscle relaxant, in monkeys and dogs.

The disposition and metabolism of afloqualone [6-amino-2-fluoromethyl-3-(o-tolyl)-4(3H)-quinazolinone, AFQ] were studied in monkeys and dogs after oral administration of 14C-AFQ. In both species the blood radioactivity reached a maximum 1 to 2 h after the administration, and decreased with apparent half-lives of 3.2 h in the monkey and 7.2 h in the dog. A total of about 90% of the administered radioactivity was recovered from the urine (monkey, 72.3%; dog, 51.8%) and feces (monkey, 19.4%; dog, 36.7%) within 4 or 5 d. AFQ was extensively metabolized in both species. There were species differences in the composition of the urinary metabolites. In the dog, AFQ was monohydroxylated at the 2-, 2'-, 3'- and principally 4'-position and each metabolite was further conjugated with glucuronic acid. N-Acetylated metabolites were not detected. In the monkey, N-acetylation was the main initial step of metabolism followed by hydroxylation at the acetyl-methyl, 2'-methyl and 2-fluoromethyl groups. Phenolic metabolites such as 3'- and 4'-hydroxylated AFQ were not detected. Both animals excreted sulfur-containing metabolites such as the 2-methylthio, 2-methylsulfinyl and 2-methylsulfonyl derivatives of AFQ.

Animals↗

[Studies on the etiology of infectious disease of female internal genitalia - bacterial flora in the female genitalia and surrounding tissues].

The present studies were carried out to clarify the indigenous bacterial flora in the female internal genitalia and surrounding tissues and the pathogenesis of parametritis. Twenty nine patients with uterine tumors which consisted of sixteen carcinomas and thirteen benign tumors underwent abdominal total hysterectomies. Each tissue aseptically collected from the uterus and adnexae was cultured for 48 hours under aerobic or anaerobic conditions and the bacterial species were isolated and identified. In benign uterine tumors, anaerobic bacteria were isolated in six patients and aerobic or anaerobic bacteria were identified In the endometrium, fallopian tube and parametrium of five of the patients. In a group of carcinoma in situ (stage 0), many bacteria were isolated in two patients after conization. In the uterine carcinomas, as the stage advanced, the rate of bacterial isolation from parametrium and lymph node became higher. The rate of anaerobic bacterial isolation, except for one from the vagina, was nine out of sixteen patients with carcinomas but three out of thirteen patients with benign tumors. The results revealed that the bacterial flora in the vagina spread to the internal genital organ and surrounding tissues via the ascending or cervical lymphatic pathway and remained there as nonpathologically indigenous bacterial flora. These results suggest that these indigenous bacterial flora in the internal genitalia and the surrounding tissue may cause an opportunistic infection.

Adult↗

[Gonadotropic regulation of estrogen secretion by rat ovarian follicles (author's transl)].

The present studies were carried out to clarify the mechanisms of estrogen secretion by ovarian follicles. Rats of the Wistar-Imamichi strain at 27 days of age were treated subcutaneously with 75 IU of PMS. Ovaries were resected 24 or 48 hours after treatment and incubated for 2 hours or perifused for 5 hours using medium-199 containing ovine NIH-LH and NIH-FSH at 37 degrees C. Concentration of steroids in medium and tissue was determined by RIA. Estradiol 17-beta (E2) concentration in the perifusion effluent rose markedly following LH stimulation and rose slightly following FSH or dibutyryl cyclic-AMP stimulation. Prolactin, ACTH, PG E2 and PG F2 alpha were noneffective. LH appeared to stimulate slightly progesterone and androgen secretion by ovaries perifused. The stimulatory effects of LH on E2 secretion disappeared in ovaries from which follicular fluids were removed by punctuation with a small needle. E2 concentration in incubation medium and the total amount of E2 concentration in medium and tissue were significantly increased by treatment of LH, while the concentration in tissue was decreased by the treatment. However, LH showed no effect on E2 concentration in incubation medium and tissue of ovaries with punctured follicles. These results suggest that in the fully developed follicles LH stimulates the release of E2 stored in follicular fluids, in addition to E2 biosynthesis. E2 granules were stained by an enzyme-labeled antibody technique. They were observed only in the thecal or interstitial cells of ovaries 24 hours after PMS injection and then 48 hours after injection they also appeared in the granulosa cells either. These results suggest that in the fully-developed follicles E2 is produced in the thecal and granulosa cells and stored in follicular fluids.

Animals↗