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Biomedical subjects

T Murai

Publications and source records attributed to T Murai.

At least 271 records · Page 15Linked to original sources
PubMed1986

Generalized granulomatous arteritis with aortic dissection.

A 56 year-old Japanese woman died suddenly after complaining of abdominal pain. Autopsy revealed typical aortic dissection with cardiac tamponade. Histologically, generalized granulomatosis with giant cells resembling sarcoidosis was found. The aorta was most strikingly affected so that granulomatous aortitis was regarded as the cause of the aortic dissection.

Aorta↗
PubMed1985

[Experimental and clinical studies on BRL 25000 (clavulanic acid-amoxicillin) granules in the pediatric field].

Fundamental and clinical studies have been performed on BRL 25000 (clavulanic acid 1 part-amoxicillin 2 parts) granules in the pediatric field. The antibacterial activities of BRL 25000 and amoxicillin (AMPC) were investigated against clinically isolated and laboratory stocked strains. BRL 25000 was superior to AMPC against strains of E. coli, Salmonella sp. and Klebsiella sp., and similar against Gram-positive cocci. Serum concentrations of AMPC and clavulanic acid (CVA) were measured 0.25, 0.5, 1, 2, 4 and 6 hours after administration of BRL 25000 granules at dose levels of 7.5, 10, 15 and 20 mg/kg. At 7.5 mg/kg peak level of AMPC of 2.69 micrograms/ml was achieved about 2 hours after dosing with a biological half-life of 1.64 hours; corresponding value for CVA was 0.53 micrograms/ml at 1 hour with a T 1/2 of 1.46 hours. At 10 mg/kg, AMPC also peaked after 2 hours (3.82 micrograms/ml) and the T 1/2 was 1.63 hours, whilst for CVA the value was 0.56 micrograms/ml with a T 1/2 of 1.24 hours. Value for AMPC at 15 mg/kg was 5.18 micrograms/ml at 1 hour post dose with a T 1/2 of 1.48 hours, and for CVA 4.01 micrograms/ml at 1 hour with a T 1/2 of 0.89 hour. At the highest dose of 20 mg/kg, AMPC level reached 4.21 micrograms/ml after 2 hours with a T 1/2 of 2.39 hours, and the CVA peak was 1.64 micrograms/ml at 1 hour with a T 1/2 of 1.01 hours. The 6 hours urinary recovery of AMPC and CVA following administration of the BRL 25000 granules ranged from 38-64% and 2-33%, respectively. In the clinical studies, the BRL 25000 granules are administered to 15 cases with pediatric infections and the clinical response was excellent or good in all cases treated (100%). Bacteriological investigation was performed on 13 strains from 12 cases and all strains were eradicated (100%). Regarding side effects, elevation of eosinophil was observed in 1 case and vomiting in 3 cases.

Administration, Oral↗
PubMed1985

[Fundamental and clinical studies of ceftizoxime suppositories in the pediatric field].

The fundamental and clinical studies of ceftizoxime suppository (CZX-S) in the field of pediatrics were made, with the following results. The serum concentration of CZX in the CZX-S 250 mg-administered group peaked 6.00-22.5 micrograms/ml during the period of 15 minutes to 1-hour after dosing, and gradually declined thereafter. The half-life was 1.37-3.81 hours. In the CZX-S 125 mg-administered group, the serum concentration peaked 2.25-21.0 micrograms/ml at 15-30 minutes after dosing and decreased with time. The half-life was 0.95--1.84 hours. The 6-hour urinary recovery rate of CZX in the CZX-S 250 mg group was 22.0-47.5%. The 6-hour urinary recovery rate in the CZX-S 125 mg group was 17.2-25.3%. CZX-S was given 12-73 mg/kg/day (divided into 1-3 times) to 7 children with respiratory tract infection etc. who were considered to respond well to the drug. The clinical effectiveness rate was 100% inclusive of "excellent" and "good". The side effect of pain on insertion was encountered in 1 child.

Bacterial Infections↗
PubMed1985

[Intra-arterial infusion chemotherapy combine with noradrenalin administration (an improved antitumor effect using a cancerous blood vessel].

We have performed experimental and clinical studies to observe whether higher concentrations of drugs are selectively delivered into tumor tissues through the tumor vessels and improved chemotherapy results were obtained by using noradrenaline in intraarterial chemotherapy. Noradrenaline administered into the tumor-feeding artery may enhance drug delivery into the tumor tissue and show improved chemotherapy results on Walker-256 formed tumor vessels. These advantages of using vasoconstrictive agents may be considered to be derived from the high injection pressure caused by increased vascular resistance and various other factors induced in abnormal microcirculation of the tumor vessels. MMC concentration in Walker-256 (weight 0.2 to 0.39 g) after intraarterial administration of 10 mg of MMC in 2.5 ml of physiological saline were 2.20 +/- 1.26 mcg/g (n = 11) in the noradrenaline group and 0.52 +/- 0.22 mcg/g (n = 13) in the MMC alone group. The 90-day survival ratio for intraarterial injection of 0.25 mg/kg of MMC and 2 mcg of noradrenaline was 42.9% (6/14), a result equivalent to a dose range of between 0.50 mg/kg and 0.75 mg/kg without the use of any vasoactive drug. The median survival periods for stomach cancer (Stage 4) after non-radical surgery by means of intraarterial chemotherapy with and without noradrenaline were, respectively, 12 months (n = 8) and 5.8 months (n = 6), with statistical significance (P greater than 0.05). Effective histological changes estimated microscopically by Takahashi's criteria of preoperative treatment in 31 stomach cancer patients were found in 11 patients (36.7%) with primary tumor and 12 patients (52.2%) with metastatic lymph nodes. A partial response rate of 54.5 (6/11) for hepatic tumor (Stages 3 to 4 according to was achieved with the use of the Ariel's classification) following regimen: intravenous injection of 70 mg/body of CDDP on the first day, followed by intraarterial injection of 0.1 to 0.4 mg/kg of MMC and 0.1 to 0.6 mg/kg of ADM together with 0.3 to 1.0 mg of noradrenaline in 40 to 100 ml of physiological saline for 3 to 20 minutes within one week after the first treatment. Most of the complications were due to hemorrhage from ulceration of the intestinal canal because of mucosal damage caused by the high concentration of anti-cancer drugs induced by noradrenaline. Decrease of hemoglobin of more than 1.0 g/dl was found in 19 out of 31 patients (61.3%) who received no treatment for bleeding, and in one out of 13 patients (7.7%) who was administered 200 mg of cimetidine twice a day for one week.

Animals↗
PubMed1984

Inhibitory effect of androgen on the synthesis of proteinase F in the male mouse submandibular gland.

Androgenic regulation of one of the esteroproteinases (proteinase F) in the mouse submandibular gland was studied using specific antiserum. In contrast to esteroproteinases such as proteinases A, D or P-esterase, proteinase F content in male but not in female mice was increased by gonadectomy and decreased by the injection of various androgens. In-vivo incorporation of [3H]leucine into proteinase F in males was increased after castration and decreased by the injection of testosterone propionate; androgens inhibited the de-novo synthesis of proteinase F in male mice. The dose-response curves for testosterone propionate and time-courses following castration or after the injection of testosterone propionate were reciprocal between proteinase F and total esteroproteinase activity. Proteinase F, like other esteroproteinases in the submandibular gland of the mouse, was localized in granular convoluted tubular cells. These data indicate that granular convoluted tubular cells of the male mouse submandibular gland synthesize both androgen-inducible proteinases and androgen-inhibitory proteinase (proteinase F).

Androgens↗
PubMed1984

[Fundamental and clinical evaluation of ceftriaxone in the field of pediatrics].

Fundamental and clinical evaluation on ceftriaxone (Ro 13-9904, CTRX) was performed in the field of pediatrics and the following results were obtained. The antibacterial activity of CTRX was determined against clinically isolated strains at our department. CTRX was definitely superior to CEZ and CMZ and almost equal or slightly superior to CTX in activity against Gram-negative bacteria, while the MIC of CTRX against Gram-positive bacteria was higher than that of CEZ and CMZ and about equal to that of CTX. The blood concentration of CTRX after one shot intravenous injection with 10 mg/kg was 67.98 micrograms/ml at 15 minutes, 51.96 micrograms/ml at 30 minutes, 37.51 micrograms/ml at 1 hour, 28.91 micrograms/ml at 2 hours, 20.71 micrograms/ml at 4 hours, 13.97 micrograms/ml at 6 hours and 6.45 micrograms/ml at 12 hours, while the half-life time was 3.74 hours. The blood concentration of CTRX after one shot intravenous injection with 20 mg/kg was 179.55 micrograms/ml at 15 minutes, 120.01 micrograms/ml at 30 minutes, 100.01 micrograms/ml at 1 hour, 53.75 micrograms/ml at 2 hours, 33.13 micrograms/ml at 4 hours, 26.41 micrograms/ml at 6 hours and 21.49 micrograms/ml at 12 hours, while the half-life time was 4.15 hours. The blood concentration of CTRX after intravenous drip infusion for 1 hour with 10 mg/kg was 19.54 micrograms/ml at 15 minutes, 27.19 micrograms/ml at 30 minutes, 36.57 micrograms/ml at 1 hour, 23.83 micrograms/ml at 2 hours, 19.69 micrograms/ml at 3 hours, 14.46 micrograms/ml at 5 hours, 11.02 micrograms/ml at 7 hours and 7.27 micrograms/ml at 13 hours, while the half-life time was 6.59 hours. The blood concentration of CTRX after intravenous drip infusion for 1 hour with 20 mg/kg was 61.72 micrograms/ml at 30 minutes, 108.1 micrograms/ml at 1 hour, 54.95 micrograms/ml at 2 hours, 35.68 micrograms/ml at 3 hours, 28.13 micrograms/ml at 5 hours, 20.51 micrograms/ml at 7 hours and 11.43 micrograms/ml at 13 hours, while the half-life time was 4.23 hours. There was noticed a tendency of the blood level being elevated by consecutive administration. The urinary recovery rate of CTRX ranged from 36.5 to 71.6%. The excretion rate of CTRX into the cerebrospinal fluid ranged from 5.2 to 11.6%. The excretion rate of CTRX into the pleural fluid was 31.0%. The clinical efficacy rate was 87.5% (excellent or good) in 8 children with infections treated with CTRX. The eradication of bacteria was observed in all of 5 cases bacteriologically evaluation.(ABSTRACT TRUNCATED AT 400 WORDS)

Adolescent↗
PubMed1984

Pharmacological studies of mabuterol, a new selective beta 2-stimulant. I: Bronchodilating effect.

The bronchodilating effect and other related pharmacological properties of dl-1-(4-amino-3-chloro-5-trifluoromethyl-phenyl)-2-tert.-butylamino-etha nol hydrochloride (mabuterol) were studied in comparison with those of isoprenaline (isoproterenol), salbutamol and procaterol. In relaxing the isolated normal tracheal muscle in guinea pigs, mabuterol was more potent than isoprenaline and salbutamol, and the effect seemed to be due to the activation of beta-adrenoceptors because it was inhibited by propranolol. In anesthetized guinea pigs, mabuterol given i.v. was less potent but showed a longer duration of action than isoprenaline and salbutamol in inhibiting an increase in the bronchial resistance induced by acetylcholine, histamine and serotonin. When given intraduodenally, it was 1.9-7.8 times more potent than isoprenaline and salbutamol. In conscious guinea pigs, mabuterol given subcutaneously was less potent than isoprenaline and salbutamol in experimental asthma induced by acetylcholine, histamine and antigen, but 26-102 times more potent than the reference bronchodilators when given orally. Chronic oral treatment of mabuterol showed no significant change in the inhibitory effect on the experimental asthma and no development of tolerance was observed. In the maximum increase in the heart rate in conscious guinea pigs, mabuterol given orally was less potent than isoprenaline and salbutamol. Calculation of the selectivity ratio of the drugs for the bronchial muscle vs. cardiac muscle indicated that mabuterol was about 7.4 times more selective for the bronchial muscle than salbutamol.(ABSTRACT TRUNCATED AT 250 WORDS)

Acetylcholine↗
PubMed1984

Pharmacological studies of mabuterol, a new selective beta 2-stimulant. II: Effects on the cardiovascular system and smooth muscle organs.

Effects of dl-1-(4-amino-3-chloro-5-trifluorome-thyl-phenyl)-2-tert.-bu tylamino-ethanol hydrochloride (mabuterol) on the cardiovascular system and smooth muscle organs were investigated in comparison with those of isoprenaline (isoproterenol), salbutamol and procaterol, and the following results were obtained. Mabuterol (i.v.) produced a dose-dependent decrease in the blood pressure at doses ranging from 0.3-1000 micrograms/kg, and the heart rate was slightly increased at 0.3-30 micrograms/kg but decreased at 100-1000 micrograms/kg in rats, cats and dogs. The effects of mabuterol on the blood pressure, total peripheral vascular resistance (TPR) and heart rate were respectively 14, 37 and 104 times less potent than those of isoprenaline and there were none on the maximum dp/dt in the left ventricle in cats. In dogs, mabuterol had 356 and 118 times less effect on the blood pressure and TPR than isoprenaline and slightly increased the heart rate and maximum dp/dt. Mabuterol (p.o.) decreased the blood pressure at doses ranging from 3 micrograms-100 mg/kg, and the heart rate was increased at 3 micrograms-10 mg/kg, but decreased at 100 mg/kg in conscious and anesthetized rats. In the guinea pig atria, mabuterol slightly increased the heart rate and contractile force, but in the electrically driven left atrium mabuterol had no effect whereas procaterol slightly increased the contractile force. Mabuterol inhibited the positive inotropic effect of isoprenaline at 10(-7) g/ml and decreased the maximum driving frequency at 3 X 10(-6) g/ml. Mabuterol was 3 times more potent in relaxing the isolated rat uterus, but 700 times less potent than isoprenaline in relaxing the rabbit jejunum. Mabuterol (p.o.) depressed the intestinal propulsion and was equipotent to isoprenaline and 2.5 times less potent than salbutamol. Mabuterol had no effect on alpha-adrenergic, acetylcholine and histamine receptors. These results suggest that mabuterol has a specific effect on beta 2-adrenoceptors with no beta 1-stimulation. In addition, mabuterol exhibited beta 1-blocking activity at dosages 200-300 times higher.

Adrenergic beta-Agonists↗
PubMed1984

Pharmacokinetic studies of mabuterol, a new selective beta 2-stimulant. II: Urinary metabolites of mabuterol in rats and their pharmacological effects.

A selective beta 2-stimulating bronchodilator, dl-1- (4-amino-3-chloro-5-trifluoromethyl-phenyl)-2-tert.-butyl-amino-ethanol hydrochloride (mabuterol), is mainly metabolized by oxidative deamination pathway. Unchanged mabuterol and the following 6 types of metabolites, M-1 (hydroxylation of tert.-butyl group), M-2 (glycol), M-3 (mandelic acid), M-4 (aldehyde), M-5 (benzoic acid) and M-6 (hippuric acid) were identified by thin-layer chromatography and mass spectroscopy. Pharmacologically, only M-1 had effects on the airway resistance, blood pressure and heart rate, and the isolated organs. But its selective beta 2-stimulating effect was 2-10 times lower than that of mabuterol. M-1 antagonized the positive inotropic action induced by isoprenaline (isoproterenol). Other metabolites showed no appreciable activity.

Adrenergic beta-Agonists↗