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Biomedical subjects

A Inoue

Publications and source records attributed to A Inoue.

At least 433 records · Page 24Linked to original sources
PubMed1988

Absorption, distribution and excretion of 14C-benidipine hydrochloride after repeated administration to rats.

The absorption, distribution and excretion of (+/-)-(R*)-2,6-dimethyl-4-(m-nitrophenyl)-1,4-dihydropyridine-3,5-dicarb oxylic acid (R*)-1-benzyl-3-piperidinyl ester, methyl ester hydrochloride (benidipine hydrochloride, KW-3049) were studied after repeated doses to rats. The results were summarized as follows: 1. After oral repeated administration once a day for 3 weeks, the radioactivities in blood and tissues increased up to the 14th day, and thereafter they tended to show the steady state. 2. The radioactivity in the tissues at 1 h after last dosing was compared with that at 1 h after single administration. Both tissue distribution patterns were not markedly different, but the concentrations in the liver, testicles, skin and descending aorta significantly increased, showing approximately the 2-fold radioactivities. 3. The radioactivities were excreted in the urine (6%) and feces (88%). The excretion of radioactivity in urine and feces did not change markedly during the repeated administration period.

Administration, Oral↗
PubMed1988

Pharmacokinetic study of benidipine hydrochloride in rats and dogs.

(+/-) - (R*) - 2,6-Dimethyl-4-(m-nitrophenyl)-1,4-dihydropyridine - 3, 5-dicarboxylic acid (R*)-1-benzyl-3-piperidinyl ester, methyl ester hydrochloride (benidipine hydrochloride, KW-3049) is presently under development as an anti-hypertensive and antianginal agent. A pharmacokinetic study in rat and dog after oral and intravenous administrations revealed that KW-3049 was rapidly absorbed from the gastrointestinal tract, distributed into tissues moderately and comparatively quickly eliminated. After oral administration, non-linearity of bioavailability with increment of doses was observed in both rat and dog. Female and male rats showed similar drug disposition after intravenous administration. Oxidation product of KW-3049 dihydropyridine ring was also measured in some plasma samples. The concentration rates of its pyridine metabolite accounted for 0 to 30% and 0 to 23% of the combined concentration of KW-3049 plus the pyridine metabolite in rat and dog.

Administration, Oral↗
PubMed1988

Identification of benidipine hydrochloride metabolites in rats and dogs.

A study of the metabolism of [14C]-(+/-)-(R*)-2,6-dimethyl-4-(m-nitrophenyl)- 1,4-dihydropyridine-3, 5- dicarboxylic acid (R*)-1-benzyl-3-piperdidinyl ester, methyl ester hydrochloride (14C-benidipine hydrochloride, 14C-KW-3049) revealed as major metabolic pathways oxidative N-dealkylation, hydrolysis of the ester moiety, dehydrogenation of the 1,4-dihydropyridine ring, hydroxylation of the methyl group and decarboxylation in rat and dog. Rat and dog showed similar metabolic pathways, but some quantitative differences were found between rat and dog.

Animals↗
PubMed1988

[A case of multiple cerebral hemorrhage related to cerebral amyloid angiopathy].

A case of multiple cerebral hemorrhage in the bilateral parietal lobes related to cerebral amyloid angiopathy (CAA) is reported. A 66-year-old man was admitted to our hospital because of headache and vomiting on Feb. 21, 1983. He had no history of hypertension, diabetes mellitus, recent head injury, or dementia. Four days prior to admission, he had behaved as if he were blind, but, had denied any blindness. On examination, he was confused and disoriented. Blood pressure was 130/80 mmHg. Abnormal findings on neurological examination included memory disturbance, apraxia for dressing, right-left disorientation, finger agnosia and Balint's syndrome. A CT scan showed multiple subcortical hematomas in the bilateral parietal lobes. Intracerebral hemorrhage related to CAA was suspected. Confirmation of the presence of amyloid in the cerebral vessels was established by examination of brain biopsy specimens. The characteristics of cerebral hemorrhage related to CAA are as follow--occurrence in elderly, sometimes demented people; localization to the cortex and subcortical white matter, with direct extension into the subarachnoid space; frequent multiple occurrence in time and/or at several sites within the cerebral hemispheres; sometimes occurrence after operative procedures or head injuries. A specific diagnosis of CAA can only be made by histological examination, but the indication of brain biopsy should be carefully decided because of hemostatic difficulty and tendency to rebleed. In conclusion, CAA should be considered as a cause of hemorrhage in elderly patients who are often normotensive and demented.

Aged↗
PubMed1987

Demyelinating neuropathy associated with hepatitis B virus infection. Detection of immune complexes composed of hepatitis B virus surface antigen.

We observed 4 patients with the Guillain-Barré syndrome (GBS) type of polyneuropathy and one patient with chronic relapsing polyneuropathy associated with hepatitis B virus infection, and examined the sera, cerebrospinal fluid (CSF) and sural nerve specimens from the patients in search of the pathogenetic factors involved. It was demonstrated that hepatitis B surface antigen(HBsAg)-immune complexes were significantly increased in both the sera and the CSF of the 4 patients with GBS. The serum levels of immune complexes were also closely related to the clinical status of these patients. In all patients, HBsAg-positive labelling of immunofluorescence was found around the endoneural small blood vessels and in the endoneurium. Electron-dense deposits, suggestive of immune complexes composed of hepatitis B virus, were demonstrated in the endoneurium of the patient with chronic relapsing polyneuropathy. These results suggest that HBsAg immune complexes may be of importance in the etiology of GBS or chronic relapsing polyneuropathy associated with hepatitis B virus infection.

Adult↗
PubMed1987

Occurrence of palytoxin in the trigger fish Melichtys vidua.

The trigger fish Melichtys vidua, collected at Pingelap Atoll in Ponape in The Federated States of Micronesia, contained a potent toxin in the viscera, flesh, and digestive tracts with contents. The toxic principle appeared identical to palytoxin on the basis of toxicity and chromatographic properties.

Acrylamides↗
PubMed1987

Inhibition by rifamycin AF/013 of thyroid hormone binding to the nuclear receptor.

Rifamycin AF/013, a potent inhibitor of nucleic acid polymerizing enzymes and of some hormone receptors, strongly inhibited thyroid hormone-binding to the isolated nuclear receptor. Fifty percent inhibition was obtained at AF/013 concentration of as low as 8 micrograms/ml. AF/013, however, only weakly promoted dissociation of the bound hormone from the receptor. The inhibitory action of AF/013 was competitive with respect to and reduced the receptor's affinity for the hormone.

Animals↗
PubMed1987

Langer-Giedion syndrome with del 8 (q24.13-q24.22).

An 8-year-old boy with the features of Langer-Giedion syndrome except for short stature is described. Chromosome analysis using high resolution G-banding techniques revealed an interstitial deletion of the long arm of chromosome 8:46,XY,del(8)(q24.13-q24.22).

Child↗
PubMed1987

Chronic relapsing demyelinating polyneuropathy associated with hepatitis B infection.

We studied a patient with chronic relapsing polyneuropathy associated with immune complexes of hepatitis B virus. There were cycles of remission and exacerbation in parallel with liver dysfunction. Immunofluorescent deposits of hepatitis B antigen, immunoglobulin, and C3 component were detected in the vasa nervorum. Ultrastructural study revealed electron-dense deposits that might have been immune complexes composed of hepatitis B virus, both around the endoneural capillary and in the endoneurium. Immune complexes composed of hepatitis B virus may play a role in the pathogenesis of chronic relapsing polyneuropathy.

Adult↗
PubMed1987

Intramedullary haemorrhage as a possible cause of avascular necrosis of the femoral head. The histology of 16 femoral heads at the silent stage.

We have studied core biopsy specimens from 16 femoral heads affected by idiopathic avascular necrosis at the silent stage, when there were no clinical or radiographic manifestations but scintigraphy was positive. All the specimens showed necrosis of trabeculae and of bone marrow, but the most common and characteristic feature was evidence of old and new haemorrhage in the marrow. In the areas of intramedullary haemorrhages, trabeculae and bone marrow were completely necrotic, with a transitional area of incomplete necrosis between these areas and those without haemorrhagic lesions, where the trabeculae and bone marrow were normal. There was good correlation between necrosis and haemorrhagic episodes, and it was concluded that repeated intramedullary haemorrhage at the silent stage is probably related to the pathogenesis of idiopathic avascular necrosis of the femoral head.

Adolescent↗
PubMed1987

Central effect of captopril on baroreflex.

To clarify effect of converting enzyme inhibitors (CEI) on heart rate regulation, captopril (2 mg/kg) was injected intravenously (i.v.) with or without pretreatment of atropine and also responses to intracisternal (i.c.) injections were examined. Captopril induced bradycardia with lowering blood pressure, and this bradycardia was abolished by pretreatment of atropine. Reduction of heart rate by i.c. injection of captopril was significantly larger than those of i.v. injection. Furthermore, to determine whether CEI can modify baroreflexes centrally, the aortic depressor nerve (ADN) was stimulated electrically in captopril treated rats. Vasodepressor and sympatho-inhibitory responses induced by ADN stimulation were significantly attenuated by captopril, while the bradycardiac response was not changed. These findings suggest that captopril attenuated centrally vasodepressor and sympatho-inhibitory responses of the baroreflex and activated centrally cardiac vagal efferent activity.

Animals↗
PubMed1987

[The significance of chemotherapy in oral cancer].

Fifty-three patients with postoperative recurrent epidermoid carcinomas of the head and neck were treated with BEAM, DP, MBD and CAP regimens. Complete response (CR) and partial response (PR) were achieved in 9% and 23% of all evaluable patients, respectively. Especially, in patients with oral cancer (17 cases), the response rate was only 23% (CR 0%, PR 23%). From our results, it was concluded that chemotherapy in any form must be palliative for a patient who has received prior unsuccessful radiotherapy or surgery. For previously untreated patients who present with Stage III or IV advanced carcinoma, combination chemotherapy with CDDP, MTX and PEP should be considered as the initial method of treatment. Adjuvant chemotherapy and intra-arterial chemotherapy for oral cancer should also be considered. Adjuvant chemotherapy combined with UFT and MTX is indicted to be effective for the prevention of local recurrence and micrometastases, but a further randomized study is necessary to confirm these findings.

Adult↗
PubMed1987

[Concentrations of cefpiramide in bone and joint tissues].

A single intravenous dose of 2 g of cefpiramide (CPM) was administered prophylactically to 11 patients at 30, 60, 120, or 180 minutes before hip surgery. Peak concentrations in different tissues of CPM were observed in 30 minutes after intravenous injection. Mean concentrations of CPM were 246.0 micrograms/ml in peripheral blood, 298.5 micrograms/ml in bone marrow blood and 77.5 micrograms/g in cancellous bone at 30 minutes after administration. Half-lives of CPM were 152 minutes in peripheral blood and 105 minutes in bone marrow blood. The concentrations of CPM observed in the above study were higher and its retention longer than expected values.

Adult↗