Showing papers by "Hiroshi Inoue published in 2005"
TL;DR: Findings suggest that the Ang II-AT(1) receptors pathway potentially are involved in OSAS and VEGF-induced vascularity and that endothelial dysfunction might be linked to this change in Ang II activity within leukocytes of OSAS patients.
42 citations
TL;DR: The results suggested that the systemic and/or pre-systemic metabolism of R- and S-carvedilol in the liver is significantly decreased in Japanese with the CYP2D6*10 allele.
Abstract: This study was performed to investigate the effect of CYP2D6*10 on the pharmacokinetics of R- and S-carvedilol in healthy Japanese volunteers. Five or 10 mg of carvedilol was orally administered to 23 subjects (22-44 years old), and blood samples were taken at 2 and 6 h after dosing. We determined the polymorphic alleles of CYP2D6 in each subject. The whole blood concentration of R- and S-carvedilol was measured by an HPLC method. The pharmacokinetic parameters in individual subjects were estimated by the Bayesian method using the nonlinear mixed effects model (NONMEM) program. The mean values of oral clearance for R- and S-carvedilol were estimated to be 1.01 and 2.15 l/h/kg, respectively. The oral clearance was highly correlated with the apparent volume of distribution among the subjects, suggesting that the interindividual difference in bioavailability was largely responsible for the pharmacokinetic variability of carvedilol. The oral clearance and also volume of distribution of both enantiomers were significantly lower in the subjects with the CYP2D6*10 allele than with the CYP2D6*1/*1 or *1/*2 genotype. These results suggested that the systemic and/or pre-systemic metabolism of R- and S-carvedilol in the liver is significantly decreased in Japanese with the CYP2D6*10 allele.
41 citations
TL;DR: The pharmacokinetic variability of bisoprolol is small even in routinely treated Japanese patients, provided that both body weight and renal function are taken into account for the prediction of oral clearance of the drug.
Abstract: The nonlinear mixed effects model (NONMEM) was used to analyze the pharmacokinetics of routinely administered bisoprolol in middle-aged and elderly Japanese patients. The subjects consisted of 29 males and 11 females with a mean age of 63.5±10.1. Data on the plasma concentration of bisoprolol from 94 blood samples obtained at steady-state following repetitive oral administration were analyzed using the NONMEM program, where a one-compartment model with repetitive bolus dosing was parameterized in terms of oral clearance (CL/F) and apparent volume of distribution (V/F). Individual CL/F values were correlated with body weight (WT) and creatinine clearance (CLcr). The relation between CLcr and the CL/F of bisoprolol was not altered by the CYP2D6 and CYP2C19 genotypes, gender, or age. The mean CL/F value estimated with NONMEM was 0.0612·WT+1.15·CLcr (l/h), and the mean V/F value was 2.61·WT (l). The residual interindividual variability of CL/F and V/F were 22.0% and 12.6%, respectively. The pharmacokinetic variability of bisoprolol is small even in routinely treated Japanese patients, provided that both body weight and renal function are taken into account for the prediction of oral clearance of the drug.
30 citations
TL;DR: Effect of substituents on both the thiazolidene and benzenesulfonamide moieties significantly enhanced anti-HIV-1 activity, whereas a 2-hydroxyphenyl group endowed potent activity against RTs, including K103N and Y181C mutants.
19 citations
TL;DR: Oral drugs used in Japan include chemical mediator release inhibitors, H 1 -antihistamines, thromboxane A 2 antagonists/ synthase inhibitors, leukotriene antagonists, and Th2 cytokine inhibitors.
Abstract: gic oral agents include chemical mediator release inhibitors, H 1 -antihistamines, thromboxane A 2 antagonists/ synthase inhibitors, leukotriene antagonists, and Th2 cytokine inhibitors. In Japan, drug compliance among patients tends to be very good with oral agents. Such oral drugs distribute well from the blood stream to the bronchi, even to areas of poor ventilation. However, higher doses are required than when administering the same drug by inhalation, and there is a higher incidence of systemic adverse effects. The physician must therefore carefully consider the balance between desired effects and potential adverse reactions when selecting an appropriate combination of inhaled and oral drugs for each patient.
13 citations
TL;DR: Evaluating the efficacy and safety of intravenously administered theophylline for the treatment of an acute exacerbation of bronchial asthma found it to be safe and effective.
Abstract: Objective: The present study was designed to evaluate the efficacy and safety of intravenously administered theophylline (IAT) for the treatment of an acute exacerbation of bronchial asthma. The theophylline was solubilized and not combined with ethylenediamine.
Methodology: The subjects were 22 asthmatic patients with mild acute exacerbation of bronchial asthma. All patients had been taking oral sustained-release theophylline and their serum concentrations of theophylline were measured. The 16 patients whose serum theophylline concentrations were <13 µg/mL were randomly selected and treated with IAT (200 mg theophylline in 200 mL saline) for 2 h. Six patients were randomly selected as controls and received 200 mL of saline. Pulmonary function and asthma severity (Borg scale) before and after treatment were measured.
Results: After IAT, both PEF (before IAT, 313 ± 79 L/min; after IAT, 335 ± 107; P < 0.05) and FEV1 (before IAT, 1.66 ± 0.47 L; after IAT, 1.83 ± 0.44; P < 0.05) increased significantly. Furthermore, their severity of asthma as assessed by the Borg scale (before IAT, 2.5 ± 1.2; after IAT, 1.3 ± 1.0; P < 0.05) improved significantly. In contrast, neither FEV1, PEF, severity of asthma or Borg scale changed significantly in the group who only received saline. None of the patients treated in this study had any adverse effects.
Conclusion: These results suggest that IAT is useful for patients with mild acute exacerbation of bronchial asthma and is safe if serum theophylline concentrations are measured.
11 citations
9 citations
TL;DR: It seemed likely that injury of the afferent fibers of the baroregulatory pathway or intracranial hypertension might have contributed to SIADH in this patient.
Abstract: A 54-year-old man suffered from a relapse of chronic inflammatory demyelinating polyneuropathy (CIDP), and developed quadriplegia and somnolence requiring mechanical ventilation for respiratory failure. Serum Na concentration remained at low levels during the clinical course, and a diagnosis of inappropriate secretion of antidiuretic hormone (SIADH) was made. The present case had not only acute aggravation of CIDP with autonomic dysfunction but also intracranial hypertension caused by increased CSF protein (maximum level, 1,315 mg/dl). It seemed likely that injury of the afferent fibers of the baroregulatory pathway or intracranial hypertension might have contributed to SIADH in this patient.
8 citations
TL;DR: Opinions on tobacco control were associated with both smoking status and education level; past and never smokers compared to current smokers and those who were educated longer tended to be affirmative about tobacco control.
Abstract: OBJECTIVE We aimed to examine knowledge of smoking-related risks and opinions on tobacco control by smoking status and education level in Japan METHODS We conducted a questionnaire survey in 2002 on a random sample of residents aged 20 to 79 years in two neighboring districts of northern Japan In a total sample of 7,136, we analyzed data from 5,638 (790%) subjects (2,659 men and 2,979 women) RESULTS The length of education was positively associated with knowledge of smoking-related risks Compared to current smokers, past male smokers and never female smokers were more likely to know about the harm of passive smoking As for causal links between smoking and lung cancer, stroke, and low birth weight, those who had been educated longer tended to be more aware of the associations in both sexes Compared to current smokers, past and never smokers of men and past smokers of women were more likely to know that smoking contributes to low birth weight, but no difference was observed between current and never female smokers in this regard Opinions on tobacco control were associated with both smoking status and education level; past and never smokers compared to current smokers and those who were educated longer tended to be affirmative about tobacco control CONCLUSION Knowledge of smoking is largely associated with education, but opinions on tobacco control are dependent on both smoking status and education
7 citations
Journal Article•
TL;DR: From October 2003 to September 2004, the specimen from 399 patients with lower respiratory tract infections in 12 institutions in Japan was collected, and the susceptibilities of isolated bacteria to various antibacterial agents and patients' characteristics were investigated.
Abstract: From October 2003 to September 2004, we collected the specimen from 399 patients with lower respiratory tract infections in 12 institutions in Japan, and investigated the susceptibilities of isolated bacteria to various antibacterial agents and patients' characteristics. Of 474 strains that were isolated from specimen (mainly from sputum) and assumed to be bacteria causing in inflammation, 469 strains were examined. The breakdown of the isolated bacteria were: Staphylococcus aureus 76, Streptococcus pneumoniae 81, Haemophilus influenzae 84, Pseudomonas aeruginosa (non-mucoid) 56, P. aeruginosa (mucoid) 11, Klebsiella pneumoniae 36, Moraxella subgenus Branhamella catarrhalis 24, etc. Of 76 S. aureus strains, those with 2 microg/ml or less of MIC of oxacillin (methicillin-susceptible S. aureus: MSSA) and those with 4 microg/ml or more of MIC of oxacillin (methicillin-resistant S. aureus: MRSA) were both 38 strains (50.0%). Against MSSA, imipenem had the most potent antibacterial activity and inhibited the growth of all the strains at 0.063 microg/mL. Against MRSA, vancomycin showed the most potent activity and inhibited the growth of all the strains at 2 microg/mL. Arbekacin also showed the potent activity and inhibited the growth of all the strains at 4 microg/mL. Carbapenems showed the most potent activities against S. pneumoniae and inhibited the growth of all the strains at 0.125-0.5 microg/mL. Cefozopran (CZOP) also had a preferable activity (MIC90:2 microg/ mL) and inhibited the growth of all the strains at 4 microg/mL. In contrast, there were high-resistant strains (MIC: 128 microg/mL or more) for cefaclor (11.1%), erythromycin (43.2%), and clindamycin (40.7%). Against H. influenzae, levofloxacin showed the most potent activity and inhibited the growth of 83 of all the strains (98.8%) at 0.063 microg/mL. Tobramycin showed the most potent activity against P. aeruginosa (both mucoid and non-mucoid) and its MIC90 was 2 microg/mL. The activity of CZOP also was preferable and its MIC90 was 4 microg/mL for the mucoid-type and 8 microg/mL for the non-mucoid type. CZOP was the most potent activities against K. pneumoniae and inhibited the growth of all the strains at 0.125 microg/mL. Also, all the agents generally showed potent activities against M. (B.) catarrhalis and the MIC90 of them were 4 microg/mL or less. The approximately half the number (54.1%) of the patients with respiratory infection were aged 70 years or older. Bacterial pneumonia and chronic bronchitis accounted for 46.1% and 30.6% of all the respiratory infection, respectively. The bacteria frequently isolated from the patients with bacterial pneumonia were S. aureus (18.6%) and H. influenzae (18.1%). In contrast, S. aureus (16.9%) and S. pneumoniae (14.9%) were frequently isolated from the patients with chronic bronchitis. Before the drug administration, the bacteria frequently isolated from the patients were S. pneumoniae (20.6%) and H. influenzae (21.5%). The bacteria relatively frequently isolated from the patients treated with cephems or macrolides were P. aeruginosa, and S. aureus was relatively frequently isolated from the patients treated with quinolones.
7 citations
TL;DR: The results suggested that CTGF might be one of the potential molecules involved in subepithelial fibrosis in murine airways with allergic inflammation.
TL;DR: In this article, a polyvinylidenefluoride (PVDF) film transducer is proposed as a new sensor for the detection of underwater shockwaves from an explosion.
Abstract: A polyvinylidenefluoride (PVDF) film transducer is proposed as a new sensor for the detection of underwater shockwaves from an explosion. The basic characteristics of the reception of the underwater shockwave by the developed PVDF transducer, such as the rise time of the received pulse, distance characteristics of the underwater shockwave, and reception of the explosion generated by a detonator, are described. It was shown that the developed transducer is capable of detecting an underwater shockwave generated by a low-energy exploding detonator.
TL;DR: In this paper, an enantioselective synthesis of (+)-aphanorphine was achieved by application of a samarium diiodide promoted reductive carbon-nitrogen bond-cleavage reaction to a 1-methoxy carbonyl-1,2,3,4-tetrahydroisoquinoline providing a benzazepinone derivative as a key step.
Abstract: An enantioselective synthesis of (+)-aphanorphine has been achieved by application of a samarium diiodide promoted reductive carbon-nitrogen bond-cleavage reaction to a 1-methoxycarbonyl-1,2,3,4-tetrahydroisoquinoline providing a benzazepinone derivative as a key step.
TL;DR: Cognitive disturbance and parkinsonism gradually decreased, and abnormal signals in the bilateral globus pallidus and the cerebral white matter were attenuated after the treatment, and Neuropsychiatric abnormalities except for a slight gait disturbance disappeared one and a half month after starting the treatment.
Abstract: A 69-year-old woman was admitted to our hospital due to an interval form of carbon monoxide (CO) poisoning one month after acute CO poisoning. On admission, she had disorientation, memory disturbance, apathy, masked face, muscle rigidity, bradykinesia and parkisonian gait. An MRI (FLAIR image) revealed high signal intensity lesions in the bilateral globus pallidus and the white matter of the frontal lobe. Hyperbaric oxygen (HBO) therapy at 2 atmospheres for 60 min was given every day, in addition to citicoline, levodopa/DCI and selegiline hydrochloride. Cognitive disturbance and parkinsonism gradually decreased, and abnormal signals in the bilateral globus pallidus and the cerebral white matter were attenuated after the treatment. Neuropsychiatric abnormalities except for a slight gait disturbance disappeared one and a half month after starting the treatment. In addition to HBO therapy, administration of citicoline, lovodopa and selegiline may be useful in the case of the interval form of CO poisoning.