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Biomedical subjects

M Horiba

Publications and source records attributed to M Horiba.

At least 55 records · Page 3Linked to original sources

[Inhibitory effects of AA-2414, a thromboxane (Tx) A2 receptor antagonist, on U-46619-, prostaglandin (PG) D2- and 9 alpha, 11 beta PGF2-induced contractions of guinea pig tracheas and isolated human bronchi].

The effects of a novel TXA2 receptor antagonist, AA-2414 [(+-)-7-(3,5,6-trimethyl-1,4-benzoquinone-2-yl)-7-phenyl-heptanoic acid], on U-46619-, PGD2- and 9 alpha, 11 beta-PGF2 alpha-induced contractions of isolated guinea pig tracheas and human bronchi were investigated. AA-2414 competitively inhibited the contractile responses of both human and guinea pig preparations induced by U-46619 with similar pA2 values (7.7 and 7.6, respectively). In addition, the compound also inhibited the contractions of both preparations caused by PGD2 and 9 alpha, 11 beta-PGF2 alpha, the IC50 values of which were 1.2 x 10(-7) and 1.8 x 10(-7) M in guinea pig tracheas and 2.8 x 10(-8) and 8.5 x 10(-8) M in human bronchi. These results suggest that AA-2414 may be a therapeutically useful drug for bronchial asthma.

15-Hydroxy-11 alpha,9 alpha-(epoxymethano)prosta-5↗

[Clinical study of patients with nocturnal asthmatic attacks admitted to an emergency room].

Over the periods of a year, we studied the patients who were admitted to the emergency room at our hospital at night with asthmatic attacks. From July 1991 to June 1992, 10,932 patients were admitted to the internal department of our emergency room, 707 (6.5%) of them because of asthmatic attacks. These 707 consisted of 364 patients (51.5%) with mild attacks, 242 (34.2%) with moderate attacks and 101 (14.3%) with severe attacks according to Mitsui's score. Most patients admitted before 23:00 and after 5:00, but more patients with severe attacks were admitted around midnight. A large part of the patients with moderate or severe attacks had chronic hypoxemia, and more than half of the patients' serum theophylline concentration was under the therapeutic rate. More than half patients were treated within 5 minutes. But within those who were not, 6 patients with mild attacks on admission needed hospitalization later. For prevention of life threatening attack, we should regard it as an important problem to follow up the patients who don't come to the hospital in the daytime in spite of frequent visits to the emergency room at night.

Asthma↗

[Relationship between limitation of daily life and prognosis in patients with sequelae of tuberculosis treated with long-term oxygen therapy].

The sequelae of tuberculosis (TBC) sometimes causes severe restrictive lung disorders. In Japan, lung tuberculosis was pandemic up to the 1950s, with TBC being a major underlying disease of chronic respiratory failure and cor pulmonale. Until the end of 1991, we encountered 95 cases of Home Oxygen Therapy (HOT) in Ogaki area, 30 of which were patients with TBC. To clarify factors affecting the prognosis of these patients, we examined background factors, directing special attention to daily activities. In this study, 10 inactive patients (Group A) whose daily activity was limited to indoors and 10 control patients (Group B) whose age, vital capacity and arterial PO2 were equal to inactive patients, from the 30 TBC cases were used. A comparison was made of the prognoses. Among the patients, activity was closely related to dyspnea grade and arterial PCO2. Group A patients showed more marked dyspnea and lower arterial PCO2 than those of group B patients. Percentage home stay and cumulative survival rates of Group A patients (percentage home stay, 59.2 +/- 38.7% and 3 year survival, 26.3%) were significantly less than those of Group B patients (91.0 +/- 16.4% and 87.5%, p < 0.05, respectively). Among chronic pulmonary emphysema patients treated with HOT, no significant relation between activity and prognosis could be found, when factors of age, arterial PO2 and forced expiratory volume in 1 sec were excluded. There would thus appear to be a close relation between activity and prognosis in TBC patients specific for underlying disease.

Activities of Daily Living↗

A tiaramide derivative, 5-chloro-3-(4-hydroxypiperadinocarbonylmethyl)benzothiazoline-2-one (HPR-611), a potent inhibitor of anaphylactic chemical mediator release--a distinctive feature from disodium cromoglycate.

Effects of a tiaramide derivative, 5-chloro-3-(4-hydroxypiperadinocarbonylmethyl)benzothiazoline++ +-2-one (HPR-611), on anaphylactic chemical mediator release from rat peritoneal exudate cells (RPEC), guinea pig lung fragments (GPLF) and human lung fragments (HLF) were investigated in comparison with those of tiaramide and disodium cromoglycate (DSCG). HPR-611 at 10(-6) - 10(-4) g/ml showed a concentration-dependent inhibition of the histamine release from RPEC regardless of its pretreatment time. Tiaramide also inhibited the release with slightly less potency than HPR-611. The treatment of DSCG 1 min before antigen challenge markedly prevented the release but the inhibitory potency was clearly deteriorated by prolongation of the pretreatment time. Tiaramide tended to influence the anaphylactic release of histamine from GPLF with only 20% inhibition of the release at either 10(-5) or 10(-4) g/ml, whereas HPR-611 at 10(-5) and 10(-4) g/ml significantly suppressed the release in a concentration-dependent fashion. DSCG was not effective on that even at higher concentrations. Anaphylactic release of not only histamine but also immunoreactive leukotriene B4 (i-LTB4) and i-LTC4 from HLF was markedly inhibited by 10(-8) - 10(-4) g/ml of HPR-611. Tiaramide inhibited the release to a somewhat less extent than HPR-611, while nominal or no inhibitions by DSCG were found. From these results, it is clearly apparent that anti-allergic actions of HPR-611 are quite different from those of DSCG.

Animals↗

Effect of AS-35 on agonist-induced contractions and the resting tonus of airway smooth muscles and the in vitro release of chemical mediators from passively sensitized lung fragments from humans and guinea pigs.

Effects of 9-[(4-acetyl-3-hydroxy-2-n-propylphenoxy)methyl]-3-(1H-tetrazol -5-yl)-4H-pyrido[1,2-alpha]pyrimidin-4-one (AS-35) on the resting tonus or contractions induced by agonists, such as leukotriene (LT) D4 and specific antigen of isolated guinea pig tracheas or human bronchi, and the in vitro anaphylactic release of histamine and LTs from human lung fragments were investigated and compared with the effects of FPL 55712 and disodium cromoglycate. AS-35 as well as FPL 55712 did not affect the contractions induced by acetylcholine and histamine of the isolated guinea pig trachea. However, the compound at relatively low concentrations obviously inhibited contractions induced by LTD4, and the antagonistic activity was stronger than that of FPL 55712. Treatment of the isolated human bronchus with AS-35 tended to induce the inhibition of both LTD4- and antigen-induced contractions and the relaxation of the resting tonus in a concentration-dependent manner. The inhibitory potency at 10(-6) g/ml was slightly stronger than that of FPL 55712, but this was not statistically significant. The anaphylactic release of histamine and LTs from the lung fragments appeared to be inhibited by the treatment with AS-35 5 min prior to the antigen challenge. From these results, it is suggested that AS-35 is effective against allergic asthma through antagonism towards peptide-LTs released anaphylactically in addition to inhibition of the chemical mediator release.

Animals↗

MCI-826 is a potent and selective antagonist of peptide leukotrienes (p-LTs) and has characteristics distinctive from those of FPL 55712.

Antagonistic effects of a newly synthesized compound, (E)-2,2-diethyl-3'-[2-[2-(4-isopropyl)thiazolyl]ethenyl]succinanilic+ ++ acid sodium salt (MCI-826) on the contraction of the isolated guinea pig trachea and human bronchus induced by various agonists including peptide leukotrienes (p-LTs), histamine, acetylcholine (ACh), prostaglandin (PG) D2 and others were investigated and compared with the effects of a p-LT antagonist, FPL 55712, in some experiments. MCI-826 potently antagonized LTD4- and LTE4-induced contractions at extremely low concentrations in the isolated guinea pig trachea with pA2 values of 8.3 and 8.9, respectively, on a molar basis. These values indicated that MCI-826 is over 100 times stronger than FPL 55712. Similarly, MCI-826 at 10(-8) g/ml (2.4 x 10(-8) M) markedly antagonized LTD4-induced contractions of the isolated human bronchus. Although FPL 55712 fairly inhibited the 10(-9) g/ml LTC4-induced contraction of the isolated guinea pig trachea, MCI-826 had little effect on the contraction at high concentrations like 3 x 10(-6) g/ml (7.1 x 10(-6) M). MCI-826 modestly affected the other agonist-induced contractions and the resting tonus of the isolated guinea pig trachea at 10(-6) g/ml (2.4 x 10(-6) M) or higher concentrations, but FPL 55712 caused fair inhibition of some of those contractions and gradually lowered the resting tonus with time. These results indicate that MCI-826 is a highly potent and selective antagonist of LTD4 and LTE4 and can be a useful tool for biological and pharmacological experiments on p-LTs.

Acetylcholine↗

Significant role of peptide leukotrienes (p-LTs) in the antigen-induced contractions of human and guinea pig lung parenchymas and bronchi or tracheas in vitro.

Chemical mediators responsible for the antigen-induced contractions of isolated, passively sensitized human and guinea pig lung parenchymas and bronchi or tracheas were evaluated by several antagonists and enzyme inhibitors, with emphasis on the effects of the potent and selective peptide leukotriene (p-LT) antagonist MCI-826. All of these preparations showed long-lasting contractions in response to an antigen challenge which lasted for more than 60 min. In either the human lung parenchyma and brochus or guinea pig lung parenchyma, pretreatment with 10(6) g/ml (2.4 x 10)-6) M) MCI-826 significantly inhibited the late phase at 10 to 60 min after the challenge of the contraction following slight suppression of the early phase. The early phase contractions of these preparations were moderately antagonized by 10(-6) g/ml mepyramine, but the late phases were not influenced or even rather enhanced. The combination treatment of MCI-826 with mepyramine additionally and markedly inhibited both phases of these preparations. On the other hand, although mepyramine apparently inhibited the early phase of the guinea pig tracheal contraction but not the late phase, no synergistic inhibitions of the contraction were observed when it was combined with MCI-826. The p-LT antagonist FPL 55712, atropine and indomethacin at 10(-6) g/ml either slightly inhibited or enhanced the contractions of human lung parenchymas, guinea pig tracheas and lung parenchymas, but the effects were not significant. From these results, it should be emphasized that p-LTs largely contribute to induction of the anaphylactic contractions of human lung parenchymas as well as human bronchi and guinea pig lung parenchymas but not guinea pig tracheas.

Animals↗

[Clinical and bacteriological study of sparfloxacin on bacterial prostatitis].

Sparfloxacin (SPFX), a new oral quinolone antimicrobial, was studied for the bacterial response, pharmacokinetics and clinical efficacy in the treatment of bacterial prostatitis. The minimum inhibitory concentration (MIC) values for 48 strains isolated from expressed prostatic secretion were measured. The values for 8 out of 12 strains of S. epidermidis were below 0.05 microgram/ml and those for all 6 strains of E. coli were below 0.025 microgram/ml. The SPFX concentrations in prostatic fluid (PF) were 0.33 to 0.49 microgram/ml at 1 to 3 hours after oral administration of 200 mg, the PF/serum ratio being 1.15 to 1.47. SPFX was administered at a dose of 200 to 400 mg daily for an average of 14.1 days to 14 patients with prostatitis (5, acute: 9, chronic). The clinical efficacy judged by physician in charge was effective in 12 cases with an efficacy rate of 85.7%. The bacterial eradication rate was 93.3% (14/15 strains), and eradication was complete in all 7 cases infected with gram-negative rods. SPFX-related abnormal laboratory values were observed in one case with transient increase of glutamic-oxalacetic transaminase, glutamic-pyruvic transaminase and alkaliphosphatase activities, and decrease of platelet. As side effects, one case with gastrointestinal symptoms and the other case with photosensitivity skin rash accompanied by sensory abnormality of palms were observed. The abnormal values or side effects in these patients recovered to normal or disappeared after completion of the treatment without any treatments. In view of the higher concentrations in PF than the MIC values with long remaining in the tissues, SPFX is considered to be effective in the treatment of bacterial prostatitis.(ABSTRACT TRUNCATED AT 250 WORDS)

Adolescent↗

[Type III procollagen N-terminal peptide (P-III-P, prolyl hydroxylase (PH), and laminin P1 levels in serum and BALF of radiotherapy patients].

The etiology of pulmonary fibrosis remains unclear, and at present there are no definite biochemical markers of its activity. We measured serum and BALF levels of type III procollagen N-terminal peptide (P-III-P), prolyl hydroxylase (PH), and laminin P1 in patients who had undergone radiotherapy for malignant neoplasms, and investigated their value as biochemical markers in a model of pulmonary fibrosis. The following results were obtained: 1) Patients with abnormal liver function had significantly higher serum P-III-P levels and showed a tendency to have higher serum PH levels. If P-III-P or PH are to be used as markers of pulmonary fibrosis, the effect of liver function must be taken into consideration; however, no significant difference was detected with respect to laminin P1 levels. 2) Serum P-III-P levels were significantly elevated by radiotherapy. 3) Laminin P1 levels rose in a similar manner to P-III-P levels after radiotherapy, but no significant change was detected. 4) In most cases, the levels of all markers in BALF were below the threshold of detection, nevertheless all three markers were elevated in a patient who developed diffuse radiation pneumonitis during radiotherapy. Increases in the lymphocyte count were found in BALF of this patient. 5) BALF hyaluronic acid levels were negative in the 3 cases assayed. 6) A significant correlation between P-III-P and laminin P1 in serum was shown, but no significant correlations could be found between the other combinations of markers in serum. Thus it appears that serum P-III-P and laminin P1 are valid biochemical markers of pulmonary fibrosis.(ABSTRACT TRUNCATED AT 250 WORDS)

Bronchoalveolar Lavage Fluid↗

[Percent home stay, an index for the clinical evaluation of home oxygen therapy].

To evaluate the usefulness of % home stay as an index for evaluation of the clinical effects of long term home oxygen therapy (HOT), we retrospectively examined 70 consecutive cases with chronic respiratory failure treated by HOT in the Ogaki area. The clinical data, underlying diseases, and survival rate of the cases were similar to recent official statistics in Japan; thus, we considered these cases to be a representative population. For evaluation, we tentatively used a % home stay of 70% as the standard level, which was determined by the 25th percentile line. To examine the usefulness of this standard, we classified the study population into 2 groups (the group with % home stay of greater than 70% (Group A, n = 54), and the group with % home stay of less than 70% (Group B, n = 16)), and compared the outcomes, survival rates, life situations, and background factors between these groups. As a result, there were significant differences in outcome (at home 34%, hospitalized 11%, and dead 22% in group A, and 6%, 44%, and 50%, respectively in group B, p less than 0.05), survival rate (p less than 0.05 by logrank test), and life situation between these groups. Thus, a % home stay of 70% is thought to be a useful standard for clinical evaluation, because it reflects both the prognosis and quality of life of patients.(ABSTRACT TRUNCATED AT 250 WORDS)

Activities of Daily Living↗

[Clinical study of cefclidin on bacterial prostatitis].

Cefclidin (CFCL), a new injectable cephem antibiotic, was used in the treatment of bacterial prostatitis. Concentration in prostatic fluid (PF): One hour after the i.v. administration of 1 g of CFCL the concentration of PF was 0.84 +/- 0.72 micrograms/ml (n = 4), the ratio of PF/serum being 2.24%. CFCL was administered at a dose of 1-2 g a day for 6.5 days on average. In acute bacterial prostatitis, the efficacy was evaluated as excellent or moderate in all 7 cases (100%), but in chronic cases, the effectiveness rate was as low as one out of 4 cases (25%). In safety profile, transient skin eruption was seen in one patient, but did not require further treatment. Besides this case, no side reactions or abnormal clinical values were encountered. In conclusion, CFCL was evaluated to be very useful in the treatment of acute bacterial prostatitis, caused by gram negative rods.

Adult↗

[Clinical study of levofloxacin (DR-3355) on uro-genital infections--with special reference to usefulness for chronic prostatitis].

The clinical usefulness of levofloxacin, an optical active isomer of ofloxacin, was investigated on uro-genital infections. Patients who were treated with the drug included 2 with complicated urinary tract infections (UTI), 29 with chronic prostatitis and 3 with chronic non-chlamydial epididymitis. Levofloxacin was given to each patient at a dose of 300 mg or 400 mg a day for 7-14 days (average 12.0 +/- 0.5 days). In 2 cases of chronic UTI, infected by P. aeruginosa in one case and P. stutzeri in another case, the isolates were eradicated, and the clinical efficacy was moderate or excellent. For evaluating the effectiveness on chronic prostatitis, the patients were divided into 2 groups; group I (G-I) was chronic bacterial (number of isolates including GNR or E. faecalis, greater than or equal to 10(4) ml) and group II (G-II) was chronic non-bacterial prostatitis (number of isolates including GPC less than or equal to 10(3)/ml). A complete bacteriological response was obtained in all 7 cases, classified in G-I, but in 20 of the 27 isolates, (74.1%) in G-II. In 3 cases of chronic non-chlamydial epididymitis, the response was moderate. In safety profile, there were slight elevations in the laboratory values of glutamic oxaloacetic transaminase (GOT), and glutamic pyruvic transaminase (GPT) in one case, and that of GOT in another case. As for side effects, a 69-year-old male complained of dizziness, and anorexia after 10 days on the drug, but recovered 2 days after discontinuance of the drug.

Adult↗

Coronary angiography by means of the percutaneous transbrachial approach.

A simplified method of coronary angiography was performed by means of the percutaneous transbrachial approach with a 5-F catheter designed for selective cannulation of the right and left coronary arteries. On 70 serial coronary angiograms, visualization of the coronary arteries was sufficient in all cases with no major complication. The preformed catheter required only simple manipulation. This method was easy, safe, and rapid in the investigation of coronary artery disease.

Angiography↗

[Course and morphology studies in penile cancer].

A 75-year-old male patient showed an extensive erosion mainly restricted to the penile site, which was found when he received appendectomy. The penile lesion had persisted for about ten years, during which period the erosion extended gradually while he missed to consult a physician. The lesion was a florid and wetting erosion, with a definite boundary, which covered the entire circumference of the penile foreskin and also extended to the suprapubic area, scrotum and external urethral orifice. Although the diagnosis could not be made by biopsy, extra mammary Paget's disease was strongly suspected. Bilateral modified inguinal lymphadenectomy and systemic evaluation were first performed to confirm that there was no metastasis or complexed disease in other organs. Then extensive wide resection of the skin lesion and reconstruction using a split-thickness skin graft were performed. Histopathological examination of the surgical specimen revealed poorly differentiated squamous cell carcinoma, although most part showed only inflammatory erosion. Clinical course and the histopathological findings including specific staining patterns led to the diagnosis of poorly differentiated squamous cell carcinoma originated from erythroplasia. During post-operative 18 months until now, no local recurrence or distant metastasis has been observed.

Aged↗

[Radical surgery with pubectomy for primary male posterior urethral cancer--a case report].

A 38-year-old male patient with the past history of polioencephalopathy was admitted with urinary retention and high grade fever. Although he was able to walk he had the intelligence of a 3-year-old child and his spine, thorax, fingers were deformed remarkably. Immediately after the admission, cystostomy was carried out and 600 ml of stinky and cloudy urine was noted. Although intensive antibiotic therapy was performed, high grade fever with leucocytosis (greater than 15,000/mm2) persisted for more than 10 days. Retrograde urethrogram showed stricture in the anterior urethra as well as irregular filling defect in the bulbomembranous urethra. After urethral dilation using urethral dilators, 18Fr nephrostomy balloon catheter was indwelled and the patient was discharged. However, the urethral irregular filling defect was unchanged and cytological examination of urine and urethral secretions revealed class V. After the readmission, endoscopic examination revealed papillary tumor lesions occupying the whole posterior urethra were found. With the diagnosis of invasive posterior urethral cancer, anterior exenteration by en bloc pubectomy, pelvic lymphadenectomy and ileal conduit urinary diversion were carried out. On the surgical specimen, the tumor occupied the bulbomembranous and prostatic urethra. Histopathological diagnosis was TCC G3 greater than SCC, stage B. Since the tumor invaded the serosa of the membranous urethra, we thought it could not be removed completely without the pubctomy.

Adult↗

[Clinical study of sparfloxacin, a new quinolone derivative, on urinary tract infection].

Sparfloxacin (SPFX) was evaluated for its clinical efficacy in 22 patients with acute uncomplicated cystitis (AUC) and 51 with chronic complicated urinary tract infection (CC-UTI). SPFX was administered in a single oral daily dose of 100 mg for 3 days to the patients with AUC. According to the UTI criteria, the efficacy rate was 100% (excellent rate was 78.9%). SPFX was also administered in a single oral dose of 200 to 300 mg mostly for 5 days to patients with CC-UTI. The efficacy rate according to the UTI criteria in the evaluable 22 cases was 45.5%. The efficacy rate according to the physicians in charge, evaluated as either excellent or good for the 23 cases treated with SPFX for 7 and 14 days was 65.2%, the overall efficacy rate in 49 cases including the administration for 5 days being 55.1%. In safety profile, subjective side effects were observed in 9 cases (12.3%), in 2 of which the medication was discontinued (2.7%). These side effects, flowever, recovered without any treatment to normal at the completion or discontinuation of the medication. The clinical laboratory values showed a slight elevation of BUN in 2 cases. SPFX was the most potent antimicrobial brug with a long blood elimination half life among the existing current new quinolones (NQs), indicating a possibility of once-a-day treatment regimen. In safety, side effects of SPFX were similar in general to those of other current NQs. Thus, SPFX is regarded as a highly useful antimicrobial drug when the drug is administered with consideration for its unique characteristics.

Adult↗

[Laboratory and clinical study of sulbactam/cefoperazone (SBT/CPZ) on bacterial prostatitis].

The cefoperazone and sulbactam concentrations in human prostatic fluid were measured following intravenous administration of sulbactam/cefoperazone (SBT/CPZ) and its clinical efficacy and safety in the treatment of 11 patients with acute or chronic bacterial prostatitis were evaluated. Cefoperazone concentrations in prostatic fluid (PF) one hour after an intravenous infusion of SBT/CPZ at a dose of 1 g and 2 g were 0.57 +/- 0.26 micrograms/ml and 1.37 +/- 0.86 micrograms/ml, respectively, both exceeding the MIC against most of the isolated strains from expressed prostatic secretion (EPS). The sulbactam levels in PF at doses of 1 g and 2 g of SBT/CPZ were 0.30 +/- 0.18 micrograms/ml and 0.38 +/- 0.13 micrograms/ml, respectively, both of which were high enough to potentiate antimicrobial activity of cefoperazone. The peak of MIC distribution of sulbactam/cefoperazone against E. coli (14 strains) and S. epidermidis (21 strains) isolated from EPS of patients with bacterial prostatitis was in a range of 0.1-0.2 micrograms/ml and 0.2-0.78 micrograms/ml as described for the cefoperazone concentration, respectively, which were superior to those of cefoperazone, ceftazidime and piperacillin, all compared as control, SBT/CPZ exhibited 8 fold or more potent antimicrobial activity than cefoperazone against beta-lactamase producing E. coli and CNS. Clinically, SBT/CPZ was given to 11 patients diagnosed as having bacterial prostatitis in a daily dose of 2-4 g for 5 to 8 days. The drug was found to be effective in all (100%) of 5 patients with acute prostatitis and in 3 (75.0%) of 4 patients who were judged to be assessable among 6 chronic patients. No side effects of any kind were observed in any of the patients treated. In laboratory tests, a transient thrombocytopenia was reported for one patient. SBT/CPZ is particularly useful in the treatment of acute bacterial prostatitis caused by GNR. This drug is useful for chronic prostatitis those, caused primarily by CNS which is susceptible to this agent. This drug is available as an injectable form, subjects for its appropriate usage will be those who show acute exacerbation of infection or who do not respond to oral therapy.

Anti-Infective Agents, Urinary↗

[A case of acute bacterial prostatitis caused by gram positive cocci].

This report describes our experience with sulbactam/cefoperazone in the treatment of a 36-year-old man with acute prostatitis (complicated with bilateral epididymitis) caused by S. salivarius. The patient had no past history suggesting the relationship between this organism and the route of infection. The isolated strain exhibited a high susceptibility to the drug and symptoms subsided after treatment with a daily dose of 4 g sulbactam/cefoperazone for 7 days. Usually, the most causative bacteria of acute prostatitis are either GNR or E. faecalis. However, as in the present case, there may be very few cases in which the infection has been caused by a strain of Streptococcus species.

Acute Disease↗