Rinsho yakuri/Japanese Journal of Clinical Pharmacology and Therapeutics
Online ISSN : 1882-8272
Print ISSN : 0388-1601
ISSN-L : 0388-1601
Volume 17, Issue 2
Displaying 1-19 of 19 articles from this issue
  • Patients with Cerebrovascular Disease
    Yasuhiro TSUNASHIMA, Tsugukazu KASHIMA, Kinya ICHIHASHI, Kazunari YAMA ...
    1986 Volume 17 Issue 2 Pages 337-345
    Published: June 20, 1986
    Released on J-STAGE: June 28, 2010
    JOURNAL FREE ACCESS
    The efficacy of E-0687 on the power spectrum of EEG was quantitatively evaluated in nine patients exhibiting chronic cerebrovascular disease.
    The power spectrum arrays were used to evaluate the stability of EEG activitieswithin all recording periods. EEG topographies were made for visual evaluation ofthe EEG changes in each patient. For quantification of the EEG power, five channels (F7, F8, T5, T6, Fz) and nine frequency bands were selected, and the EEGpowers and % powers of each band on each channel were calculated. The effects of E-0687 were revealed as a tendency to decrease in both power and % power of the delta and beta frequency bands, and to increase in the same indices of the theta andalpha bands. Statistical significance was detected in the rate of increase in % powerof the alpha bands on the leads of the non-affected sides, and in the rate of decreasein the same indices of the beta bands on the leads of both the affected and nonaffected sides. The efficacy of this drug on the non-affected side tended to be higherthan on the affected sides. These results were discussed comparing with results ofsome reported animal examinations.
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  • Tadanao TAKEDA, Yoshiyasu IKUNO, Yoshihiro KANEKO, Hisakazu YASUDA, Ka ...
    1986 Volume 17 Issue 2 Pages 347-358
    Published: June 20, 1986
    Released on J-STAGE: February 25, 2011
    JOURNAL FREE ACCESS
    The Influence of BKU (urapidil retard capsules) on diurnal variations of bloodpressure was investigated in 25 patients with essential hypertension. The drug wasgiven at 60-120 mg daily in divided doses for a period of 5-32 days (average 11.1days). Blood pressure and heart rate were measured at 9 time-points from 7: 00 a.m.to 7: 00 a.m. in the next morning before and after treatment.
    Blood pressure was reduced at each time-point, but diurnal variations of bloodpressure was not affected by administration of BKU. There was no alteration in heartrate. The drug did not cause undue effects on urine volume and body weight of thepatients. No serious side effects attributable to the drug were noted in any patients.
    These results suggest that BKU twice daily may be an effective and safe drug intreating essential hypertension.
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  • Michio OHTA, Sumiko MAJIMA, Yoriyoshi KUMAGAI
    1986 Volume 17 Issue 2 Pages 359-365
    Published: June 20, 1986
    Released on J-STAGE: February 25, 2011
    JOURNAL FREE ACCESS
    We previously reported on an optimal administration method of anticoagulantdrugs solved mathematically for an average patient. In this report, we suggest anoptimal administration method to reach and maintain the desired prothrombin levelsfor each individual patient with unknown parameters, which is the case in clinical applications. For the first two days, the standard administration criteria should be applied in principle since the data is insufficient to identify the three parameters of thepatient model. From the third day, parameter identification is theoretically possible, but the least square method was not successfully applicable, as it was found to selectunrealistic values of no use. We had to choose, as a most direct method, a best-fitmodel from models with wide varieties of parameter sets by comparing the model output and the clinical data. Simulation using patient models with two kinds of noiselevels has successfully explained this situation of parameter identification and thepossibility of regulating prothrombin levels by our identification and administrationmethod.
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  • Yoshio IGARASHI, Hisashi MAESHIRO, Takuro NOGUCHI, Matsuo TAKAMATSU, H ...
    1986 Volume 17 Issue 2 Pages 367-378
    Published: June 20, 1986
    Released on J-STAGE: June 28, 2010
    JOURNAL FREE ACCESS
    Plasma concentrations of bromperidol (BPD) were studied by the single andrepeated administration in schizophrenic patients, and were compared with that ofhaloperidol (HPD). At the same time, plasma levels of prolactin (PRL) were measuredin order to clarify the neuroendocrinological properties of BPD. As the results, therewas no difference between BPD and HPD in pharmacokinetic paramaters observed bythe single administration, but time-concentration curves showed a biphasic pattern, andthe elimination half life of the β phase of BPD was 31.1 hr. and that of HPD was 27.1 hr.When BPD were administered at the daily dose of 9 mg for 28 days, there was nosignificant difference in plasma concentrations between the doses of 3 times a day andonce a day, although HPD concentrations were lower in the administration of once a daythan in 3 times a day. In PRL levels no significant differece was observed between bothdrugs in the single administration, but there was significant correlation between plasma BPD concentration and PRL level in the repeated administration of BPD both in 3times a day and once a day.
    From these results, it was noted that BPD showed no significant difference in itsplasma concentrasions between the doses of 3 times a day and once a day. Further, significant correlation was found between plasma BPD concentrations and PRL levels.
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  • Fumio KIMURA, Hiroshi MITAMURA, Shoko FUKAZAWA, Kayo SHONAI, Fumiko SA ...
    1986 Volume 17 Issue 2 Pages 379-389
    Published: June 20, 1986
    Released on J-STAGE: June 28, 2010
    JOURNAL FREE ACCESS
    The effects of disopyramide on blood glucose and plasma immunoreactive insulin (IRI) were studied in Donryu and Long-Evans strain rats. The configurations of the blood glucose curves after oral administration of disopyramide could be grouped into two types, initial and sustained hypoglycemia. Initial hypoglycemia, which seemed insulin independent, was observable in all of the tested rats, while sustained response, in which the hypoglycemia was accompanied by a rise in plasma IRI, could be found only in a few of thetested animals. The incidence for the sustained response was four out of nineteen. Afterpretreatment with propranolol, this rate rose to thirteen out of sixteen, while pretreatmentwith phentolamine or hexamethonium did not have any significant effect. In the isolatedpancreas in situ perfusion experiment, the incidence of cases showing stimulated insulinrelease induced by perfusion of disopyramide was two out of six, and pretreatment withpropranolol produced a significant rise of the rate to five out of six. In the isolated pancreatic islet perifusion experiment, disopyramide always produced an increase in insulinrelease from the islets, but the addition of propranolol did not lead to any change in thedisopyramide-induced insulin hypersecretion. Disopyramide was concluded to producetwo distinct effects: one was the direct stimulation of insulin release from B cells, and theother was elevation of the activity of the β-adrenergic neuron, which plays a physiological role in suppressing insulin secretion.
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  • Comparison with Propranolol
    Akio EBIHARA, Kazuoki KONDOH, Kyoichi OHASHI
    1986 Volume 17 Issue 2 Pages 391-401
    Published: June 20, 1986
    Released on J-STAGE: June 28, 2010
    JOURNAL FREE ACCESS
    The pharmacodynamic and pharmacological effects of nipradilol (K-351) were studied in a cross-over double blind fashion with propranolol as reference drug, using healthy adult male volunteers. They received orally 6 mg and 12 mg of nipradilol and 20 mg of propranolol.
    1) The sitting blood pressure at rest was continously lowered both for systolic blood pressure (SBP) and diastolic blood pressure (DBP). Heat rate (HR) was transiently reduced.
    2) No influence was seen on blood pressure or heart rate under the condition of postural change by 50°tilting.
    3) Both elevated SBP and increased heart rate due to a submaximal exercise load were suppressed.
    4) The time-course of plasma concentration of nipradilol accorded with the one compartment model. The plasma concentration of nipradilol reached to the peak at 1.5 hours after dosing. The plasma concentration of denitro-nipradilol, the main metabolite, was approximately 2 times that of nipradilol.
    5) The half life of elimination was approximately 6 hours.
    6) The plasma concentration of nipradilol correlated significantly with the reduction rate [%R] HR in exercise-induced tachycardia and the suppressive rate [%I] SBPin exercise-induced elevation of SBP. The time-course in [%R] HR almost corresponded to that in the plasma concentration, which suggested that nipradilol had a long-duration effect.
    7) [%R] HR was dose-dependent. Beta-blocking potency of nipradilol was considered to be 5 or 6 times that of propranolol.
    8) There were no subjective complaints except for slight drowsiness seen in one case each in the 6 and 12 mg dosings. There were no abnormalities regarding pulmonary function or the laboratory investigation tests.
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  • [in Japanese], [in Japanese]
    1986 Volume 17 Issue 2 Pages 403-404
    Published: June 20, 1986
    Released on J-STAGE: June 28, 2010
    JOURNAL FREE ACCESS
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  • [in Japanese]
    1986 Volume 17 Issue 2 Pages 405-408
    Published: June 20, 1986
    Released on J-STAGE: June 28, 2010
    JOURNAL FREE ACCESS
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  • [in Japanese]
    1986 Volume 17 Issue 2 Pages 409-411
    Published: June 20, 1986
    Released on J-STAGE: June 28, 2010
    JOURNAL FREE ACCESS
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  • [in Japanese]
    1986 Volume 17 Issue 2 Pages 413-414
    Published: June 20, 1986
    Released on J-STAGE: June 28, 2010
    JOURNAL FREE ACCESS
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  • [in Japanese]
    1986 Volume 17 Issue 2 Pages 415-420
    Published: June 20, 1986
    Released on J-STAGE: June 28, 2010
    JOURNAL FREE ACCESS
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  • [in Japanese]
    1986 Volume 17 Issue 2 Pages 421-424
    Published: June 20, 1986
    Released on J-STAGE: June 28, 2010
    JOURNAL FREE ACCESS
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  • [in Japanese]
    1986 Volume 17 Issue 2 Pages 425-428
    Published: June 20, 1986
    Released on J-STAGE: June 28, 2010
    JOURNAL FREE ACCESS
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  • [in Japanese], [in Japanese]
    1986 Volume 17 Issue 2 Pages 429-435
    Published: June 20, 1986
    Released on J-STAGE: June 28, 2010
    JOURNAL FREE ACCESS
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  • [in Japanese]
    1986 Volume 17 Issue 2 Pages 437-440
    Published: June 20, 1986
    Released on J-STAGE: June 28, 2010
    JOURNAL FREE ACCESS
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  • [in Japanese]
    1986 Volume 17 Issue 2 Pages 441-443
    Published: June 20, 1986
    Released on J-STAGE: June 28, 2010
    JOURNAL FREE ACCESS
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  • [in Japanese]
    1986 Volume 17 Issue 2 Pages 445-446
    Published: June 20, 1986
    Released on J-STAGE: June 28, 2010
    JOURNAL FREE ACCESS
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  • [in Japanese]
    1986 Volume 17 Issue 2 Pages 447-450
    Published: June 20, 1986
    Released on J-STAGE: June 28, 2010
    JOURNAL FREE ACCESS
    Download PDF (591K)
  • [in Japanese]
    1986 Volume 17 Issue 2 Pages 451-456
    Published: June 20, 1986
    Released on J-STAGE: June 28, 2010
    JOURNAL FREE ACCESS
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