巻号一覧
22 巻 (1991)
- 4 号 p. 723-
- 3 号 p. 593-
- 2 号 p. 425-
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22 巻, 3 号
選択された号の論文の13件中1～13を表示しています
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瀬部 俊彦, 斎藤 史郎, 西内 健, 小富 正昭, 加地 公代, 清水 剛文1991 年 22 巻 3 号 p. 593-600
発行日: 1991/09/30
公開日: 2010/04/30
ジャーナル フリーThe effect on haemodynamics, pharmacokinetics, and safety of BTS 49 465 (flosequinan; 7-fluoro-1-methyl-3-methylsulphinyl-4-quinolone) were investigated in six healthy volunteers after single oral administration and in six other healthy volunteers after repeated oral administration.
The antihypertensive action of BTS 49 465 was observed beginning from 30min after single oral administration and continuing for 6hr. Pulse rate increased in accordance with the decrease in blood pressure. A steady state of plasma BTS 53 554, a major metabolite of flosequinan, was achieved on day 6 of multiple oral administration.
The t1/2 (biological half life) after the final dose of the repeated administration was the same as that after single administration.
This study demonstrated that BTS 49 465 is rapidly absorbed by the gastrointestinal tract given that the tmax (peak time) of BTS 49 465 is 30min. The t1/2 of BTS 49 465 is 2.1hr, while the t1/2z of BTS 53 554 is 29hr, which supports a once-daily regimen. Two percent of BTS 49 465 and 51% of BTS 53 554 were excreted in the urine within 96hr after flosequinan administration. After multiple oral administration BTS 53 554 plasma concentration reached a steady state on day 6 and on day 10. After final dosing, the t1/2 was comparable to that after single oral administration.
BTS 49 465 and BTS 53 554 did not accumulate in the body after multiple oral administration. Absorption and excretion after multiple oral administration were comparable to those after single oral administration.
Adverse reaction was limited to mild headache in all volunteers after single oral administration and in 5 of 6 volunteers after multiple oral administration. This symptom was, however, transient and improved without any treatment. There were no abnormal findings in the physiological or laboratory examinations.抄録全体を表示PDF形式でダウンロード (800K) -
大橋 和史, 小林 正文1991 年 22 巻 3 号 p. 601-609
発行日: 1991/09/30
公開日: 2010/04/30
ジャーナル フリーThe pharmacokinetics and safety of ranitidine injection, a histamine H2-receptor antagonist, were studied in 7 healthy male volunteers. The study was carried out by an intravenous (iv) drip infusion of ranitidine of 100mg for 1hr, given on a once daily schedule and on a thrice daily schedule at the same speed.
The ranitidine plasma concentration time curve after completion of the iv drip infusion was examined by the two compartment model. Its Cmax was about 1, 760ng·ml-1.
In the ranitidine iv drip infusion of 300mg daily, the ranitidine plasma concentration time curve was well in agreement with the actual measured values after the first and second administrations. We surmise that there is no accumulation of ranitidine in this administration method, because the Cmax and the elimination curve after the third dose were similar to those after the first and the second doses.
The cummulative urinary excretion rate of unchanged ranitidine as measured up to 24hr after the iv drip infusion of 100mg was about 89%.
Although the gastrin, secretin, and prolactin levels in plasma showed somewhat irregular fluctuation, in comparison with the preadministration value they were not affected by ranitidine.
No abnormality attributable to ranitidine was noted in blood pressures, pulse, or clinical laboratory findings.抄録全体を表示PDF形式でダウンロード (956K) -
とくにα1-acid glycoprotein (AAG) 濃度との相関植田 孝子, 小林 真一, 安原 一1991 年 22 巻 3 号 p. 611-616
発行日: 1991/09/30
公開日: 2010/04/30
ジャーナル フリーPirmenol is a newly developed antiarrythmic drug. The binding of pirmenol to albumin, AAG, in vitro or in vivo was studied using the ultrafiltration method. Regarding the in vitro study, pirmenol bound to a single class binding site of purified human serum AAG (AAG-P), which was characterized by a higher affinity (Kd was 1.14×10-6M) than that of human serum albumin (HSA, Kd was not detectable). The percent of binding of pirmenol to AAG-P and HSA was mainly related to the concentration of AAG-P. Regarding the in vivo study: a single dose of 75, 100, and 150mg, of pirmenol was administered to 16 patients with ventricular arrythmia. The peak plasma concentrations were 0.606±0.32, 0.875±0.44, or 1.29±0.49μg/ml, respectively. The binding percent was 63-87% in the plasma and the relationship between the binding/free pirmenol concentration ratio and the AAG concentration in the plasma was shown to be the relation constant 0.48 with P<0.01. The plasma concentration of AAG in these patients was almost within normal range and also the pirmenol concentration in plasma was lower; therefore, the relation constant was a low value. On the other hand, plasma concentrations of AAG in 174 volunteers (21-98yrs) showed a good corelation between age and plasma concentrations of AAG (r=0.78, P<0.01). These data suggest that the free fraction of pirmenol in plasma may be influenced by pathological conditions and age, due to a change in plasma AAG concentration.抄録全体を表示PDF形式でダウンロード (685K) -
中野 重行, 成尾 鉄朗, 渡辺 浩毅, 高岡 伸行, 大戸 茂弘, 小川 暢也, 宮内 俊次, 三木 吉治1991 年 22 巻 3 号 p. 617-626
発行日: 1991/09/30
公開日: 2010/04/30
ジャーナル フリーThe dose-response relation (study I) and the effect of the timing of administration (study II) with respect to the antihistaminic activity of a H1-blocking agent, WAL 801 CL (Epinastine), were investigated. In study I, a 10, 20, and 40mg dose of WAL 801 CL or a placebo was administered to 11 healthy male volunteer students (X±SD=23.3±1.3yrs) after breakfast (8:30) by a double-blind fashion using the Latin square design, and the histamine intradermal reaction and psychomotor functions were subsequently examined. In study II, either 20mg of WAL 801 CL or a placebo were administeredto 8 healthy male volunteer students (23.8±1.4yrs) after breakfast (8:00) or after dinner (20:30) in the same way as in Study I, and the histamine intradermal reaction was subsequently examined. WAL 801 CL inhibited the histamine intradermal reaction dose-dependently, and no findings suggesting any effects on the CNS were observed. The inhibitory effect of WAL 801 CL on the histamine intradermal reaction tended to last longer when it was administered in the morning, while the effect tended to be stronger when it was administered in the evening, but the differences were not significant. Thus the results show that WAL 801 CL is a nonsedative H1-blocking agent and that the timing of administration does not critically influence the antihistaminic activity of the drug.抄録全体を表示PDF形式でダウンロード (1032K) -
年齢, 血漿レニン活性, 基礎血圧および急性効果からの検討岩岡 大輔, 梅田 照久, 井上 準之助, 佐々木 雅人, 佐藤 辰男1991 年 22 巻 3 号 p. 627-634
発行日: 1991/09/30
公開日: 2010/04/30
ジャーナル フリーPredictors of the chronic antihypertensive effect of nifedipine slow-release, tablet was examined with respect to age, plasma renin activity, basal blood pressure, and acute response to the nifedipine capsule. Following the acute oral administration of 10mg of nifedipine capsule, 10mg of nifedipine slow-release tablet twice a day was prescribed in 17 patients with essential hypertension. They were divided into two groups based on their blood pressure after 4wks of treatment. Group I consisted of 9 patients in whom both systolic and diastolic blood pressure dropped below 150/90mmHg. The remaining patients, in whom either systolic or diastolic blood pressure was higher than that level, were classified as group II. The fall of mean blood pressure at 60min after the acute administration was not significantly different between the two groups, while the efficacy after 4wks of treatment was greater in group I than in group II (-32.2±10.8 vs. -14.5±7.5mmHg, P<0.01). There were no significant differences between the two groups in the levels of serum albumin, serum creatinine, plasma renin activity, plasma aldosterone, and norepinephrine concentrations. However, the mean age in group I was significantly greater than that in grouplI (67.7±6.6 vs. 55.5±6.7yr, P<0.01). If a blood pressure lower than 150/90mmHg is considered as normal, then 8 of 10 patients 60yrs or older normalized their blood pressure compared with 1 of 7 patients younger than 60yrs (P<0.01 by Chi-square test). The fall in mean blood pressure 4wks after the chronic administration had a positive correlation with that measured 60min after the acute administration (r=0.577, P<0.02, n=17), but had no correlation with pretreatment mean blood pressure was evident. These results showed that age was the factor most related to the effect of the low dose nifedipine slow-release tablet.抄録全体を表示PDF形式でダウンロード (831K) -
Einosuke TANAKA, Akio ISHIKAWA, Hironori ETOH, Shogo MISAWA, Katashi F ...1991 年 22 巻 3 号 p. 635-639
発行日: 1991/09/30
公開日: 2010/04/30
ジャーナル フリーFive male patients with extrahepatic cholelithasis and ten male patients with liver cirrhosis were administered simultaneously 4mg/kg trimethadione (TMO) and 500mg/man antipyrine (AP). Changes in phase I (AP and TMO) and phase II (AP) reactions of the model substrates in liver disease were examined. The patients with liver cirrhosis exhibited prolonged half-life (t1/2) and decreased metabolic clearance (CL) of AP when compared with cholelithasis patients, while no change was found in the apparent volume of distribution (Vd). The serum dimethadione (DMO)/TMO ratio at 4hr after oral administration of TMO was apparently decreased in the cirrhotic patients. The cirrhotic patients also exhibited significant decreases in urinary excretion and clearance for production of three major AP metabolites (4-hydroxyantipyrine, 3-hydroxymethyl-3-norantipyrine, and 3-hydroxymethylantipyrine), while no significant differences between the cirrhotic patients and cholelithasis patients were noted in percentages of either total or individual glucuronidation of these metabolites. These findings suggest that AP and TMO metabolisms (phase I) are severely impaired in cirrhotic patients, whereas glucuronidation of AP is unaffected (phase II).抄録全体を表示PDF形式でダウンロード (538K) -
Captopril 錠1日3回投与法との比較井尻 裕, 向山 茂雄, 駒谷 隆雄, 鶴田 育男, 河埜 功, 石井 博之, 沢登 貴雄, 岩崎 康一, 中村 享道, 斉藤 勇三, 田村 ...1991 年 22 巻 3 号 p. 641-649
発行日: 1991/09/30
公開日: 2010/04/30
ジャーナル フリーThe purpose of this study was to evaluate the efficacy of captopril-retard (C-R) and captopril (C) chronobiologically in patients with essential hypertension. Doses of C-R of 18.75mg twice a day and C of 12.5-25mg three times a day were administered at least 6wk in each of 9 patients. The blood pressure (BP) monitoring was repeated before and after the treatment for 48hr every 30min with an ambulatory instrument (ABPM-630, Nippon Colin, Japan). These data were analyzed with conventional statistical and cosinor methods. The hyper- and hypobaric indices of BP were calculated based on our reference limits. The least square fit of a cosine curve with a period of 24hr was calculated to obtain a midline estimating statistic of rhythm (MESOR), amplitude, and acropase. A circadian rhythm cycle of about 24hr was found in the BP in all cases. C-R lowered MESOR of systolic BP (SBP) and diastolic BP (DBP) from 134.6±9.7mmHg to 129.9±9.9mmHg and 77.4±4.3mmHg to 70.2±5.7mmHg (P<0.01), and C decreased MESOR of DBP and DBP from 138.1±11.1mmHg to 129.0±8.8mmHg and 78.5±8.5mmHg to 72.5±7.0mmHg, respectively (P<0.01). The hyperbaric index of SBP significantly decreased with C-R and C (P<0.05). However, the amplitude and acrophase of BP showed no significant changes in either group. In conclusion, C-R and C showed definite antihypertensive effect, preserving the circadian rhythm of BP similarly.抄録全体を表示PDF形式でダウンロード (989K) -
河埜 功, 向山 茂雄, 岩崎 康一, 沢登 貴雄, 石井 博之, 鶴田 育男, 駒谷 隆雄, 中村 享道, 田村 康二1991 年 22 巻 3 号 p. 651-659
発行日: 1991/09/30
公開日: 2010/04/30
ジャーナル フリーThe aim of this study was to assess the efficacy of diltiazem monotherapy on deviant blood pressure (BP) profiles of essential hypertension.
METHODS: 30 or 60mg of diltiazem was administered three times a day for 4wk. 13 untreated patients with essential hypertension were monitored by an ambulatory blood pressure monitoring device (ABPM-630, Nippon Colin, Japan) for 48hr before and during the treatment. BP data were analyzed with the conventional statistical and cosinor method for rhythmometory. The deviant pressure was quantified as pressure-time magnitude (hyperbaric index) compared with 90% reference interval matched for age and gender of our 334 individuals.
RESULTS AND CONCLUSIONS: Diltiazem was revealed to have an antihypertensive effect on the circadian profile in essential hypertension. The mean of systolic and diastolic BP of 48hr decreased from 148±12mmHg to 132±8mmHg and from 87±9mmHg to 76±6mmHg, respectively (P<0.001). The hyperbaric index of systolic and diastolic BP significantly decreased (P<0.01). The mean of heart rate of 48 hours showed no significant change. The hyperbaric index of BP significantly decreased during the night resting span.抄録全体を表示PDF形式でダウンロード (928K) -
ニセルゴリン散 (TA-079散) について井上 寛, 福間 悦夫, 渡辺 憲, 土井 清, 小松原 孝介, 松下 棟治, 猪原 淳, 久葉 周作, 杉原 徳郎, 橘 久之, 今岡 健 ...1991 年 22 巻 3 号 p. 661-671
発行日: 1991/09/30
公開日: 2010/04/30
ジャーナル フリーA powder preparation of the nicergoline “Sermion®” (TA-079 powder, containing 5mg of nicergoline in a 0.5g pouch) was administered to 29 patients with mild to moderate dementia due to cerebrovascular disease (15mg/day for eight weeks), and its efficacy, safety, and utility were evaluated.
Marked improvement was noted in delirium, headache, heavy-headedness, anxiety, irritation, bad temper, and problem behavior.
The final overall improvement ratings were as follows: improved or better, 37.9%; slightly improved or better, 69%; unchanged, 27.6%; and aggravated, 3.4% (1 case).
This drug for cerebrovascular disease was slightly useful or better in 69%.
Side effects were not found in all cases.抄録全体を表示PDF形式でダウンロード (965K) -
単回投与試験および連続投与試験成績中島 光好, 金丸 光隆, 植松 俊彦, 佐藤 隆一, 水野 淳宏, 長嶋 悟, 滝口 祥令, 田中 作彌, 日比 盛英, 斉藤 照夫, 吉 ...1991 年 22 巻 3 号 p. 673-683
発行日: 1991/09/30
公開日: 2010/04/30
ジャーナル フリーThe newly developed calcium channel blocker, NZ-105, was orally administered to 26 healthy adult male volunteers in single-dose (10, 20, 40mg) and multiple-dose (40mg b. i. d.) studies to investigate the safety and pharmacodynamics and pharmacological properties.
The following results were obtained.
1. Subjective symptoms were reported for the 20mg and 40mg single-dose and the multiple-dose studies, although these conditions were mild and transient.
There were no abnormal findings in clinical laboratory tests.
2. A reduction in systolic and diastolic blood pressures was observed after the single administration of 20mg and 40mg doses of NZ-105. The maximum reduction was attained about 3 to 6hr after drug administration. Pulse rate increased along with the reduction in blood pressure. The multiple-dose study showed a stable and continued reduction in systolic and diastolic blood pressures.
3. NZ-105 showed a stable diuretic effect in the single-dose and the multiple-dose studies.
4. The maximum plasma concentration (Cmax) and the area under the blood concentration vs. the time curve (AUC) were dose-dependent in the single-dose study. The AUC at day 1 and day 7 in the multiple-dose study was 52.8ng·hr/ml and 60.1ng·hr/ml, respectively. It is thus concluded that NZ-105 has no drug accumulation ascribable to the multiple dosing.抄録全体を表示PDF形式でダウンロード (1245K) -
Eleanor NEALON, 佐久間 昭1991 年 22 巻 3 号 p. 685-695
発行日: 1991/09/30
公開日: 2010/04/30
ジャーナル フリーPDF形式でダウンロード (1557K) -
小林 真一, 安原 一, 川村 芳江, 荒木 日出之助, 横山 裕子1991 年 22 巻 3 号 p. 697-701
発行日: 1991/09/30
公開日: 2010/04/30
ジャーナル フリーPDF形式でダウンロード (705K) -
本間 光夫, 風祭 元, 木島 昂, 小林 拓郎, 佐久間 昭, 清水 直容, 朝長 文弥, 内藤 周幸, 春見 建一1991 年 22 巻 3 号 p. 703-713
発行日: 1991/09/30
公開日: 2010/04/30
ジャーナル フリーPDF形式でダウンロード (1676K)
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