巻号一覧
13 巻 (1982)
- 4 号 p. 495-
- 3 号 p. 363-
- 2 号 p. 221-
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13 巻, 2 号
選択された号の論文の12件中1～12を表示しています
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花岡 一雄, 釘野 豊城, 山村 秀夫1982 年 13 巻 2 号 p. 221-227
発行日: 1982/06/30
公開日: 2010/06/28
ジャーナル フリーZomepirac sodium is a new non-narcotic analgesic antiphlogistic developed by McNeil Laboratories, U. S. A., particularly noted for its strong analgesic effect upon oral administration.
As reported in this paper, a comparative study of the analgesic effect of zomepirac sodium was conducted in comparison with aspirin and a placebo based on pain meter measurements.
The pain meter used was the Nakahama-type NYT-model 5 which is an improved version of the original pain meter developed by Hardy et al.
Two methods were used in recording pain: The intensity method in which the duration of the stimulus was set at a fixed standard and the amount of radiant energy was measured and the time method in which the amount of radiant energy was set at a fixed standard and the duration of the pain was measured.
The subjects were 9 healthy male volunteers who were divided into three groups, namely the 200 mg zomepirac group, the 500 mg aspirin group and the placebo group.Measurements were taken on the hand, leg, and breast.
The results obtained indicate that it is impossible to detect any significant difference between zomepirac sodium, aspirin and the placebo in either the time or intensity methods.
It is said that in general such non-narcotic analgesics as zomepirac sodium do not respond well to mechanical stimuli such as used during this experiment and our results support this conclusion. This analgesic exhibits quite different characteristics in comparison with CNS analgesics such as pentazocine.抄録全体を表示PDF形式でダウンロード (732K) -
猿田 享男1982 年 13 巻 2 号 p. 229-242
発行日: 1982/06/30
公開日: 2010/06/28
ジャーナル フリーThe bioavailability of methyldopa was assessed in 9 normal male subjects in a cross-over study following single doses of 500 mg of methyldopa fine granules and 500 mg tablets. The following results were obtained:
1 . Methyldopa fine granules and tablets were shown to be bioequivalent, with no statistically significant difference in plasma concentration at each time and pharmacokinetic parameters including Cmax, Tmax, [AUC], t1/2 and clr.
2. No significant difference in the 24 hour urinary excretion was observed between two forms.
3. No significant difference in normal blood pressure and pulse rate was detected between two forms.
4. Peripheral blood counts, blood chemistry and urine tests showed no abnormali-ties.抄録全体を表示PDF形式でダウンロード (1422K) -
単回および反復経口投与について安原 一, 亀井 勝彦, 後藤 裕美, 坂本 浩二1982 年 13 巻 2 号 p. 243-252
発行日: 1982/06/30
公開日: 2010/06/28
ジャーナル フリーEither single (50mg) or multiple (25mg/day × 4 days) dose of etretinate was administered orally into 5 healthy volunteers once a day 30 minutes after breakfast.After the administration with a single dose of 50mg or the initial dose of 25mg, the AUC (Area Under the Curve) of the blood level of unchanged etretinate was 1, 305 ng · Ehr/ml with 50mg and 267 ng · Ehr /ml with 25mg. The approximate half-life was 2 hr with 25 mg and 3.6 hr with 50mg. The AUC of the main metabolite, Ro 10-1670, was 2.7 times as large as that of unchanged etretinate with the first dose of 25 mg, but the AUC with 50mg was merely 1.5 times as large as that with the first dose of 25mg.
On the 4 th day of the administration with 25 mg/day, the AUC of unchanged etretinate became 1.6 times as large as the 1st day, but the AUC of the main metabolite was decreased on the 4 th day down to 61% of the level on the 1st day. The amount equivalent to 49% (28.0-66.%) of the dose was excreted into feces. Fecal excretion rate was 3.3%for the main metabolite. No changed etretinate nor its main metabolite was detected in the urine. Main adverse reactions attributable to etretinate were itching of the skin, dryness, headache and desquamation. These results suggest that etretinate was not absorbed well but metabolized rapidly after absorbed and the metabolism would be saturated and the hepatic metabolic capacity for etretinate in maximum seemed to be 30 to 40mg. That is, the pharmacokinetic process of etretinate was considered to take place not in the first order kinetics but zero order kinetics.抄録全体を表示PDF形式でダウンロード (1127K) -
Hiroko TOGASHI, Masaru MINAMI, Yukihide BANDO, Keiichi SHIMAMURA, Yuic ...1982 年 13 巻 2 号 p. 253-264
発行日: 1982/06/30
公開日: 2010/06/28
ジャーナル フリーThe present experiment was undertaken to elucidate the simultaneous effect of clonidine on ambulatory activity and water drinking behavior in spontaneously hypertensive rats (SHR). An attempt was also made to determine the role of sympathetic nerve activity in the mechanism of clonidine-induced sedation in SHR. The sensitive method developed by Tadokoro et al. for simultaneous determination of ambulatory activity and drinking behavio in rats was used. Clonidine (150μ Eg/kg, po twice daily) produced a significant decrease in ambulatory activity and water drinking behavior at the beginning of the dark phase in twenty week old male SHR of Wistar Okamoto strain. Clonidine produced an increase in water drinking behavior in the light phase which was not observed in the control period. Under the same experimental conditions, the lowering of brain stem norepinephrine content produced by diethyl dithiocarbamate appeared to be inhibited in clonidine-treated SHR in the dark phase. Clonidine significantly decreased urinary norepinephrine content in the dark phase. On the other hand, clonidine (30μ g/kg, iv) produced a decrease in efferent nerve discharges of splanchnic nerve and sympathetic adrenal nerve in SHR. These findings suggest that decreased sympathetic nerve activity via a centrally mediated mechanism is at least in part associated with the decreased ambulatory activity induced by clonidine.抄録全体を表示PDF形式でダウンロード (1331K) -
海老原 昭夫, 岡 太一, 田原 一二, 大橋 京一, 近藤 和興, 渡部 烈, 沖山 雅彦, 萬宝 国久1982 年 13 巻 2 号 p. 265-271
発行日: 1982/06/30
公開日: 2010/06/28
ジャーナル フリーThe pharmacokinetics of ranitidine, a new H2-receptor blocking agent, and its effects on tetragastrin-induced gastric acid serection were studied in five healthy volunteers. The ranitidine concentrations in plasma and urine were determined by HPLC.
After single oral administration of ranitidine (100 mg or 150 mg tablet), the peak plasma concentration of the drug was attained in 2-2.5 hrs and the elimination half-life was 2-2.5 hrs when they were obtained from the 24-hr plasma concentration-time curve. After the administration of 100 mg and 150 mg, the maximum plasma levels were in the ratio of 1: 1.57 and the AUCs were, 1: 1.53 which were roughly coincident with the dose ratio. Recovery of unmetabolized ranitidine from urine over a 24-hr period accounted for 40-45% of the administered drug.
In the multiple oral doses of ranitidine (150mg b. i d., for 14 days), the actually measured plasma concentrations of the drug were nearly in agreement with the simulation curves obtained from the single dose.
A single dose of ranitidine (150mg/10ml) significantly reduced gastric volume rate and the output concentration of the acid induced by tetragastrin.
No abnormality attributable to ranitidine was noted in physical findings, clinical laboratory findings or subjective symptoms.抄録全体を表示PDF形式でダウンロード (785K) -
大橋 和史, 角尾 道夫, 永井 俊彦, 常岡 健二, 渋谷 正則1982 年 13 巻 2 号 p. 273-283
発行日: 1982/06/30
公開日: 2010/06/28
ジャーナル フリーInfluence of liver disease on metabolism and pharmacokinetics of cephalothin (CET) was studied. CET was given 1g bolus intravenously to 7 patients with liver cirrhosis, 7 patients with hepatitis (3 cases of acute hepatitis and 4 of chronic active hepatitis) and 7 patients with normal liver function. Serum consentration of CET and deacetyl CET was measured by High Performance Liquid Chromatography.
Ratio of deacetyl CET to CET was less in cirrhosis compared to that in hepatitis or control group, demonstrating impaired metabolism of CET to deacetyl CET in cirrhosis. Deacetyl CET/CET ratio was correlated to such liver function test as BSP retention rate, prothrombin time or serum γ -globulin level which were characteristic in chronic liver disease, while not correlated to GP T, GOT, γ -GTP, total bilirubin which are characteristic in acute hepatic parenchymal disorders.
Pharmacokinetic parameters calculated as two compartment open model were not statistically different among three groups.
These results show that severe chronic liver disease impairs the biotransformation of CET to deacetyl CET, but does not affect pharmacokinetics of CET.抄録全体を表示PDF形式でダウンロード (1487K) -
蓮沼 正明, 豊寺 一彦, 中島 光好1982 年 13 巻 2 号 p. 285-299
発行日: 1982/06/30
公開日: 2010/06/28
ジャーナル フリーThe influence of penbutolol on hypertension and its diurnal variation wereinvestigated in 12 inpatients with essential hypertension. The study extended for 14 days. Placebo was administered b.i.d., i.e., after breakfast (8 a.m.) and dinner (5 p.m.) for the first 7 days (pretreatment period). Penbutolol 40 mg was administered in the same manner for the latter 7 days (treatment period). Blood pressure and pulse weremeasured 3 times, i.e., at arising in the morning (5 a.m.), after lunch (1 p.m.) and before going to bed (7 p.m.), daily for the 14 days. On the 7 th day of each period, these parameters were measured not only at the above 3 points of time but also at 7 a.m., 9 a.m., 11 a.m., 3 p.m. and 5 p.m..
The following results were obtained:
1) Blood pressure and pulse were significantly reduced in 8 and 9 patients, respectively.
2) An analysis of measurements made 3 times daily showed that systolic blood pressure (SBP), diastolic blood pressure (DBP) and pulse were significantly decreased at all given times on the 3 rd to 7 th days of the treatment. Diurnal variations of both SBP and DBP were also significantly reduced.
3) An analysis of measurements made 8 times on the 7th day showed that a significantly decrease was observed in SBP at 5a.m., 11a.m., 1p.m., 3p.m. and 7p.m.; DBP at the last 5 points of time; and, pulse at all points of time. Only SBP showed a significantly reduction in diurnal variation.抄録全体を表示PDF形式でダウンロード (1432K) -
健常人, 慢性腎不全例, 肝硬変症例での検討藤原 研司, 尾形 逸郎, 三代 俊治, 太田 裕彦, 林茂 樹, 山形 陽1982 年 13 巻 2 号 p. 301-310
発行日: 1982/06/30
公開日: 2010/06/28
ジャーナル フリーSerum concentrations, urinary excretion and diuretic effect of piretanide werestudied in 9 subjects (3 healthy volumteers, 3 patients with chronic renal failure and 3 patients with liver cirrhosis) after a single 6mg oral dose. The following results were obtained:
(1) Peak serum concentrations of piretanide were attained within 2 hours after treatment in all subjects. Peak serum concentrations and the AUC of the serum concentration curve did not indicate any marked inter-subject variations in absorption.
(2) The disappearance of piretanide from the serum was prolonged in patients with reduced renal function. After 24 hours, however, no appreciable amounts of piretanide were detected, even in patients with chronic renal failure.
(3) Urinary piretanide excretion was generally completed within 24 hours after treatment in all three groups. The excretion in the renal failure group was, however, lower than in the other two groups.
(4) 24-hour urine volumes were comparable in all three groups. Electrolyte (Na+, K+, Cl-), creatinine and uric acid excretion was lower in the renal failure group.
(5) In the healthy volunteer and liver cirrhosis groups, serum concentrations and urinary excretion of piretanide both closely reflected diuretic effect. In the renal failure group, diuretic activity was only correlated with urinary excretion of piretanide and not with serum concentrations of drug.抄録全体を表示PDF形式でダウンロード (1182K) -
多施設二重盲検比較試験村尾 覚, 木村 栄一1982 年 13 巻 2 号 p. 311-326
発行日: 1982/06/30
公開日: 2010/06/28
ジャーナル フリー我が国で発見, 開発されたnicorandil (15～45 mg/日, 3分服) の狭心症に対する臨床効果をpropranolol (30～90mg/日, 3分服) のそれと比較するため, 多施設二重盲検法を行い下記の成績を得た.
1) 試験の対象として採用された症例はnicorandil群36例, propranolol群44例であった. 観察期間は, 原則として2週間, 第3週はnicorandil 15mgないしはpropranolol 30mg, 第4週はnicorandil 30mgまたはpropranolol 60mgと増量し, 第5週は変量期とした.
2) 狭心症発作回数は両群とも有意の減少を示し, その減少率は第4, 第5週において nicorandil群の方が有意に大であった. 亜硝酸剤消費量も有意の減少を示したが, 両群間に有意差は認められなかった.
3) 全般改善度では, 著明改善率において, nicofandil 群の方が有意に大であり, 第4, 第5週における週別改善度もnicorandil群で有意に大であった.
4) 有用度も nicorandil群が有意に大であった (U-test). 特に, 「極めて有用」に占める比率が有意に高かった.
5) 心拍数は両群で, 血圧はpropranolol群で減少した. その度合は propranolol 群で大なる傾向を示した.
6) ST偏位からみた心電図改善率はnicorandil 群45.8%, propranolol群 56.0%と有意差はなかった.
7) 副作用出現率はnicorandil群13.5%, propranolol群16.7%と有意差はなかった. Nicorandilの副作用としては頭痛が最も多かった. 副作用に基づく投薬中止ないし減量はnicorandil群1例, propranolol群2例であった.
以上, nicorandilはニコチン酸誘導体の亜硝酸エステルではあるが, nitroglycerinなどの亜硝酸剤とは薬理作用が異なるため, 抗狭心症剤分類において新しいカテゴリーに入るとみなされ, 臨床上有用な薬剤と判断された.
なお, 本試験に用いたpropranolol錠は星薬科大学薬剤学教室・永井恒司教授により含量試験, 崩壊試験, 溶出試験のいずれも市販 propranolol錠の条件に適合することが証明されるとともに, 市販propranolol錠と生物学的に同等であることも確認された. ここに付記し, 感謝の意を表する.抄録全体を表示PDF形式でダウンロード (1672K) -
梅田 照久, 大石 誠一, 岩岡 大輔, 三浦 央博, 藤井 弓子, 佐藤 辰男1982 年 13 巻 2 号 p. 327-333
発行日: 1982/06/30
公開日: 2010/06/28
ジャーナル フリーLabetalol which has the combined α - and β -adrenoceptor blocking actions was administered in doses of 300 to 600mg/day for one month to a patient with essential hypertension to observe endocrine homeostatic action.
Antihypertensive effect was noted from the first day of administration and the effect became more marked with dose-dependency with neither any side effect nor remarkablechange in the laboratory findings as the dose was increased from 300mg/day to 400mg and 600mg/day. Marked suppressions on PRA, secretion of aldosterone and manifestation of borderline diabetic data in glucose tolerance test were noted after labetalol. No difference in THS levels between before and after the administration, but lowering of the prolactin level and increase in LH and FSH responses were noted.抄録全体を表示PDF形式でダウンロード (611K) -
[Clinical Pharmacology Today―International Survey of Present Status and Problems] 記録1982 年 13 巻 2 号 p. 335-346
発行日: 1982/06/30
公開日: 2010/06/28
ジャーナル フリーPDF形式でダウンロード (1544K) -
1982 年 13 巻 2 号 p. e1
発行日: 1982年
公開日: 2011/02/25
ジャーナル フリーPDF形式でダウンロード (23K)
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