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Volume 14 (1983)
- Issue 4 Pages 559-
- Issue 3 Pages 437-
- Issue 2 Pages 357-
- Issue 1 Pages 7-
Volume 14, Issue 2
Displaying 1-10 of 10 articles from this issue
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In Vitro and In Vivo StudiesNaoki TANIGUCHI, Hirohiko FURUI, Kazunobu YAMAUCHI, Iwao SOTOBATA1983 Volume 14 Issue 2 Pages 357-363
Published: June 30, 1983
Released on J-STAGE: June 28, 2010
JOURNAL FREE ACCESSThe present study was undertaken to estimate in vitro and in vivo effects of dilazep on the hemoglobin-oxygen dissociation curve of venous blood from 16 healthy men.
Dilazep (5×10-6 to 5×10-4M) significantly shifted the oxygen dissociation curve of the hemoglobin to the right but did not affect the 2, 3-DPG contents on incubation of blood samples for 2 to 4 hours with the drug. In vivo administration of dilazep (300mg/day for one week), however, produced a significant shift of the curve to the left. This leftward shift was accompanied with a tendency for contents of 2, 3-DPG to decrease without a significant changes in HbAIC levels. There were no changes observed in P50, 2, 3-DPG and HbAlc levels with a lower dosage of dilazep (150 mg/day for oneweek).
These findings suggested that the increased oxygen binding to hemoglobin induced by dilazep in vivo resulted from a probable increase in systemic oxygen delivery due to its vasodilating effects.View full abstractDownload PDF (848K) -
Phase I Clinical TrialKazuo HANAOKA, Megumi TAGAMI, Yutaka INADA, Hideo YAMAMURA, W. D. BECH ...1983 Volume 14 Issue 2 Pages 365-377
Published: June 30, 1983
Released on J-STAGE: June 28, 2010
JOURNAL FREE ACCESSA phase I study of brotizolam has been performed with 9 healthy male Japanese volunteers. After a single oral administration of 0.125 mg, 0.25 mg and 0.5 mg in 3 volunteers respectively, psychic and physical symptoms, vital signs, ECG, laboratory values (urine, blood and blood chemistry tests) and blood levels were examined.
1. Induction of sleep due to the action of the drug and decrease in blood pressure due to the induced sleep were observed dose-dependently. A tendency of decrease in respiratory rate was also noted, but it was not a clinically meaningful change. A peak of these effects appeared around 2 hrs after administration and thereafter disappeared gradually in approximate conformity with the change of plasma concentration of brotizolam.
2 . The secondary effects such as unsteadiness, dizziness and dullness, and other symptoms, e. g. dry mouth, were observed, but these symptoms were mild and appearedto have no clinical significance.
3. No abnormal laboratory findings were noted.
4 . Plasma concentration of brotizolam reached its maximum at 0.5-4 hours after oral administration. Almost linear correlation was found in the relations between Cmax and administration doses, and between AUC and administration doses.
The above results establish the safety of brotizolam in healthy Japanese volunteers.View full abstractDownload PDF (1459K) -
Receptor AntagonistAkio EBIHARA, Masanobu TSURU, Kyoichi OHASHI, Kazuoki KONDO, Taichi OK ...1983 Volume 14 Issue 2 Pages 379-385
Published: June 30, 1983
Released on J-STAGE: June 28, 2010
JOURNAL FREE ACCESSPharmacokinetic and Pharmacological effects of injected ranitidine, a new histamine H2-receptor antagonist, were studied on six male healthy volunteers. Inhibition of tetragastrin-induced gastric acid secretion and changes of various hormones in plasma were also studied after ranitidine administrations by double-blind cross-over comparison with placebo.
Plasma ranitidine concentration-time curve was well fitted to the two compartment open model. Following intravenous administration of 50mg ranitidine, the apparent volume of distribution (Vd) was 81. 4±4.81 and total body clearance (Clp) and renal clearance (Clr) were 38.0±2.9 and 32.2±2.4 l/hr, respectively, and elimination half-life (t1/2β) was 1.9±0.09hr. The fraction of drug excreted unchanged in urine expressed as a percentage of administered dose, was 85%within 24 hours after administration. Tetragastrin-induced gastric acid secretion was significantly inhibted until two hours after administration of ranitidine.
Plasma prolactin and parathormone concentrations were not influenced by ranitidine.Plasma gastrin and secretin were not influenced by ranitidine except for slight changes at three hours and one hour, respectively, after administration of ranitidine.View full abstractDownload PDF (781K) -
Akira KISHIMOTO, Chikara OGURA, Rokuro MIZUKAWA, Toshio TSUTSUI, Fumia ...1983 Volume 14 Issue 2 Pages 387-398
Published: June 30, 1983
Released on J-STAGE: June 28, 2010
JOURNAL FREE ACCESSTo compare adverse reactions due to zimelidine (ZMD) and imipramine (IMP), double blind control trials were performed in healthy young (mean age: 23.4 years) male volunteers.
Influence on self-ratings and physiological measurements were compared in cross-over fashion between a single oral administration of ZMD 50 mg and that of IMP 25 mg, and ZMD 100 mg and IMP 50 mg, respectively.
ZMD hardly changed heart rate, but IMP 50 mg induced tachycardia 3 to 24 hrs after the administration. ZMD did not influence systolic blood pressure. On the other hand, IMP 50 mg decreased systolic blood pressure and there was a significant difference between the two drugs 4 hrs after the administration (p<0.05). Postual hypotention was recognized in the case of IMP administration.
ZMD 100mg decreased critical fusion frequency of flicker less than IMP 50mg (p<0.05-0.01).
ZMD did not influence salivary rate, but after IMP 25 mg or 50 mg of IMP intense decrease of salivary rate was observed.
There were no significant differences after the two drugs in the measurements of function of equibrium, tapping rate, accomodation width and standing ability on one foot.View full abstractDownload PDF (1585K) -
[in Japanese], [in Japanese], [in Japanese], [in Japanese], [in Japane ...1983 Volume 14 Issue 2 Pages 399-401
Published: June 30, 1983
Released on J-STAGE: June 28, 2010
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[in Japanese]1983 Volume 14 Issue 2 Pages 403-408
Published: June 30, 1983
Released on J-STAGE: June 28, 2010
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[in Japanese]1983 Volume 14 Issue 2 Pages 409-411
Published: June 30, 1983
Released on J-STAGE: June 28, 2010
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[in Japanese]1983 Volume 14 Issue 2 Pages 413-415
Published: June 30, 1983
Released on J-STAGE: June 28, 2010
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[in Japanese]1983 Volume 14 Issue 2 Pages 417-418
Published: June 30, 1983
Released on J-STAGE: June 28, 2010
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[in Japanese]1983 Volume 14 Issue 2 Pages 419-421
Published: June 30, 1983
Released on J-STAGE: June 28, 2010
JOURNAL FREE ACCESSDownload PDF (317K)
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