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Volume 79 (1982)
- Issue 6 Pages 461-
- Issue 5 Pages 343-
- Issue 4 Pages 237-
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- Issue 2 Pages 77-
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Volume 79, Issue 6
Displaying 1-11 of 11 articles from this issue
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Kohei KYUKI1982 Volume 79 Issue 6 Pages 461-485
Published: 1982
Released on J-STAGE: March 09, 2007
JOURNAL FREE ACCESSA procedure which can serve as a possible basis for the laboratory study of the topical effect of NSAID was investigated in rats or guinea pigs. The effect of NSAID was greatly influenced by physical characteristics of the preparation such as drug particle size, solubility, ointment base and concentration of drug. Moreover, it was also found to be affected by many technical factors such as animal fixation, drug application times and methods (rubbing times or occlusive dressing technique) and amounts applied which play an important role in topical preparation. The topical application of NSAID ointment (1% of indomethacin, ketoprofen or diclofenac sodium) markedly inhibited the paw edema by carrageenin in rats. The inhibitory activity was the same as that of steroidal ointment (0.12% betamethasone 17-valerate or 0.05% fluocinonide), but was less than that by oral administration of these NSAID. Also, the NSAID ointment obviously inhibited the ultraviolet erythema in guinea pigs and the swelling in the hind feet of adjuvant arthritic rats. The inhibitory activities of NSAID ointments on these inflammatory responses were almost the same as those obtained by oral administration of such NSAID and more potent than those of steroidal ointments. Furthermore, NSAID ointments increased the pain threshold in the inflamed foot as determined by the method of Randall and Selitto. The analgesic activity of NSAID ointment was more potent than that of steroidal ointment, but less than that of NSAID administered orally. On the other hand, neither the systemic effects such as decrease in weight of the adrenals and thymus which were noted when steroidal ointment was used, nor the gastrointestinal lesions which were found by oral administration of NSAID, were recognized in rats in which NSAID ointment was applied topically. The anti-inflammatory effects of NSAID ointment correlated well with the drug concentration at the site of inflammation. These findings suggest that NSAID ointment has a clinical use in the treatment of inflammatory diseases.View full abstractDownload PDF (11477K) -
Taeko HATA, Tomitaro KITA, Eiji ITOH, Akio NAMIMATSU1982 Volume 79 Issue 6 Pages 487-492
Published: 1982
Released on J-STAGE: March 09, 2007
JOURNAL FREE ACCESSElectrocardiography (ECG) was performed for SART stressed (repeated cold stressed) mice which had changes in blood pressure and blood flow to examine the effects of this treatment on heart function. In the ECG of mice subjected to SART stress for 5 days, potentiations of the R and T voltage, a shortening of the PQ interval, a prolongation of the QRS interval, and a slight increase of the heart rate were observed; and such changes in the EGG were maintained for several days. Recovery from all these changes was observed after a single dose or consecutive administrations of propranolol. From these results, it is considered that sympathetic nerve activity may be increased in the function of the heart in SART stressed mice, as contrasted to the partial vagotonia in the duodenum. Neurotropin (NSP), a nerve sedative, was then administered to mice once daily for 5 days during the SART stress. ' NSP prevented the changes of the PQ and QRS interval in SART stressed mice, but could not prevent the potentiation of the R and T voltage and the heart rate increase. In particular, the potentiations of the R and T voltages were thought to be induced by the increase of sympathetic nerve activity; therefore, it is thought that NSP may not have direct actions at least on the sympathetic nerve sites in autonomic nervous systems.View full abstractDownload PDF (2909K) -
Hideo NAKAMURA, Katsumi ISHII, Chieko IMAZU, Satoru MOTOYOSHI, Yuichi ...1982 Volume 79 Issue 6 Pages 493-508
Published: 1982
Released on J-STAGE: March 09, 2007
JOURNAL FREE ACCESSThe analgesic activity of zomepirac sodium was compared with that of various types of analgesics. Zomepirac sodium, like other non-steroidal anti-inflammatory drugs, was more active in the tests of Randall-Selitto (rats), silver nitrate-induced arthritic pain (rats), algesic-induced writhing (mice and rats), and bradykinin intraarterial injection (dogs), but inactive in the tests of D'Amour-Smith (mice), Haffner (rats), and electrical tooth pulp stimulation (dogs). The analgesic activity of zomepirac sodium was 0.5 to 1.7 times that of indomethacin, 2.1 to 19 times that of diclofenac sodium, and 48 to 200 times that of aspirin in these tests. The therapeutic index of the analgesic activity of zomepirac sodium (6.5 to 157) was larger than that of other anti-inflammatory drugs tested. Codeine and high doses of aminopyrine showed analgesic activity in all these tests, but pentazocine was inactive in the D'Amour-Smith test. Zomepirac sodium showed a potent anti-pyretic activity in the yeast and LPS-induced febrile rats or rabbits. From these results, it was concluded that zomepirac sodium had potent analgesic activity compared to that of indomethacin; and the mode of its analgesic action, unlike anti-pyretic, narcotic, and narcotic-antagonist analgesics, was similar to that of other acidic non-steroidal anti-inflammatory drugs.View full abstractDownload PDF (7285K) -
Hideo NAKAMURA, Yuichi YOKOYAMA, Satoru MOTOYOSHI, Yasuhiro SETO, Masa ...1982 Volume 79 Issue 6 Pages 509-527
Published: 1982
Released on J-STAGE: March 09, 2007
JOURNAL FREE ACCESSAnti-inflammatory and gastrointestinal ulcerogenic activities of zomepirac sodium were investigated in experimental animals. The inhibitory activity of zomepirac sodium against carrageenin hind paw edema in rats, acetic acid-induced increase in vascular permeability in mice, and UV-erythema in guinea pigs was more potent than that of indomethacin. Anti-edema activity of zomepirac sodium was seen in adrenalectomized rats. Zomepirac sodium, like indomethacin, inhibited the delayed phase of hind paw edema produced by mixed phlogistics, but not the early phase mediated by histamine and serotonin in rats. Zomepirac sodium produced a dose-dependent inhibition against granuloma formation, established adjuvant arthritis, and development of adjuvant arthritis in rats; and its activity was slightly less potent than that of indomethacin. The inhibitory activity of zomepirac sodium on PGE2 biosynthesis in vitro was about one-third that of indomethacin. The ulcerogenic activity of zomepirac sodium was about 5 times weaker than that of indomethacin. From these results, it was suggested that zomepirac sodium was effective on various types of inflammation and showed particularly potent inhibitory activity against acute inflammation. These findings suggest that the mode of action of zomepirac sodium is similar to that of other acidic non-steroidal anti-inflammatory drugs.View full abstractDownload PDF (9156K) -
Kazuhiro KUBO, Tony JAGENEAU1982 Volume 79 Issue 6 Pages 529-541
Published: 1982
Released on J-STAGE: March 09, 2007
JOURNAL FREE ACCESS1) Flunarizine (0.3 and 1 mg/kg, i.v.) and papaverine (1 mg/kg, i.v.) caused significant increases in cerebral blood flow and decreases in cerebral vascular resistance with concomitant increases in cerebrospinal fluid pressure, in spite of decreases in systemic blood pressure. The durations of these effects by flunarizine were longer than those by papaverine. 2) Heart rate increased markedly with papaverine, while it decreased with flunarizine only at a dose of 1 mg/kg, i.v. Central venous pressure increased slightly and temporarily with flunarizine, but it was not changed with papaverine. 3) Cerebral arteriovenous oxygen difference decreased with either of the drugs at a dose of 1 mg/kg, i.v. Meanwhile, cerebral oxygen consumption was not affected by flunarizine or papaverine. 4) Either of the drugs increased the P02 of the cerebral venous blood temporarily and slightly, but significantly, as well as the end tidal CO2 concentration. These results suggested that flunarizine has a longer acting cerebral vasodilatating effect than papaverine does without any effect on the cerebral oxygen consumption.View full abstractDownload PDF (5814K) -
Saizo YANAURA, Junzo KAMEI, Kazuhiro GOTO, Tomokazu HOSOKAWA, Tameo HI ...1982 Volume 79 Issue 6 Pages 543-550
Published: 1982
Released on J-STAGE: March 09, 2007
JOURNAL FREE ACCESSThe phrenic nerve activity is an appropriate indicator for the output of the respiratory center as a whole, although a quantitative analysis of each of the frequency band components that constitute the neural activities during the respiratory reflex has not yet been made by other investigators. In the present study, we have made a quantitative analysis of each of the frequency band components of phrenic nerve activity during the cough reflex in anesthetized dogs. The efferent activities of the phrenic nerve were recorded from the central cut end of the phrenic nerve. Each fraction of phrenic nerve activity was separated into bands spanning a range of 100 Hz each by a variable filter and analyzed using a program for the power spectrum. The cough reflex was induced by mechanical stimulation of the tracheal mucosa. In the power spectrum analysis of each frequency band, increase in the power of each of the frequency band components was observed during the cough reflex. Particularly, the power of the 2 ?? 100 Hz band components increased significantly as compared with the other frequency band components. Such an increase in the power of the 2 ?? 100 Hz band components toward the other frequency band components during the cough reflex was not observed after an i.v. administration of DMPP and lobeline, but the power increased extended over every frequency band. These findings suggest that the process for integrating the cough reflex was different from that of the other respiratory reflexes and that the present method is useful for investigating the central mechanisms of the cough reflex.View full abstractDownload PDF (3308K) -
Masayoshi YANAGIHARA, Kenji OKADA, Masakatsu NOZAKI, Kaito TSURUMI, Ha ...1982 Volume 79 Issue 6 Pages 551-560
Published: 1982
Released on J-STAGE: March 09, 2007
JOURNAL FREE ACCESSFifty to 500 mg/kg doses of the cephem antibiotics were intravenously injected to male rats twice a day for 3 days. After the last injection, the rats were fasted for 17 hours and then orally administered 2 g/kg of 20% ethanol. The blood levels of ethanol and acetaldehyde (AcH) were determined by gas chromatography. Cefotiam, cefsulodin, and cefazolin did not affect the blood levels of ethanol and AcH as compared with those of the control. Cefmetazole, cefamandole, and cefoperazone did not change the blood ethanol level, but these antibiotics increased the blood AcH level dose-dependently. Cefamandole was especially able to sustatin a high blood AcH level for over 8 hours. All of the antibiotics which increased blood AcH levels contain the 1-methyl-1H-tetrazole-5-thiol (TZ) group in their chemical structure. Intravenous injection of TZ caused a significant increase of the blood AcH level without influence on the blood ethanol level. 1-(2-Dimethylaminoethyl)-1H-tetrazole-5-thiol (MTZ), the functional group which is contained in cefotiam, did not affect the blood levels of ethanol and AcH. These results suggested that the disulfiram-like reaction of cefmetazole, cefamandole, and cefoperazone results from an increase of the blood AcH level, and the 3-substituent group in aminocephalosporanic acid, i.e., TZ, is an important factor for the reaction.View full abstractDownload PDF (4265K) -
Haruo OHNISHI, Chihiro ITO, Kazuo SUZUKI, Yutaka KITAMURA, Minoru SHIM ...1982 Volume 79 Issue 6 Pages 561-569
Published: 1982
Released on J-STAGE: March 09, 2007
JOURNAL FREE ACCESSEffects of protizinic acid (PRT) on prostaglandins (PG) and the production of oxygen radicals were compared with those of other non-steroidal anti-inflammatory agents. Oral administration of 30 mg/kg of PRT, indomethacin (IM), or ibuprofen (IB) significantly inhibited arachidonic acid-induced erythema in guinea pigs. Although 30 mg/kg of PRT significantly inhibited PGE2-induced erythema, IM and IB did not significantly inhibit it. PRT inhibited phospholipase A2 (PLA2) activity, and the IC50 value was 2.1 × 10-4M. On the other hand, IM and IB exerted no effect on the PLA2 activity at 3 × 10-4M. These results suggest that PRT possesses a broader pharmacological activity on the PG system than IM and III. As for effects on the production of oxygen radicals, the order of relative inhibitory potency was PRT> metiazinic acid (MA) = IM>IB=phenylbutazone (PB) in the xanthine oxidase assay, PB> IM> PRT> MA=IB in the rabbit neutrophil myeloperoxidase assay, and IM> PB> PRT> MA> IB in the guinea pig macrophage assay. In the rabbit neutrophil and aggregated IgG-bound micropore filter assay, the order was PRT<MA<PB<IM=IB. Thus, the inhibitory effects of PRT was verified in all experiments on the production of oxygen radicals in contrast to IB. In particular, it could be especially meaningful that PRT showed the most potent activity in the aggregated IgG-bound micropore filter assay which has been reported to be a good model for studying the pathogenesis of inflammatory diseases believed to be caused by immune complexes.View full abstractDownload PDF (4541K) -
Saizo YANAURA, Kazuhiro GOTO, Harumi KITAGAWA, Tomokazu HOSOKAWA, Miwa ...1982 Volume 79 Issue 6 Pages 571-579
Published: 1982
Released on J-STAGE: March 09, 2007
JOURNAL FREE ACCESSThe role of the vagal reflex in bronchoconstriction induced by histamine, acetylcholine, serotonin, and PGF2α was investigated in anesthetized dogs using a complete vagal blockade by cooling. We devised a thermode for vagal cooling. The vagal cooling was performed by circulating cold water through the thermode attached to fit snugly around the bilateral cervical vagus nerves. Airway musculature response was measured as a change in ventilation overflow with a modification of the Konzett-Rössler method. Drugs were injected close intraarterially into the right bronchial artery and inhaled into the airway. Afferent impulses of the vagus nerve were abolished by cooling at 0°C. When the vagus nerves were cooled to 0°C, the ventilation overflow decreased. On the other hand, when the nerves were rewarmed, the ventilation overflow increased again. Bronchoconstriction was produced by close intraarterial injection of histamine, acetylcholine, serotonin, or PGF2α at a dosage of 10 μg each. The bronchoconstrictions produced by these agents were inhibited by vagal cooling. The bronchoconstrictions induced by histamine, acetylcholine, and serotonin were all 0.00125%, and that by PGF2α was 0.0001%. Inhalations for 10 min were also inhibited by vagal cooling. These findings indicate that the thermode devised in this study is useful for vagal cooling and that vagally mediated bronchoconstriction is a relatively major component of bronchoconstriction induced by chemical mediators.View full abstractDownload PDF (3925K) -
Junya IKUTA, Yoichi YAMAUCHI, Sadahiro SHIMIZU1982 Volume 79 Issue 6 Pages 581-589
Published: 1982
Released on J-STAGE: March 09, 2007
JOURNAL FREE ACCESSCombined effects of prazepam and trichlormethiazide (TCM) which were given simultaneously were studied in renal hypertensive rats (1-kidney type) and DOCA hypertensive rats. In this study the blood pressure was measured by the plethysmographic method. Orally administered prazepam alone did not show any appreciable effect on the blood pressure, while TCM, even when administered alone, exhibited marked and long-lasting hypotensive effects in both hypertensive rats. In addition, the hypotensive effect of TCM was apparently potentiated by the concurrent use of prazepam. In the experiment where conscious and unconstricted spontaneous hypertensive rats (SHR) were used, the pressor response and tachycardia were observed when foot shock (acute stress) was loaded. This pressor response was the “ all or none ” type and a threshold existed. In contrast to the pressor response, the degree of tachycardia varied depending on the intensity of the stress. The similar responses were also observed in normotensive rats, although the degrees of the responses were significantly weaker than those in SHR. Prazepam given alone obviously suppressed the cardiovascular responses mentioned above. The present results suggest that prazepam is an useful drug for the treatment of hypertension.View full abstractDownload PDF (3819K) -
Manabu MURAKAMI, Zenji SASAKI, Fumio MISAKI, Keiichi KAWAI, Tsuneo WAK ...1982 Volume 79 Issue 6 Pages 591-597
Published: 1982
Released on J-STAGE: March 09, 2007
JOURNAL FREE ACCESSThe effects of various antiulcer drugs and hormones on the cell kinetics of the mouse gastric mucosa were studied using an autoradiographic technique with 3H-thymidine. The drugs or hormones were administered orally or parenterally once or twice a day for 7 consecutive days, and 3H-thymidine was injected after the last administration of the drug. The autoradiograph was prepared and then the labeling index was counted. Cimetidine (100 mg/kg × 2/day, p.o.), geranylgeranylacetone (GGA, 100 mg/kg × 2/day, p.o.), and Cu-chlorophyllin-Na (300 mg/kg × 2/day, p.o.) did not show any effect on the labeling indices in both the tissues of the fundic and pyloric glands, while carbenoxolone (100 mg/kg x 2/day, p.o.) reduced the labeling index in the pyloric glands. Tetragastrin (1 mg/kg × 1 /day, i.m.) increased the labeling index in the fundic glands, whereas secretin did not affect it. Hydrocortisone (100 mg/kg × 1/day, s.c.) reduced the labeling index in the fundic glands, and this reducing effect was prevented by combining hydrocortisone with GGA. From these results, it was indicated that the labeling index in the normal mouse gastric generative zone was not influenced by the tested antiulcer drugs, except carbenoxolone; but the index was influenced by tetragastrin and hydrocortisone, especially in the fundic glands. It was also suggested that the changes in the cell kinetics of the gastric mucosa could be related to the etiology of gastric ulcer since there was a possibility that geranylgeranylacetone could control the action of hydrocortisone, an ulcerogenic agent, on the gastric mucosal cell-cycle.View full abstractDownload PDF (4141K)
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