著者

中川 靖一

出版者

公益社団法人 日本薬学会

雑誌

YAKUGAKU ZASSHI (ISSN:00316903)

巻号頁・発行日

vol.133, no.5, pp.561-574, 2013-05-01 (Released:2013-05-01)

参考文献数

65

被引用文献数

1 5

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Cardiolipin (CL) is a phospholipid, which is exclusively located in mitochondria, and has a unique structure that consists of 2 phosphate residues and 4 kinds of fatty acyl chains. Cardiolipin plays an important role in regulating various kinds of mitochondrial proteins such as electron transport complexes, carrier proteins and phosphate kinases, and is also essential for the organization of particular mitochondrial structures such as cristae and contact sites. Mitochondrial phospholipase D hydrolyzes CL to produce phosphatidic acid, which is required for mitochondrial fusion. Oxidative stress-induced peroxidation of CL occurs because CL is rich in polyunsaturated fatty acids, especially linoleic acid. Accumulation of CL hydroperoxide (CLOOH) triggers the initiation of apoptosis. Formation of CLOOH causes the release of proapoptotic factors such as cytochrome c from the inner mitochondrial membrane and triggers opening of the permeability transition pore. Levels of CL decrease in the heart following ischemia or disease. Apoptosis is enhanced in temperature-dependent mutant cells whose amounts of CL reduce to half when compared to that of wild type cells. Low levels of CL cause the accumulation of CLOOH and enhance sensitivity to apoptosis. Accumulation of CLOOH in mitochondria causes instability of the membrane, because swelling of mitochondria is induced by the presence of CLOOH in the membrane and is significantly enhanced in CLOOH-loaded mitochondria by the addition of inducer of swelling.

著者

大嶋 繁 原 彩伽 阿部 卓巳 秋元 勇人 大原 厚祐 根岸 彰生 冲田 光良 大島 新司 井上 直子 沼尻 幸彦 小川 越史 齋木 実 小林 大介

出版者

公益社団法人 日本薬学会

雑誌

YAKUGAKU ZASSHI (ISSN:00316903)

巻号頁・発行日

vol.137, no.5, pp.623-633, 2017 (Released:2017-05-01)

参考文献数

20

被引用文献数

5

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Pharmacists applied deprescribing, which is a process for the rational use of drugs, for 13 at-home patients. The standard used for the rational use of drugs was the “Guidelines for Medical Treatment and Its Safety in the Elderly” (the Guidelines). The results of the deprescribing were discussed with physicians to determine prescriptions. After the prescription change, activities of daily living (ADL) and QOL were assessed using the Barthel Index and SF-36v2, respectively. Potentially inappropriate medications (PIMs) were detected in 10 of the 13 patients (76.9%). This detection rate is higher than previous PIM detection rates of 48.4% and 40.4% reported in prescriptions for home-care patients in Japan under the Beers and STOPP/START criteria. The Guidelines appeared useful as a decision support tool for deprescribing. The patients continuing the changed prescriptions showed no decrease in ADL or QOL after deprescribing, suggesting its rationality. The 10 measurement items of the Barthel Index were all suitable for evaluating the physical conditions of the patients. Meanwhile, SF-36v2 includes many items, but few indexes were directly applicable.

著者

内林 政夫

出版者

公益社団法人 日本薬学会

雑誌

YAKUGAKU ZASSHI (ISSN:00316903)

巻号頁・発行日

vol.127, no.1, pp.217-224, 2007-01-01 (Released:2007-01-01)

参考文献数

15

被引用文献数

2 2

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A biography of Leo Sternbach, an inventor of benzodiazepine tranquillizers, is presented. It consists of (1) a societal desire for lifestyle pills, (2) Leo's birth in 1908 and youth, (3) education, (4) in Vienna, (5) in Zurich, (6) at Hoffmann-La Roche, Basel, (7) to the New World, (8) at Roche, Nutley NJ, (9) invention of the new drugs, (10) revolution of people's lifestyle, and (11) reward, retirement and obituary in 2005. This paper may be the first comprehensive biography of this remarkable chemist written in Japanese.

著者

今井 志乃ぶ

出版者

公益社団法人 日本薬学会

雑誌

YAKUGAKU ZASSHI (ISSN:00316903)

巻号頁・発行日

vol.141, no.2, pp.169-174, 2021-02-01 (Released:2021-02-01)

参考文献数

16

被引用文献数

1

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Medical big data, also referred to as ‘real-world data’ (RWD) is defined as “data related to patient health status and/or health care delivery collected routinely from a variety of sources”. This includes data from disease and drug registries, electronic health records, claims and billing data and census data collected from clinicians, hospitals, and payers. Observational studies using RWD collected during general clinical practice are considered complementary to randomized control trials. However, since this design does not allow the random assignment of patients, causal inference analyses are required. Researchers should study the protocol properly before considering the combination of study design, the characteristics of data source, calculation of the appropriate sample size and the validity of outcomes. Data definition using data code should also be considered. Furthermore, the reliability of the source studies must be considered and discussed when the article is written. This review aims to outline the methods for performing reliable observational studies using RWD.

著者

高谷 甲波 大谷 道輝 野澤 茜 眞部 遥香 山村 喜一 大野 嘉子 赤羽 喜文 石井 宏幸

出版者

公益社団法人 日本薬学会

雑誌

YAKUGAKU ZASSHI (ISSN:00316903)

巻号頁・発行日

vol.135, no.12, pp.1371-1375, 2015-12-01 (Released:2015-12-01)

参考文献数

14

被引用文献数

1

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White petrolatum is frequently used as an oleaginous base, but has a drawback of poor usability. In this trial, white petrolatum was prepared at a lower melting point to improve its usability. Characteristic pharmaceutical values such as melting point, yield, and consistency were compared between a conventional product and ophthalmic white petrolatum. Usability was compared by administering a survey questionnaire and evaluating the comparable moisturizing effect by conductivity in humans. The melting point and yield value of the improved product were significantly lower compared with other white petrolatum products. In the survey, the improved product was rated excellent in five criteria. On a scale of 1 to 5, the average values for the five criteria for the improved product were 4.7, while the conventional product and ophthalmic white petrolatum were rated 3.0 and 3.5, respectively. No difference in moisturizing effect was observed among all petrolatums after application, from day 1 to day 14. In conclusion, the improved white petrolatum demonstrated better usability, and the moisturizing effect was equivalent to conventional product, suggesting that the use of this improved product may lead to improved adherence.

著者

岩﨑 綾乃 辻 明弘 今井 公江 中西 邦夫

出版者

公益社団法人 日本薬学会

雑誌

YAKUGAKU ZASSHI (ISSN:00316903)

巻号頁・発行日

vol.134, no.6, pp.775-780, 2014-06-01 (Released:2014-06-01)

参考文献数

13

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There is little information regarding the acid-neutralizing capacity of over-the-counter (OTC) gastrointestinal medicines. In this study, we assessed the acid-neutralizing capacity of OTC and prescribed gastrointestinal drugs based on the Japanese Pharmacopoeia 16th Edition. The acid-neutralizing capacity of the OTC drugs was calculated using experimental results for the crude materials found in the prescribed drugs based on OTC antacid quantity. The measured acid-neutralizing capacities of the OTC drugs agreed with the respective calculated values. These results indicate that the acid-neutralizing capacity of OTC drugs labeled as an antacid without information on their capacity can be estimated based on the quantity and capacity of the antacid components.

著者

富田 隆 後藤 英和 吉村 勇哉 坪内 良子 中西 利恵 小島 千賀子 米島 美穂子 吉田 正 田中 勝也 住谷 賢治 幸田 幸直

出版者

公益社団法人 日本薬学会

雑誌

YAKUGAKU ZASSHI (ISSN:00316903)

巻号頁・発行日

vol.135, no.6, pp.835-840, 2015-06-01 (Released:2015-06-01)

参考文献数

8

被引用文献数

11 17

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It has been reported that magnesium oxide tablets are excreted in a non-disintegrated state in the stool of patients when the tablets are administered after being immersed in a food thickener. Therefore we examined whether immersion in a food thickener affects the pharmacological effect in patients taking magnesium oxide tablets, and whether immersion affects its disintegration and solubility. The mean dosage (1705 mg/d) was higher for patients who took tablets after immersion in a food thickener than for those who took non-immersed tablets (1380 mg/d). The disintegration time and dissolution rate of the immersed tablets were lower than those of non-immersed tablets in vitro. Furthermore, components that constitute the food thickener and differences in composition concentrations differentially affect the disintegration and solubility of magnesium oxide tablets. This suggests that commercially available food thickeners are likely to be associated with changes in the degradation of magnesium oxide tablets, and they therefore should be carefully used in certain clinical situations.

著者

田村 悦臣

出版者

公益社団法人 日本薬学会

雑誌

YAKUGAKU ZASSHI (ISSN:00316903)

巻号頁・発行日

vol.140, no.11, pp.1351-1363, 2020-11-01 (Released:2020-11-01)

参考文献数

30

被引用文献数

4

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Epidemiological studies have shown that coffee consumption may be associated with a lower risk of developing several chronic disorders. To elucidate the molecular mechanism of the effects of coffee, we analyzed molecular response upon exposure to coffee extract using cellular and animal models of these diseases. As obesity is recognized as a major risk factor for these chronic diseases, we investigated the effect of coffee on adipogenesis using mouse preadipocyte 3T3-L1 cells. We found that coffee induced proteasomal degradation of IRS-1, leading to reduction of PPARγ expression, a master transcription factor for adipogenesis. Reduction in weight as well as in IRS-1 expression was detected in the fat tissues of the high fat-diet-fed mice when reared with 60% coffee for 7 weeks. As for Alzheimer's disease, we analyzed the effect of coffee on amyloid β (Aβ) production in human neuronal SH-SY5Y cells. We found a 20% reduction in Aβ production when treated with 2.5% coffee for 2 d. This reduction was due to proteasomal degradation of BACE1 (β-secretase), which was activated by protein kinase A. In addition, coffee ameliorates LPS-induced inflammatory responses in RAW264.7 macrophages by reducing NFκB activity and Nrf2 activation. Roasted coffee prevents selenite-induced cataractogenesis by ameliorating antioxidant loss. Pyrocatechol, a component of roasted coffee, also reduced Aβ production and exhibits anti-inflammatory effects by a similar mechanism as coffee. Our results suggest that roasting coffee beans to generate pyrocatechol is necessary for the preventive effects of coffee intake on the chronic diseases.

著者

篠田 梨恵 篠田 康孝 森 卓之 吉村 知哲

出版者

公益社団法人 日本薬学会

雑誌

YAKUGAKU ZASSHI (ISSN:00316903)

巻号頁・発行日

vol.141, no.2, pp.281-288, 2021-02-01 (Released:2021-02-01)

参考文献数

24

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Tolvaptan (TLV) carries the risk of serious side effects, and its introduction requires hospitalization. Therefore, it is important from the viewpoints of safety and medical economics to predict in advance, the patients for whom it will be effective and introduce it. The purpose of this study was to investigate the noninvasive and simple predictors for identifying TLV responders. We conducted a retrospective observational study of patients with heart failure who had TLV introduced at our hospital from January 1, 2017, to December 31, 2018. By using the body weight and BNP reduction as the effect indices, predictors of body weight and BNP reduction were extracted by logistic analysis. The sensitivity and specificity at the cutoff value obtained by ROC analysis were also examined. Among 85 subjects, urine sodium concentration >63 mEq/L [odds ratio (OR): 6.11, 95% confidence interval (CI): 1.36-27.4] was detected as a predictor of body weight reduction. The sensitivity at this cutoff value was 81%, and the specificity was 70%. Serum osmolarity>291 mOsm/L (OR: 3.76, 95% CI: 1.00-14.2), urine potassium concentration<21 mEq/L (OR: 4.45, 95% CI: 1.09-18.2), and urine sodium concentration>71 mEq/L (OR: 7.38, 95% CI: 2.05-26.6) were detected as predictors of BNP reduction. The sensitivities were 62%, 53%, and 73%, and the specificities were 58%, 68%, and 68%, respectively. Therefore, it was suggested that urine sodium concentration may be useful as a predictor of body weight and BNP decrease after TLV induction.

著者

原田 亜紀子 杉原 数美 渡部 容子 山路 誠一 北村 繁幸 太田 茂

出版者

公益社団法人 日本薬学会

雑誌

YAKUGAKU ZASSHI (ISSN:00316903)

巻号頁・発行日

vol.135, no.10, pp.1185-1196, 2015 (Released:2015-10-01)

参考文献数

22

被引用文献数

8

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Aryl hydrocarbon receptor (AhR) ligand activity of the extracts of 62 herbal medicines was examined using yeast reporter assay. Fifty-eight herbal extracts exhibited AhR ligand activity. The highest activity was observed with Ogon (Scutellariae Radix), followed by Oren (Coptidis Rhizoma), Kujin (Sophorae Radix) and Shoma (Cimicifiigae Rhizoma). When these extracts were treated with hesperinase, a hydrolase for sugar conjugates, the aglycones showed higher activity than the parent extracts. Among the constituents of Ogon extract, baicalein and wogonin showed AhR ligand activity, while the sugar conjugate of baicalein, baicalin, was inactive. Among the flavonoid components of these herbal medicines, flavone and chrysin exhibited high ligand activity for AhR. Ethoxyresorufin O-dealkylase (EROD) activity due to CYP1A1 in HepG2 cells was enhanced by the addition of baicalein. Baicalein also decreased the 3-methylcholanthrene-induced increase of EROD activity, but this effect was not statistically significant. When wogonin or baicalein was orally administered at the dose of 100 mg/kg to mice, EROD activity in liver was only slightly changed. Furthermore, when Ogon extract was co-administered with 3-methylcholanthrene, the EROD and methoxyresorufin O-dealkylase activities were not significantly changed. These results indicate that many herbal extracts have AhR ligand activity, and their inducing effect on CYP1A1/2 can be evaluated in HepG2 cells.

著者

水田 栄之助

出版者

公益社団法人 日本薬学会

雑誌

YAKUGAKU ZASSHI (ISSN:00316903)

巻号頁・発行日

vol.135, no.6, pp.789-792, 2015-06-01 (Released:2015-06-01)

参考文献数

12

被引用文献数

1 3

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Individual taste sensitivity affects one's eating habits, and could thus play a role in the development of lifestyle-related diseases, such as obesity, hypertension and dyslipidemia. However, only a handful of studies have been conducted to investigate these associations. Therefore, we performed taste sensitivity tests on approximately 250 patients with lifestyle-related diseases who were undergoing outpatient treatment at the Department of Internal Medicine, or received a health check-up in order to examine the associations of individual taste sensitivity with their eating habits and lifestyle-related diseases. Our findings showed that sensitivity to sweet or salt taste was significantly lower in patients with cardiovascular diseases, and sensitivity to umami taste was significantly lower in obese patients. These findings suggest that taste sensitivity disorders may be linked not only to eating habits and lifestyle-related diseases, but also to the onset of cardiovascular diseases. Many of the drugs used in the treatment of lifestyle-related diseases and cardiovascular diseases, including antihypertensive agents, statins, fibrates, and allopurinol, are known to form zinc chelates and thereby possibly cause drug-induced taste disorders. Focusing on individual taste sensitivity to improve or maintain intake levels may become a new target for drug development in the areas of lifestyle-related and cardiovascular diseases.

著者

松村 美奈 中山 拓人 寒水 孝司

出版者

公益社団法人 日本薬学会

雑誌

YAKUGAKU ZASSHI (ISSN:00316903)

巻号頁・発行日

vol.136, no.11, pp.1563-1571, 2016-11-01 (Released:2016-11-01)

参考文献数

7

被引用文献数

4 1

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A survey of introductory statistics courses at Japanese medical schools was published as a report in 2014. To obtain a complete understanding of the way in which statistics is taught at the university level in Japan, it is important to extend this survey to related fields, including pharmacy, dentistry, and nursing. The current study investigates the introductory statistics courses offered by faculties of pharmaceutical sciences (six-year programs) at Japanese universities, comparing the features of these courses with those studied in the survey of medical schools. We collected relevant data from the online syllabi of statistics courses published on the websites of 71 universities. The survey items included basic course information (for example, the course names, the targeted student grades, the number of credits, and course classification), textbooks, handouts, the doctoral subject and employment status of each lecturer, and course contents. The period surveyed was July-September 2015. We found that these 71 universities offered a total of 128 statistics courses. There were 67 course names, the most common of which was “biostatistics (iryou toukeigaku).” About half of the courses were designed for first- or second-year students. Students earned fewer than two credits. There were 62 different types of textbooks. The lecturers held doctoral degrees in 18 different subjects, the most common being a doctorate in pharmacy or science. Some course content differed, reflecting the lecturers' academic specialties. The content of introductory statistics courses taught in pharmaceutical science programs also differed slightly from the equivalent content taught in medical schools.

著者

齋藤 充生

出版者

公益社団法人 日本薬学会

雑誌

YAKUGAKU ZASSHI (ISSN:00316903)

巻号頁・発行日

vol.136, no.2, pp.245-249, 2016-02-01 (Released:2016-02-01)

参考文献数

5

被引用文献数

7

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According to the “Japan Revitalization Strategy” established in June 2013, “the government will promote better contributions of local pharmacies and pharmacists in encouraging self-medication of citizens by making pharmacies the community-based hub for providing information, giving advice on the proper use of non-prescription drugs, etc. and offering consultation and information service concerning health”. In addition, the “Demanded Function and Ideal Form of Pharmacy,” published in January 2014, requested a change, from pharmacies that specialized in dispensing medicines to pharmacies that serve as whole healthcare stations, providing pharmaceutical care based on patients' medical history, including the intake of dietary supplements. The medication fee was revised in April 2014 to enhance family pharmacy services and the management of pharmaceutical care. At that time, blood testing at a registered pharmacy was officially allowed under strict regulation. Revision of the “Pharmacist Law” in June 2014 included a request to pharmacists to provide pharmaceutical advice in addition to information. For the mitigation of drug-induced tragedies, the “Pharmaceutical Affairs Law” was amended to the “Pharmaceutical and Medical Device Act (PMD Act)” in November 2014, and proper use of medicines was imposed on healthcare professionals and other stakeholders. Patients were also requested to learn and understand the safety and harmful effects of medicines, and were requested to use medicines appropriately. As mentioned above, the status of pharmacies and pharmacists has dramatically changed in the past 2 years, and such changes over time are required.

著者

村山 義温 篠崎 好三

出版者

公益社団法人 日本薬学会

雑誌

藥學雜誌 (ISSN:00316903)

巻号頁・発行日

vol.51, no.5, pp.379-384, 1931-05-26 (Released:2009-11-13)

被引用文献数

2

著者

辻 敏和 永田 健一郎 川尻 雄大 山田 孝明 入佐 俊弘 村上 裕子 金谷 朗子 江頭 伸昭 増田 智先

出版者

公益社団法人 日本薬学会

雑誌

YAKUGAKU ZASSHI (ISSN:00316903)

巻号頁・発行日

vol.136, no.11, pp.1573-1584, 2016 (Released:2016-11-01)

参考文献数

20

被引用文献数

3

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There are many reports regarding various medical institutions' attempts at the prevention of dispensing errors. However, the relationship between occurrence timing of dispensing errors and subsequent danger to patients has not been studied under the situation according to the classification of drugs by efficacy. Therefore, we analyzed the relationship between position and time regarding the occurrence of dispensing errors. Furthermore, we investigated the relationship between occurrence timing of them and danger to patients. In this study, dispensing errors and incidents in three categories (drug name errors, drug strength errors, drug count errors) were classified into two groups in terms of its drug efficacy (efficacy similarity (−) group, efficacy similarity (+) group), into three classes in terms of the occurrence timing of dispensing errors (initial phase errors, middle phase errors, final phase errors). Then, the rates of damage shifting from “dispensing errors” to “damage to patients” were compared as an index of danger between two groups and among three classes. Consequently, the rate of damage in “efficacy similarity (−) group” was significantly higher than that in “efficacy similarity (+) group”. Furthermore, the rate of damage is the highest in “initial phase errors”, the lowest in “final phase errors” among three classes. From the results of this study, it became clear that the earlier the timing of dispensing errors occurs, the more severe the damage to patients becomes.

著者

小野 秀樹

出版者

公益社団法人 日本薬学会

雑誌

YAKUGAKU ZASSHI (ISSN:00316903)

巻号頁・発行日

vol.139, no.5, pp.767-781, 2019-05-01 (Released:2019-05-01)

参考文献数

67

被引用文献数

2 2

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Although the anti-influenza virus drug oseltamivir ameliorates the fever of influenza, adverse events related to its hypothermic effect have been reported. We found that oseltamivir causes dose-dependent hypothermia in normal mice, and have been studying the pharmacological mechanisms responsible for 12 years. Oseltamivir blocks nicotinic cholinergic transmission at sympathetic ganglia and reduces sympathetic modulation of brown adipose tissue (BAT), a heat generator. Oseltamivir was found to target the ion channels of nicotinic acetylcholine receptors, as demonstrated by patch clamp experiments with cells expressing the human α3β4 nicotinic receptor. Metabolized oseltamivir carboxylate, which inhibits the influenza virus neuraminidase, did not elicit hypothermia and ion channel suppression. Body temperature was decreased by intracerebroventricular administration of oseltamivir. Because this hypothermic effect was inhibited by dopamine D2 receptor blockade, it was suggested that oseltamivir centrally stimulates the D2 receptor. In Japan, the package inserts for oseltamivir and amantadine indicate very similar adverse neuropsychiatric reactions for the two drugs (abnormal behavior, consciousness disturbance, convulsion, delirium, delusion, hallucination). A literature search revealed that in some previous studies, oseltamivir and amantadine were shown to block the ion channel systems and activate the dopaminergic nervous system via several mechanisms. Therefore the similarity of the adverse reactions elicited by oseltamivir and amantadine was considered attributable to their similar pharmacological effects.

著者

小林 正義 山元 正昭

出版者

公益社団法人 日本薬学会

雑誌

YAKUGAKU ZASSHI (ISSN:00316903)

巻号頁・発行日

vol.95, no.8, pp.959-965, 1975-08-25 (Released:2008-05-30)

参考文献数

9

被引用文献数

3 3

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Acceleration of gelation reaction of limulus lysate was observed by the addition of a concentration higher than 10-3M of alkaline earth metals, such as Mg2+, Ca2+, B2+, or Sr2+. The limulus lysate containing Mg2+ or Ca2+ in a concentration of 10-1M as an additive showed the highest sensitivity which was 500 times that of original lysate. The sensitivity of the limulus lysates with Sr2+ or Ba2+ as an additive was lower than that of the limulus lysates with Mg2+ or Ca2+ as an additive. Acceleration of gelation reaction was interrupted by the use of any of alkaline earth metals in 1M concentration, and especially by the addition of Ca2+ in 1M concentration, approximately complete inhibition of gelation reaction being observed. Addition of a chelating agent such as ethylenediaminetetraacetic acid (EDTA) or diethylenetriamine-N, N, N', N", N"-pentaacetic acid (DTPA) reduced the sensitivity of limulus lysates to one-tenth of the sensitivity of the original limulus lysate in 10-2M concentration of such a chelating agent. The lowering of pH resulting from chelating streng-thens the lowering of the sensitivity of the limulus lysates. Complete inhibition of the gelation reaction was observed with marked lowering of the pH by the addition of EDTA to the limulus lysate containing a higher concentration of Mg2+. Correlation between the sensitivity of the limulus lysates and concentration of Mg2+ or Ca2+ was not observed. Reexamination of the optimum pH for the gelation readion necessitated the correction of pH to 6.75-7.25 from the previously reported pH range of 6, 50-6.75.

著者

寺崎 展幸

出版者

公益社団法人 日本薬学会

雑誌

YAKUGAKU ZASSHI (ISSN:00316903)

巻号頁・発行日

vol.136, no.8, pp.1125-1128, 2016-08-01 (Released:2016-08-01)

参考文献数

4

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Hyogo Prefectural Amagasaki General Medical Center has formed a heart failure team. Here, I report on the role of the pharmacist in this heart failure team at this hospital. Patient education is one of the roles of the pharmacist. It is the pharmacist's responsibility to improve medication adherence among patients. For this purpose, the pharmacist uses a brochure created by the heart failure team. The brochure outlines drug information in an easy-to-understand manner. The roles of a pharmacist were addressed in a lecture presented to the heart failure team. These lectures helped improve the pharmaceutical knowledge of the team, allowing the team to prescribe medicines more safely and appropriately. Maintaining co-operation between hospital and community pharmacies is another important role of a hospital pharmacist. This allows patients to be properly educated by pharmacists even after discharge from the hospital.

著者

渡辺 俊明 田中 正彦 渡邉 和俊 高松 康雄 戸部 昭広

出版者

公益社団法人 日本薬学会

雑誌

YAKUGAKU ZASSHI (ISSN:00316903)

巻号頁・発行日

vol.124, no.3, pp.99-111, 2004-03-01 (Released:2004-02-25)

参考文献数

51

被引用文献数

84 86

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Increasing data suggest that oxygen free radical species play detrimental roles in ischemic diseases. A free radical scavenger capable of inhibiting oxidative injury is expected to become a new drug for the treatment of ischemic diseases such as cerebral ischemia. Edaravon (3-methyl-1-phenyl-2-pyrazolin-5-one), which has been developed as an neuroprotective agent for more than 15 years since its discovery, is approved for the treatment of acute cerebral infarction. In this paper, the pharmacologic characteristics and clinical effects of edaravone are reviewed. In early stage of investigation, edaravone was found to have promising activities as an antioxidative radical scavenger, quenching hydroxyl radical (•OH) and inhibiting both •OH-dependent and •OH-independent lipid peroxidation. Edaravone showed inhibitory effects on both water-soluble and lipid-soluble peroxyl radical-induced peroxidation systems, which are different from the inhibitory effects of vitamins C and E in each system, respectively. Oxidative injury to cultured endothelial cells caused by arachidonate (AA) peroxides is prevented in the existence of edaravone. To clarify the characteristics of this free radical scavenger, further investigation was carried out. Edaravone ameliorated exacerbation of cortical edema induced by a focal ischemia-reperfusion model in rats, suggesting inhibitory effects on oxidative injury to the blood-brain barrier (BBB). Additionally, edaravone also prevented rat cortical edema caused by intracortical AA infusion in which free radical production and subsequent oxidative injury to the BBB are involved. With advances in in vivo measurement technology of oxygen radicals, edaravone was shown to inhibit postischemic increases in •OH production and tissue injury in the penumbral or recirculated area in rat cerebral ischemia models. In clinical studies, edaravone improved the core neurologic deficits, activities of daily living, and functional outcome of stroke patients. Furthermore, a study using proton magnetic resonance spectroscopic techniques showed that edaravone preserved N-acetyl-aspartate in stroke patients, a promising neuronal marker in the brain. Further investigation is essential for a better understanding of free radical-mediated cerebral injury during ischemia followed by recirculation. We hope that edaravone represents a promising neuroprotectant for drug therapy in acute cerebral ischemia.

著者

近藤 あゆみ

出版者

公益社団法人 日本薬学会

雑誌

YAKUGAKU ZASSHI (ISSN:00316903)

巻号頁・発行日

vol.136, no.1, pp.89-94, 2016

被引用文献数

1

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The increasing number of law-evading drug users in Japan is becoming a serious social problem. Previous studies have shown that law-evading drug users are younger, more educated, and less antisocial than methamphetamine users. They also tend to have some type of psychiatric disorder before starting drug use; therefore one of the reasons that they start using drugs may be to alleviate certain psychiatric symptoms. Furthermore, if drug users are successful in avoiding arrest, they often lack the motivation to stop, which makes treatment difficult. Therapists are required to be non-confrontational, to keep pace with their patients, and to take their patients' other existing disorders into account. Recently, the Matrix Model has shown promise as a new treatment strategy for drug abusers in Japan. The Matrix Model, which was originally developed in response to the 1980s cocaine epidemic in the USA, is an intensive outpatient treatment approach for drug abuse and dependence. The Matrix Model integrates cognitive-behavioral therapy, contingency management, motivational interviewing, 12-step facilitation, family involvement, and so on, with a directive, non-confrontational approach, and this style of therapy seems to fit with law-evading drug users. A Matrix Model-based treatment program was first established in Japan in 2006. The aim of this report is to introduce and assess the benefits of the TAMA Mental Health and Welfare Center Relapse Prevention Program, a Matrix Model-based treatment program established at the Tama Mental Health and Welfare Center in 2007.<br>