著者
荒田 洋治
出版者
公益社団法人 日本薬学会
雑誌
ファルマシア (ISSN:00148601)
巻号頁・発行日
vol.51, no.6, pp.575_1, 2015 (Released:2018-08-26)

ハンフリー・デービー(1778~1829)は,ホウ素,ナトリウム,マグネシウム,カリウム,カルシウム,バリウムを発見したことでその名を知られるイギリスの化学者である.6種類もの新元素を発見したのは,化学の歴史の中で,デービーただ1人である.
著者
西山 成
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.132, no.4, pp.455-459, 2012-04-01 (Released:2012-04-01)
参考文献数
29
被引用文献数
3 3

In recent years, the focus of interest on the role of the renin-angiotensin system (RAS) in the pathophysiology of hypertension and organ injury has changed to a major emphasis on the role of the local RAS in specific tissues. In the kidney, all of the RAS components are present and intrarenal angiotensin II (Ang II) is formed by independent multiple mechanisms. Ang II is compartmentalized in the renal interstitial fluid and the proximal tubular compartments with much higher concentrations than those existing in the circulation. It has also been revealed that inappropriate activation of the intrarenal RAS is an important contributor to the pathogenesis of chronic kidney disease (CKD). Indeed, most national guideline groups now recommend the use of RAS inhibitors in preference to other antihypertensive agents for hypertensive patients with CKD. In this review, we will briefly summarize our current understanding of independent regulation of the intrarenal RAS. We will also discuss the impact of RAS inhibitors in preventing the progressive increases in the intrarenal RAS during the development of CKD.
著者
坂上 隆彦
出版者
公益社団法人 日本薬学会
雑誌
ファルマシア (ISSN:00148601)
巻号頁・発行日
vol.52, no.5, pp.428-429, 2016 (Released:2016-05-01)

樋屋奇応丸は主にジャコウ、ユウタン、ジンコウ、ニンジンを含む小児五疳薬であり、「夜なき、かんむし」の薬として広く知られている。最小で直径約1.3mm、金箔・銀箔コーティングが特徴の丸剤は、1622年に初代樋屋坂上忠兵衛が創業して以来約400年にわたり製造・販売が続いている。江戸時代には大人の薬として庶民に普及していたが、現在は乳幼児にも服用できる薬として親しまれている。
著者
三輪 芳弘 山路 昭 中浜 肇 折田 義正 福原 吉典 鎌田 武信 石橋 道男 市川 靖二 高原 史郎 園田 孝夫
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.108, no.11, pp.1087-1092, 1988-11-25 (Released:2008-05-30)
参考文献数
15
被引用文献数
1 1

A method of high performance liquid chromatography for the determination of unchanged furosemide and its metabolites in the plasma and urine of human subjects is reported. A reversed phase Hibar Lichrosorb RP-8 column was applied to the present method. Furosemide from samples was extracted with diethylether. Beta-glucronidate of furosemide was determined after the addition of beta-glucronidase. 4-Chloro-5-sulfamoyl-anthranilic acid (CSA) was determined by the supernatant obtained from ten minutes centrifugation of the urine with ethanol. In the plasma and urine concentrations of unchanged furosemide of healthy volunteers, there were recognized differences among individuals. In patients with chronic renal failure, urine concentration of beta-glucronidate of furosemide increased in response to impairment of creatinine clearance. CSA could be detected only in the urine of patients receiving renal transplantation under a large dose administration of furosemide (above 200mg/d during rejection). And CSA does not seem to be an artifact product by the procedures of extraction. No interference could be observed by the drugs co-administered with furosemide. The present method can be utilized for a routine drug monitoring system of furosemide. Mechanism of formation of metabolites of furosemide should be further studied.
著者
大谷 直子
出版者
公益社団法人 日本薬学会
雑誌
ファルマシア (ISSN:00148601)
巻号頁・発行日
vol.53, no.11, pp.1101_1, 2017 (Released:2017-11-01)

細胞老化した細胞からは,様々な分泌タンパク質(炎症性サイトカイン,ケモカイン,細胞外マトリクス分解酵素などのプロテアーゼ類,増殖因子など)が産生されることが明らかになり,その現象は「細胞老化随伴分泌現象(senescence-associated secretory phenotype, SASP)」と呼ばれる.SASP因子はパラクライン的に自己以外の細胞に作用し,周囲の細胞の細胞老化を誘導したり,場合によっては増殖させたり,また免疫細胞を遊走させ,老化細胞のクリアランスに働くことが知られている.オートクライン的に働き,自己の細胞老化をより強化することも示されている.重要な生理作用として,組織の損傷治癒の際に一時的にSASPが誘導されることが示された.
著者
川口 高徳
出版者
公益社団法人 日本薬学会
雑誌
ファルマシア (ISSN:00148601)
巻号頁・発行日
vol.52, no.4, pp.346, 2016 (Released:2016-04-01)
参考文献数
4

糖尿病患者では,合併症として胃腸の蠕動運動障害に伴う胃不全麻痺,下痢および便秘などの消化器症状が多く見られる.糖尿病性の下痢は約22%の患者に見られ,時に重篤かつ難治性であるため臨床的に注目度が高い.従来,糖尿病性下痢の治療には,ロペラミドやタンニン酸アルブミンなどの止痢剤が用いられてきたが奏効しないことも多く,新たな治療法の開発が望まれている.この原因として,糖尿病モデルラットを用いた解析では,回腸および結腸の腸管粘膜からの水分や電解質の吸収が低下していることが報告されているが,糖尿病性下痢と特定のイオントランスポーターやチャネルとの間の因果関係についてはいまだ明らかとなっていない.これまでに,solute carrier(SLC)トランスポーターに属するNa+/H+交換輸送体NHE3などのイオントランスポーターが消化管での電解質バランスの維持に関わっており,NHE3欠損マウスでは重篤な下痢が生じることが報告されている.近年,このようなトランスポーターが足場タンパク質の1つであるNHE regulatory factor(NHERF),IP3受容体結合タンパク質 IRBIT,アクチン結合タンパク質ezrinと分子複合体を形成することが,頂端膜上でのトランスポーターの発現制御や基質輸送において重要であることが明らかとなりつつある.本稿では,膵臓β細胞を選択的に破壊したストレプトゾトシン誘発性の1型糖尿病モデルマウスを用い,腸管上皮細胞の刷子縁膜におけるNHE3とその結合タンパク質の発現の低下,複合体形成の減少が糖尿病性下痢を引き起こすことを明らかにしたHeらの論文について紹介する.なお,本稿は下記の文献に基づいて,その研究成果を紹介するものである.1) Chang E. B. et al., J. Clin. Invest., 75, 1666-1670 (1985).2) Schultheis P. J. et al., Nat. Genet., 19, 282-285 (1998).3) Donowitz M. et al., J. Exp. Biol., 212, 1638-1646 (2009).4) He P. et al., J. Clin. Invest., 125, 3519-3531 (2015).
著者
北川 勲 石津 隆 大橋 一慶 澁谷 博孝
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.120, no.10, pp.1017-1023, 2000-10-01 (Released:2008-05-30)
参考文献数
20
被引用文献数
6 9

Monthly changes of the content-ratio between S-(-)-and R-(+)-hyoscyamine as well as those between S-(-)-and R-(+)-scopolamine in the leaves of Datura metel L. cultivated in the field, were quantitatively analyzed by the use of HPLC with a chiral adsorbent. It was found that S-(-)-isomer was predominant for hyoscyamine and the ratio of R-(+)-isomer gradually increased during the growth, whereas in the case of scopolamine, S-(-)-isomer was the sole one found throughout the cultivation period. The 1H-NMR study in the CD3OD solution has suggested that S-(-)-hyoscyamine (1) and S-(-)-scopolamine (2) take a "face-to-face"conformation between their tropane skeletons and the benzene rings of the tropic acid moieties. In the presence of an equimolar NaOD in the CD3OD solution, the racemization at C-2' of 1 and 2 proceeded more rapidly than the hydrolysis at the tropic acid ester bond, presumably due to the steric hindrance caused by their"face-to-face"conformations. In the D2O and H2O solutions, on the other hand, the racemization and the hydrolysis of 1 proceeded smoothly, while those of 2 did not occur. It has been supposed that these individual reaction manners are ascribable in considerable extent to the different basicity of N atom in each tropane skeleton of 1 and 2 and to stronger intramolecular hydrogen bond occurring between the carbonyl oxygen at C-1' and the hydroxyl group at C-3' in the tropic acid moiety of 1.
著者
佐々木 順一 北澤 京子 中山 健夫
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.138, no.5, pp.631-635, 2018-05-01 (Released:2018-05-01)
参考文献数
18
被引用文献数
1 3

This research aimed to clarify the present status and challenges of evidence-based medicine (EBM) education in schools of pharmacy. We sent a questionnaire to 268 faculty members in August 2015, and a total of 192 were completed. The educational contents by respondents differed considerably. Only about 30% of respondents self-assessed the current EBM courses they taught as “fulfilling”. Challenges such as “time deficits”, “lack of exercise lessons and practical training”, “limited awareness and skills of teachers”, “lack of appropriate educational tools”, and “insufficient academic ability of students” were mentioned.
著者
加藤 洋美 吉井 美智子 小澤 光一郎
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.12, pp.2035-2044, 2007-12-01 (Released:2007-12-01)
参考文献数
12
被引用文献数
13 9

In the present study, we tested three kinds of sleeping drugs, consisting mainly of triazolam, brotizolam, and flunitrazepam, to compare the drug efficacy of generic drugs with that of original drugs. After these drugs were administered orally to mice, drug efficacy was evaluated in terms of ambulation, onset time of sleep, and duration of sleep in the open field test. For all kinds of sleep-inducing drugs, the drug efficacy of most generic drugs is not necessarily equal to that of the original drug. The main reason for the difference appears to be due to differences in the rate of absorption of the main drug. Any other differences between an original drug and a generic drug are caused by drug additives, the crystal form of the main drug, the formulation, and so on. In this study, the formulation was not the reason for the differences because all of the drugs were pulverized in a mortar and had no special coating. The drug additives for all the drugs are listed and the drug efficacy compared. Unfortunately, the information was not sufficient to shed any light on the differences in drug efficacy. For effective drug therapy, more information on drug additives should be provided.
著者
古山 渓行
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.138, no.6, pp.731-742, 2018-06-01 (Released:2018-06-01)
参考文献数
44
被引用文献数
2

The combination of several aromatic rings and/or heterocycles can induce novel functions. This phenomenon is observed in porphyrin derivatives, commonly found in hemoglobin, in the active sites of P-450, etc. The ability of these structures to interact strongly with visible light accounts for today's increased interest in the development of rationally designed porphyrinoid-based optical materials. In the pharmaceutical sciences, designing near-IR materials can be a challenge due to the high transparency of near-IR light in biological samples. Phthalocyanines (Pcs) are robust organic dyes that are absorbed in visible light. A theoretical investigation of molecular orbitals of Pcs has revealed that the introduction of a phosphorus(V) atom into a macrocyclic core leads to a narrower highest occupied molecular orbital-lowest unoccupied molecular orbital (HOMO-LUMO) gap. Following these studies, we found that certain types of Pc phosphorus(V) complexes display main absorptions beyond 1000 nm. Additionally, phosphorus(V) complexes with other azaporphyrinoids have been designed and synthesized via a relatively simple procedure. These complexes showed novel optical properties which are potentially useful in the pharmaceutical and material sciences. Furthermore, we have overcome the problem of organic radicals and antiaromatic compounds, which are generally considered to be unstable, by using a combination of serendipitous synthetic methodologies and spectroscopic techniques. These novel azaporphyrin compounds are robust and free from transition metals. They are relatively easy to synthesize and also exhibit predictable properties.
著者
大神田 淳子
出版者
公益社団法人 日本薬学会
雑誌
ファルマシア (ISSN:00148601)
巻号頁・発行日
vol.50, no.11, pp.1101-1106, 2014 (Released:2016-09-30)
参考文献数
25

タンパク質間相互作用(protein-protein interactions:PPIs)を対象とした創薬が広く注目されている.従来,作用面が広く浅いPPIsに対する低分子創薬は著しく困難な問題と考えられてきた.しかし近年,PPIsの分子機構に関する理解が進み,阻害剤設計の手掛かりが見えてきた.また,PPI阻害剤の分子サイズにパラダイムシフトが起こり,PPIsは以前にも増してdruggableな標的として認識されつつある.同時に,PPIsを安定化する有機分子にも,新しい切り口の医薬品や化学生物学研究の分子ツールへの応用が期待されている.本稿では,こうした背景のもと発展したPPI創薬の動向について触れると共に,我々のPPI標的型合成分子の設計に関する研究を紹介したい.
著者
砂川 智子 藤田 次郎 中村 克徳
出版者
公益社団法人 日本薬学会
雑誌
ファルマシア (ISSN:00148601)
巻号頁・発行日
vol.55, no.12, pp.1116-1119, 2019

2018年3月、インフルエンザ新薬「ゾフルーザ<sup>&reg;</sup>」が発売された。最先端の薬を早く提供する目的で厚生労働省が設けた「先駆け審査指定制度」が適用され、申請から5か月での発売となった。ゾフルーザ<sup>&reg;</sup>の導入により、抗インフルエンザ薬の販売シェアが大きく変化し、また耐性ウイルスの出現が話題となった。新薬も加え、現在、我が国で使用可能な抗インフルエンザ薬の薬理学的特性について、症例の背景因子を考慮しつつ概説した。
著者
井出 直仁 佐藤 誠太郎 澤口 和代
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.12, pp.1609-1614, 2019-12-01 (Released:2019-12-01)
参考文献数
24
被引用文献数
9

It has been reported that the risk of acute kidney injury (AKI) is higher during treatment with vancomycin and piperacillin/tazobactam compared to use of vancomycin and cefepim or meropenem. We investigated the risk of AKI in patients receiving vancomycin and piperacillin/tazobactam versus those receiving vancomycin and meropenem or doripenem. The subjects were patients over 18 years old who received either vancomycin and piperacillin/tazobactam (V+P/T therapy) or vancomycin and carbapenems (meropenem or doripenem) (V+C therapy) for at least 48 h between 1 May 2013 and 28 February 2019. The primary endpoint was the incidence of AKI in patients receiving V+P/T or V+C therapy, while the secondary outcome was the timing of AKI in each group. The incidence of AKI was 33.3% (9/27) in patients receiving V+P/T therapy versus 9.1% (5/55) in those receiving V+C therapy, and its incidence was significantly higher with the former regimen (χ2=5.90, p=0.015). Multiple logistic regression analysis confirmed that V+P/T therapy was associated with an increased risk of AKI compared to V+C therapy (adjusted odds ratio: 5.05, 95% confidence interval: 1.46-17.5, p=0.01). The time to onset of AKI after initiation of treatment was not significantly different between patients receiving V+T/P or V+C therapy [median (interquartile range): 4 d (2-6 d) versus 7 d (3-10 d); p=0.282]. V+P/T therapy was associated with a significantly higher incidence of AKI than alternative regimens, suggesting that it should be avoided. When broad spectrum antibacterial therapy is required, V+C therapy should be considered instead.
著者
山梨 義英
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.12, pp.1485-1494, 2019-12-01 (Released:2019-12-01)
参考文献数
38
被引用文献数
2

Several fat-soluble compounds such as cholesterol and fat-soluble vitamins have important physiological activities in the body, and their excess and/or deficiency have been reported to be closely associated with the onset and progression of several conditions such as lifestyle-related diseases. It is important to clarify not only the physiological activities but also in vivo kinetics of fat-soluble compounds to understand their in vivo activity (toxicity). This review introduces our recent (reverse) translational research in a combination of basic and clinical studies to reveal the regulatory mechanisms of in vivo behaviors of fat-soluble compounds and effects of their disruption in humans.
著者
高木 修造 山木 正枝 増田 京子 西浜 幸江 先名 淳
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.101, no.7, pp.657-659, 1981-07-25 (Released:2008-05-30)
参考文献数
8
被引用文献数
8 11

From Hedyotis corymbosa LAM., which has been recently used in chinese medicine as a useful drug against some tumors, were isolated six iridoids, asperuloside, scandoside methyl ester, asperulosidic acid, geniposidic acid, scandoside and deacetylasperulosidic acid.