トシル酸スプラタスト、スプラタストトシル酸塩

関: suplatast

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2017/07/17 16:06:51」(JST)

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Suplatast tosilate (INN) is a Th2 cytokine inhibitor^[1] which is used as an antiallergic drug. Often used in the treatment of Kimura's disease.^[2]^[3]

References

^ Tamaoki J, Kondo M, Sakai N, et al. (July 2000). "Effect of suplatast tosilate, a Th2 cytokine inhibitor, on steroid-dependent asthma: a double-blind randomised study. Tokyo Joshi-Idai Asthma Research Group". Lancet. 356 (9226): 273–8. PMID 11071181. doi:10.1016/S0140-6736(00)02501-0.
^ Ueda T, Arai S, Amoh Y, Katsuoka K (2011). "Kimura's disease treated with suplatast tosilate and loratadine". European Journal of Dermatology. 21 (6): 1020–1. PMID 21914581. doi:10.1684/ejd.2011.1539.
^ Tsukagoshi H, Nagashima M, Horie T, et al. (December 1998). "Kimura's disease associated with bronchial asthma presenting eosinophilia and hyperimmunoglobulinemia E which were attenuated by suplatast tosilate (IPD-1151T)". Internal Medicine. 37 (12): 1064–7. PMID 9932643. doi:10.2169/internalmedicine.37.1064.

UpToDate Contents

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1. 好酸球性胃腸炎 eosinophilic gastroenteritis

English Journal

The effects of suplatast tosilate on acutely dissociated sensory and paratracheal ganglia neurons.

Zhou JR1, Shirasaki T2, Soeda F2, Takahama K3.
American journal of physiology. Lung cellular and molecular physiology.Am J Physiol Lung Cell Mol Physiol.2016 Aug 26:ajplung.00451.2016. doi: 10.1152/ajplung.00451.2015. [Epub ahead of print]
In this study, we investigated the effects of suplatast on acutely dissociated single neurons of sensory and paratracheal ganglia using a patch-clamp technique. Suplatast had little effect on various responses caused by capsaicin, acid, bradykinin, serotonin and adenosine 5'-triphosphate in rat sens
PMID 27566004

Suplatast tosilate alleviates nasal symptoms through the suppression of nuclear factor of activated T-cells-mediated IL-9 gene expression in toluene-2,4-diisocyanate-sensitized rats.

Mizuguchi H1, Orimoto N2, Kadota T3, Kominami T3, Das AK3, Sawada A3, Tamada M3, Miyagi K3, Adachi T3, Matsumoto M3, Kosaka T3, Kitamura Y4, Takeda N4, Fukui H5.
Journal of pharmacological sciences.J Pharmacol Sci.2016 Mar;130(3):151-8. doi: 10.1016/j.jphs.2015.12.008. Epub 2016 Jan 6.
Histamine H1 receptor (H1R) gene is upregulated in patients with pollinosis; its expression level is highly correlated with the nasal symptom severity. Antihistamines are widely used as allergy treatments because they inhibit histamine signaling by blocking H1R or suppressing H1R signaling as invers
PMID 26874672

Vitiligo-like depigmentation with perifollicular pigment retention in systemic sclerosis treated successfully with suplatast tosilate.

Fujimoto N1, Hamaguchi Y2, Tanaka T1.
European journal of dermatology : EJD.Eur J Dermatol.2016 Jan-Feb;26(1):110-2. doi: 10.1684/ejd.2015.2687.
PMID 26841835

Japanese Journal

発熱・肝腫大を呈した小児特発性好酸球増多症候群

森永信吾,高木一孝,定明子 [他],松井利充
臨床血液 53(1), 83-86, 2012-01-30
NAID 10030830013

薬剤中止後トシル酸スプラタスト併用で改善したカルボシステインによる薬剤性肺障害の1例

緒方賢一,諸岡三之
気管支学 : 日本気管支研究会雑誌 34(1), 54-57, 2012-01-25
背景.薬剤性肺障害は種々の薬剤によって発生する.今回我々は,薬剤中止後ステロイドを使用せずトシル酸スプラタスト併用で改善したカルボシステインによる薬剤性肺障害を経験した.症例.30歳の男性.インフルエンザAに罹患してオセルタミビルとカルボシステインを投与されたが,服薬5日後も発熱と咳嗽が持続したため近医に入院.その後胸部X線写真の浸潤影が悪化して,当院転院になった.カルボシステインを中止し,トシル …
NAID 110009327982

ヘパリン-リドカイン混合液膀胱内注入療法が有効であった間質性膀胱炎の1例

松尾朋博,志田洋平,林田靖 [他],酒井英樹
泌尿器科紀要 57(9), 513-516, 2011-09-00
… She underwent intravesical treatment with combined heparin and alkalinized lidocaine for IC, since prior medical treatments (imipramine, solifenacin, suplatast tosilate, and kampo extracts) and hydrodistention of bladder had little or no effect on her symptoms. …
NAID 40018993725

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「スプラタスト」

Suplatast tosilate
Clinical data
AHFS/Drugs.com	International Drug Names
Routes of; administration	Oral
ATC code	none;
Legal status
Legal status	In general: ℞ (Prescription only);
Identifiers
	IUPAC name (3-{[4-(3-ethoxy-2-hydroxypropoxy)phenyl]amino}-3-oxopropyl)(dimethyl)sulfonium 4-methylbenzenesulfonate;
CAS Number	94055-76-2 ;
PubChem CID	71773;
ChemSpider	64811 ;
UNII	C9J89787U1;
KEGG	D01423 ;
ChEMBL	CHEMBL115435 ;
ECHA InfoCard	100.220.132
Chemical and physical data
Formula	C23H33NO7S2
Molar mass	499.64 g/mol
3D model (JSmol)	Interactive image;
	SMILES CCOCC(COC1=CC=C(C=C1)NC(=O)CC[S+](C)C)O.CC1=CC=C(C=C1)S(=O)(=O)[O-] ;
	InChI InChI=1S/C16H25NO4S.C7H8O3S/c1-4-20-11-14(18)12-21-15-7-5-13(6-8-15)17-16(19)9-10-22(2)3;1-6-2-4-7(5-3-6)11(8,9)10/h5-8,14,18H,4,9-12H2,1-3H3;2-5H,1H3,(H,8,9,10) ; Key:RYVJQEZJUFRANT-UHFFFAOYSA-N ;
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　　[★]

英: suplatast
化: トシル酸スプラタスト suplatast tosilate スプラタストトシル酸塩
商: アイピーディ、トシラート

抗アレルギー薬

T細胞のIL-4,IL-5産生抑制

ヒスタミン受容体拮抗作用無し→予防薬

作用機序

Th2細胞に作用しIL-4,IL-5分泌を抑制
IL-4, IL-5いずれもT細胞や肥満細胞から分泌される

IL-4は、B細胞活性化、IgEスイッチ

IL-5は、好酸球成長・分化

Th2細胞によるこれらのインターロイキン酸性を抑制することでIgE抗体産生抑制と好酸球の活性化が抑制される。

薬理作用

IgE抗体産生抑制
好酸球浸潤抑制
化学伝達物質遊離抑制

[pmid11071181-1] Tamaoki J, Kondo M, Sakai N, et al. (July 2000). "Effect of suplatast tosilate, a Th2 cytokine inhibitor, on steroid-dependent asthma: a double-blind randomised study. Tokyo Joshi-Idai Asthma Research Group". Lancet. 356 (9226): 273–8. PMID 11071181. doi:10.1016/S0140-6736(00)02501-0.

[2] Ueda T, Arai S, Amoh Y, Katsuoka K (2011). "Kimura's disease treated with suplatast tosilate and loratadine". European Journal of Dermatology. 21 (6): 1020–1. PMID 21914581. doi:10.1684/ejd.2011.1539.

[3] Tsukagoshi H, Nagashima M, Horie T, et al. (December 1998). "Kimura's disease associated with bronchial asthma presenting eosinophilia and hyperimmunoglobulinemia E which were attenuated by suplatast tosilate (IPD-1151T)". Internal Medicine. 37 (12): 1064–7. PMID 9932643. doi:10.2169/internalmedicine.37.1064.

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案内

suplatast tosilate