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單挫林

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維基百科,自由的百科全書
「單挫林」的各地常用名稱
中國大陸丹曲林
臺灣單挫林
單挫林
Structural formula of dantrolene
Space-filling model of the dantrolene molecule
臨床資料
商品名英語Drug nomenclatureDantrium
Dantrolen
Dantamacrin
AHFS/Drugs.comMonograph
給藥途徑口服靜脈注射
ATC碼
藥物動力學數據
生物利用度70%
藥物代謝
排泄途徑膽管
識別資訊
  • 1-{[5-(4-nitrophenyl)-2-furyl]methylideneamino}
    imidazolidine-2,4-dione
CAS號7261-97-4  checkY
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard英語CompTox Chemicals Dashboard (EPA)
ECHA InfoCard100.027.895 編輯維基數據鏈接
化學資訊
化學式C14H10N4O5
摩爾質量314.26 g·mol−1
3D模型(JSmol英語JSmol
  • [O-][N+](=O)c3ccc(c2oc(C=NN1C(=O)NC(=O)C1)cc2)cc3
  • InChI=1S/C14H10N4O5/c19-13-8-17(14(20)16-13)15-7-11-5-6-12(23-11)9-1-3-10(4-2-9)18(21)22/h1-7H,8H2,(H,16,19,20) checkY
  • Key:OZOMQRBLCMDCEG-UHFFFAOYSA-N checkY

單挫林INN:dantrolene)又稱丹曲林,是一種突觸後肌肉鬆弛劑,可減輕骨骼肌收縮。它與雷諾丁受體(ryanodine receptor)RyR1結合[1],抑制肌質網鈣離子釋放而減弱肌肉收縮[2][3][4]。單挫林是治療和預防因全身麻醉而引發的罕見且致命的惡性高熱之主要藥物。早年惡性高熱的死亡率高達70%,使用單挫林其死亡率已低於5%。

單挫林也用於抗精神藥物惡性症候群英語neuroleptic malignant syndromeneuroleptic malignant syndrome,NMS)管理,或是肌肉痙攣(例如中風截癱腦性麻痺、疼痛伴隨多發性硬化症[5],或用於2,4-二硝基苯酚中毒時[6][7][8]。另外,如達諾殺英語Dinoseb(或稱「地樂酚」,一般為殺蟲劑、除草劑)、特樂酚等相關化合物[6]

截至2015年,美國典型藥物治療費用為100至200美元[9];在台灣,該藥物一劑的成本為新台幣5000元。[10]

瓶裝

參考文獻

  1. ^ Lanner JT, Georgiou DK, Joshi AD, et al. Ryanodine receptors: structure, expression, molecular details, and function in calcium release. Cold Spring Harb Perspect Biol. 2010 Nov;2(11):a003996. doi: 10.1101/cshperspect.a003996. Epub 2010 Oct 20. PMID 20961976; PMCID: PMC2964179.
  2. ^ Paul-Pletzer K, Yamamoto T, Bhat MB, Ma J, Ikemoto N, Jimenez LS, Morimoto H, Williams PG, Parness J 2002. Identification of a Dantrolene-binding Sequence on the Skeletal Muscle Ryanodine Receptor. J Biol Chem 277: 34918–34923
  3. ^ Kobylarz D, Noga M, Frydrych A, et al. Antidotes in Clinical Toxicology-Critical Review. Toxics. 2023 Aug 23;11(9):723. doi: 10.3390/toxics11090723. PMID 37755734; PMCID: PMC10534475.
  4. ^ Zucchi, R; Ronca-Testoni, S. The sarcoplasmic reticulum Ca2+ channel/ryanodine receptor: modulation by endogenous effectors, drugs and disease states.. Pharmacological reviews. March 1997, 49 (1): 1–51. PMID 9085308. 
  5. ^ Pinder, RM; Brogden, RN; Speight, TM; Avery, GS. Dantrolene sodium: a review of its pharmacological properties and therapeutic efficacy in spasticity.. Drugs. January 1977, 13 (1): 3–23. PMID 318989. doi:10.2165/00003495-197713010-00002. 
  6. ^ 6.0 6.1 Krause T, Gerbershagen MU, Fiege M, Weisshorn R, Wappler F. Dantrolene – a review of its pharmacology, therapeutic use and new developments. Anaesthesia. 2004, 59 (4): 364–73 [2017-09-23]. PMID 15023108. doi:10.1111/j.1365-2044.2004.03658.x. (原始內容存檔於2018-12-20). 
  7. ^ Kumar S, Barker K, Seger D. Dinitrophenol-Induced Hyperthermia Resolving With Dantrolene Administration. Abstracts of the North American Congress of Clinical Toxicology. Clin Toxicol. 2002, 40: 599–673. doi:10.1081/clt-120016859. 
  8. ^ Barker K, Seger D, Kumar S. Comment on "Pediatric fatality following ingestion of Dinitrophenol: postmortem identification of a 'dietary supplement'". Clin Toxicol (Phila). 2006, 44 (3): 351. PMID 16749560. doi:10.1080/15563650600584709. 
  9. ^ Hamilton, Richart. Tarascon Pocket Pharmacopoeia 2015 Deluxe Lab-Coat Edition. Jones & Bartlett Learning. 2015: 2. ISBN 9781284057560. 
  10. ^ 白映俞, 劉育志. 麻醉醫師的噩夢─惡性高熱》一個醫師看《麻醉風暴》有感:別為了省錢不顧人命!. 商業週刊. 2015-04-27 [2017-11-04]. (原始內容存檔於2019-12-07). 

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