單挫林

药物

單挫林INN:dantrolene)又称单挫林,是一種突觸後肌肉鬆弛劑,可減輕骨骼肌收缩。它与雷诺丁受体(ryanodine receptor)RyR1结合[1],抑制肌质网钙离子释放而减弱肌肉收缩[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恶性高热之主要藥物。早年恶性高热的死亡率高達70%,使用單挫林其死亡率已低於5%。

「單挫林」的各地常用名稱
中国大陸丹曲林
臺灣單挫林
單挫林
Structural formula of dantrolene
Space-filling model of the dantrolene molecule
臨床資料
商品名英语Drug nomenclatureDantrium
Dantrolen
Dantamacrin
AHFS/Drugs.comMonograph
给药途径口服靜脈注射
ATC碼
藥物動力學數據
生物利用度70%
药物代谢
排泄途徑膽管
识别信息
  • 1-{[5-(4-nitrophenyl)-2-furyl]methylideneamino}
    imidazolidine-2,4-dione
CAS号7261-97-4  checkY
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard英语CompTox Chemicals Dashboard (EPA)
ECHA InfoCard100.027.895 編輯維基數據鏈接
化学信息
化学式C14H10N4O5
摩尔质量314.26 g·mol−1
3D模型(JSmol英语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

單挫林也用於抗精神藥物惡性症候群英语neuroleptic malignant syndromeneuroleptic malignant syndrome,NMS)管理,或是肌肉痙攣(例如中風截癱腦性麻痺、疼痛伴隨多发性硬化症[5],或用於2,4-二硝基苯酚中毒時[6][7][8]。另外,如達諾殺英语Dinoseb(或稱「地樂酚」,一般為殺蟲劑、除草劑)、特乐酚等相關化合物[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. (原始内容存档于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]. (原始内容存档于2019-12-07). 

外部連結