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丹曲林

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维基百科,自由的百科全书
“丹曲林”的各地常用名称
中国大陆丹曲林
台湾单挫林
丹曲林
Structural formula of dantrolene
Space-filling model of the dantrolene molecule
临床资料
商品名英语Drug nomenclatureDantrium
Dantrolen
Dantamacrin
AHFS/Drugs.comMonograph
给药途径口服静脉注射
ATC码
药物动力学数据
生物利用度70%
药物代谢
排泄途径胆管
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 编辑维基数据链接
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

丹曲林INN:dantrolene)又称单挫林,是一种突触后肌肉松弛剂,可减轻骨骼肌收缩。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]。丹曲林是治疗和预防因全身麻醉而引发的罕见且致命的恶性高热之主要药物。早年恶性高热的死亡率高达70%,使用丹曲林其死亡率已低于5%。

丹曲林也用于抗精神药物恶性症候群英语neuroleptic malignant syndromeneuroleptic malignant syndrome,NMS)管理,或是肌肉痉挛(例如中风截瘫脑性麻痹、疼痛伴随多发性硬化症[5],或用于2,4-二硝基苯酚中毒时[6][7][8]。另外,如达诺杀英语Dinoseb(或称“地乐酚”,一般为杀虫剂、除草剂)、特乐酚等相关化合物[6]

截至2015年,美国典型药物治疗费用为100至200美元[9];在台湾,该药物一剂的成本为新台币5000元。[10]

瓶装

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参考文献

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  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, 刘育志. 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!. 商业周刊. 2015-04-27 [2017-11-04]. (原始内容存档于2019-12-07). 

外部链接

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