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,可減輕骨骼肌的收缩。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 | |
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中国大陸 | 丹曲林 |
臺灣 | 單挫林 |
臨床資料 | |
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商品名 | Dantrium Dantrolen Dantamacrin |
AHFS/Drugs.com | Monograph |
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 | 肝 |
排泄途徑 | 膽管、腎 |
识别信息 | |
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CAS号 | 7261-97-4 |
PubChem CID | |
IUPHAR/BPS | |
DrugBank | |
ChemSpider | |
UNII | |
KEGG | |
ChEBI | |
ChEMBL | |
CompTox Dashboard (EPA) | |
ECHA InfoCard | 100.027.895 |
化学信息 | |
化学式 | C14H10N4O5 |
摩尔质量 | 314.26 g·mol−1 |
3D模型(JSmol) | |
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單挫林也用於抗精神藥物惡性症候群(neuroleptic 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(或稱「地樂酚」,一般為殺蟲劑、除草劑)、特乐酚等相關化合物[6]。
瓶裝
參考文獻
- ^ 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.
- ^ 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
- ^ 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.
- ^ 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.
- ^ 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.
- ^ 6.0 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).
- ^ 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.
- ^ 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.
- ^ Hamilton, Richart. Tarascon Pocket Pharmacopoeia 2015 Deluxe Lab-Coat Edition. Jones & Bartlett Learning. 2015: 2. ISBN 9781284057560.
- ^ 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).