来氟米特

来氟米特
临床资料
商品名（英语：Drug nomenclature）	艾炎宁/Arava, 雅奴麻/Arheuma, 希关炎/Pharnomide
AHFS/Drugs.com	Monograph
MedlinePlus	a600032
核准状况	欧 EMA: yes; 美 DailyMed: Leflunomide;
怀孕分级	澳: X (高风险) ; ;
给药途径	口服给药
ATC码	L04AK01 (WHO) ;
法律规范状态
法律规范	澳：限医生处方（S4）; 加：处方药（℞-only）; 欧：Rx-only; 英：处方药（℞-only） (POM); 美：处方药（℞-only）;
药物动力学数据
生物利用度	80%
血浆蛋白结合率	>99%
药物代谢	胃肠道粘膜和肝脏
代谢产物	特立氟胺（英语：Teriflunomide）
生物半衰期	14–18天
排泄途径	粪便（48%）、尿液（43%）
识别信息
	IUPAC命名法 5-methyl-N-[4-(trifluoromethyl) phenyl]-isoxazole-4-carboxamide; ;
CAS号	75706-12-6
PubChem CID	3899;
IUPHAR/BPS	6825;
DrugBank	DB01097 ;
ChemSpider	3762 ;
UNII	G162GK9U4W;
KEGG	D00749 ;
ChEBI	CHEBI:6402 ;
ChEMBL	ChEMBL960 ;
CompTox Dashboard（英语：CompTox Chemicals Dashboard） (EPA)	DTXSID9023201 ;
ECHA InfoCard	100.123.883
化学信息
化学式	C12H9F3N2O2
摩尔质量	270.21 g·mol−1
3D模型（JSmol（英语：JSmol））	交互式图像;
	SMILES O=C(Nc1ccc(cc1)C(F)(F)F)c2c(onc2)C;
	InChI InChI=1S/C12H9F3N2O2/c1-7-10(6-16-19-7)11(18)17-9-4-2-8(3-5-9)12(13,14)15/h2-6H,1H3,(H,17,18) ; Key:VHOGYURTWQBHIL-UHFFFAOYSA-N ;

来氟米特（英语：Leflunomide）是用于治疗类风湿性关节炎、干癣性关节炎及预防器官移植后排斥的口服药物^[7] ^[8]。用药到药效发生一般会在 6 周内^[8]。

常见副作用包括腹泻、肝炎、脱发和皮疹^[7]。其他副作用包括可能感染、血小板减少、白血球减少和癌症^[7]。怀孕期间使用可能会造成胎儿异常^[7]。它是一种改善病情的抗风湿药物(DMARD) 和免疫抑制剂^[7] ^[8]。作用机转是阻断二氢乳清酸脱氢酶而减少淋巴细胞^[8]。

来氟米特分别在 1998 年及1999年，在美国及欧洲取得医疗使用许可^[7] ^[8]。目前已有数种学名药在医疗上使用^[9]。英国国民保健署在2021 年的治疗费用约为 5 英镑^[9]，在美国则大约是 100 美元^[10]。

参考文献

^ Arava Product Information (PDF). TGA eBusiness Services. sanofi-aventis australia pty ltd. 7 August 2012 [11 March 2014].
^ Arava 10mg Tablets - Summary of Product Characteristic. electronic Medicines Compendium. Sanofi. 21 February 2014 [11 March 2014].
^ Arava (leflunomide) tablet, film coated [sanofi-aventis U.S. LLC]. DailyMed. sanofi-aventis U.S. LLC. November 2012 [11 March 2014].
^ Arava EPAR. European Medicines Agency. 25 August 2023 [26 August 2023].
^ ^5.0 ^5.1 ^5.2 ^5.3 ^5.4 Arava (leflunomide) dosing, indications, interactions, adverse effects, and more. Medscape Reference. WebMD. [11 March 2014].
^ Anvisa. RDC Nº 784 - Listas de Substâncias Entorpecentes, Psicotrópicas, Precursoras e Outras sob Controle Especial [Collegiate Board Resolution No. 784 - Lists of Narcotic, Psychotropic, Precursor, and Other Substances under Special Control]. Diário Oficial da União（英语：Diário Oficial da União）. 31 March 2023 (4 April 2023) [16 August 2023]. （原始内容存档于3 August 2023）（巴西葡萄牙语）.
^ ^7.0 ^7.1 ^7.2 ^7.3 ^7.4 ^7.5 Leflunomide Monograph for Professionals. Drugs.com. [2021-11-21]. （原始内容存档于2021-04-04）（英语）.
^ ^8.0 ^8.1 ^8.2 ^8.3 ^8.4 Arava. [21 November 2021]. （原始内容存档于30 March 2021）.
^ ^9.0 ^9.1 BNF 81: March-September 2021. BMJ Group and the Pharmaceutical Press. 2021: 1146. ISBN 978-0857114105.
^ Leflunomide Prices, Coupons & Patient Assistance Programs. Drugs.com. [21 November 2021]. （原始内容存档于6 March 2021）（英语）.

延伸阅读

Shankaranarayana S, Barrett C, Kubler P. 來氟米特的安全性. Australian Prescriber. February 2013, 36 (1): 28–32. doi:10.18773/austprescr.2013.010 .

[TGA-1] Arava Product Information (PDF). TGA eBusiness Services. sanofi-aventis australia pty ltd. 7 August 2012 [11 March 2014].

[Arava_SmPC-2] Arava 10mg Tablets - Summary of Product Characteristic. electronic Medicines Compendium. Sanofi. 21 February 2014 [11 March 2014].

[Arava_FDA_label-3] Arava (leflunomide) tablet, film coated [sanofi-aventis U.S. LLC]. DailyMed. sanofi-aventis U.S. LLC. November 2012 [11 March 2014].

[Arava_EPAR-4] Arava EPAR. European Medicines Agency. 25 August 2023 [26 August 2023].

[MSR-5] 5.0 ^5.1 ^5.2 ^5.3 ^5.4 Arava (leflunomide) dosing, indications, interactions, adverse effects, and more. Medscape Reference. WebMD. [11 March 2014].

[6] Anvisa. RDC Nº 784 - Listas de Substâncias Entorpecentes, Psicotrópicas, Precursoras e Outras sob Controle Especial [Collegiate Board Resolution No. 784 - Lists of Narcotic, Psychotropic, Precursor, and Other Substances under Special Control]. Diário Oficial da União（英语：Diário Oficial da União）. 31 March 2023 (4 April 2023) [16 August 2023]. （原始内容存档于3 August 2023）（巴西葡萄牙语）.

[AHFS2021-7] 7.0 ^7.1 ^7.2 ^7.3 ^7.4 ^7.5 Leflunomide Monograph for Professionals. Drugs.com. [2021-11-21]. （原始内容存档于2021-04-04）（英语）.

[EPAR2021-8] 8.0 ^8.1 ^8.2 ^8.3 ^8.4 Arava. [21 November 2021]. （原始内容存档于30 March 2021）.

[BNF81-9] 9.0 ^9.1 BNF 81: March-September 2021. BMJ Group and the Pharmaceutical Press. 2021: 1146. ISBN 978-0857114105.

[10] Leflunomide Prices, Coupons & Patient Assistance Programs. Drugs.com. [21 November 2021]. （原始内容存档于6 March 2021）（英语）.

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