雷洛昔芬

雷洛昔芬
临床资料
商品名（英语：Drug nomenclature）	Evista, Optruma, others
其他名称	Keoxifene; Pharoxifene; LY-139481; LY-156758; CCRIS-7129
AHFS/Drugs.com	Monograph
MedlinePlus	a698007
核准状况	欧 EMA: yes; 美 DailyMed: Raloxifene;
怀孕分级	澳: X (高风险) ; ;
给药途径	By mouth
药物类别（英语：Drug class）	Selective estrogen receptor modulator
ATC码	G03XC01 (WHO) ;
法律规范状态
法律规范	欧：Rx-only; 美：处方药（℞-only）; 处方药（℞-only）;
药物动力学数据
生物利用度	2%
血浆蛋白结合率	>95%
药物代谢	Liver, intestines (glucuro-; nidation); CYP450 system not involved
生物半衰期	Single-dose: 28 hours; Multi-dose: 33 hours
排泄途径	Feces
识别信息
	IUPAC命名法 [6-hydroxy-2-(4-hydroxyphenyl)-benzothiophen-3-yl]-[4-[2-(1-piperidyl)ethoxy]phenyl]-methanone; ;
CAS号	84449-90-1 ; 82640-04-8
PubChem CID	5035;
IUPHAR/BPS	2820;
DrugBank	DB00481 ;
ChemSpider	4859 ;
UNII	YX9162EO3I; as HCl: 4F86W47BR6;
KEGG	D08465; as HCl: D02217;
ChEBI	CHEBI:8772 ;
ChEMBL	ChEMBL81 ;
PDB配体ID	RAL (PDBe, RCSB PDB);
CompTox Dashboard（英语：CompTox Chemicals Dashboard） (EPA)	DTXSID3023550 ;
ECHA InfoCard	100.212.655
化学信息
化学式	C28H27NO4S
摩尔质量	473.59 g·mol−1
3D模型（JSmol（英语：JSmol））	交互式图像;
	SMILES O=C(c1c3ccc(O)cc3sc1c2ccc(O)cc2)c5ccc(OCCN4CCCCC4)cc5;
	InChI InChI=1S/C28H27NO4S/c30-21-8-4-20(5-9-21)28-26(24-13-10-22(31)18-25(24)34-28)27(32)19-6-11-23(12-7-19)33-17-16-29-14-2-1-3-15-29/h4-13,18,30-31H,1-3,14-17H2 ; Key:GZUITABIAKMVPG-UHFFFAOYSA-N ;

雷洛昔芬（英语：Raloxifene）的商品名为易维特（Evista），是一种用于预防和治疗绝经后妇女和使用糖皮质激素的妇女的骨质疏松症的药物。^[4]对于骨质疏松症，它不如双磷酸盐类药物受欢迎。^[4] 它也被用于降低高危人群患乳腺癌的风险。^[4]它是口服的。^[4]

常见的副作用包括潮热、腿抽筋、肿胀和关节疼痛。^[4]严重的副作用可能包括血栓和中风。^[4]怀孕期间使用可能会伤害婴儿。^[4]该药可能使月经症状恶化。^[5]雷洛昔芬是一种选择性雌激素受体调节剂（SERM），因此是雌激素受体（ER）的混合激动剂-拮抗剂。^[4]它在骨骼中具有雌激素作用，在乳房和子宫中具有抗雌激素作用。^[4]

雷洛昔芬于1997年被批准在美国用于医疗用途。^[4]它可以作为一种通用药物使用。^[4]^[6]2017年，它是美国最常见的330种处方药之一，有超过90万张处方。^[7]

参考文献

^ ^1.0 ^1.1 ^1.2 ^1.3 ^1.4 ^1.5 Morello, Karla C.; Wurz, Gregory T.; DeGregorio, Michael W. Pharmacokinetics of Selective Estrogen Receptor Modulators. Clinical Pharmacokinetics. 2003, 42 (4): 361–372. ISSN 0312-5963. PMID 12648026. S2CID 13003168. doi:10.2165/00003088-200342040-00004.
^ ^2.0 ^2.1 ^2.2 ^2.3 ^2.4 ^2.5 Hochner-Celnikier D. Pharmacokinetics of raloxifene and its clinical application. Eur. J. Obstet. Gynecol. Reprod. Biol. 1999, 85 (1): 23–9. PMID 10428318. doi:10.1016/s0301-2115(98)00278-4.
^ Jeong, Eun Ju; Liu, Yong; Lin, Huimin; Hu, Ming. Species- and Disposition Model-Dependent Metabolism of Raloxifene in Gut and Liver: Role of UGT1A10. Drug Metabolism and Disposition (ASPET). 2005-03-15, 33 (6): 785–794. PMID 15769887. S2CID 24273998. doi:10.1124/dmd.104.001883.
^ ^4.00 ^4.01 ^4.02 ^4.03 ^4.04 ^4.05 ^4.06 ^4.07 ^4.08 ^4.09 ^4.10 Raloxifene Hydrochloride Monograph for Professionals. Drugs.com. American Society of Health-System Pharmacists. [22 March 2019]. （原始内容存档于2019-03-30）（英语）.
^ Yang, Z. D.; Yu, J.; Zhang, Q. Effects of raloxifene on cognition, mental health, sleep and sexual function in menopausal women: a systematic review of randomized controlled trials. Maturitas. August 2013, 75 (4): 341–348. ISSN 1873-4111. PMID 23764354. doi:10.1016/j.maturitas.2013.05.010.
^ British national formulary : BNF 76 76. Pharmaceutical Press. 2018: 736–737. ISBN 9780857113382.
^ Raloxifene Hydrochloride - Drug Usage Statistics. ClinCalc. [11 April 2020]. （原始内容存档于2021-01-30）.

[MorelloWurz2003-1] 1.0 ^1.1 ^1.2 ^1.3 ^1.4 ^1.5 Morello, Karla C.; Wurz, Gregory T.; DeGregorio, Michael W. Pharmacokinetics of Selective Estrogen Receptor Modulators. Clinical Pharmacokinetics. 2003, 42 (4): 361–372. ISSN 0312-5963. PMID 12648026. S2CID 13003168. doi:10.2165/00003088-200342040-00004.

[pmid10428318-2] 2.0 ^2.1 ^2.2 ^2.3 ^2.4 ^2.5 Hochner-Celnikier D. Pharmacokinetics of raloxifene and its clinical application. Eur. J. Obstet. Gynecol. Reprod. Biol. 1999, 85 (1): 23–9. PMID 10428318. doi:10.1016/s0301-2115(98)00278-4.

[Jeong-3] Jeong, Eun Ju; Liu, Yong; Lin, Huimin; Hu, Ming. Species- and Disposition Model-Dependent Metabolism of Raloxifene in Gut and Liver: Role of UGT1A10. Drug Metabolism and Disposition (ASPET). 2005-03-15, 33 (6): 785–794. PMID 15769887. S2CID 24273998. doi:10.1124/dmd.104.001883.

[AHFS2019-4] 4.00 ^4.01 ^4.02 ^4.03 ^4.04 ^4.05 ^4.06 ^4.07 ^4.08 ^4.09 ^4.10 Raloxifene Hydrochloride Monograph for Professionals. Drugs.com. American Society of Health-System Pharmacists. [22 March 2019]. （原始内容存档于2019-03-30）（英语）.

[5] Yang, Z. D.; Yu, J.; Zhang, Q. Effects of raloxifene on cognition, mental health, sleep and sexual function in menopausal women: a systematic review of randomized controlled trials. Maturitas. August 2013, 75 (4): 341–348. ISSN 1873-4111. PMID 23764354. doi:10.1016/j.maturitas.2013.05.010.

[BNF76-6] British national formulary : BNF 76 76. Pharmaceutical Press. 2018: 736–737. ISBN 9780857113382.

[7] Raloxifene Hydrochloride - Drug Usage Statistics. ClinCalc. [11 April 2020]. （原始内容存档于2021-01-30）.

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