倍他米松

倍他米松
临床资料
商品名（英语：Drug nomenclature）	Celestone、Eleuphrat及其他
AHFS/Drugs.com	Monograph
MedlinePlus	a682799
核准状况	美 DailyMed: Betamethasone;
怀孕分级	澳: C ; ;
给药途径	口服给药、外用药物及肌肉注射
ATC码	A07EA04 (WHO) C05AA05 D07AC01 D07BC01 D07CC01 D07XC01 H02AB01 R01AD06 R03BA04 S01BA06 S01BB04 S01CA05 S01CB04 S02BA07 S03BA03 S03CA06;
法律规范状态
法律规范	澳：限医生处方（S4）; 英：处方药（℞-only） (POM); 美：处方药（℞-only）; 处方药（℞-only）;
药物动力学数据
药物代谢	肝脏CYP3A4
生物半衰期	36-54小时
排泄途径	肾脏 (经由尿液排出人体)
识别信息
	IUPAC命名法 (8S,9R,10S,11S,13S,14S,16S,17R)-9-Fluoro- 11,17-dihydroxy-17-(2-hydroxyacetyl)-10,13,16-trimethyl- 6,7,8,9,10,11,12,13,14,15,16,17-dodecahydro- 3H-cyclopenta[a]phenanthren-3-one; ;
CAS号	378-44-9
PubChem CID	9782;
IUPHAR/BPS	7061;
DrugBank	DB00443 ;
ChemSpider	9399 ;
UNII	9842X06Q6M;
KEGG	D00244 ;
ChEBI	CHEBI:3077 ;
ChEMBL	ChEMBL632 ;
CompTox Dashboard（英语：CompTox Chemicals Dashboard） (EPA)	DTXSID3022667 ;
ECHA InfoCard	100.006.206
化学信息
化学式	C22H29FO5
摩尔质量	392.47 g·mol−1
3D模型（JSmol（英语：JSmol））	交互式图像;
	SMILES O=C(CO)[C@]3(O)[C@]2(C[C@H](O)[C@]4(F)[C@@]/1(\C(=C/C(=O)\C=C\1)CC[C@H]4[C@@H]2C[C@@H]3C)C)C;
	InChI InChI=1S/C22H29FO5/c1-12-8-16-15-5-4-13-9-14(25)6-7-19(13,2)21(15,23)17(26)10-20(16,3)22(12,28)18(27)11-24/h6-7,9,12,15-17,24,26,28H,4-5,8,10-11H2,1-3H3/t12-,15-,16-,17-,19-,20-,21-,22-/m0/s1 ; Key:UREBDLICKHMUKA-DVTGEIKXSA-N ;

倍他米松（英语：Betamethasone）是一种类固醇药物，^[3]用于治疗多种疾病，包括类风湿性关节炎和全身性红斑狼疮等风湿性疾病、皮肤炎和干癣等皮肤病、气喘和血管性水肿等过敏性疾病、促进早产婴儿肺部发育、克隆氏症、白血病等癌症，以及与氟氢可的松（英语：fludrocortisone）联合使用以治疗肾上腺功能不全等。^[3]给药方式有口服、肌肉注射或在皮肤上涂抹（通常有霜剂、乳液或液体形式）。^[3]^[4]

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使用此药物后严重的副作用有感染风险增加、肌肉无力、严重过敏反应和思觉失调。^[3]长期使用可能会导致肾上腺功能不全。^[3]长期使用后突然停药可能会有严重性后果。^[3]使用霜剂通常会导致毛发增长和皮肤不适。^[4]倍他米松属于糖皮质素类药物。^[3]它是地塞米松的立体异构体，这两种化合物仅在16位甲基的空间构型上有所不同（参见类固醇#命名法）。^[5]

医疗用途

倍他米松是一种皮质类固醇，有丸剂、注射剂、软膏、乳膏、乳液、凝胶或皮肤用喷雾剂，以及用于头皮的泡沫剂。^[6]经注射给药时，抗炎性作用约会在两小时内开始，并持续7天。^[3]

乳膏可用于缓解皮肤不适（例如皮肤炎引起的瘙痒和剥落）。它用作局部干癣的治疗，与二丙酸倍他米松（英语：betamethasone dipropionate）（倍他米松衍生物）或是水杨酸的作用相似，或与卡泊三醇/倍他米松二丙酸（英语：Calcipotriol/betamethasone dipropionate）组成复方剂使用。（参见卡泊三醇/二丙酸倍他米松#Regulation}}）倍他米松磷酸钠（英语：Betamethasone phosphate）可作口服剂和注射剂，其适应症与其他类固醇相同。很多以倍他米松为基础的药物都含有戊酸酯类固醇。(如Betamethasone valerate（英语：倍他米松二丙酸酯）与倍他米松二丙酸（英语：betamethasone dipropionate）)

在一项随机对照试验中，倍他米松被证明可将与共济失调微血管扩张症候群 (A-T) 相关的一些共济失调症状减轻28-31%。^[7]

倍他米松也用于刺激胎儿肺脏成熟，以预防新生儿呼吸窘迫症候群 (IRDS) ，并降低早产儿颅内出血的发生率和死亡率。^[8]

含有0.05%倍他米松的乳膏似乎可有效治疗男孩的包茎问题，^[9]而通常因此能避免包皮环切术。^[10]^[11]^[12]此药物已成为英国国民保健署体系中一些医生的首选，用以避免包皮环切的治疗方式。^[13]^[14]

副作用

欣快感^[15]
抑郁症^[15]
肾上腺功能不全^[15]
高血压^[15]
皮下微血管群变明显，出现瘀点^[15]
多毛症^[15]
瘀斑^[15]

在大面积皮肤、破损或裸露皮肤、皮肤皱褶或密封敷料之下长时间使用如倍他米松的皮质类固醇药物，在极少数情况下可能会导致吸收过多，所产生的副作用例如有局部皮肤变薄，及导致肾上腺减少产生天然激素。

倍他米松也可在早产儿分娩前使用，以帮助其肺部发育。

当注射到人体硬膜外腔（英语：epidural space）或脊柱时，可能会导致严重的副作用，如视力丧失、中风和瘫痪。^[16]

药理学

形式

倍他米松有多种化合物形式：二丙酸倍他米松（品牌有Diprosone、Diprolene、Celestamine、Procort（于巴基斯坦）等）、倍他米松磷酸钠（于意大利，品牌名称有Bentelan）和倍他米松二丙酸酯（品牌名称有Audavate、Betnovate 、Celestone、Fucibet（夫西地酸/倍他米松二丙酸酯（英语：Fusidic acid/betamethasone valerate）复方药））等。在美国和加拿大，倍他米松与克催玛汝混合，以Lotrisone和Lotriderm的品牌销售。它还与水杨酸组合用于治疗干癣（品牌名称为Diprosalic）。在一些国家，它也与克催玛汝和庆大霉素（两者皆为（抗细菌药）混合贩售。

倍他米松磷酸钠与醋酸倍他米松（英语：betamethasone acetate）的混合物在美国以Celestone Soluspan的品牌名称出售。^[17]

社会与文化

倍他米松的专利于1958年在美国提出申请，于1961年获得，也于1961年取得美国的核准用于医疗用途。^[3]^[18]此药物的霜剂和软膏已列入世界卫生组织基本药物标准清单之中。^[19]由于专利已过期，市面有其通用名药物贩售。^[3]此药物于2021年在美国最常用处方药中排名第251，开立的处方笺数量超过100万张。^[20]^[21]

参见

倍他米松/右氯苯那敏（英语：Betamethasone/dexchlorpheniramine）

参考文献

[1]
Betamethasone Use During Pregnancy. Drugs.com. 2019-12-30 [2020-03-29]. （原始内容存档于2020-12-01）.
[2]
Betamethasone 500 microgram Soluble Tablets - Summary of Product Characteristics (SmPC). (emc). 2018-04-05 [2020-03-29]. （原始内容存档于2020-03-29）.
[3]
Betamethasone. The American Society of Health-System Pharmacists. [2015-12-02]. （原始内容存档于2015-12-08）.
[4]
Betamethasone topical. The American Society of Health-System Pharmacists. [2015-12-02]. （原始内容存档于2015-12-08）.
[5]
Antignac JP, Le Bizec B, Monteau F, Andre F. Differentiation of betamethasone and dexamethasone using liquid chromatography/positive electrospray tandem mass spectrometry and multivariate statistical analysis. Journal of Mass Spectrometry. January 2002, 37 (1): 69–75. Bibcode:2002JMSp...37...69A. PMID 11813313. doi:10.1002/jms.260.
[6]
Betamethasone Topical. MedlinePlus. 2020-03-19 [2020-03-29]. （原始内容存档于2020-03-29）.
[7]
Zannolli R, Buoni S, Betti G, Salvucci S, Plebani A, Soresina A, et al. A randomized trial of oral betamethasone to reduce ataxia symptoms in ataxia telangiectasia. Movement Disorders. September 2012, 27 (10): 1312–1316. PMID 22927201. S2CID 23696748. doi:10.1002/mds.25126.
[8]
Antenatal Corticosteroid Therapy for Fetal Maturation. ACOC Clinical. August 2017 [2024-03-31]. （原始内容存档于2024-03-31）.
[9]
Moreno G, Corbalán J, Peñaloza B, Pantoja T. Topical corticosteroids for treating phimosis in boys. The Cochrane Database of Systematic Reviews. September 2014, 9 (9): CD008973. PMC 10765470 . PMID 25180668. doi:10.1002/14651858.CD008973.pub2.
[10]
Van Howe RS. Cost-effective treatment of phimosis. Pediatrics. October 1998, 102 (4): E43. PMID 9755280. doi:10.1542/peds.102.4.e43 . （原始内容存档于2009-08-19）. A review of estimated costs and complications of 3 phimosis treatments.
[11]
Esposito C, Centonze A, Alicchio F, Savanelli A, Settimi A. Topical steroid application versus circumcision in pediatric patients with phimosis: a prospective randomized placebo controlled clinical trial. World Journal of Urology (Springer Science and Business Media LLC). April 2008, 26 (2): 187–190. PMID 18157674. S2CID 8922151. doi:10.1007/s00345-007-0231-2.
[12]
Zampieri N, Corroppolo M, Zuin V, Bianchi S, Camoglio FS. Phimosis and topical steroids: new clinical findings. Pediatric Surgery International. April 2007, 23 (4): 331–335. PMID 17308904. S2CID 22849471. doi:10.1007/s00383-007-1878-x.
[13]
Berdeu D, Sauze L, Ha-Vinh P, Blum-Boisgard C. Cost-effectiveness analysis of treatments for phimosis: a comparison of surgical and medicinal approaches and their economic effect. BJU International. February 2001, 87 (3): 239–244. PMID 11167650. S2CID 2161551. doi:10.1046/j.1464-410x.2001.02033.x .
[14]
Chu CC, Chen KC, Diau GY. Topical steroid treatment of phimosis in boys. The Journal of Urology. September 1999, 162 (3 Pt 1): 861–863. PMID 10458396. doi:10.1097/00005392-199909010-00078.
[15]
betamethasone (PDF). F.A. Davis. 2017 [2017-03-07]. （原始内容存档 (PDF)于2017-09-08）.
[16]
FDA Drug Safety Communication: FDA requires label changes to warn of rare but serious neurologic problems after epidural corticosteroid injections for pain. FDA. 2014-04-23 [2016-08-15]. （原始内容存档于2016-08-11）.
[17]
Celestone Soluspan- betamethasone acetate and betamethasone sodium phosphate injection, suspension. DailyMed. 2019-11-18 [2020-03-29]. （原始内容存档于2020-08-04）.
[18]
Fischer J, Ganellin CR. Analogue-based Drug Discovery. John Wiley & Sons. 2006: 485 [2024-04-10]. ISBN 9783527607495. （原始内容存档于2023-01-10）.
[19]
World Health Organization. World Health Organization model list of essential medicines: 21st list 2019. Geneva: World Health Organization. 2019. hdl:10665/325771 . WHO/MVP/EMP/IAU/2019.06. License: CC BY-NC-SA 3.0 IGO.
[20]
The Top 300 of 2021. ClinCalc. [2024-01-14]. （原始内容存档于2024-01-15）.
[21]
Betamethasone - Drug Usage Statistics. ClinCalc. [2024-01-14]. （原始内容存档于2024-02-29）.

Template:Nasal preparations

模板:皮肤病用抗生素和化疗药

[Drugs.com_pregnancy-1] [1]
Betamethasone Use During Pregnancy. Drugs.com. 2019-12-30 [2020-03-29]. （原始内容存档于2020-12-01）.

[2] [2]
Betamethasone 500 microgram Soluble Tablets - Summary of Product Characteristics (SmPC). (emc). 2018-04-05 [2020-03-29]. （原始内容存档于2020-03-29）.

[AHFS2015-3] [3]
Betamethasone. The American Society of Health-System Pharmacists. [2015-12-02]. （原始内容存档于2015-12-08）.

[AHFS2015Top-4] [4]
Betamethasone topical. The American Society of Health-System Pharmacists. [2015-12-02]. （原始内容存档于2015-12-08）.

[5] [5]
Antignac JP, Le Bizec B, Monteau F, Andre F. Differentiation of betamethasone and dexamethasone using liquid chromatography/positive electrospray tandem mass spectrometry and multivariate statistical analysis. Journal of Mass Spectrometry. January 2002, 37 (1): 69–75. Bibcode:2002JMSp...37...69A. PMID 11813313. doi:10.1002/jms.260.

[6] [6]
Betamethasone Topical. MedlinePlus. 2020-03-19 [2020-03-29]. （原始内容存档于2020-03-29）.

[A_Randomized_Trial_of_Oral_Betamethazone_to_Reduce_Ataxia_Symptoms_in_Ataxia_Telangiectasia-7] [7]
Zannolli R, Buoni S, Betti G, Salvucci S, Plebani A, Soresina A, et al. A randomized trial of oral betamethasone to reduce ataxia symptoms in ataxia telangiectasia. Movement Disorders. September 2012, 27 (10): 1312–1316. PMID 22927201. S2CID 23696748. doi:10.1002/mds.25126.

[ACOC_Clinical-8] [8]
Antenatal Corticosteroid Therapy for Fetal Maturation. ACOC Clinical. August 2017 [2024-03-31]. （原始内容存档于2024-03-31）.

[9] [9]
Moreno G, Corbalán J, Peñaloza B, Pantoja T. Topical corticosteroids for treating phimosis in boys. The Cochrane Database of Systematic Reviews. September 2014, 9 (9): CD008973. PMC 10765470 . PMID 25180668. doi:10.1002/14651858.CD008973.pub2.

[vanHowe1998-10] [10]
Van Howe RS. Cost-effective treatment of phimosis. Pediatrics. October 1998, 102 (4): E43. PMID 9755280. doi:10.1542/peds.102.4.e43 . （原始内容存档于2009-08-19）. A review of estimated costs and complications of 3 phimosis treatments.

[World_Journal_of_Urology-11] [11]
Esposito C, Centonze A, Alicchio F, Savanelli A, Settimi A. Topical steroid application versus circumcision in pediatric patients with phimosis: a prospective randomized placebo controlled clinical trial. World Journal of Urology (Springer Science and Business Media LLC). April 2008, 26 (2): 187–190. PMID 18157674. S2CID 8922151. doi:10.1007/s00345-007-0231-2.

[Pediatric_Surgery_International-12] [12]
Zampieri N, Corroppolo M, Zuin V, Bianchi S, Camoglio FS. Phimosis and topical steroids: new clinical findings. Pediatric Surgery International. April 2007, 23 (4): 331–335. PMID 17308904. S2CID 22849471. doi:10.1007/s00383-007-1878-x.

[Berdue2001-13] [13]
Berdeu D, Sauze L, Ha-Vinh P, Blum-Boisgard C. Cost-effectiveness analysis of treatments for phimosis: a comparison of surgical and medicinal approaches and their economic effect. BJU International. February 2001, 87 (3): 239–244. PMID 11167650. S2CID 2161551. doi:10.1046/j.1464-410x.2001.02033.x .

[Chu1999-14] [14]
Chu CC, Chen KC, Diau GY. Topical steroid treatment of phimosis in boys. The Journal of Urology. September 1999, 162 (3 Pt 1): 861–863. PMID 10458396. doi:10.1097/00005392-199909010-00078.

[Davis-15] [15]
betamethasone (PDF). F.A. Davis. 2017 [2017-03-07]. （原始内容存档 (PDF)于2017-09-08）.

[16] [16]
FDA Drug Safety Communication: FDA requires label changes to warn of rare but serious neurologic problems after epidural corticosteroid injections for pain. FDA. 2014-04-23 [2016-08-15]. （原始内容存档于2016-08-11）.

[17] [17]
Celestone Soluspan- betamethasone acetate and betamethasone sodium phosphate injection, suspension. DailyMed. 2019-11-18 [2020-03-29]. （原始内容存档于2020-08-04）.

[Fis2006-18] [18]
Fischer J, Ganellin CR. Analogue-based Drug Discovery. John Wiley & Sons. 2006: 485 [2024-04-10]. ISBN 9783527607495. （原始内容存档于2023-01-10）.

[WHO21st-19] [19]
World Health Organization. World Health Organization model list of essential medicines: 21st list 2019. Geneva: World Health Organization. 2019. hdl:10665/325771 . WHO/MVP/EMP/IAU/2019.06. License: CC BY-NC-SA 3.0 IGO.

[20] [20]
The Top 300 of 2021. ClinCalc. [2024-01-14]. （原始内容存档于2024-01-15）.

[21] [21]
Betamethasone - Drug Usage Statistics. ClinCalc. [2024-01-14]. （原始内容存档于2024-02-29）.

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