头孢氨苄

**头孢氨苄**
系统（IUPAC）命名名称
	IUPAC_name = （6R，7R）-3-甲基-7-[（R）-2-氨基-2-苯乙酰氨基]-8-氧代-5-硫杂-1-氮杂双环[4.2.0]辛-2-烯-2-甲酸 ; (7R)-3-Methyl-7- (α- D -phenylglycylamino) -3-cephem-4-carboxylic acid monohydrate
临床数据
读音	/ˌsɛfəˈlɛksɪn/
商品名	Keflex, Cepol, Ceporexine, Ceporex
Drugs.com	Monograph
MedlinePlus	a682733
医疗法规	US FDA: Keflex;
妊娠分级	AU: A ; US: B (非人类研究中表明无风险) ; ;
给药途径	口服
合法状态
合法状态	AU: 限医生处方 (S4) ; UK: 处方药（℞-only） (POM) ; US: 处方药（℞-only） ;
药代动力学数据
生物利用度	吸收良好
蛋白结合度	15%
代谢	80% excreted unchanged in urine within 6 hours of administration
生物半衰期	For an adult with normal renal function, the serum half-life is 0.5–1.2 hours
排泄	肾
识别信息
CAS注册号	15686-71-2
ATC代码	J01DB01 QJ51DB01
PubChem	CID 2666
IUPHAR/BPS	4832
DrugBank	DB00567
ChemSpider	25541
UNII	5SFF1W6677
KEGG	D00263
ChEBI	CHEBI:3534
ChEMBL	CHEMBL1727
化学信息
化学式	C16H17N3O4S
摩尔质量	347.39 g/mol
	SMILES O=C2N1/C(=C(\CS[C@@H]1[C@@H]2NC(=O)[C@@H](c3ccccc3)N)C)C(=O)O; ;
	InChI InChI=1S/C16H17N3O4S/c1-8-7-24-15-11(14(21)19(15)12(8)16(22)23)18-13(20)10(17)9-5-3-2-4-6-9/h2-6,10-11,15H,7,17H2,1H3,(H,18,20)(H,22,23)/t10-,11-,15-/m1/s1 ; Key:ZAIPMKNFIOOWCQ-UEKVPHQBSA-N ;
物理性质
熔点	326.8 °C（620.2 °F）

头孢氨苄（英语：Cefalexin或英语：Cephalexin，又译先锋霉素Ⅳ、又作赐福力欣、头孢力欣、赐尔复新、西华烈信、施华林、喜化幸、雪华力欣、或赐泛立信等^[3]）。是一种半合成的第一代口服头孢霉素类类抗生素药物，可用于数种细菌感染的抗生素。头孢氨苄是口服药，借由干扰细菌细胞壁的合成来杀死革兰氏阳性菌和部分革兰氏阴性菌^[4]。头孢氨苄属于第一代头孢菌素，它与其他同类的抗生素如静脉施打的头孢唑啉具有相似的作用^[5]。

头孢氨苄被以于治疗中耳炎、链球菌性咽炎、肺炎、骨与关节感染、蜂窝性组织炎、以及泌尿道感染等，它也可以被用于预防感染性心内膜炎。头孢氨苄对于抗药性金黄色葡萄球菌没有效果。头孢氨苄可以使用在对青霉素有轻微至普通程度过敏反应的病人身上，但对于有强烈过敏反应的病人而言则不适合使用。头孢氨苄对病毒感染并没有效果^[4]。在台湾，由于组织穿透性不佳以及抗药性菌株较多，除蜂窝性组织炎及经确认菌株无抗药性的泌尿道感染^[6]仍使用头孢氨苄作首选治疗药物，上述其他病症（中耳炎^[7]、咽炎^[8]、肺炎^[9]、骨与关节感染^[10]、以及感染心内膜炎^[11]）已经建议使用其他抗生素治疗^[12]^[13]。

头孢氨苄的可能副作用包括过敏、肠胃不适、伪膜性结肠炎等等^[4]。对于孕妇而言，本药品在许多孕妇使用后仍没有证据显示它会对孕妇或胎儿造成伤害^[4]^[14]（等同于美国的怀孕用药等级B；与澳洲的等级A），在哺乳期间使用本药品也是安全的^[15]。儿童与65岁以上的老人都可以安全的使用本药。肾功能不佳的病人在使用本药品时应依指示减少剂量^[4]。

2012年时头孢氨苄名列美国前百大最常使用药物^[16]，在澳洲则跻身前十五强^[17]。它在1969-1970年间由葛兰素史克与礼来发现，并分别以Keflex与Ceporex为名上市^[1]^[18]。今日，市面上已经有许多本药品的学名药可供选择，价格也不昂贵^[4]^[19]。本品列名于世界卫生组织基本药物标准清单上，这张清单列出世界卫生组织建议医疗系统中应有的最重要的药物^[20]。

适应症

头孢氨苄可用于治疗敏感菌所致呼吸道（包括鼻窦炎、中耳炎、咽炎、扁桃体炎及肺炎）、泌尿道、皮肤及软组织、生殖器官等部位感染的治疗。抗菌谱与头孢噻吩、头孢噻啶基本相同，但抗菌效力比两者要弱。

用法及用量

成人通常每6小时服250毫克或每8至12小时服500毫克，儿童用量通常以每日每公斤体重服25毫克计，分多次服用。如症状严重，医生可根据病人情况增加剂量。通常服7至10日，或依医生指示。

不良反应

有些人服药后出现了不良反应，以下是一些较为常见者：

肠胃不适，例如腹泻、恶心及呕吐。
头痛
过敏反应，例如皮肤红疹、痕痒、荨麻疹等。如情况严重，应立即求医。

注意事项

对头孢菌素过敏者、卟啉症（Porphyria）患者禁用头孢氨苄及其它头孢菌素。

对盘尼西林类抗生素过敏者、肾功能不全者、孕妇或授乳妇女应小心使用头孢氨苄及其它头孢菌素。对盘尼西林类抗生素过敏者中，大约10%的人也会对头孢菌素产生过敏反应。

外部链接

参见

头孢菌素

参考来源

↑ ^1.0 ^1.1 McPherson, Edwin M. Pharmaceutical Manufacturing Encyclopedia. 3rd. Burlington: Elsevier. 2007: 915. ISBN 9780815518563.
↑ McEvoy, G.K. (ed.). American Hospital Formulary Service — Drug Information 95. Bethesda, MD: American Society of Hospital Pharmacists, Inc., 1995 (Plus Supplements 1995)., p. 166
↑ 卫生福利部病历中文化字彙查询. [2015-01-10].
↑ ^4.0 ^4.1 ^4.2 ^4.3 ^4.4 ^4.5 Cephalexin. The American Society of Health-System Pharmacists. [2014-04-21].
↑ Brunton, Laurence L. 53, Penicillins, Cephalosporins, and Other β-Lactam Antibiotics. Goodman & Gilman's pharmacological basis of therapeutics. 12th. New York: McGraw-Hill. 2011. ISBN 978-0071624428.
↑ 詹雅惠. 台湾门诊泌尿道感染抗生素处方型态分析及其影响因素. 阳明大学医务管理研究所. 2006 [2015-01-11].
↑ 台湾中耳炎治疗现以高剂量阿莫西林为一线用药，见表5Diagnosis and Treatment of Otitis Media. American Academy of Family Physicians. [2015-01-10].
↑ 台湾咽炎治疗现以高剂量阿墨西林为一线用药，Diagnosis and Treatment of Streptococcal Pharyngitis. American Academy of Family Physicians. [2015-01-10].
↑ 肺炎临床诊疗指引，国卫院肺炎治疗指引 (PDF). : 72. ；表七Infectious Diseases Society of America/AmericanThoracic Society Consensus Guidelines on the Management of Community-Acquired Pneumonia in Adults (PDF). 2007 [2015-01-11].
↑ 骨与关节感染(septic arthritis与osteomyelitis)也不会用此药治疗，血清浓度可能不够，组织穿透性也不够好，详见下列文献表四Mathews, C. J., Kingsley, G., Field, M., Jones, A., Weston, V. C., Phillips, M., … Coakley, G. Management of septic arthritis: a systematic review. Annals of the Rheumatic Diseases. 2007. doi:10.1136/ard.2006.058909. 以及下列文献的表三JOHN HATZENBUEHLER, MD, and THOMAS J. PULLING, MD, Maine Medical Center, Portland, Maine. Diagnosis and Management of Osteomyelitis. American Academy of Family Physicians.
↑ Prevention of Infective Endocarditis. 2007 [2015-01-11]. doi:10.1161/CIRCULATIONAHA.106.183095.
↑ Harrison's Principle of ...
↑ Kalpana Gupta, Thomas M. Hooton, Kurt G. Naber, Bjo¨rn Wullt, Richard Colgan, Loren G. Miller, Gregory J. Moran, Lindsay E. Nicolle, Raul Raz, Anthony J. Schaeffer, and David E. Soper. International Clinical Practice Guidelines for the Treatment of Acute Uncomplicated Cystitis and Pyelonephritis in Women: A 2010 Update by the Infectious Diseases Society of America and the European Society for Microbiology and Infectious Diseases (PDF). 2011 [2015-01-11]. doi:10.1093/cid/ciq257.
↑ Prescribing medicines in pregnancy database. Australian Government. 2014-03-03 [2014-04-22].
↑ Wendy Jones. Breastfeeding and Medication. Routledge. 2013: 227. ISBN 9781136178153.
↑ Bartholow, Michael. Top 200 Drugs of 2012. Pharmacy Times. [2014-04-22].
↑ Australia's Health 2012: The Thirteenth Biennial Health Report of the Australian Institute of Health and Welfare. Australian Institute of Health and Welfare. 2012: 408. ISBN 9781742493053.
↑ Ravina, Enrique. The evolution of drug discovery : from traditional medicines to modern drugs 1. Aufl. Weinheim: Wiley-VCH. 2011: 267. ISBN 9783527326693.
↑ Hanlon, Geoffrey; Hodges, Norman. Essential Microbiology for Pharmacy and Pharmaceutical Science. Hoboken: Wiley. 2012: 140. ISBN 9781118432433.
↑ WHO Model List of EssentialMedicines (PDF). World Health Organization: 6. October 2013 [2014-04-22].

[McP2007-1] 1.0 ^1.1 McPherson, Edwin M. Pharmaceutical Manufacturing Encyclopedia. 3rd. Burlington: Elsevier. 2007: 915. ISBN 9780815518563.

[2] McEvoy, G.K. (ed.). American Hospital Formulary Service — Drug Information 95. Bethesda, MD: American Society of Hospital Pharmacists, Inc., 1995 (Plus Supplements 1995)., p. 166

[3] 卫生福利部病历中文化字彙查询. [2015-01-10].

[AHFS2014-4] 4.0 ^4.1 ^4.2 ^4.3 ^4.4 ^4.5 Cephalexin. The American Society of Health-System Pharmacists. [2014-04-21].

[5] Brunton, Laurence L. 53, Penicillins, Cephalosporins, and Other β-Lactam Antibiotics. Goodman & Gilman's pharmacological basis of therapeutics. 12th. New York: McGraw-Hill. 2011. ISBN 978-0071624428.

[6] 詹雅惠. 台湾门诊泌尿道感染抗生素处方型态分析及其影响因素. 阳明大学医务管理研究所. 2006 [2015-01-11].

[7] 台湾中耳炎治疗现以高剂量阿莫西林为一线用药，见表5Diagnosis and Treatment of Otitis Media. American Academy of Family Physicians. [2015-01-10].

[8] 台湾咽炎治疗现以高剂量阿墨西林为一线用药，Diagnosis and Treatment of Streptococcal Pharyngitis. American Academy of Family Physicians. [2015-01-10].

[9] 肺炎临床诊疗指引，国卫院肺炎治疗指引 (PDF). : 72. ；表七Infectious Diseases Society of America/AmericanThoracic Society Consensus Guidelines on the Management of Community-Acquired Pneumonia in Adults (PDF). 2007 [2015-01-11].

[10] 骨与关节感染(septic arthritis与osteomyelitis)也不会用此药治疗，血清浓度可能不够，组织穿透性也不够好，详见下列文献表四Mathews, C. J., Kingsley, G., Field, M., Jones, A., Weston, V. C., Phillips, M., … Coakley, G. Management of septic arthritis: a systematic review. Annals of the Rheumatic Diseases. 2007. doi:10.1136/ard.2006.058909. 以及下列文献的表三JOHN HATZENBUEHLER, MD, and THOMAS J. PULLING, MD, Maine Medical Center, Portland, Maine. Diagnosis and Management of Osteomyelitis. American Academy of Family Physicians.

[11] Prevention of Infective Endocarditis. 2007 [2015-01-11]. doi:10.1161/CIRCULATIONAHA.106.183095.

[12] Harrison's Principle of ...

[13] Kalpana Gupta, Thomas M. Hooton, Kurt G. Naber, Bjo¨rn Wullt, Richard Colgan, Loren G. Miller, Gregory J. Moran, Lindsay E. Nicolle, Raul Raz, Anthony J. Schaeffer, and David E. Soper. International Clinical Practice Guidelines for the Treatment of Acute Uncomplicated Cystitis and Pyelonephritis in Women: A 2010 Update by the Infectious Diseases Society of America and the European Society for Microbiology and Infectious Diseases (PDF). 2011 [2015-01-11]. doi:10.1093/cid/ciq257.

[TGA2014-14] Prescribing medicines in pregnancy database. Australian Government. 2014-03-03 [2014-04-22].

[Breast2013-15] Wendy Jones. Breastfeeding and Medication. Routledge. 2013: 227. ISBN 9781136178153.

[16] Bartholow, Michael. Top 200 Drugs of 2012. Pharmacy Times. [2014-04-22].

[17] Australia's Health 2012: The Thirteenth Biennial Health Report of the Australian Institute of Health and Welfare. Australian Institute of Health and Welfare. 2012: 408. ISBN 9781742493053.

[18] Ravina, Enrique. The evolution of drug discovery : from traditional medicines to modern drugs 1. Aufl. Weinheim: Wiley-VCH. 2011: 267. ISBN 9783527326693.

[19] Hanlon, Geoffrey; Hodges, Norman. Essential Microbiology for Pharmacy and Pharmaceutical Science. Hoboken: Wiley. 2012: 140. ISBN 9781118432433.

[20] WHO Model List of EssentialMedicines (PDF). World Health Organization: 6. October 2013 [2014-04-22].

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