苯海拉明

**苯海拉明**
系统（IUPAC）命名名称
	2-(diphenylmethoxy)-N,N-dimethylethanamine
临床数据
商品名	Benadryl, Unisom, Sominex, ZzzQuil
Drugs.com	Monograph
MedlinePlus	a682539
妊娠分级	AU: A ; US: B (非人类研究中表明无风险) ; ;
依赖性	极低
给药途径	口服、肌注、静注等
合法狀態
合法状态	AU: 限药店出售 (S2) ; US: OTC ;
药代动力学数据
生物利用度	40–60%
蛋白结合度	98–99%
代谢	多种细胞色素P450肝酶: CYP2D6 (80%), CYP3A4 (10%)
生物半衰期	7 小时(儿童); 12 小时(成人); 17 小时(老年)
排泄	94%经尿液，6%经粪便
识别信息
CAS注册号	58-73-1
ATC代码	D04AA32 D04AA33, R06AA02
PubChem	CID 3100
IUPHAR/BPS（英语：IUPHAR/BPS）	1224
DrugBank	DB01075
ChemSpider	2989
UNII	8GTS82S83M
KEGG	D00669
ChEBI	CHEBI:4636
ChEMBL（英语：ChEMBL）	CHEMBL657
化学信息
化学式	C17H21NO
摩尔质量	255.355 g/mol
	SMILES O(CCN(C)C)C(c1ccccc1)c2ccccc2; ;
	InChI InChI=1S/C17H21NO/c1-18(2)13-14-19-17(15-9-5-3-6-10-15)16-11-7-4-8-12-16/h3-12,17H,13-14H2,1-2H3 ; Key:ZZVUWRFHKOJYTH-UHFFFAOYSA-N ;

苯海拉明（英語：Diphenhydramine）是一種抗組胺藥，主要用於治療過敏症^[5]，也可以用於治療失眠、感冒症狀、帕金森氏症震顫和噁心^[5]。給藥方式是口服、靜脈注射及肌肉注射^[5]。最大效果通常在給藥後約兩小時，效果可持續長達七小時^[5]。

苯海拉明常見的副作用包括嗜睡、方向感不佳以及反胃^[5]，不建議給嬰兒服用^[5]。目前還不清楚在懷孕時使用的風險，不過不建議在哺乳時服用此藥物^[6]。苯海拉明是第一代的H1拮抗劑（英语：H1 antihistamine），會阻斷一些組織胺的作用^[5]。苯海拉明也是抗膽鹼劑^[7]。

苯海拉明最早是由George Rieveschl（英语：George Rieveschl）製備，在1946年開始販售^[8]^[9]。目前是通用名药物^[5]。在发展中國家的藥價是每劑美金0.01元^[10]。在美國，每個月的藥費小於美金25元^[11]。苯海拉明的商品名有Benadryl，也有其他的名稱^[5]。

引用[编辑]

^ Paton DM, Webster DR. Clinical pharmacokinetics of H1-receptor antagonists (the antihistamines). Clin. Pharmacokinet. 1985, 10 (6): 477–97. PMID 2866055. doi:10.2165/00003088-198510060-00002.
^ Showing Diphenhydramine (DB01075). DrugBank. [5 September 2009].
^ ^3.0 ^3.1 ^3.2 Simons KJ, Watson WT, Martin TJ, Chen XY, Simons FE. Diphenhydramine: pharmacokinetics and pharmacodynamics in elderly adults, young adults, and children. J. Clin. Pharmacol. July 1990, 30 (7): 665–71. PMID 2391399. doi:10.1002/j.1552-4604.1990.tb01871.x.
^ Garnett WR. Diphenhydramine. Am. Pharm. February 1986, NS26 (2): 35–40. PMID 3962845.
^ ^5.0 ^5.1 ^5.2 ^5.3 ^5.4 ^5.5 ^5.6 ^5.7 ^5.8 Diphenhydramine Hydrochloride. Drugs.com. American Society of Health-System Pharmacists. 6 September 2016 [28 September 2016]. （原始内容存档于15 September 2016）.
^ Diphenhydramine Pregnancy and Breastfeeding Warnings. Drugs.com. [28 September 2016]. （原始内容存档于2 October 2016）.
^ Ayd, Frank J. Lexicon of Psychiatry, Neurology, and the Neurosciences. Lippincott Williams & Wilkins. 2000: 332. ISBN 978-0-7817-2468-5. （原始内容存档于8 September 2017）.
^ Dörwald, Florencio Zaragoza. Lead Optimization for Medicinal Chemists: Pharmacokinetic Properties of Functional Groups and Organic Compounds. John Wiley & Sons. 2013: 225. ISBN 978-3-527-64565-7. （原始内容存档于2 October 2016）.
^ Benadryl. Ohio History Central. [28 September 2016]. （原始内容存档于17 October 2016）.
^ Diphenhydramine. International Drug Price Indicator Guide. [28 September 2016].
^ Hamilton, Richart. Tarascon Pocket Pharmacopoeia 2015 Deluxe Lab-Coat Edition. Jones & Bartlett Learning. 2015: 240. ISBN 978-1-284-05756-0.

延伸閲讀[编辑]

Lieberman JA. History of the use of antidepressants in primary care (PDF). Primary Care Companion J. Clinical Psychiatry. 2003, 5 (supplement 7): 6–10.
Cox D, Ahmed Z, McBride AJ. Diphenhydramine dependence. Addiction. March 2001, 96 (3): 516–7. PMID 11310441.
Björnsdóttir I, Einarson TR, Gudmundsson LS, Einarsdóttir RA. Efficacy of diphenhydramine against cough in humans: a review. Pharmacy World & Science. December 2007, 29 (6): 577–83. PMID 17486423. doi:10.1007/s11096-007-9122-2.

外部連結[编辑]

Drugs.com: Diphenhydramine

[pmid2866055-1] Paton DM, Webster DR. Clinical pharmacokinetics of H1-receptor antagonists (the antihistamines). Clin. Pharmacokinet. 1985, 10 (6): 477–97. PMID 2866055. doi:10.2165/00003088-198510060-00002.

[2] Showing Diphenhydramine (DB01075). DrugBank. [5 September 2009].

[pmid2391399-3] 3.0 ^3.1 ^3.2 Simons KJ, Watson WT, Martin TJ, Chen XY, Simons FE. Diphenhydramine: pharmacokinetics and pharmacodynamics in elderly adults, young adults, and children. J. Clin. Pharmacol. July 1990, 30 (7): 665–71. PMID 2391399. doi:10.1002/j.1552-4604.1990.tb01871.x.

[pmid3962845-4] Garnett WR. Diphenhydramine. Am. Pharm. February 1986, NS26 (2): 35–40. PMID 3962845.

[AHSP2016-5] 5.0 ^5.1 ^5.2 ^5.3 ^5.4 ^5.5 ^5.6 ^5.7 ^5.8 Diphenhydramine Hydrochloride. Drugs.com. American Society of Health-System Pharmacists. 6 September 2016 [28 September 2016]. （原始内容存档于15 September 2016）.

[6] Diphenhydramine Pregnancy and Breastfeeding Warnings. Drugs.com. [28 September 2016]. （原始内容存档于2 October 2016）.

[7] Ayd, Frank J. Lexicon of Psychiatry, Neurology, and the Neurosciences. Lippincott Williams & Wilkins. 2000: 332. ISBN 978-0-7817-2468-5. （原始内容存档于8 September 2017）.

[8] Dörwald, Florencio Zaragoza. Lead Optimization for Medicinal Chemists: Pharmacokinetic Properties of Functional Groups and Organic Compounds. John Wiley & Sons. 2013: 225. ISBN 978-3-527-64565-7. （原始内容存档于2 October 2016）.

[9] Benadryl. Ohio History Central. [28 September 2016]. （原始内容存档于17 October 2016）.

[10] Diphenhydramine. International Drug Price Indicator Guide. [28 September 2016].

[Ric2015-11] Hamilton, Richart. Tarascon Pocket Pharmacopoeia 2015 Deluxe Lab-Coat Edition. Jones & Bartlett Learning. 2015: 240. ISBN 978-1-284-05756-0.

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苯海拉明

引用[编辑]

延伸閲讀[编辑]

外部連結[编辑]

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