阿普唑仑

阿普唑仑
臨床資料
读音	/ælˈpræzəlæm/ 或 /ælˈpreɪzəlæm/
商品名（英语：Drug nomenclature）	Xanax, Xanor, Niravam, others
AHFS/Drugs.com	Monograph
MedlinePlus	a684001
核准狀況	美 DailyMed: Alprazolam;
懷孕分級	澳: C ; ;
依賴性	High
给药途径	口服
藥物類別（英语：Drug class）	Benzodiazepine
ATC碼	N05BA12 (WHO) ;
法律規範狀態
法律規範	澳：受管控（S8）; 加：Schedule IV; 中：第二类精神药品; 德：Anlage III (in doses higher than 1 mg); 英：Class C; 美：附表IV; UN：Psychotropic Schedule IV; 处方药（℞-only）;
藥物動力學數據
生物利用度	80–90%
血漿蛋白結合率	80%
药物代谢	代谢，via cytochrome P450 3A4
代謝產物	Alpha-hydroxyalprazolam, 4-hydroxyalprazolam, beta-hydroxyalprazolam
藥效起始時間（英语：Onset of action）	20~60分钟
生物半衰期	完全释放：11~13小时; 缓释：11~16小时
作用時間	完全释放：6小时; 缓释：11.3小时
排泄途徑	Kidney
识别信息
	IUPAC命名法 8-Chloro-1-methyl-6-phenyl-4H-[1,2,4]triazolo[4,3-a] [1,4]benzodiazepine; ;
CAS号	28981-97-7
PubChem CID	2118;
IUPHAR/BPS	7111;
DrugBank	DB00404 ;
ChemSpider	2034 ;
UNII	YU55MQ3IZY;
KEGG	D00225 ;
ChEBI	CHEBI:2611 ;
ChEMBL	ChEMBL661 ;
CompTox Dashboard（英语：CompTox Chemicals Dashboard） (EPA)	DTXSID4022577 ;
ECHA InfoCard	100.044.849
化学信息
化学式	C17H13ClN4
摩尔质量	308.77 g·mol−1
3D模型（JSmol（英语：JSmol））	交互式图像;
	SMILES Cc1nnc2n1-c1ccc(Cl)cc1C(c1ccccc1)=NC2;
	InChI InChI=1S/C17H13ClN4/c1-11-20-21-16-10-19-17(12-5-3-2-4-6-12)14-9-13(18)7-8-15(14)22(11)16/h2-9H,10H2,1H3 ; Key:VREFGVBLTWBCJP-UHFFFAOYSA-N ;

阿普唑仑（INN：alprazolam），商品名贊安諾（Xanax），是三唑并苯二氮䓬类中的中效速效镇静剂，它是与三唑环融合的苯二氮䓬类 (BZD)^[1]。它最常用于焦虑症的短期管理，特别是恐慌症或广泛性焦虑症 (GAD)^[2]。其他用途包括治疗化疗引起的恶心，以及其他治疗方法^[3]。GAD 改善一般在一周内发生^[4]^[5]。阿普唑仑通常口服^[3]。

事实速览 臨床資料, 读音 ...

关闭

常见的副作用包括嗜睡、抑郁、头痛、感觉疲倦、口干和记忆力问题。^[3]一些镇静和疲倦可能会在几天内得到改善。^[6]由于担心误用，一些人不推荐阿普唑仑作为恐慌症的初始治疗。^[7]如果突然减少使用，可能会出现戒断或反弹症状；^[3]可能需要在数周或数月内逐渐减少剂量。^[4]其他罕见的风险包括自杀^[8]^[9]和全因死亡风险增加两倍。^[10]阿普唑仑与其他苯二氮䓬类药物一样，通过GABA_A受体起作用。^[3]

阿普唑仑于1971年获得专利，并于1981年在美国获准用于医疗用途。^[3]^[11]阿普唑仑是附表IV受控物质，是一种常见的滥用药物。^[12]它可作为通用名药物使用。^[2]2019年，它是美国第41位最常用的处方药，有超过1700万张处方。^[13]^[14]

阿普唑仑主要用于短期治疗焦虑症、恐慌症和化疗引起的恶心。^[4]阿普唑仑适用于治疗成人广泛性焦虑症和恐慌症伴或不伴广场恐惧症。^[2]FDA标签建议医生应定期重新评估药物的有效性。^[2]

恐慌症

阿普唑仑可有效缓解中度至重度焦虑和惊恐发作。^[2]然而，自从开发出选择性5-羟色胺再摄取抑制剂以来，它并不是一线治疗。由于对耐受性、依赖性和滥用的担忧，澳大利亚不推荐阿普唑仑用于治疗恐慌症。^[7]大多数证据表明，阿普唑仑治疗恐慌症的益处仅持续四到十周。然而，恐慌症患者已经接受了长达八个月的公开治疗，而没有明显的益处损失。^[2]

阿普唑仑被世界生物精神病学联合会 (WFSBP) 推荐用于没有耐受或依赖史的恐慌症难治性病例。^[15]

焦虑症

与抑郁症相关的焦虑对阿普唑仑有反应。临床研究表明，对焦虑症的疗效仅限于 4 个月。^[2]然而，对阿普唑仑抗抑郁特性的研究很差，只评估了它对抑郁症的短期影响。^[16]在一项研究中，一些长期高剂量服用阿普唑仑的人出现了可逆性抑郁症。^[17]在美国，阿普唑仑被FDA批准用于治疗焦虑症（与APA诊断和统计手册DSM-IV-TR 诊断广泛性焦虑症最接近的病症）或短期缓解焦虑症状。在英国，阿普唑仑被推荐用于严重急性焦虑症的短期治疗（2-4周）。^[2]^[18]^[19]

可能的副作用包括：

失控(Disinhibition)^[20]
性慾變化^[21]
黄疸（非常罕見）^[22]
幻觉（罕见）^[23]
口乾（不频繁）^[24]
失調、鬆弛發音^[25]
自殺意念（罕见）^[26]^[27]
尿瀦留（不频繁）^[28]
疹、通氣不足（respiratory depression）、便秘^[29]^[30]
顺行性遗忘症^[31] 及注意集中等問題
睡意(Somnolence)、暈眩（dizziness）、頭重腳輕（lightheadedness）、疲倦、不穩定及受損的运动协调、眩暈（vertigo）^[29]^[30]

異常反應

使用阿普唑仑有可能會發生下面的異常反應：

視覺變化
醉酒感
興奮
侵略^[32]
憤怒、敵意^[20]
震顫（Fasciculations）及手震^[33]
瘋狂（Mania）、躁動（Psychomotor agitation）、肺熱（hyperactivity）、慌張（restlessness）^[34]^[35]^[36]

食品和藥物相互作用

阿普唑崙的代謝主要是通過CYP₃A₄進行^[37]，結合CYP₃A₄临床上，抑製劑諸如西咪替丁、紅黴素、氟西汀、氟伏沙明、伊曲康唑、酮康唑、奈法唑酮（Nefazodone）、丙氧芬（Propoxyphene）、利托那韋（Ritonavir）等可以延緩阿普唑崙的肝清除率，但是這可能導致阿普唑崙在人体内部的過度積纍^[38]，如此很有可能會導致其不良反應更加的惡化^[39]^[40]。

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U.S. National Library of Medicine: Drug Information Portal – Alprazolam （页面存档备份，存于互联网档案馆）
Erowid Alprazolam (Xanax) Research （页面存档备份，存于互联网档案馆）
神經系統-鎮靜、催眠、精神安定劑-Amprazo(柔安) （页面存档备份，存于互联网档案馆）

[1] [1]
Goldberg, Ray. Drugs across the spectrum 6th. Belmont, CA: Wadsworth, Cengage Learning. 2010. ISBN 978-0-495-55793-7. OCLC 429504239.

[dailymed-2] [2]
XANAX- alprazolam tablet. DailyMed. [2022-06-20]. （原始内容存档于2021-01-17）.

[drugs-3] [3]
Alprazolam Monograph for Professionals. Drugs.com. [2022-06-20]. （原始内容存档于2010-12-07）（英语）.

[wiley-4] [4]
Verster, Joris C.; Volkerts, Edmund R. Clinical pharmacology, clinical efficacy, and behavioral toxicity of alprazolam: a review of the literature. CNS drug reviews. 2004, 10 (1) [2022-06-20]. ISSN 1080-563X. PMC 6741717 . PMID 14978513. doi:10.1111/j.1527-3458.2004.tb00003.x. （原始内容存档于2022-06-23）.

[5] [5]
Tampi, Rajesh R. Comprehensive review of psychiatry. Philadelphia, PA: Wolters Kluwer/Lippincott Williams & Wilkins Health. 2008. ISBN 978-0-7817-7176-4. OCLC 191317979.

[6] [6]
Marder, Stephen R.; Pavuluri, Mani N. Principles and practice of psychopharmacotherapy 5th. Philadelphia: Wolters Kluwer Health/Lippincott Williams & Wilkins. 2011. ISBN 1-4511-2502-X. OCLC 703840461.

[sagepub-7] [7]
Moylan, Steven; Giorlando, Francesco; Nordfjærn, Trond; Berk, Michael. The role of alprazolam for the treatment of panic disorder in Australia. The Australian and New Zealand Journal of Psychiatry. 2012-03, 46 (3) [2022-06-20]. ISSN 1440-1614. PMID 22391278. doi:10.1177/0004867411432074. （原始内容存档于2022-04-21）.

[8] [8]
Dodds, Tyler J. Prescribed Benzodiazepines and Suicide Risk: A Review of the Literature. The primary care companion for CNS disorders. 2017-03-02, 19 (2) [2022-06-20]. ISSN 2155-7780. PMID 28257172. doi:10.4088/PCC.16r02037. （原始内容存档于2022-02-16）.

[9] [9]
McCall, W. Vaughn; Benca, Ruth M.; Rosenquist, Peter B.; Riley, Mary Anne; McCloud, Laryssa; Newman, Jill C.; Case, Doug; Rumble, Meredith; Krystal, Andrew D. Hypnotic Medications and Suicide: Risk, Mechanisms, Mitigation, and the FDA. The American Journal of Psychiatry. 2017-01-01, 174 (1) [2022-06-20]. ISSN 1535-7228. PMC 5205566 . PMID 27609243. doi:10.1176/appi.ajp.2016.16030336. （原始内容存档于2022-06-23）.

[10] [10]
Xu, Kevin Y.; Hartz, Sarah M.; Borodovsky, Jacob T.; Bierut, Laura J.; Grucza, Richard A. Association Between Benzodiazepine Use With or Without Opioid Use and All-Cause Mortality in the United States, 1999-2015. JAMA network open. 2020-12-01, 3 (12) [2022-06-20]. ISSN 2574-3805. PMC 7726637 . PMID 33295972. doi:10.1001/jamanetworkopen.2020.28557. （原始内容存档于2022-06-25）.

[11] [11]
Fischer, János; Ganellin, C. R. Analogue-based drug discovery. Weinheim: Wiley-VCH. 2006: 536 [2022-06-20]. ISBN 978-3-527-60749-5. OCLC 77601762. （原始内容存档于2020-05-30）.

[12] [12]
Ait-Daoud, Nassima; Hamby, Allan Scott; Sharma, Sana; Blevins, Derek. A Review of Alprazolam Use, Misuse, and Withdrawal. Journal of Addiction Medicine. 2018 Jan/Feb, 12 (1) [2022-06-20]. ISSN 1935-3227. PMC 5846112 . PMID 28777203. doi:10.1097/ADM.0000000000000350. （原始内容存档于2022-07-01）. 请检查|date=中的日期值 (帮助)

[13] [13]
The Top 300 of 2019. ClinCalc. [2022-06-20]. （原始内容存档于2020-03-18）.

[14] [14]
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恐慌症

焦虑症

異常反應

食品和藥物相互作用

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阿普唑仑

恐慌症

焦虑症

異常反應

食品和藥物相互作用

Wikiwand in your browser!

医疗用途

副作用

參考資料

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