阿普唑仑

阿普唑仑(商品名:Xanax)是三唑并苯二氮卓类中的中效速效镇静剂,它是与三唑环融合的苯二氮卓类 (BZD)。[1]它最常用于焦虑症的短期管理,特别是恐慌症广泛性焦虑症 (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]

阿普唑仑
Alprazolam structure.svg
Alprazolam ball-and-stick model.png
臨床資料
读音/ælˈpræzəlæm/ or /ælˈprzəlæm/
商品名英语Drug nomenclatureXanax, Xanor, Niravam, others
AHFS英语American Society of Health-System Pharmacists/Drugs.comMonograph
MedlinePlusa684001
核准狀況
懷孕分級
  • : C
依賴性High
给药途径口服
藥物類別英语Drug classBenzodiazepine
ATC碼
法律規範狀態
法律規範
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 action20~60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
CAS号28981-97-7  ✓
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard100.044.849 編輯維基數據鏈接
化学信息
化学式C17H13ClN4
摩尔质量308.77 g·mol−1
3D model (JSmol)
  (verify)

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卓类药物一样,通过GABAA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]

医疗用途编辑

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]

恐慌症编辑

阿普唑仑可有效缓解中度至重度焦虑惊恐发作[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) 推荐用于没有耐受依赖史的恐慌症难治性病例。[15]

焦虑症编辑

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]

副作用编辑

 
Xanax(阿普唑崙)2毫克三片連狀錠劑

可能的副作用包括:

異常反應编辑

 
阿普唑崙的副作用.

使用阿普唑仑有可能會發生下面的異常反應:

食品和藥物相互作用编辑

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]

參考資料编辑

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外部連結编辑

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