阿普唑仑
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阿普唑仑 臨床資料 读音 或 商品名 Xanax, Xanor, Niravam, others AHFS /Drugs.com Monograph MedlinePlus a684001 核准狀況
懷孕分級 依賴性 High 给药途径 口服 藥物類別 Benzodiazepine 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 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
8-Chloro-1-methyl-6-phenyl-4H -[1,2,4]triazolo[4,3-a] [1,4]benzodiazepine
CAS号 28981-97-7 Y PubChem CID IUPHAR/BPS DrugBank ChemSpider UNII KEGG ChEBI ChEMBL CompTox Dashboard (EPA ) ECHA InfoCard 100.044.849 化学信息 化学式 C 17 H 13 Cl N 4 摩尔质量 308.77 g·mol−1 3D模型(JSmol )
Cc1nnc2n1-c1ccc(Cl)cc1C(c1ccccc1)=NC2
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
Y Key:VREFGVBLTWBCJP-UHFFFAOYSA-N
Y
阿普唑仑 (英語: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]
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
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]
副作用
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
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
阿普唑崙的代謝主要是通過CYP3 A4 進行[37] ,結合CYP3 A4 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] 。
參考資料
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外部連結
迷幻药物 5-HT2A R 激動劑
1-甲基-5-甲氧基二异丙基色胺
2,N,N-三甲基色胺
4,5-DHP-AMT
4,5-DHP-DMT
4-AcO-DALT
4-AcO-DET
4-AcO-DiPT
4-AcO-DMT
4-AcO-DPT
4-AcO-MiPT
4-HO-5-MeO-DMT
4-羟基-N,N-二丁基色胺
4-羟基-N,N-二丙基色胺
4-羟基-N-甲基-N-乙基色胺
4-HO-MPMI
4-羟基-N-甲基-N-丙基色胺
4,N,N-三甲基色胺
4-PrO-DMT
5,6-diBr-DMT
5-AcO-DMT
5-溴-N,N-二甲基色胺
5-Me-MIPT
5-MeO-2,N ,N -TMT
5-MeO-4,N ,N -TMT
5-MeO-α,N,N-TMT
5-MeO-α-ET
5-MeO-α-MT
5-MeO-DALT
5-MeO-DET
5-甲氧基二异丙基色胺
5-甲氧基二甲基色胺
5-MeO-DPT
5-MeO-EiPT
5-MeO-MET
5-MeO-MiPT
5-MeO-MPMI
5,N,N-TMT
7,N,N-三甲基色胺
α-ET
α-MT
α,N,N-三甲基色胺
Aeruginascin
Baeocystin
蟾毒色胺
DALT
DBT
DCPT
DET
DIPT
DMT
DPT
EiPT
4-羟二乙基色胺
4-磷酸二乙基色胺
4-羟二异丙基色胺
MET
Miprocin
MiPT
Norbaeocystin
PiPT
脱磷酸裸盖菇素
裸盖菇素
其它藥物
解离性药物 NMDAR 拮抗劑
致谵妄药 mAChR 拮抗劑 其它相關藥物
中华人民共和国《
精神药品 品种目录》(2013年版)
第一类 第二类