阿普唑侖

阿普唑侖INN:alprazolam),商品名贊安諾Xanax),是三唑並苯二氮䓬類中的中效速效鎮靜劑,它是與三唑環融合的苯二氮䓬類 (BZD)[1]。它最常用於焦慮症的短期管理,特別是恐慌症廣泛性焦慮症 (GAD)[2]。其他用途包括治療化療引起的噁心,以及其他治療方法[3]。GAD 改善一般在一周內發生[4][5]。阿普唑侖通常口服[3]

阿普唑侖
臨床資料
讀音/ælˈpræzəlæm//ælˈprzəlæm/
商品名英語Drug nomenclatureXanax, Xanor, Niravam, others
AHFS/Drugs.comMonograph
MedlinePlusa684001
核准狀況
懷孕分級
  • : C
依賴性High
給藥途徑口服
藥物類別英語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%
藥物代謝代謝,via cytochrome P450 3A4
代謝產物Alpha-hydroxyalprazolam, 4-hydroxyalprazolam, beta-hydroxyalprazolam
藥效起始時間英語Onset of action20~60分鐘
生物半衰期完全釋放:11~13小時
緩釋:11~16小時
作用時間完全釋放:6小時
緩釋:11.3小時
排泄途徑Kidney
識別資訊
  • 8-Chloro-1-methyl-6-phenyl-4H-[1,2,4]triazolo[4,3-a] [1,4]benzodiazepine
CAS號28981-97-7  checkY
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard英語CompTox Chemicals Dashboard (EPA)
ECHA InfoCard100.044.849 編輯維基數據鏈接
化學資訊
化學式C17H13ClN4
摩爾質量308.77 g·mol−1
3D模型(JSmol英語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 checkY
  • Key:VREFGVBLTWBCJP-UHFFFAOYSA-N checkY

常見的副作用包括嗜睡、抑鬱、頭痛、感覺疲倦、口乾和記憶力問題[3]一些鎮靜和疲倦可能會在幾天內得到改善。[6]由於擔心誤用,一些人不推薦阿普唑侖作為恐慌症的初始治療。[7]如果突然減少使用,可能會出現戒斷或反彈症狀;[3]可能需要在數周或數月內逐漸減少劑量[4]其他罕見的風險包括自殺[8][9]和全因死亡風險增加兩倍。[10]阿普唑侖與其他苯二氮䓬類藥物一樣,通過GABAA受體起作用。[3]

阿普唑侖於1971年獲得專利,並於1981年在美國獲准用於醫療用途。[3][11]阿普唑侖是附表IV受控物質,是一種常見的濫用藥物。[12]它可作為學名藥使用。[2]2019年,它是美國第41位最常用的處方藥,有超過1700萬張處方。[13][14]

醫療用途

阿普唑侖主要用於短期治療焦慮症、恐慌症和化療引起的噁心[4]阿普唑侖適用於治療成人廣泛性焦慮症和恐慌症伴或不伴廣場恐懼症[2]FDA標籤建議醫生應定期重新評估藥物的有效性。[2]

恐慌症

阿普唑侖可有效緩解中度至重度焦慮驚恐發作[2]然而,自從開發出選擇性5-羥色胺再攝取抑制劑以來,它並不是一線治療。由於對耐受性、依賴性和濫用的擔憂,澳大利亞不推薦阿普唑侖用於治療恐慌症。[7]大多數證據表明,阿普唑侖治療恐慌症的益處僅持續四到十周。 然而,恐慌症患者已經接受了長達八個月的公開治療,而沒有明顯的益處損失。[2]

阿普唑侖被世界生物精神病學聯合會 (WFSBP) 推薦用於沒有耐受依賴史的恐慌症難治性病例。[15]

焦慮症

與抑鬱症相關的焦慮對阿普唑侖有反應。臨床研究表明,對焦慮症的療效僅限於 4 個月。[2]然而,對阿普唑侖抗抑鬱特性的研究很差,只評估了它對抑鬱症的短期影響。[16]在一項研究中,一些長期高劑量服用阿普唑侖的人出現了可逆性抑鬱症。[17]在美國,阿普唑侖被FDA批准用於治療焦慮症(與APA診斷和統計手冊DSM-IV-TR 診斷廣泛性焦慮症最接近的病症)或短期緩解焦慮症狀。在英國,阿普唑侖被推薦用於嚴重急性焦慮症的短期治療(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.

使用阿普唑侖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CYP3A4進行[37],結合CYP3A4臨床上,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體內部的過度積纍[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