阿普唑仑

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阿普唑仑
IUPAC命名
8-chloro-1-methyl-6-phenyl-4H-
[1,2,4]triazolo[4,3-α][1,4]benzodiazepine
中文名:1-甲基-6-苯基-8-氯-1H-
[1,2,4]三唑[4,3-α][1,4]苯并二氮杂䓬
識別
CAS號 28981-97-7
ATC編碼 N05BA12
PubChem CID 2118
DrugBank APRD00280
ChemSpider 2034
化學性質
化學式 C17H13ClN4 
分子量 308.765
SMILES 搜尋Jmol 3D模型eMoleculesPubChem
药代动力学性質
生物利用度 80-90%
代謝 肝脏,通过细胞色素P4503A4
半衰期 立即釋放: 11.2小時;[1] 延緩釋放: 10.7-15.8小時[2]
排泄
治療考量
懷孕分級 D ()
合法狀態 管制藥物 (S8) () POM () 附錄四 ()
依賴傾向 高度
途徑 口服、舌下含服

阿普唑仑(Alprazolam、商品名Xanax),又名佳静安定,与氯硝西泮同为常见的精神药物。

此药只有片剂,0.4mg/片,临床一般用于抗焦虑催眠。该药的药效与氯硝西泮的镇静作用不同,有一定改善情绪的作用,因而"佳静安定"多用于「抑郁伴有失眠或焦虑」的病人,"氯硝西泮"多用于「兴奋躁动」的精神病人。

不良反應[编辑]

Xanax(阿普唑崙)2公絲三片連狀錠劑

過敏反應不太可能發生。唯一常見的副作用是開始治療時嗜睡症狀。

可能的副作用包括:

異常反應[编辑]

阿普唑崙的副作用.

雖然是不尋常,下面的異常反應已被證實會發生:

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。[20] 結合CYP3A4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)等延緩阿普唑崙的肝清除率,這可能導致阿普唑崙的過度積纍。[21] 如此能會導致其不良反應更加的惡化。[22][23]

化學程序[编辑]

Alprazolam synthesis.svg

商標名稱[编辑]

  • Amprazo(柔安)(淺粉紅色橢圓形)錠劑0.5公絲,"中國化學製藥股份有限公司". Amprazo 0.5mg(Alprazolam) tablet。

參考資料[编辑]

  1. ^ First DataBank. Xanax (Alprazolam) clinical pharmacology - prescription drugs and medications at RxList. RxList. 2008.July. 
  2. ^ First DataBank. Xanax XR (Alprazolam) clinical pharmacology - prescription drugs and medications at RxList. RxList. 2008.July. 
  3. ^ 3.0 3.1 Michel, L.; Lang, J. P. Benzodiazépines et passage à l'acte criminel [Benzodiazepines and Forensic Aspects]. Encephale. 2003, 29 (6): 479–485 [9 April 2013]. PMID 15029082 (French). 
  4. ^ ALPRAZOLAM – ORAL (Xanax) side effects, medical uses, and drug interactions. Medicinenet.com. [2 August 2007](原始内容存档于25 August 2007). 
  5. ^ Noyes, R.; DuPont, R. L.; Pecknold, J. C.; Rifkin, A.; Rubin, R. T.; Swinson, R. P. et al. Alprazolam in Panic Disorder and Agoraphobia: Results from a Multicenter Trial. II. Patient Acceptance, Side Effects, and Safety. Archives of General Psychiatry. 1988, 45 (5): 423–428. doi:10.1001/archpsyc.1988.01800290037005. PMID 3358644. 
  6. ^ Complete Alprazolam Information. Drugs.com. [2 August 2007](原始内容存档于5 August 2007). 
  7. ^ Elie, R.; Lamontagne, Y. Alprazolam and Diazepam in the Treatment of Generalized Anxiety. Journal of Clinical Psychopharmacology. 1984, 4 (3): 125–129. doi:10.1097/00004714-198406000-00002. PMID 6145726. 
  8. ^ Cassano, G. B.; Toni, C.; Petracca, A.; Deltito, J.; Benkert, O.; Curtis, G. et al. Adverse Effects Associated with the Short-term Treatment of Panic Disorder with Imipramine, Alprazolam or Placebo. European Neuropsychopharmacology. 1994, 4 (1): 47–53. doi:10.1016/0924-977X(94)90314-X. PMID 8204996. 
  9. ^ Hori, A. Pharmacotherapy for Personality Disorders. Psychiatry and Clinical Neurosciences. 1998, 52 (1): 13–19. doi:10.1111/j.1440-1819.1998.tb00967.x. PMID 9682928. 
  10. ^ Kravitz, H. M.; Fawcett, J.; Newman, A. J. Alprazolam and Depression: A Review of Risks and Benefits. Journal of Clinical Psychiatry. 1993, 54 (Supplement): 78–84; discussion 85. PMID 8262892. 
  11. ^ Alprazolam Side Effects, Interactions and Information. Drugs.com. [2 August 2007](原始内容存档于19 August 2007). 
  12. ^ 12.0 12.1 Rawson, N. S.; Rawson, M. J. Acute Adverse Event Signalling Scheme Using the Saskatchewan Administrative Health Care Utilization Datafiles: Results for Two Benzodiazepines. Canadian Journal of Clinical Pharmacology. 1999, 6 (3): 159–166. PMID 10495368. 
  13. ^ 13.0 13.1 Alprazolam – Complete Medical Information Regarding This Treatment of Anxiety Disorders. Medicinenet.com. MedicineNet. [2 August 2007]. 
  14. ^ Barbee, J. G. Memory, Benzodiazepines, and Anxiety: Integration of Theoretical and Clinical Perspectives. The Journal of Clinical Psychiatry. 1993, 54 (Suppl): 86–97; discussion 98–101. PMID 8262893. 
  15. ^ Rapaport, M.; Braff, D. L. Alprazolam and Hostility. American Journal of Psychiatry. 1985, 142 (1): 146. PMID 2857070. 
  16. ^ Béchir, M.; Schwegler, K.; Chenevard, R.; Binggeli, C.; Caduff, C.; Büchi, S. 等. Anxiolytic Therapy with Alprazolam Increases Muscle Sympathetic Activity in Patients with Panic Disorders. Autonomic Neuroscience. 2007, 134 (1–2): 69–73. doi:10.1016/j.autneu.2007.01.007. PMID 17363337. 
  17. ^ Arana, G. W.; Pearlman, C.; Shader, R. I. Alprazolam-Induced Mania: Two Clinical Cases. American Journal of Psychiatry. 1985, 142 (3): 368–369. PMID 2857534. 
  18. ^ Strahan, A.; Rosenthal, J.; Kaswan, M.; Winston, A. Three Case Reports of Acute Paroxysmal Excitement Associated with Alprazolam Treatment. American Journal of Psychiatry. 1985, 142 (7): 859–861. PMID 2861755. 
  19. ^ Reddy, J.; Khanna, S.; Anand, U.; Banerjee, A. Alprazolam-Induced Hypomania. Australia and New Zealand Journal of Psychiatry. 1996, 30 (4): 550–552. doi:10.3109/00048679609065031. PMID 8887708. 
  20. ^ Otani, K. Cytochrome P450 3A4 and Benzodiazepines. Seishin Shinkeigaku Zasshi. 2003, 105 (5): 631–642. PMID 12875231 (Japanese). 
  21. ^ Dresser, G. K.; Spence, J. D.; Bailey, D. G. Pharmacokinetic-Pharmacodynamic Consequences and Clinical Relevance of Cytochrome P450 3A4 Inhibition. Clinical Pharmacokinetics. 2000, 38 (1): 41–57. doi:10.2165/00003088-200038010-00003. PMID 10668858. 
  22. ^ Greenblatt, D. J.; Wright, C. E. Clinical Pharmacokinetics of Alprazolam. Therapeutic Implications. Clinical Pharmacokinetics. 1993, 24 (6): 453–471. doi:10.2165/00003088-199324060-00003. PMID 8513649. 
  23. ^ Wang, J. S.; Chase, C. L. Pharmacokinetics and Drug Interactions of the Sedative Hypnotics (PDF). Psychopharmacological Bulletin. 2003, 37 (1): 10–29. doi:10.1007/BF01990373. PMID 14561946. (原始内容存档于2007-07-09). 

外部鏈接[编辑]