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阿普唑仑

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阿普唑仑
Alprazolam structure.svg
Alprazolam ball-and-stick model.png
系统(IUPAC)命名名称
8-Chloro-1-methyl-6-phenyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine
临床数据
商品名Xanax
Drugs.comMonograph
MedlinePlusa684001
妊娠分级
  • US: D (证据表明有风险)
依赖性
给药途径口服,舌下
合法狀態
合法状态
药代动力学数据
生物利用度80–90%
代谢肝脏, 通过CYP3A4
生物半衰期普释片: 11.2 小时,[1]
缓释片: 10.7–15.8 小时[2]
排泄肾脏
识别信息
CAS注册号28981-97-7 ✓
ATC代码N05BA12
PubChemCID 2118
IUPHAR/BPS英语IUPHAR/BPS7111
DrugBankDB00404 ✓
ChemSpider2034 ✓
UNIIYU55MQ3IZY ✓
KEGGD00225 ✓
ChEBICHEBI:2611 ✓
ChEMBL英语ChEMBLCHEMBL661 ✓
化学信息
化学式C17H13ClN4
摩尔质量308.765
Alprazolam synthesis.svg

阿普唑侖拉丁語Alprazolam),又名佳静安定,欧美部分国家商品名赞安诺Xanax),是一種短效的苯二氮䓬類藥物[3]。常見商品名稱為贊安諾(英語:Xanax)。最常用於焦慮症,尤其會用於短期治療恐慌症廣泛性焦慮症(GAD)[4];另有用途為與其他藥物並用於治療化療引起的噁心症狀英语Chemotherapy-induced nausea and vomiting[5]。廣泛性焦慮症通常在一週內就能緩和[6][7]。 本品可經口服給藥[5]

常見的副作用有嗜睡、憂鬱、頭痛、感到疲倦、口乾和記性變差[5];不過開始服藥幾天後,部分鎮靜和疲倦問題或許就會有所改善[8]。由於擔心可能引發藥物濫用,不建議某些人使用本品作為恐慌症的初始治療[9]。驟然降低用量有可能帶來藥物戒斷病況反彈英语rebound symptoms的症狀。其他罕見風險為自殺,其肇因或許是失去抑制作用英语loss of inhibition[10];用藥者可能需要在數週或數月內逐漸降低劑量[6]。如同其他苯二氮䓬類藥物,本品也是透過GABAA受體發揮作用[5]

1971 年,阿普唑侖取得專利,1981年,在美國核准作為醫療用途[5][11]。本品是一種第四級管制藥物英语Schedule IV,也是常見的濫用藥物[12][13]。市面上有學名藥流通[14]。截至 2018 年,在美國單劑批發價低於 0.03 美元[15]。2016年,本品名列美國處方藥排名的第十九名,處方數量超過 2700 萬[16]

在中国大陆销售的阿普唑仑片

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[34],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[35],如此很有可能會導致其不良反應更加的惡化[36][37]

參考資料[编辑]

  1. ^ Xanax (Alprazolam) Clinical Pharmacology – Prescription Drugs and Medications. RxList. First DataBank. July 2008. 
  2. ^ Xanax XR (Alprazolam) Clinical Pharmacology – Prescription Drugs and Medications. RxList. First DataBank. July 2008. 
  3. ^ Goldberg R. Drugs Across the Spectrum. Cengage Learning. 2009: 195. ISBN 9781111782009. 
  4. ^ Alprazolam Tablets, USP. dailymed.nlm.nih.gov. July 2017 [25 October 2018]. 
  5. ^ 5.0 5.1 5.2 5.3 5.4 American Society of Health-System Pharmacists. Alprazolam Monograph for Professionals. Drugs.com. 13 November 2017 [25 October 2018]. 
  6. ^ 6.0 6.1 Verster JC, Volkerts ER. Clinical pharmacology, clinical efficacy, and behavioral toxicity of alprazolam: a review of the literature. CNS Drug Reviews. 2004, 10 (1): 45–76. PMC 6741717. PMID 14978513. doi:10.1111/j.1527-3458.2004.tb00003.x. 
  7. ^ Tampi RR, Muralee S, Weder ND, Penland H (编). Comprehensive Review of Psychiatry. Philadelphia, PA: Wolters Kluwer/ Lippincott Williams & Wilkins Health. 2008: 226. ISBN 978-0-7817-7176-4. 
  8. ^ Tampi RR, Muralee S, Weder ND, Penland H (编). Comprehensive Review of Psychiatry. Philadelphia, PA: Wolters Kluwer/ Lippincott Williams & Wilkins Health. 2008: 226. ISBN 978-0-7817-7176-4. 
  9. ^ Moylan S, Giorlando F, Nordfjærn T, Berk M. The role of alprazolam for the treatment of panic disorder in Australia (PDF). The Australian and New Zealand Journal of Psychiatry. March 2012, 46 (3): 212–24. PMID 22391278. doi:10.1177/0004867411432074. 
  10. ^ Dodds TJ. Prescribed Benzodiazepines and Suicide Risk: A Review of the Literature. The Primary Care Companion for CNS Disorders. March 2017, 19 (2). PMID 28257172. doi:10.4088/PCC.16r02037.  已忽略未知参数|doi-access= (帮助)
  11. ^ Fischer, Jnos; Ganellin, C. Robin. Analogue-based Drug Discovery. John Wiley & Sons. 2006: 536. ISBN 9783527607495 (英语). 
  12. ^ Ait-Daoud N, Hamby AS, Sharma S, Blevins D. A Review of Alprazolam Use, Misuse, and Withdrawal. Journal of Addiction Medicine. 2018, 12 (1): 4–10. PMC 5846112. PMID 28777203. doi:10.1097/ADM.0000000000000350. 
  13. ^ Malamed SF. Sedation: A Guide to Patient Management. Elsevier Health Sciences. 2009: 105. ISBN 978-0323075961. 
  14. ^ In Pictures: The Most Popular Prescription Drugs. Forbes. [16 June 2015]. 
  15. ^ NADAC as of 2018-10-24. Centers for Medicare and Medicaid Services. [26 October 2018]. 
  16. ^ The Top 300 of 2019. clincalc.com. [22 December 2018]. 
  17. ^ 17.0 17.1 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 (法语). 
  18. ^ 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). 
  19. ^ Noyes, R.; DuPont, R. L.; Pecknold, J. C.; Rifkin, A.; Rubin, R. T.; Swinson, R. P.; 等. 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. PMID 3358644. doi:10.1001/archpsyc.1988.01800290037005. 
  20. ^ Complete Alprazolam Information. Drugs.com. [2 August 2007]. (原始内容存档于5 August 2007). 
  21. ^ Elie, R.; Lamontagne, Y. Alprazolam and Diazepam in the Treatment of Generalized Anxiety. Journal of Clinical Psychopharmacology. 1984, 4 (3): 125–129. PMID 6145726. doi:10.1097/00004714-198406000-00002. 
  22. ^ Cassano, G. B.; Toni, C.; Petracca, A.; Deltito, J.; Benkert, O.; Curtis, G.; 等. Adverse Effects Associated with the Short-term Treatment of Panic Disorder with Imipramine, Alprazolam or Placebo. European Neuropsychopharmacology. 1994, 4 (1): 47–53. PMID 8204996. doi:10.1016/0924-977X(94)90314-X. 
  23. ^ Hori, A. Pharmacotherapy for Personality Disorders. Psychiatry and Clinical Neurosciences. 1998, 52 (1): 13–19. PMID 9682928. doi:10.1111/j.1440-1819.1998.tb00967.x. 
  24. ^ 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. 
  25. ^ Alprazolam Side Effects, Interactions and Information. Drugs.com. [2 August 2007]. (原始内容存档于19 August 2007). 
  26. ^ 26.0 26.1 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. 
  27. ^ 27.0 27.1 Alprazolam – Complete Medical Information Regarding This Treatment of Anxiety Disorders. Medicinenet.com. MedicineNet. [2 August 2007]. 
  28. ^ 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. 
  29. ^ Rapaport, M.; Braff, D. L. Alprazolam and Hostility. American Journal of Psychiatry. 1985, 142 (1): 146. PMID 2857070. 
  30. ^ 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. PMID 17363337. doi:10.1016/j.autneu.2007.01.007. 
  31. ^ 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. 
  32. ^ 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. 
  33. ^ Reddy, J.; Khanna, S.; Anand, U.; Banerjee, A. Alprazolam-Induced Hypomania. Australia and New Zealand Journal of Psychiatry. 1996, 30 (4): 550–552. PMID 8887708. doi:10.3109/00048679609065031. 
  34. ^ Otani, K. Cytochrome P450 3A4 and Benzodiazepines. Seishin Shinkeigaku Zasshi. 2003, 105 (5): 631–642. PMID 12875231 (日语). 
  35. ^ 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. PMID 10668858. doi:10.2165/00003088-200038010-00003. 
  36. ^ Greenblatt, D. J.; Wright, C. E. Clinical Pharmacokinetics of Alprazolam. Therapeutic Implications. Clinical Pharmacokinetics. 1993, 24 (6): 453–471. PMID 8513649. doi:10.2165/00003088-199324060-00003. 
  37. ^ Wang, J. S.; Chase, C. L. Pharmacokinetics and Drug Interactions of the Sedative Hypnotics (PDF). Psychopharmacological Bulletin. 2003, 37 (1): 10–29. PMID 14561946. doi:10.1007/BF01990373. (原始内容 (PDF)存档于2007-07-09). 

外部連結[编辑]

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