阿普唑仑
此條目可参照英語維基百科相應條目来扩充。 |
臨床資料 | |
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商品名 | Xanax |
AHFS/Drugs.com | Monograph |
MedlinePlus | a684001 |
依賴性 | 高 |
给药途径 | 口服,舌下 |
ATC碼 | |
法律規範狀態 | |
法律規範 |
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藥物動力學數據 | |
生物利用度 | 80–90% |
药物代谢 | 肝脏, 通过CYP3A4酶 |
生物半衰期 | 普释片: 11.2 小时,[1] 缓释片: 10.7–15.8 小时[2] |
排泄途徑 | 肾脏 |
识别信息 | |
| |
CAS号 | 28981-97-7 |
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 | C17H13ClN4 |
摩尔质量 | 308.765 |
3D模型(JSmol) | |
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阿普唑侖(英語:Alprazolam),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與廣泛性焦慮症(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[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或病況反彈的症狀。其他罕見風險為自殺,其肇因或許是失去抑制作用[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,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]。
副作用
可能的副作用包括:
- 失控(Disinhibition)[17]
- 性慾變化[18]
- 黄疸(非常罕見)[19]
- 幻觉(罕见)[20]
- 口乾(不频繁)[21]
- 失調、鬆弛發音[22]
- 自殺意念(罕见)[23][24]
- 尿瀦留(不频繁)[25]
- 疹、通氣不足(respiratory depression)、便秘[26][27]
- 顺行性遗忘症[28] 及注意集中等問題
- 睡意(Somnolence)、暈眩(dizziness)、頭重腳輕(lightheadedness)、疲倦、不穩定及受損的运动协调、眩暈(vertigo)[26][27]
異常反應
使用阿普唑仑有可能會發生下面的異常反應:
- 視覺變化
- 醉酒感
- 興奮
- 打电话、网络聊天
- 驾驶车辆
- 侵略[29]
- 憤怒、敵意[17]
- 震顫(Fasciculations)及手震[30]
- 瘋狂(Mania)、躁動(Psychomotor agitation)、肺熱(hyperactivity)、慌張(restlessness)[31][32][33]
食品和藥物相互作用
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
- ^ Xanax (Alprazolam) Clinical Pharmacology – Prescription Drugs and Medications. RxList. First DataBank. July 2008.
- ^ Xanax XR (Alprazolam) Clinical Pharmacology – Prescription Drugs and Medications. RxList. First DataBank. July 2008.
- ^ Goldberg R. Drugs Across the Spectrum. Cengage Learning. 2009: 195. ISBN 9781111782009.
- ^ Alprazolam Tablets, USP. dailymed.nlm.nih.gov. July 2017 [25 October 2018].
- ^ 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].
- ^ 6.0 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.
- ^ 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.
- ^ 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.
- ^ 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.
- ^ 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 .
- ^ Fischer, Jnos; Ganellin, C. Robin. Analogue-based Drug Discovery. John Wiley & Sons. 2006: 536. ISBN 9783527607495 (英语).
- ^ 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.
- ^ Malamed SF. Sedation: A Guide to Patient Management. Elsevier Health Sciences. 2009: 105. ISBN 978-0323075961.
- ^ In Pictures: The Most Popular Prescription Drugs. Forbes. [16 June 2015].
- ^ NADAC as of 2018-10-24. Centers for Medicare and Medicaid Services. [26 October 2018].
- ^ The Top 300 of 2019. clincalc.com. [22 December 2018].
- ^ 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).
- ^ 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).
- ^ 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. PMID 3358644. doi:10.1001/archpsyc.1988.01800290037005.
- ^ Complete Alprazolam Information. Drugs.com. [2 August 2007]. (原始内容存档于5 August 2007).
- ^ 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.
- ^ 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. PMID 8204996. doi:10.1016/0924-977X(94)90314-X.
- ^ 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.
- ^ 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.
- ^ Alprazolam Side Effects, Interactions and Information. Drugs.com. [2 August 2007]. (原始内容存档于19 August 2007).
- ^ 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.
- ^ 27.0 27.1 Alprazolam – Complete Medical Information Regarding This Treatment of Anxiety Disorders. Medicinenet.com. MedicineNet. [2 August 2007].
- ^ 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.
- ^ Rapaport, M.; Braff, D. L. Alprazolam and Hostility. American Journal of Psychiatry. 1985, 142 (1): 146. PMID 2857070.
- ^ Béchir, M.; Schwegler, K.; Chenevard, R.; Binggeli, C.; Caduff, C.; Büchi, S.; et al. 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.
- ^ 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.
- ^ 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.
- ^ 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.
- ^ Otani, K. Cytochrome P450 3A4 and Benzodiazepines. Seishin Shinkeigaku Zasshi. 2003, 105 (5): 631–642. PMID 12875231 (日语).
- ^ 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.
- ^ 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.
- ^ 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).