阿普唑仑

阿普唑仑
臨床資料
商品名（英语：Drug nomenclature）	Xanax
AHFS/Drugs.com	Monograph
MedlinePlus	a684001
依賴性	高
给药途径	口服，舌下
ATC碼	N05BA12 (WHO) ;
法律規範狀態
法律規範	澳：受管控（S8）; 加：Schedule IV; 英：Class C; 美：附表IV; UN：《精神药物公约》附表四; 第二类精神药品（中国大陆）;
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,; 缓释片: 10.7–15.8 小时
排泄途徑	肾脏
识别信息
	IUPAC命名法 8-Chloro-1-methyl-6-phenyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine; ;
CAS号	28981-97-7
PubChem CID	2118;
IUPHAR/BPS	7111;
DrugBank	DB00404 ;
ChemSpider	2034 ;
UNII	YU55MQ3IZY;
KEGG	D00225 ;
ChEBI	CHEBI:2611 ;
ChEMBL	ChEMBL661 ;
CompTox Dashboard（英语：CompTox Chemicals Dashboard） (EPA)	DTXSID4022577 ;
ECHA InfoCard	100.044.849
化学信息
化学式	C17H13ClN4
摩尔质量	308.765
3D模型（JSmol（英语：JSmol））	交互式图像;
	SMILES ClC1=CC2=C(C=C1)N3C(C)=NN=C3CN=C2C4=CC=CC=C4;
	InChI 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 ; Key:VREFGVBLTWBCJP-UHFFFAOYSA-N ;

阿普唑仑（Alprazolam）又名佳静安定，欧美部分国家商品名为赞安诺（Xanax）。长期服用会导致成瘾。此药在中国通常为0.4mg/片的片剂，临床一般用于抗焦虑和催眠。

与氯硝西泮的镇静作用不同，该药的药效镇静的同时又有一定改善情绪的作用，因而阿普唑仑多用于抑郁伴有失眠或焦虑的患者，而氯硝西泮多用于伴有兴奋、躁动的精神疾病患者。

副作用

可能的副作用包括：

失控(Disinhibition)^[3]
性慾變化^[4]
黄疸（非常罕見）^[5]
幻觉（罕见）^[6]
口乾（不频繁）^[7]
失調、鬆弛發音^[8]
自殺意念（罕见）^[9]^[10]
尿瀦留（不频繁）^[11]
疹、通氣不足（respiratory depression）、便秘^[12]^[13]
顺行性遗忘症^[14] 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）^[12]^[13]

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^[15]
憤怒、敵意^[3]
震顫（Fasciculations）及手震^[16]
瘋狂（Mania）、躁動（Psychomotor agitation）、肺熱（hyperactivity）、慌張（restlessness）^[17]^[18]^[19]

食品和藥物相互作用

阿普唑崙的代謝主要是通過CYP₃A₄進行^[20]，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^[21]，如此很有可能會導致其不良反應更加的惡化^[22]^[23]。

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.
^ ^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 （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）.
^ ^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.
^ ^13.0 ^13.1 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）.

外部連結

[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.

[Michel_L,_Lang_JP_2003_479–85-3] 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 （法语）.

[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. PMID 3358644. doi:10.1001/archpsyc.1988.01800290037005.

[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. PMID 6145726. doi:10.1097/00004714-198406000-00002.

[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. PMID 8204996. doi:10.1016/0924-977X(94)90314-X.

[hori-9] 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.

[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.

[ase-11] Alprazolam Side Effects, Interactions and Information. Drugs.com. [2 August 2007]. （原始内容存档于19 August 2007）.

[drftb-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.

[acmirttoadom-13] 13.0 ^13.1 Alprazolam – Complete Medical Information Regarding This Treatment of Anxiety Disorders. Medicinenet.com. MedicineNet. [2 August 2007].

[Barbee95-14] 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.; 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.

[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. PMID 8887708. doi:10.3109/00048679609065031.

[Otani-2003-20] Otani, K. Cytochrome P450 3A4 and Benzodiazepines. Seishin Shinkeigaku Zasshi. 2003, 105 (5): 631–642. PMID 12875231 （日语）.

[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. PMID 10668858. doi:10.2165/00003088-200038010-00003.

[cpoati-22] 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.

[23] 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）.

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查论编苯二氮䓬类药物
1,4-苯二氮䓬类	2-氧代夸西泮 3-羟基芬纳西泮溴西泮 BMS-906024 * 卡马西泮卡布西泮甲氨二氮䓬西那西泮西诺西泮氯硝西泮 Cloniprazepam 氯拉䓬酸环丙西泮地洛西泮地莫西泮去甲基氟硝西泮地伐西匹 * 地西泮地克西泮 Difludiazepam（英语：Difludiazepam）度氟西泮依法西泮乙卡氟特地䓬乙酯氯氟䓬乙酯氟溴西泮氟乙西泮氟地西泮氟硝西泮氟西泮氟替马西泮氟托西泮膦西泮吉达西泮哈拉西泮伊氯西泮伊拉西平凯他西平凯他唑仑劳拉西泮氯甲西泮鲁夫拉朵 * 甲氯西泮美达西泮甲硝西泮美他西泮莫曲西泮 N-去烷基氟西泮硝氟西泮硝甲西泮尼特西泮硝西泮氯䓬酸去甲西泮诺替西泮奥沙西泮芬那西泮匹那西泮匹伏西泮普拉西泮丙氟西泮夸西泮 QH-II-66 瑞氯西泮 RO4491533 * Ro05-4082 Ro5-4864 * Ro07-5220 Ro07-9749 Ro20-8065 Ro20-8552 SH-I-048A 硫西泮替马西泮四氢西泮替氟朵 * 替美洛坦甲磺西泮三氟去甲西泮妥氯西泮乌达西泮
1,5-苯二氮䓬类	阿芬达占氯巴占 CP-1414S 洛芬达占三氟巴占
2,3-苯二氮䓬类 *	吉立索泮 GYKI-52466 GYKI-52895 奈立索泮他仑帕奈托非索泮
三唑并苯二氮䓬类	阿地唑仑阿普唑仑巴洛伐普坦溴唑仑氯硝唑仑艾司唑侖氟阿地唑仑氟阿普唑仑氟溴唑仑氟硝唑仑硝唑仑苯那唑仑吡唑仑利马唑仑三唑仑
咪唑并苯二氮䓬类	溴他西尼氯马唑仑 EVT-201 FG-8205 氟马西尼米达西尼 ¹²³碘-碘西尼 L-655,708 氯普唑仑咪达唑仑 PWZ-029 瑞马唑仑 Ro15-4513 Ro48-6791 Ro48-8684 Ro4938581 沙马西尼 SH-053-R-CH3-2′F
𫫇唑并苯二氮䓬类	氯𫫇唑仑氟他唑仑卤𫫇唑仑美沙唑仑奥沙唑仑
噻吩并二氮䓬类	苯他西泮氯噻西泮 Ro09-9212
噻吩并三唑并二氮䓬类	溴替唑仑环氯唑仑去氯依替唑仑依替唑仑氟溴替唑仑氟氯替唑仑氟依替唑仑伊拉帕泛 JQ1 * 美替唑仑
噻吩并苯二氮䓬类	奥氮平替仑西平
吡啶并二氮䓬类	氯吡西泮
吡啶并三唑并二氮䓬类	扎吡唑仑
吡唑并二氮䓬类	雷唑巴占 * 利帕西泮唑拉西泮唑美巴占佐美他平 *
吡咯并二氮䓬类	普瑞西泮
四氢异喹啉并苯二氮䓬类	克拉唑仑
吡咯并苯二氮䓬类	蒽霉素
苯二氮䓬类前药	阿普唑仑三唑并二苯甲酮阿维扎封利马扎封
* 非典型活性谱 (非GABA_A受体的配体)