右旋安非他命
右旋安非他命（英语：Dextroamphetamine）[注 1]是强力中枢神经兴奋剂，也是苯丙胺（“安非他命”） 的对映异构体，是注意力不足过动症（ADHD）和发作性嗜睡病的处方药。[10]此外，它也被用作提升运动员能力的兴奋剂，也是一种益智药，同时人们在享乐时也将其用作春药和产生欣快感的药。此外，空军也将右旋安非他命广泛用作“抗睡丸”，在诸如夜间轰炸之类的容易疲倦的任务中使用。第二次世界大战期间，该药物也被用来治疗疲倦。
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| 临床资料 | |
|---|---|
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a605027 |
| 核准状况 | |
| 怀孕分级 |
|
| 依赖性 | 生理依赖：无 精神依赖：中 |
| 成瘾性 | 中 |
| 给药途径 | 口服 |
| ATC码 | |
| 法律规范状态 | |
| 法律规范 |
|
| 药物动力学数据 | |
| 生物利用度 | Oral 75–100%[1] |
| 血浆蛋白结合率 | 15–40% |
| 药物代谢 | CYP2D6，多巴胺β羟化酶，[9] FMO3 |
| 药效起始时间 | IR服用：0.5至1.5小时[2][3] XR服用：1.5至2小时[4][5] |
| 生物半衰期 | 9至11小时[6] 不同的PH值：8至31小时 |
| 作用时间 | IR服用：3至7小时[4][7] XR服用：12小时[4][5][7] |
| 排泄途径 | 肾（45%）；[8]取决于尿液的pH值 |
| 识别信息 | |
| |
| CAS号 | 51-64-9  |
| PubChem CID | |
| IUPHAR/BPS | |
| DrugBank | |
| ChemSpider | |
| UNII | |
| KEGG | |
| ChEBI | |
| ChEMBL | |
| CompTox Dashboard (EPA) | |
| ECHA InfoCard | 100.000.103 |
| 化学信息 | |
| 化学式 | C9H13N |
| 摩尔质量 | 135.20622 |
| 3D模型（JSmol） | |
| 密度 | 0.913 g/cm3 |
| 沸点 | 201.5 °C（394.7 °F） |
| 水溶性 | 20 mg/mL (20 °C) |
| |
| |
脚注
编辑参考资料
编辑- ^ Dextromphetamine. DrugBank. [2013-11-05]. （原始内容存档于2019-08-06）.
|section=被忽略 (帮助) - ^ Green-Hernandez, Carol; Singleton, Joanne K.; Aronzon, Daniel Z. Primary Care Pediatrics. Lippincott Williams & Wilkins. 2001-01-01: 243 [2017-05-07]. ISBN 9780781720083. （原始内容存档于2016-05-23）.|quote = Table 21.2 Medications for ADHD ... D-amphetamine ... Onset: 30 min.
- ^ Dexedrine, ProCentra(dextroamphetamine) dosing, indications, interactions, adverse effects, and more. reference.medscape.com. [2015-10-04]. （原始内容存档于2018-11-06）.
Onset of action: 1–1.5 hr
- ^ 4.0 4.1 4.2 Millichap JG. Chapter 9: Medications for ADHD. Millichap JG (编). Attention Deficit Hyperactivity Disorder Handbook: A Physician's Guide to ADHD 2nd. New York, USA: Springer. 2010: 112. ISBN 9781441913968.
Table 9.2 Dextroamphetamine formulations of stimulant medication
Dexedrine [Peak:2–3 h] [Duration:5–6 h] ...
Adderall [Peak:2–3 h] [Duration:5–7 h]
Dexedrine spansules [Peak:7–8 h] [Duration:12 h] ...
Adderall XR [Peak:7–8 h] [Duration:12 h]
Vyvanse [Peak:3–4 h] [Duration:12 h] - ^ 5.0 5.1 Brams M, Mao AR, Doyle RL. Onset of efficacy of long-acting psychostimulants in pediatric attention-deficit/hyperactivity disorder. Postgrad. Med. September 2008, 120 (3): 69–88. PMID 18824827. doi:10.3810/pgm.2008.09.1909.
Onset of efficacy was earliest for d-MPH-ER at 0.5 hours, followed by d, l-MPH-LA at 1 to 2 hours, MCD at 1.5 hours, d, l-MPH-OR at 1 to 2 hours, MAS-XR at 1.5 to 2 hours, MTS at 2 hours, and LDX at approximately 2 hours. ... MAS-XR, and LDX have a long duration of action at 12 hours postdose
- ^ Adderall IR Prescribing Information (PDF). United States Food and Drug Administration. Teva Pharmaceuticals USA, Inc.: 1–6. October 2015 [2016-05-18]. （原始内容存档 (PDF)于2018-09-15）.
- ^ 7.0 7.1 Mignot EJ. A practical guide to the therapy of narcolepsy and hypersomnia syndromes. Neurotherapeutics. October 2012, 9 (4): 739–752. PMC 3480574
. PMID 23065655. doi:10.1007/s13311-012-0150-9.
- ^ dextrostat (dextroamphetamine sulfate) tablet [Shire US Inc.]. DailyMed. Wayne, PA: Shire US Inc. August 2006 [2013-11-08]. （原始内容存档于2012-01-13）.
- ^ Lemke TL, Williams DA, Roche VF, Zito W. Foye's Principles of Medicinal Chemistry 7th. Philadelphia: Wolters Kluwer Health/Lippincott Williams & Wilkins. 2013: 648. ISBN 1609133455.
Alternatively, direct oxidation of amphetamine by DA β-hydroxylase can afford norephedrine.
- ^ Dexedrine Prescribing Information (PDF). United States Food and Drug Administration. Amedra Pharmaceuticals LLC: 1–7. February 2015 [2015-09-04]. （原始内容存档 (PDF)于2017-02-17）.
