右旋安非他命
右旋安非他命(英語:Dextroamphetamine)[注 1]是强力中樞神經兴奋剂,也是苯丙胺(“安非他命”) 的对映异构体,是注意力不足過動症(ADHD)和發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。
臨床資料 | |
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AHFS/Drugs.com | Monograph |
MedlinePlus | a605027 |
核准狀況 | |
懷孕分級 |
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依賴性 | 生理依赖:无 精神依赖:中 |
成癮性 | 中 |
给药途径 | 口服 |
ATC碼 | |
法律規範狀態 | |
法律規範 |
|
藥物動力學數據 | |
生物利用度 | Oral 75–100%[1] |
血漿蛋白結合率 | 15–40% |
药物代谢 | CYP2D6,多巴胺β羟化酶,[9] FMO3 |
藥效起始時間 | 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 |
作用時間 | IR服用:3至7小时[4][7] XR服用:12小时[4][5][7] |
排泄途徑 | 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) |
| |
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脚注
参考资料
- ^ 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).