加巴喷丁

加巴噴丁
(Gabapentin)
臨床資料
商品名英语Drug nomenclatureNeurontin,其它[1]
AHFS/Drugs.comMonograph
MedlinePlusa694007
核准狀況
懷孕分級
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27-60%(与剂量成反比;高脂饮食会提高生物利用度)[2][3]
血漿蛋白結合率低於3%[2][3]
药物代谢沒有明顯代謝[2][3]
生物半衰期五至七小時[2][3]
排泄途徑腎臟[2][3]
识别信息
  • 1-(aminomethyl)cyclohexaneacetic acid
CAS号60142-96-3  checkY
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
PDB配體ID
CompTox Dashboard英语CompTox Chemicals Dashboard (EPA)
ECHA InfoCard100.056.415 編輯維基數據鏈接
化学信息
化学式C9H17NO2
摩尔质量171.24 g·mol−1
3D模型(JSmol英语JSmol
  • O=C(O)CC1(CN)CCCCC1
  • InChI=1S/C9H17NO2/c10-7-9(6-8(11)12)4-2-1-3-5-9/h1-7,10H2,(H,11,12) checkY
  • Key:UGJMXCAKCUNAIE-UHFFFAOYSA-N checkY


加巴喷丁拉丁語Gabapentin),研發廠商品名為Neurontin,用於治療癫痫神經痛潮熱以及睡眠腳動症[4][5]。這種藥物一般用於治療局部癫痫英语partial seizures[6]加巴噴丁也是治療糖尿病神經炎英语diabetic neuropathy皰疹後的劇痛英语post-herpetic neuralgia、以及central neuropathic pain英语central neuropathic pain等疾病的神經性病痛的首選[6],約14%神經性病變疼痛的患者可獲得改善[7]

副作用包含嗜睡和暈眩。嚴重副作用可能包括提高自殺風險、躁動行為及嗜酸粒細胞增多以及全身性症狀英语drug reaction with eosinophilia and systemic symptoms[4]。對妊娠母乳餵養的危害尚不明確[8]腎功能衰竭患者應使用較低劑量。加巴噴丁會對抑制性的神經傳遞物Γ-氨基丁酸(GABA)有所影響,但作用方式尚無定論[4]

加巴噴丁在1993年首次通過美国食品药品监督管理局批准[9][10]。批價約在每日1.35美元[11]。在美國,此藥從2004年開始可以通用名药物方式取得[4],2015年,在美國一個月的藥物成本在100到200美金間[12]。1990年代,派德藥廠英语Parke-Davis輝瑞子公司)透過一系列手法鼓勵美國的醫生在非常規情況使用英语off-label use加巴噴丁[13]

引用

  1. ^ Drugs.com international listings for Gabapentin页面存档备份,存于互联网档案馆) Page accessed Feb. 9, 2016
  2. ^ 2.0 2.1 2.2 2.3 2.4 Neurontin, Gralise (gabapentin) dosing, indications, interactions, adverse effects, and more. Medscape Reference. WebMD. [6 April 2014]. (原始内容存档于2014-12-16). 
  3. ^ 3.0 3.1 3.2 3.3 3.4 Goa, KL; Sorkin, EM. Gabapentin. A review of its pharmacological properties and clinical potential in epilepsy.. Drugs. September 1993, 46 (3): 409–27. PMID 7693432. doi:10.2165/00003495-199346030-00007. 
  4. ^ 4.0 4.1 4.2 4.3 Gabapentin. The American Society of Health-System Pharmacists. [Oct 23, 2015]. (原始内容存档于2017-09-08). 
  5. ^ Wijemanne, S; Jankovic, J. Restless legs syndrome: clinical presentation diagnosis and treatment.. Sleep medicine. June 2015, 16 (6): 678–90. PMID 25979181. doi:10.1016/j.sleep.2015.03.002. 
  6. ^ 6.0 6.1 Attal N, Cruccu G, Baron R, et al. EFNS guidelines on the pharmacological treatment of neuropathic pain: 2010 revision. Eur. J. Neurol. September 2010, 17 (9): 1113–e88. PMID 20402746. doi:10.1111/j.1468-1331.2010.02999.x. 
  7. ^ Moore, RA; Wiffen, PJ; Derry, S; Toelle, T; Rice, AS. Gabapentin for chronic neuropathic pain and fibromyalgia in adults.. The Cochrane database of systematic reviews. 27 April 2014, 4: CD007938. PMID 24771480. 
  8. ^ Gabapentin Pregnancy and Breastfeeding Warnings. [13 March 2016]. (原始内容存档于2017-09-08). 
  9. ^ 存档副本. [2017-06-11]. (原始内容存档于2017-06-29). 
  10. ^ Pitkänen, Asla; Schwartzkroin, Philip A.; Moshé, Solomon L. Models of Seizures and Epilepsy.. Burlington: Elsevier. 2005: 539 [2016-11-19]. ISBN 9780080457024. (原始内容存档于2020-02-19). 
  11. ^ Gabapentin. International Drug Price Indicator Guide. [13 March 2016]. [永久失效連結]
  12. ^ Hamilton, Richart. Tarascon Pocket Pharmacopoeia 2015 Deluxe Lab-Coat Edition. Jones & Bartlett Learning. 2015: 327. ISBN 9781284057560. 
  13. ^ Henney JE. Safeguarding patient welfare: who's in charge? (PDF). Annals of Internal Medicine英语Annals of Internal Medicine. August 2006, 145 (4): 305–7 [2016-11-19]. PMID 16908923. doi:10.7326/0003-4819-145-4-200608150-00013. (原始内容存档 (PDF)于2009-12-22). 

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