羟考酮是一种用于緩解疼痛口服鴉片類藥物,于1916年首次在德国制成。[7]它具有高度成瘾性[8],因此容易被滥用[9][10][9]服用藥物後該藥在十五分钟内就能開始缓解疼痛,藥效可以持续六個小时。[9]

羟考酮
臨床資料
读音ɒksɪˈkəʊdəʊn
商品名英语Drug nomenclatureOxyContin, Endone, others
其他名稱Eukodal, eucodal; dihydrohydroxycodeinone, 7,8-dihydro-14-hydroxycodeinone, 6-deoxy-7,8-dihydro-14-hydroxy-3-O-methyl-6-oxomorphine[1]
AHFS/Drugs.comMonograph
MedlinePlusa682132
核准狀況
懷孕分級
依賴性[3]
给药途径口服给药, 口腔黏膜吸收, 肌肉注射, 靜脈注射, 鼻腔给药, 皮下注射, 經皮给药英语transdermal administration, 直肠给药英语rectal administration, 硬脊膜外麻醉[4]
ATC碼
法律規範狀態
法律規範
藥物動力學數據
生物利用度口服: 60–87%[5][6]
血漿蛋白結合率45%[5]
排泄途徑尿 (83%)[5]
识别信息
  • (5R,9R,13S,14S)-4,5α-Epoxy-14-hydroxy-3-methoxy-17-methylmorphinan-6-one
CAS号76-42-6  checkY
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard英语CompTox Chemicals Dashboard (EPA)
ECHA InfoCard100.000.874 編輯維基數據鏈接
化学信息
化学式C18H21NO4
摩尔质量315.37 g·mol−1
3D模型(JSmol英语JSmol
熔点219 °C(426 °F)
水溶性166 (HCl)
  • O=C4[C@@H]5Oc1c2c(ccc1OC)C[C@H]3N(CC[C@]25[C@@]3(O)CC4)C
  • InChI=1S/C18H21NO4/c1-19-8-7-17-14-10-3-4-12(22-2)15(14)23-16(17)11(20)5-6-18(17,21)13(19)9-10/h3-4,13,16,21H,5-9H2,1-2H3/t13-,16+,17+,18-/m1/s1 checkY
  • Key:BRUQQQPBMZOVGD-XFKAJCMBSA-N checkY

該藥常见的副作用有欣快便秘恶心呕吐食欲不振、嗜睡、頭暈、瘙痒、口乾和出汗。[9]严重的副作用可能包括上瘾、物質依賴物質濫用、易怒、抑鬱狂躁譫妄幻觉換氣不足心跳过缓低血壓[9]

参考文献 编辑

  1. ^ O'Neil MJ (编). The Merck index 14th. Whitehouse Station, NJ: Merck & Co. 2006. ISBN 978-0-911910-00-1. 
  2. ^ Oxycodone Use During Pregnancy. Drugs.com. 14 October 2019 [12 April 2020]. (原始内容存档于2020-06-19). 
  3. ^ Bonewit-West K, Hunt SA, Applegate E. Today's Medical Assistant: Clinical and Administrative Procedures. Elsevier Health Sciences. 2012: 571 [2022-07-10]. ISBN 978-1-4557-0150-6. (原始内容存档于2020-07-28) (英语). 
  4. ^ Kalso E. Oxycodone. Journal of Pain and Symptom Management. May 2005, 29 (5 Suppl): S47–S56. PMID 15907646. doi:10.1016/j.jpainsymman.2005.01.010 . 
  5. ^ 5.0 5.1 5.2 Roxicodone, OxyContin (oxycodone) dosing, indications, interactions, adverse effects, and more. Medscape Reference. WebMD. [8 April 2014]. (原始内容存档于2014-04-13). 
  6. ^ Elliott JA, Smith HS. Handbook of Acute Pain Management. CRC Press. 19 April 2016: 82– [2022-07-10]. ISBN 978-1-4665-9635-1. (原始内容存档于2021-04-17). 
  7. ^ Drug discovery: a history. Hoboken, NJ: Wiley. 2005: 119. ISBN 978-0-471-89980-8. 
  8. ^ Remillard D, Kaye AD, McAnally H. Oxycodone's Unparalleled Addictive Potential: Is it Time for a Moratorium?. Current Pain and Headache Reports. February 2019, 23 (2): 15. PMID 30820686. S2CID 73488265. doi:10.1007/s11916-019-0751-7. 
  9. ^ 9.0 9.1 9.2 9.3 9.4 Oxycodone Monograph for Professionals. Drugs.com. AHFS. [28 December 2018]. (原始内容存档于2018-12-28). 
  10. ^ Pergolizzi JV, Taylor R, LeQuang JA, Raffa RB. Managing severe pain and abuse potential: the potential impact of a new abuse-deterrent formulation oxycodone/naltrexone extended-release product. Journal of Pain Research. 2018, 11: 301–311. PMC 5810535 . PMID 29445297. doi:10.2147/JPR.S127602.