吡喹酮

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吡喹酮
Praziquantel.svg
Praziquantel.gif
系统(IUPAC)命名名称
(RS)-2-(Cyclohexylcarbonyl)-1,2,3,6,7,11b-hexahydro-4H-pyrazino[2,1-a]isoquinolin-4-one
临床数据
商品名 Biltricide
Drugs.com Monograph
MedlinePlus a608048
妊娠分级
  • Only when clearly needed (lack of sufficient data in humans)
给药途径 oral
合法狀態
合法状态
  • U.S.: Rx-only (human use), over-the-counter (veterinary use)[1]
药代动力学数据
生物利用度 relatively small
代谢 hepatic
生物半衰期 0.8至1.5 hours (Main Metabolites 4至5 hours)
排泄 mainly in urine
识别信息
CAS注册号55268-74-1 ✓
ATC代码 P02BA01 QP52英语ATCvet code QP52AA01
PubChem CID 4891
DrugBank DB01058 ✓
ChemSpider 4722 ✓
UNII 6490C9U457 ✓
KEGG D00471 ✓
ChEMBL英语ChEMBL CHEMBL976 ✓
化学信息
化学式 C19H24N2O2
摩尔质量 312.411

吡喹酮(英語:Praziquantel,或英語:Biltricide)為一種用於人類及動物的驅蟲藥,專門治療絛蟲吸蟲。對於血吸蟲中華肝吸蟲廣節裂頭絛蟲英语Diphyllobothrium latum特別有效,吡喹酮為世界卫生组织基本药物标准清单上的藥物,為世界上對於基本公共衛生最重要的藥物之一。[1]1970年代由拜耳公司的藥學部研發成功。

醫療用途[编辑]

吡喹酮可以用於治療人類、哺乳類,以及魚類的寄生蟲病。包含腸胃道或是外部的感染,以下為其適用疾病:

副作用[编辑]

商品名[编辑]

  • Biltricide (Bayer) 600 mg Tablets:人類使用
  • Cesol (Merck) Tablets
  • Cestoved (Vedco) :藥片或注射劑,獸醫使用
  • Cysticide (Merck) Tablets
  • Distocide (Shin Poong Pharm. Co. Ltd) 600mg tablet:人類使用
  • Distoside (Chandra Bhagat Pharma Pvt Ltd) 600mg tablet:人類使用
  • Droncit (Bayer) :獸醫使用
  • Drontal (combination with pyrantel pamoate英语pyrantel pamoate) (Bayer):獸醫使用
  • D-Worm (Farnum) for veterinary use; note that D-Worm also makes roundworm medicine containing piperidine which is not effective against tapeworms.
  • Fish Tapes (Thomas Labs) for aquarium use
  • Kaicide (Taiwan)
  • Milbemax (combination with milbemycin oxime英语milbemycin oxime) (Novartis):獸醫使用
  • Popantel (Jurox)
  • PraziPro (Hikari) :水生動物飼養使用
  • Praz-Tastic (NFP/National Fish Pharmaceuticals) :水生動物飼養使用
  • Pure Prazi (COTS Koi/Children of the Sun Koi):水生動物飼養使用
  • PraziPure (J.K.O., Inc. d/b/a Kodama Koi Farm & Kodama Koi Garden; licensed by COTS Koi):水生動物飼養使用
  • Profender (combination with emodepside英语emodepside) (Bayer) :獸醫使用
  • Tape Worm Tabs (Trade Winds) :獸醫使用
  • Zentozide (Berich (Thailand) Co)

核准狀況[编辑]

吡喹酮名列世界卫生组织基本药物标准清单之中, 是世界上对于基本公共卫生最重要的药物之一。[1]

在英国,吡喹酮并未获准在人体上使用。但在必要时可以根据在患者实名的情况下进口。[16]在英国吡喹酮可以作为兽用驱虫药销售。

在美国,吡喹酮被FDA批准用于血吸虫病及肝吸虫病的治疗,尽管它对其他种类的感染也有效。[17]

參考文獻[编辑]

  1. ^ 1.0 1.1 WHO Model List of EssentialMedicines (PDF). World Health Organization. October 2013 [22 April 2014]. 
  2. ^ Matthaiou DK, Panos G, Adamidi ES, Falagas ME. Carabin, Hélène, 编. Albendazole versus Praziquantel in the Treatment of Neurocysticercosis: A Meta-analysis of Comparative Trials. PLoS Negl Trop Dis. 2008, 2 (3): e194. PMC 2265431. PMID 18335068. doi:10.1371/journal.pntd.0000194. 
  3. ^ Bowman, Dwight D.; Hendrix, Charles M.; Lindsay, David S.; Barr, Steven C. Feline clinical parasitology First. Ames, Iowa: Iowa State University. 2002: 275. ISBN 0-8138-0333-0. 
  4. ^ Tchuenté LA, Shaw DJ, Polla L, Cioli D, Vercruysse J. Efficacy of praziquantel against Schistosoma haematobium infection in children. Am. J. Trop. Med. Hyg. December 2004, 71 (6): 778–82. PMID 15642971. 
  5. ^ 5.0 5.1 The Carter Center. Schistosomiasis Control Program. [2008-07-17]. 
  6. ^ Shen C, Kim J, Lee JK; 等. Collection of Clonorchis sinensis adult worms from infected humans after praziquantel treatment. The Korean Journal of Parasitology. June 2007, 45 (2): 149–52. PMC 2526309. PMID 17570980. doi:10.3347/kjp.2007.45.2.149. (原始内容存档于2012-12-20). 
  7. ^ Mas-Coma S, Bargues MD, Valero MA. Fascioliasis and other plant-borne trematode zoonoses. Int. J. Parasitol. October 2005, 35 (11-12): 1255–78. PMID 16150452. doi:10.1016/j.ijpara.2005.07.010. 
  8. ^ Treatment of fish parasites. 2. Effects of praziquantel, niclosamide, levamisole-HCl, and metrifonate on monogenea (Gyrodactylus aculeati, Diplozoon paradoxum). 
  9. ^ Ridtitid W, Wongnawa M, Mahatthanatrakul W, Punyo J, Sunbhanich M. Rifampin markedly decreases plasma concentrations of praziquantel in healthy volunteers. Clin. Pharmacol. Ther. November 2002, 72 (5): 505–13. PMID 12426514. doi:10.1067/mcp.2002.129319. 
  10. ^ Quinn DI, Day RO. Drug interactions of clinical importance. An updated guide. Drug Saf. June 1995, 12 (6): 393–452. PMID 8527014. doi:10.2165/00002018-199512060-00005. 
  11. ^ Masimirembwa CM, Naik YS, Hasler JA. The effect of chloroquine on the pharmacokinetics and metabolism of praziquantel in rats and in humans. Biopharm Drug Dispos. January 1994, 15 (1): 33–43. PMID 8161714. doi:10.1002/bdd.2510150103. 
  12. ^ Metwally A, Bennett JL, Botros S, Ebeid F. Effect of cimetidine, bicarbonate and glucose on the bioavailability of different formulations of praziquantel. Arzneimittelforschung. April 1995, 45 (4): 516–8. PMID 7779153. 
  13. ^ Jung H, Medina R, Castro N, Corona T, Sotelo J. Pharmacokinetic study of praziquantel administered alone and in combination with cimetidine in a single-day therapeutic regimen. Antimicrob. Agents Chemother. June 1997, 41 (6): 1256–9. PMC 163896. PMID 9174180. 
  14. ^ http://bayer.naccvp.com/view_label.php
  15. ^ Woelfle, Michael; Seerden, Jean-Paul; de Gooijer, Jesse; Pouwer, Kees; Olliaro, Piero; Todd, Matthew H. Geary, Timothy G., 编. Resolution of Praziquantel. PLoS Neglected Tropical Diseases (Public Library of Science (PLoS)). 2011-09-20, 5 (9): e1260. ISSN 1935-2735. doi:10.1371/journal.pntd.0001260. 
  16. ^ Antihelmintics - Medicines for Worms; threadword, roundworm. Patient. [2015-06-15]. 
  17. ^ Brunton, Laurence; Chabner, Bruce; Knollman, Bjorn. Goodman and Gilman's The Pharmacological Basis of Therapeutics, Twelfth Edition 12 edition. New York: McGraw-Hill Education / Medical. 2011-01-10. ISBN 9780071624428. 

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