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法莫替丁INN:famotidine),商品名稱為Pepcid,是一種组胺H2受体阻抗剂,主要用於抑制胃酸的分泌,並用于治疗消化性溃疡胃食道逆流。與西咪替丁不同,法莫替丁等第二代H2受體阻抗劑細胞色素P450酶沒有明顯的抑制作用,因此法莫替丁的药物相互作用並不明顯。[2]法莫替丁於1979年首次發現,並在1981年投入市場。[3]

法莫替丁
Famotidine.svg
Famotidine ball-and-stick model.png
系统(IUPAC)命名名称
3-[({2-[(diaminomethylidene)amino]-1,3-thiazol-4-yl}methyl)sulfanyl]-N-sulfamoylpropanimidamide
临床数据
读音 /fəˈmɒtɪdn/
商品名 Pepcid
Drugs.com Monograph
MedlinePlus a687011
医疗法规
妊娠分级
  • AU: B1
  • US: B (非人类研究中表明无风险)
给药途径 口服、靜脈注射
合法狀態
合法状态
药代动力学数据
生物利用度 40–45%(口服)[1]
蛋白结合度 15–20%[1]
代谢 肝臟
生物半衰期 2.5–3.5小時[1]
排泄 腎臟(25–30%不變)[1]
识别信息
CAS注册号76824-35-6
ATC代码 A02BA03
PubChem CID 3325
IUPHAR/BPS英语IUPHAR/BPS 7074
DrugBank DB00927
ChemSpider 3208
UNII 5QZO15J2Z8
KEGG D00318
ChEBI CHEBI:4975
ChEMBL英语ChEMBL CHEMBL902
化学信息
化学式 C8H15N7O2S3
摩尔质量 337.449 g/mol

历史编辑

法莫替丁由山之內製藥英语Yamanouchi_Pharmaceutical開發。[4]默克藥廠在20世紀80年代中期獲得法莫替丁的授權,[5]並由默克和強生公司的合資企業銷售。在法莫替丁上,原本西咪替丁的咪唑環被2-胍基噻唑環取代。法莫替丁的效力比同為H2受體阻抗劑雷尼替丁高出9倍,更比西咪替丁的效力高出32倍。[6] 法莫替丁在1986年由美國食品藥品監督管理局批准在美國銷售。[7]而商品名為Pepcid RPD的法莫替丁口腔崩散劑則於1998年獲得批准。[8]法莫替丁的仿製藥在2001年開始上市,商品名包括Fluxid、Quamatel等。[9]

在美國和加拿大,另有商品名為Pepcid Complete的複方咀嚼片,該藥品將法莫替丁與抗酸藥結合,以快速舒緩胃酸過多的症狀。[10]在英國,該藥品亦被稱為Pepcidtwo,但已在2015年4月停產。[11]

因為法莫替丁在胃內的酸性環境下溶解度低,故此口服法莫替丁的生物利用度僅有50%。當法莫替丁與抗酸劑組合使用,抗酸劑能促進法莫替丁局部運送至胃壁細胞上的受體。因此,研究人員正在開發創新配方的口服片劑,例如胃滯留藥物輸送系統。胃滯留片劑能在胃內停留更久,從而改善生物利用度;而法莫替丁的局部運送還能增加胃壁受體部位的生物利用度,從而增強減少胃酸分泌的功效。[12]

研究编辑

有些證據表示法莫替丁能作為治療抵抗精神分裂症的附加治療。在一項試驗中,它使治療抵抗精神分裂症患者的症狀嚴重性降低了10%。[13]

医疗用途编辑

法莫替丁主要用於舒緩胃灼熱消化不良[14];治療胃及十二指肠潰瘍[14]佐埃二氏症英语Zollinger–Ellison_syndrome多發性內分泌腫瘤英语Multiple_endocrine_neoplasia等病理性胃酸過度分泌、[6][15]胃食道逆流(GERD)[14]食道炎英语Esophagitis等上消化道病症。[16]

雖然奧美拉唑可能更有效,法莫替丁也可作為治療幽門螺桿菌感染藥物的一部分。[17][18][19][20][21][22]

法莫替丁也可用於预防因服用非甾体抗炎药所诱發的胃溃疡[23][24]和減少手術後吸入性肺炎的風險。[25][26][27]

劑型编辑

 
在中国大陆销售的高舒达®法莫替丁口服片,规格为20mg×30片
 
法莫替丁學名藥20mg口服片
 
法莫替丁,香港公立醫院開出藥品的新包裝

某些法莫替丁的劑型可作為非處方藥銷售。如在美國加拿大,10毫克和20毫克的法莫替丁口服片,有時與抗酸藥組成複方,可以作為非處方藥銷售。[28]較大劑量的法莫替丁仍然屬於處方藥。法莫替丁與布洛芬的複方藥由Horizon Pharma英语Horizon_Pharma以商品名稱Duexis銷售。[29]

副作用编辑

與法莫替丁相關的副作用包括頭痛頭暈便秘腹瀉[30]

参考文献编辑

  1. ^ 1.0 1.1 1.2 1.3 Truven Health Analytics, Inc. DRUGDEX® System (Internet) [cited 2013 Oct 10]. Greenwood Village, CO: Thomsen Healthcare; 2013.
  2. ^ Humphries TJ, Merritt GJ. Review article: drug interactions with agents used to treat acid-related diseases (pdf). Aliment. Pharmacol. Ther. August 1999, 13 (Suppl 3): 18–26 [2015-09-27]. PMID 10491725. doi:10.1046/j.1365-2036.1999.00021.x. (原始内容存档于2015-12-03). 
  3. ^ Fischer, Janos. Analogue-based Drug Discovery II. John Wiley & Sons. 2010: 4. ISBN 978-3-527-63212-1. 
  4. ^ US patent 4283408, Yasufumi Hirata, Isao Yanagisawa, Yoshio Ishii, Shinichi Tsukamoto, Noriki Ito, Yasuo Isomura and Masaaki Takeda, "Guanidinothiazole compounds, process for preparation and gastric inhibiting compositions containing them", issued 11 August 1981US4,283,408 (PDF 版本) (於1981年08月11日注册) Yasufumi Hirata, Isao Yanagisawa, Yoshio Ishii, Shinichi Tsukamoto, Noriki Ito, Yasuo Isomura and Masaaki Takeda——Guanidinothiazole compounds, process for preparation and gastric inhibiting compositions containing them。 
  5. ^ Sankyo Pharma. Skyscape Mediwire. 2002 [2009-10-31]. (原始内容存档于2009-02-23). 
  6. ^ 6.0 6.1 J.M. Howard, A.N. Chremos, M.J. Collen, K.E. Mcarthur, J.A. Cherner, P.N. Maton, C.A. Ciarleglio, M.J. Cornelius, J.D. Gardner, R.T. Jensen. Famotidine, a New, Potent, Long-Acting Histamine H2-Receptor Antagonist: Comparison With Cimetidine and Ranitidine in the Treatment of Zollinger-Ellison Syndrome. Gastroenterology. 1985-04, 88 (4): 1026–1033 [2018-09-11]. ISSN 0016-5085. doi:10.1016/s0016-5085(85)80024-x. 
  7. ^ Drugs@FDA: Pepcid. [2018-09-11]. 
  8. ^ Drug Approval Package: Pecid RPD (Famotidine) NDA# 020752. [2018-09-11]. 
  9. ^ Drugs@FDA: Fluxid. [2018-09-11]. 
  10. ^ Drugs@FDA: Pepcid Complete. [2018-09-13]. 
  11. ^ PepcidTwo Chewable Tablet. [2015-06-07]. (原始内容存档于2016-07-18). 
  12. ^ Formulation and Evaluation of Gastroretentive Floating Tablets of Famotidine. Farmavita.Net. 2008 [2009-01-31]. (原始内容存档于2016-03-29). 
  13. ^ Meskanen, K; Ekelund, H; Laitinen, J; Neuvonen, PJ; Haukka, J; Panula, P; Ekelund, J. A randomized clinical trial of histamine 2 receptor antagonism in treatment-resistant schizophrenia.. Journal of Clinical Psychopharmacology. August 2013, 33 (4): 472–478. PMID 23764683. doi:10.1097/JCP.0b013e3182970490. 
  14. ^ 14.0 14.1 14.2 Australian Medicines Handbook,2005. Adelaide: Australian Medicines Handbook. ISBN 0-9578521-9-3
  15. ^ Zollinger-Ellison syndrome - Diagnosis and treatment - Mayo Clinic. www.mayoclinic.org. [2018-09-11] (英语). 
  16. ^ Esophagitis - Diagnosis and treatment - Mayo Clinic. www.mayoclinic.org. [2018-09-11] (英语). 
  17. ^ Kanayama, S. Proton-pump inhibitors versus H2-receptor antagonists in triple therapy for Helicobacter pylori eradication. Nihon rinsho. Japanese journal of clinical medicine. January 1999, 57 (1): 153–6. PMID 10036954. 
  18. ^ Soga, T; Matsuura, M; Kodama, Y; Fujita, T; Sekimoto, I; Nishimura, K; Yoshida, S; Kutsumi, H; Fujimoto, S. Is a proton pump inhibitor necessary for the treatment of lower-grade reflux esophagitis?. Journal of gastroenterology. August 1999, 34 (4): 435–40. PMID 10452673. doi:10.1007/s005350050292. 
  19. ^ Borody, TJ; Andrews, P; Fracchia, G; Brandl, S; Shortis, NP; Bae, H. Omeprazole enhances efficacy of triple therapy in eradicating Helicobacter pylori.. Gut. October 1995, 37 (4): 477–81. PMC 1382896. PMID 7489931. doi:10.1136/gut.37.4.477. 
  20. ^ Hu, FL; Jia, JC; Li, YL; Yang, GB. Comparison of H2-receptor antagonist- and proton-pump inhibitor-based triple regimens for the eradication of Helicobacter pylori in Chinese patients with gastritis or peptic ulcer.. The Journal of international medical research. 2003, 31 (6): 469–74. PMID 14708410. doi:10.1177/147323000303100601. 
  21. ^ Kirika, NV; Bodrug, NI; Butorov, IV; Butorov, SI. [Efficacy of different schemes of anti-helicobacter therapy in duodenal ulcer].. Terapevticheskii arkhiv. 2004, 76 (2): 18–22. PMID 15106408. 
  22. ^ Fujiwara, Y; Higuchi, K; Nebiki, H; Chono, S; Uno, H; Kitada, K; Satoh, H; Nakagawa, K; Kobayashi, K. Famotidine vs. omeprazole: a prospective randomized multicentre trial to determine efficacy in non-erosive gastro-oesophageal reflux disease.. Alimentary Pharmacology & Therapeutics. June 2005,. 21 Suppl 2: 10–8. PMID 15943841. doi:10.1111/j.1365-2036.2005.02468.x. 
  23. ^ La Corte, R; Caselli, M; Castellino, G; Bajocchi, G; Trotta, F. Prophylaxis and treatment of NSAID-induced gastroduodenal disorders.. Drug safety. June 1999, 20 (6): 527–43. PMID 10392669. doi:10.2165/00002018-199920060-00006. 
  24. ^ Laine, L; Kivitz, AJ; Bello, AE; Grahn, AY; Schiff, MH; Taha, AS. Double-blind randomized trials of single-tablet ibuprofen/high-dose famotidine vs. ibuprofen alone for reduction of gastric and duodenal ulcers.. The American Journal of Gastroenterology. March 2012, 107 (3): 379–86. PMC 3321505. PMID 22186979. doi:10.1038/ajg.2011.443. 
  25. ^ Escolano, F; Castaño, J; López, R; Bisbe, E; Alcón, A. Effects of omeprazole, ranitidine, famotidine and placebo on gastric secretion in patients undergoing elective surgery.. British journal of anaesthesia. October 1992, 69 (4): 404–6. PMID 1419452. doi:10.1093/bja/69.4.404. 
  26. ^ Vila, P; Vallès, J; Canet, J; Melero, A; Vidal, F. Acid aspiration prophylaxis in morbidly obese patients: famotidine vs. ranitidine.. Anaesthesia. November 1991, 46 (11): 967–9. PMID 1750602. doi:10.1111/j.1365-2044.1991.tb09860.x. 
  27. ^ Jahr, JS; Burckart, G; Smith, SS; Shapiro, J; Cook, DR. Effects of famotidine on gastric pH and residual volume in pediatric surgery.. Acta anaesthesiologica Scandinavica. July 1991, 35 (5): 457–60. PMID 1887750. doi:10.1111/j.1399-6576.1991.tb03328.x. 
  28. ^ Famotidine. [2018-09-11]. (原始内容存档于2016-07-05). 
  29. ^ Drugs.com duexis 页面存档备份,存于互联网档案馆
  30. ^ Pepcid Side Effects & Drug Interactions. RxList.com. 2008 [2008-07-31]. (原始内容存档于2008-09-06). 

參見编辑