法莫替丁
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临床资料 | |
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读音 | /fəˈmɒtɪdiːn/ |
商品名 | Pepcid |
AHFS/Drugs.com | Monograph |
MedlinePlus | a687011 |
核准状况 |
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怀孕分级 |
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给药途径 | 口服、静脉注射 |
ATC码 | |
法律规范状态 | |
法律规范 | |
药物动力学数据 | |
生物利用度 | 40–45%(口服)[1] |
血浆蛋白结合率 | 15–20%[1] |
药物代谢 | 肝脏 |
生物半衰期 | 2.5–3.5小时[1] |
排泄途径 | 肾脏(25–30%不变)[1] |
识别信息 | |
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CAS号 | 76824-35-6 |
PubChem CID | |
IUPHAR/BPS | |
DrugBank | |
ChemSpider | |
UNII | |
KEGG | |
ChEBI | |
ChEMBL | |
CompTox Dashboard (EPA) | |
ECHA InfoCard | 100.116.793 |
化学信息 | |
化学式 | C8H15N7O2S3 |
摩尔质量 | 337.449 g/mol |
3D模型(JSmol) | |
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法莫替丁(INN:famotidine),商品名Gaster、Pepcid等,是一种组胺H2受体阻抗剂,主要用于抑制胃酸的分泌,并用于治疗消化性溃疡和胃食道逆流。与西咪替丁不同,法莫替丁等第二代H2受体阻抗剂对细胞色素P450酶没有明显的抑制作用,因此法莫替丁的药物相互作用并不明显。[2]法莫替丁于1979年首次发现,并在1981年投入市场。[3]
历史
法莫替丁由山之内制药开发。[4]默克药厂在20世纪80年代中期获得法莫替丁的授权,[5]并由默克和强生公司的合资企业销售。在法莫替丁上,原本西咪替丁的咪唑环被2-胍基噻唑环取代。法莫替丁的效力比同为H2受体阻抗剂的雷尼替丁高出9倍,更比西咪替丁的效力高出32倍。[6] 法莫替丁在1986年由美国食品药品监督管理局批准在美国销售。[7]而商品名为Pepcid RPD的法莫替丁口腔崩散剂则于1998年获得批准。[8]法莫替丁的仿制药在2001年开始上市,商品名包括Fluxid、Quamatel等。[9]
在美国和加拿大,另有商品名为Pepcid Complete的复方咀嚼片,该药品将法莫替丁与抗酸药结合,以快速舒缓胃酸过多的症状。[10]在英国,该药品亦被称为Pepcidtwo,但已在2015年4月停产。[11]
因为法莫替丁在胃内的酸性环境下溶解度低,故此口服法莫替丁的生物利用度仅有50%。当法莫替丁与抗酸剂组合使用,抗酸剂能促进法莫替丁局部运送至胃壁细胞上的受体。因此,研究人员正在开发创新配方的口服片剂,例如胃滞留药物输送系统。胃滞留片剂能在胃内停留更久,从而改善生物利用度;而法莫替丁的局部运送还能增加胃壁受体部位的生物利用度,从而增强减少胃酸分泌的功效。[12]
研究
有些证据表示法莫替丁能作为治疗抵抗精神分裂症的附加治疗。在一项试验中,它使治疗抵抗精神分裂症患者的症状严重性降低了10%。[13]
医疗用途
法莫替丁主要用于舒缓胃灼热和消化不良[14];治疗胃及十二指肠溃疡[14]如佐埃二氏症和多发性内分泌肿瘤等病理性胃酸过度分泌、[6][15]胃食道逆流(GERD)[14]与食道炎等上消化道病症。[16]
虽然奥美拉唑可能更有效,法莫替丁也可作为治疗幽门螺杆菌感染药物的一部分。[17][18][19][20][21][22]
法莫替丁也可用于预防因服用非甾体抗炎药所诱发的胃溃疡[23][24]和减少手术后吸入性肺炎的风险。[25][26][27]
剂型
![](http://images.weserv.nl/?url=//upload.wikimedia.org/wikipedia/commons/thumb/0/0a/Gaster_Sales_In_China.jpg/220px-Gaster_Sales_In_China.jpg)
![](http://images.weserv.nl/?url=//upload.wikimedia.org/wikipedia/commons/thumb/5/57/Famotidine_20mg_generic.jpg/220px-Famotidine_20mg_generic.jpg)
![](http://images.weserv.nl/?url=//upload.wikimedia.org/wikipedia/commons/thumb/1/1d/Famotidine_New_Package.jpg/220px-Famotidine_New_Package.jpg)
某些法莫替丁的剂型可作为非处方药销售。如在美国和加拿大,10毫克和20毫克的法莫替丁口服片,有时与抗酸药组成复方,可以作为非处方药销售。[28]较大剂量的法莫替丁仍然属于处方药。法莫替丁与布洛芬的复方药由Horizon Pharma以商品名称Duexis销售。[29]
副作用
参考文献
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- ^ 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).
- ^ Fischer, Janos. Analogue-based Drug Discovery II. John Wiley & Sons. 2010: 4 [2018-09-11]. ISBN 978-3-527-63212-1. (原始内容存档于2020-07-29).
- ^ 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 1981美国专利4283408 (于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。
- ^ Sankyo Pharma. Skyscape Mediwire. 2002 [2009-10-31]. (原始内容存档于2009-02-23).
- ^ 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. (原始内容存档于2019-08-20).
- ^ Drugs@FDA: Pepcid. [2018-09-11]. (原始内容存档于2021-03-21).
- ^ Drug Approval Package: Pecid RPD (Famotidine) NDA# 020752. [2018-09-11]. (原始内容存档于2021-03-31).
- ^ Drugs@FDA: Fluxid. [2018-09-11].
- ^ Drugs@FDA: Pepcid Complete. [2018-09-13]. (原始内容存档于2021-03-22).
- ^ PepcidTwo Chewable Tablet. [2015-06-07]. (原始内容存档于2016-07-18).
- ^ 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).
- ^ 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.
- ^ 14.0 14.1 14.2 Australian Medicines Handbook (页面存档备份,存于互联网档案馆),2005. Adelaide: Australian Medicines Handbook. ISBN 0-9578521-9-3。
- ^ Zollinger-Ellison syndrome - Diagnosis and treatment - Mayo Clinic. www.mayoclinic.org. [2018-09-11]. (原始内容存档于2020-09-18) (英语).
- ^ Esophagitis - Diagnosis and treatment - Mayo Clinic. www.mayoclinic.org. [2018-09-11]. (原始内容存档于2021-01-21) (英语).
- ^ 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.
- ^ 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.
- ^ 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.
- ^ 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.
- ^ 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.
- ^ 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.
- ^ 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.
- ^ 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.
- ^ 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.
- ^ 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.
- ^ 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.
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- ^ Drugs.com duexis (页面存档备份,存于互联网档案馆)
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参见
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