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词条 Famotidine
释义

  1. Medical uses

  2. Side effects

  3. Interactions

  4. History

  5. Preparations

  6. References

{{Redirect|Cepal|the international organization|United Nations Economic Commission for Latin America and the Caribbean}}{{Drugbox
| Watchedfields = changed
| verifiedrevid = 458958452
| IUPAC_name = 3-[({2-[(diaminomethylidene)amino]-1,3-thiazol-4-yl}methyl)sulfanyl]-N-sulfamoylpropanimidamide
| image = Famotidine.svg
| width = 275
| image2 = Famotidine ball-and-stick model.png
| pronounce = {{IPAc-en|f|ə|ˈ|m|ɒ|t|ɪ|d|iː|n}}
| tradename = Pepcid, others
| Drugs.com = {{drugs.com|monograph|famotidine}}
| MedlinePlus = a687011
| licence_US = Famotidine
| pregnancy_AU = B1
| pregnancy_US = B
| legal_AU = S3
| legal_AU_comment = /S4; pharmacist only
| legal_UK = GSL
| legal_US = OTC
| routes_of_administration = Oral (tablets), Intravenous
| bioavailability = 40–45% (oral)[1]
| protein_bound = 15–20%[1]
| metabolism = hepatic
| elimination_half-life = 2.5–3.5 hours[1]
| excretion = Renal (25-30% unchanged [Oral])[1]
| IUPHAR_ligand = 7074
| CAS_number_Ref = {{cascite|correct|??}}
| CAS_number = 76824-35-6
| ATC_prefix = A02
| ATC_suffix = BA03
| PubChem = 3325
| DrugBank_Ref = {{drugbankcite|correct|drugbank}}
| DrugBank = DB00927
| ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}}
| ChemSpiderID = 3208
| UNII_Ref = {{fdacite|correct|FDA}}
| UNII = 5QZO15J2Z8
| KEGG_Ref = {{keggcite|correct|kegg}}
| KEGG = D00318
| ChEBI_Ref = {{ebicite|correct|EBI}}
| ChEBI = 4975
| ChEMBL_Ref = {{ebicite|correct|EBI}}
| ChEMBL = 902
| PDB_ligand = FO9
| C=8 | H=15 | N=7 | O=2 | S=3
| molecular_weight = 337.449 g/mol
| smiles = NS(=O)(=O)/N=C(\)CCSCc1csc(n1)N=C(N)N
| StdInChI_Ref = {{stdinchicite|correct|chemspider}}
| StdInChI = 1S/C8H15N7O2S3/c9-6(15-20(12,16)17)1-2-18-3-5-4-19-8(13-5)14-7(10)11/h4H,1-3H2,(H2,9,15)(H2,12,16,17)(H4,10,11,13,14)
| StdInChIKey_Ref = {{stdinchicite|correct|chemspider}}
| StdInChIKey = XUFQPHANEAPEMJ-UHFFFAOYSA-N
}}Famotidine, sold under the trade name Pepcid among others, is a medication that decreases stomach acid production.[5] It is used to treat peptic ulcer disease, gastroesophageal reflux disease, and Zollinger-Ellison syndrome.[5] It is taken by mouth or by injection into a vein.[5] It begins working within an hour.[5]

Common side effects include headache, intestinal upset, and dizziness.[5] Serious side effects may include pneumonia and seizures.[5][11] Use in pregnancy appears safe but has not been well studied while use during breastfeeding is not recommended.[2] It is a histamine H2 receptor antagonist.[3]

Famotidine was patented in 1979 and came into medical use in 1985.[4] It is available as a generic medication.[5] A month supply in the United Kingdom costs the NHS about 30 ₤ as of 2019.[5] In the United States the wholesale cost of this amount is about 2 USD.[6] In 2016 it was the 125th most prescribed medication in the United States with more than 5 million prescriptions.[7]

Medical uses

  • Relief of heartburn, acid indigestion, and sour stomach
  • Treatment for gastric and duodenal ulcers
  • Treatment for pathologic gastrointestinal hypersecretory conditions such as Zollinger–Ellison syndrome and multiple endocrine adenomas
  • Treatment for gastroesophageal reflux disease (GERD)
  • Treatment for esophagitis
  • Part of a multidrug regimen for Helicobacter pylori eradication, although omeprazole may be somewhat more effective.[8][9][10][11][12][13]
  • Prevention of NSAID-induced peptic ulcers.[14][15]
  • Given to surgery patients before operations to reduce the risk of aspiration pneumonitis.[16][17][18]

Famotidine is also given to dogs and cats with acid reflux.[19] Famotidine has been used in combination with an H1 antagonist to treat and prevent urticaria caused by an acute allergic reaction.[20]

Side effects

The most common side effects associated with famotidine use include headache, dizziness, and constipation or diarrhea.[21][22]

Interactions

Unlike cimetidine, the first H2 antagonist, famotidine has no effect on the cytochrome P450 enzyme system, and does not appear to interact with other drugs.[23]

History

Famotidine was developed by Yamanouchi Pharmaceutical Co.[24] It was licensed in the mid-1980s by Merck & Co.[25] and is marketed by a joint venture between Merck and Johnson & Johnson. The imidazole ring of cimetidine was replaced with a 2-guanidinothiazole ring. Famotidine proved to be nine times more potent than ranitidine, and thirty-two times more potent than cimetidine.[26]

It was first marketed in 1981. Pepcid RPD orally disintegrating tablets were released in 1999. Generic preparations became available in 2001, e.g. Fluxid (Schwarz) or Quamatel (Gedeon Richter Ltd.).

In the United States and Canada, a product called Pepcid Complete, which combines famotidine with an antacid in a chewable tablet to quickly relieve the symptoms of excess stomach acid, is available. In the UK, this product was known as Pepcidtwo prior to its discontinuation in April 2015.[27]

Famotidine suffers from poor bioavailability (50%), as it is poorly soluble in the low pH of the stomach. When used in combination with antacids, it promotes local delivery of these drugs to the receptor of the parietal cell wall. Therefore, researchers are developing innovative formulations of tablets, such as gastroretentive drug delivery systems. Such tablets are retained in the stomach for a longer period of time, thereby improving the bioavailability of drugs. Local delivery also increases bioavailability at the stomach wall receptor site and increases the efficacy of drugs to reduce acid secretion.[28]

Preparations

Certain preparations of famotidine are available over the counter (OTC) in various countries. In the United States and Canada, 10 mg and 20 mg tablets, sometimes in combination with an antacid,[29][30] are available OTC. Larger doses still require a medical prescription.

Formulations of famotidine in combination with ibuprofen were marketed by Horizon Pharma under the trade name Duexis.[31]

References

1. ^1 2 3 Truven Health Analytics, Inc. DRUGDEX® System (Internet) [cited 2013 Oct 10]. Greenwood Village, CO: Thomsen Healthcare; 2013.
2. ^{{cite web |title=Famotidine Use During Pregnancy |url=https://www.drugs.com/pregnancy/famotidine.html |website=Drugs.com |accessdate=3 March 2019 |language=en}}
3. ^1 2 3 4 5 6 {{cite web |title=Famotidine Monograph for Professionals |url=https://www.drugs.com/monograph/famotidine.html |website=Drugs.com |publisher=American Society of Health-System Pharmacists |accessdate=3 March 2019 |language=en}}
4. ^{{cite book |last1=Fischer |first1=Jnos |last2=Ganellin |first2=C. Robin |title=Analogue-based Drug Discovery |date=2006 |publisher=John Wiley & Sons |isbn=9783527607495 |page=444 |url=https://books.google.ca/books?id=FjKfqkaKkAAC&pg=PA444 |language=en}}
5. ^1 2 {{cite book|title=British national formulary : BNF 76|date=2018|publisher=Pharmaceutical Press|isbn=9780857113382|pages=74-75|edition=76}}
6. ^{{cite web |title=NADAC as of 2019-02-27 |url=https://data.medicaid.gov/Drug-Pricing-and-Payment/NADAC-as-of-2019-02-27/s7c9-pfa6 |website=Centers for Medicare and Medicaid Services |accessdate=3 March 2019 |language=en}}
7. ^{{cite web |title=The Top 300 of 2019 |url=https://clincalc.com/DrugStats/Top300Drugs.aspx |website=clincalc.com |accessdate=22 December 2018}}
8. ^{{cite journal|last1=Kanayama|first1=S|title=Proton-pump inhibitors versus H2-receptor antagonists in triple therapy for Helicobacter pylori eradication |journal=Nihon Rinsho. Japanese Journal of Clinical Medicine |date=January 1999|volume=57|issue=1|pages=153–6|pmid=10036954}}
9. ^{{cite journal|last1=Soga|first1=T|last2=Matsuura|first2=M|last3=Kodama|first3=Y|last4=Fujita|first4=T|last5=Sekimoto|first5=I|last6=Nishimura|first6=K|last7=Yoshida|first7=S|last8=Kutsumi|first8=H|last9=Fujimoto|first9=S|title=Is a proton pump inhibitor necessary for the treatment of lower-grade reflux esophagitis?|journal=Journal of Gastroenterology|date=August 1999|volume=34|issue=4|pages=435–40|pmid=10452673|doi=10.1007/s005350050292}}
10. ^{{cite journal|last1=Borody|first1=TJ|last2=Andrews|first2=P|last3=Fracchia|first3=G|last4=Brandl|first4=S|last5=Shortis|first5=NP|last6=Bae|first6=H|title=Omeprazole enhances efficacy of triple therapy in eradicating Helicobacter pylori.|journal=Gut|date=October 1995|volume=37|issue=4|pages=477–81|pmid=7489931|doi=10.1136/gut.37.4.477|pmc=1382896}}
11. ^{{cite journal|last1=Hu|first1=FL|last2=Jia|first2=JC|last3=Li|first3=YL|last4=Yang|first4=GB|title=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.|journal=The Journal of International Medical Research|date=2003|volume=31|issue=6|pages=469–74|pmid=14708410|doi=10.1177/147323000303100601}}
12. ^{{cite journal|last1=Kirika|first1=NV|last2=Bodrug|first2=NI|last3=Butorov|first3=IV|last4=Butorov|first4=SI|title=[Efficacy of different schemes of anti-helicobacter therapy in duodenal ulcer].|journal=Terapevticheskii Arkhiv|date=2004|volume=76|issue=2|pages=18–22|pmid=15106408}}
13. ^{{cite journal|last1=Fujiwara|first1=Y|last2=Higuchi|first2=K|last3=Nebiki|first3=H|last4=Chono|first4=S|last5=Uno|first5=H|last6=Kitada|first6=K|last7=Satoh|first7=H|last8=Nakagawa|first8=K|last9=Kobayashi|first9=K|last10=Tominaga|first10=K|last11=Watanabe|first11=T|last12=Oshitani|first12=N|last13=Arakawa|first13=T|title=Famotidine vs. omeprazole: a prospective randomized multicentre trial to determine efficacy in non-erosive gastro-oesophageal reflux disease.|journal=Alimentary Pharmacology & Therapeutics|date=June 2005|volume=21 Suppl 2|pages=10–8|pmid=15943841|doi=10.1111/j.1365-2036.2005.02468.x}}
14. ^{{cite journal|last1=La Corte|first1=R|last2=Caselli|first2=M|last3=Castellino|first3=G|last4=Bajocchi|first4=G|last5=Trotta|first5=F|title=Prophylaxis and treatment of NSAID-induced gastroduodenal disorders.|journal=Drug Safety|date=June 1999|volume=20|issue=6|pages=527–43|pmid=10392669|doi=10.2165/00002018-199920060-00006}}
15. ^{{cite journal|last1=Laine|first1=L|last2=Kivitz|first2=AJ|last3=Bello|first3=AE|last4=Grahn|first4=AY|last5=Schiff|first5=MH|last6=Taha|first6=AS|title=Double-blind randomized trials of single-tablet ibuprofen/high-dose famotidine vs. ibuprofen alone for reduction of gastric and duodenal ulcers.|journal=The American Journal of Gastroenterology|date=March 2012|volume=107|issue=3|pages=379–86|doi=10.1038/ajg.2011.443|pmid=22186979|pmc=3321505}}
16. ^{{cite journal|last1=Escolano|first1=F|last2=Castaño|first2=J|last3=López|first3=R|last4=Bisbe|first4=E|last5=Alcón|first5=A|title=Effects of omeprazole, ranitidine, famotidine and placebo on gastric secretion in patients undergoing elective surgery.|journal=British Journal of Anaesthesia|date=October 1992|volume=69|issue=4|pages=404–6|pmid=1419452|doi=10.1093/bja/69.4.404}}
17. ^{{cite journal|last1=Vila|first1=P|last2=Vallès|first2=J|last3=Canet|first3=J|last4=Melero|first4=A|last5=Vidal|first5=F|title=Acid aspiration prophylaxis in morbidly obese patients: famotidine vs. ranitidine.|journal=Anaesthesia|date=November 1991|volume=46|issue=11|pages=967–9|pmid=1750602|doi=10.1111/j.1365-2044.1991.tb09860.x}}
18. ^{{cite journal|last1=Jahr|first1=JS|last2=Burckart|first2=G|last3=Smith|first3=SS|last4=Shapiro|first4=J|last5=Cook|first5=DR|title=Effects of famotidine on gastric pH and residual volume in pediatric surgery.|journal=Acta Anaesthesiologica Scandinavica|date=July 1991|volume=35|issue=5|pages=457–60|pmid=1887750|doi=10.1111/j.1399-6576.1991.tb03328.x}}
19. ^{{cite web|url=http://www.petmd.com/pet-medication/famotidine|title=Famotidine|publisher=}}
20. ^{{cite web | url = http://www.bestbets.org/bets/bet.php?id=353 | title = Combination therapy with H2 and H1 antihistamines in acute, non compromising allergic reactions | author = Fogg TB, Semple D | date = 29 November 2007 | work = BestBets | publisher = Manchester Royal Infirmary | location = Manchester, England | accessdate = 26 April 2011 }}
21. ^{{Cite web|url=https://www.rxlist.com/pepcid-side-effects-drug-center.htm|title=Common Side Effects of Pepcid (Famotidine) Drug Center|website=RxList|language=en|access-date=2019-03-02}}
22. ^{{Cite web|url=https://www.webmd.com/drugs/2/drug-5035-2033/famotidine-oral/famotidine-oral/details|title=Drugs & Medications|website=www.webmd.com|language=en|access-date=2019-03-02}}
23. ^{{cite journal | author = Humphries TJ, Merritt GJ | title = Review article: drug interactions with agents used to treat acid-related diseases | journal = Aliment. Pharmacol. Ther. |date=August 1999 | volume = 13 | issue = Suppl 3 | pages = 18–26 | pmid = 10491725 | doi = 10.1046/j.1365-2036.1999.00021.x }}
24. ^{{US patent reference |number=4283408 |issue-date=11 August 1981 |inventor=Yasufumi Hirata, Isao Yanagisawa, Yoshio Ishii, Shinichi Tsukamoto, Noriki Ito, Yasuo Isomura and Masaaki Takeda | title = Guanidinothiazole compounds, process for preparation and gastric inhibiting compositions containing them }}
25. ^{{cite web|url=http://mediwire.skyscape.com/main/Default.aspx?P=Content&ArticleID=23882 |title=Sankyo Pharma |publisher=Skyscape Mediwire |year=2002 |accessdate=31 October 2009 |deadurl=yes |archiveurl=https://web.archive.org/web/20090223125527/http://mediwire.skyscape.com/main/Default.aspx?P=Content&ArticleID=23882 |archivedate=23 February 2009 }}
26. ^{{cite journal|last1=Howard|first1=JM|last2=Chremos|first2=AN|last3=Collen|first3=MJ|last4=McArthur|first4=KE|last5=Cherner|first5=JA|last6=Maton|first6=PN|last7=Ciarleglio|first7=CA|last8=Cornelius|first8=MJ|last9=Gardner|first9=JD|last10=Jensen|first10=RT|title=Famotidine, a new, potent, long-acting histamine H2-receptor antagonist: comparison with cimetidine and ranitidine in the treatment of Zollinger-Ellison syndrome.|journal=Gastroenterology|date=April 1985|volume=88|issue=4|pages=1026–33|pmid=2857672}}
27. ^{{cite web|url=http://www.medicines.org.uk/emc/medicine/20012|title=PepcidTwo Chewable Tablet|accessdate=7 June 2015}}
28. ^{{cite web |url =http://www.farmavita.net/content/view/1012/84/ |title = Formulation and Evaluation of Gastroretentive Floating Tablets of Famotidine |year = 2008 |accessdate=31 January 2009 |publisher = Farmavita.Net}}
29. ^Pepcid Complete
30. ^{{cite web|url=https://www.nlm.nih.gov/medlineplus/druginfo/meds/a687011.html|title=Famotidine|publisher=}}
31. ^Drugs.com {{Drugs.com|parent|duexis}}
{{-}}{{Histaminergics}}{{Drugs for peptic ulcer and GORD}}

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