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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2015/07/09 11:11:33」(JST)

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Famotidine (/fəˈmɒtɪdiːn/l trade name Pepcid) is a histamine H₂-receptor antagonist that inhibits stomach acid production. It is commonly used in the treatment of peptic ulcer disease and gastroesophageal reflux disease. 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.^[2]

Medical use

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 (GERD)
Treatment for Esophagitis
Part of a multidrug regimen for H. pylori eradication, although omeprazole may be somewhat more effective.^[3]^[4]^[5]^[6]^[7]^[8]
Prevention of NSAID induced peptic ulcers.^[9]^[10]
Given to surgery patients before operations to reduce the risk of aspiration pneumonitis.^[11]^[12]^[13]

Famotidine is also given to dogs and cats with acid reflux.^[14] Famotidine has been used in combination with an H1 antagonist to treat and prevent urticaria caused by an acute allergic reaction.^[15]

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,^[16]^[17] are available OTC. Larger doses still require a prescription.

Side effects

Side effects associated with famotidine use include headache, dizziness, and constipation or diarrhea.^[18]

History

Famotidine was developed by Yamanouchi Pharmaceutical Co.^[19] It was licensed in the mid-80s by Merck & Co.^[20] 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 9 times more potent than ranitidine, and 32 times more potent than cimetidine.^[21]

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.^[22]

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.^[23]

Research

Famotidine has been investigated as an adjunct in treatment-resistant schizophrenia. In one trial, it caused a 10% reduction in schizophrenic symptom severity in treatment-resistant patients.^[24]

References

^ ^a ^b ^c ^d Truven Health Analytics, Inc. DRUGDEX® System (Internet) [cited 2013 Oct 10]. Greenwood Village, CO: Thomsen Healthcare; 2013.
^ Humphries TJ, Merritt GJ (August 1999). "Review article: drug interactions with agents used to treat acid-related diseases" (PDF). Aliment. Pharmacol. Ther. 13 (Suppl 3): 18–26. doi:10.1046/j.1365-2036.1999.00021.x. PMID 10491725.
^ Kanayama, S (January 1999). "[Proton-pump inhibitors versus H2-receptor antagonists in triple therapy for Helicobacter pylori eradication].". Nihon rinsho. Japanese journal of clinical medicine 57 (1): 153–6. PMID 10036954.
^ Soga, T; Matsuura, M; Kodama, Y; Fujita, T; Sekimoto, I; Nishimura, K; Yoshida, S; Kutsumi, H; Fujimoto, S (August 1999). "Is a proton pump inhibitor necessary for the treatment of lower-grade reflux esophagitis?". Journal of gastroenterology 34 (4): 435–40. PMID 10452673.
^ Borody, TJ; Andrews, P; Fracchia, G; Brandl, S; Shortis, NP; Bae, H (October 1995). "Omeprazole enhances efficacy of triple therapy in eradicating Helicobacter pylori.". Gut 37 (4): 477–81. PMID 7489931.
^ Hu, FL; Jia, JC; Li, YL; Yang, GB (2003). "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 31 (6): 469–74. PMID 14708410.
^ Kirika, NV; Bodrug, NI; Butorov, IV; Butorov, SI (2004). "[Efficacy of different schemes of anti-helicobacter therapy in duodenal ulcer].". Terapevticheskii arkhiv 76 (2): 18–22. PMID 15106408.
^ Fujiwara, Y; Higuchi, K; Nebiki, H; Chono, S; Uno, H; Kitada, K; Satoh, H; Nakagawa, K; Kobayashi, K; Tominaga, K; Watanabe, T; Oshitani, N; Arakawa, T (June 2005). "Famotidine vs. omeprazole: a prospective randomized multicentre trial to determine efficacy in non-erosive gastro-oesophageal reflux disease.". Alimentary pharmacology & therapeutics. 21 Suppl 2: 10–8. PMID 15943841.
^ La Corte, R; Caselli, M; Castellino, G; Bajocchi, G; Trotta, F (June 1999). "Prophylaxis and treatment of NSAID-induced gastroduodenal disorders.". Drug safety 20 (6): 527–43. PMID 10392669.
^ Laine, L; Kivitz, AJ; Bello, AE; Grahn, AY; Schiff, MH; Taha, AS (March 2012). "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 107 (3): 379–86. doi:10.1038/ajg.2011.443. PMID 22186979.
^ Escolano, F; Castaño, J; López, R; Bisbe, E; Alcón, A (October 1992). "Effects of omeprazole, ranitidine, famotidine and placebo on gastric secretion in patients undergoing elective surgery.". British journal of anaesthesia 69 (4): 404–6. PMID 1419452.
^ Vila, P; Vallès, J; Canet, J; Melero, A; Vidal, F (November 1991). "Acid aspiration prophylaxis in morbidly obese patients: famotidine vs. ranitidine.". Anaesthesia 46 (11): 967–9. PMID 1750602.
^ Jahr, JS; Burckart, G; Smith, SS; Shapiro, J; Cook, DR (July 1991). "Effects of famotidine on gastric pH and residual volume in pediatric surgery.". Acta anaesthesiologica Scandinavica 35 (5): 457–60. PMID 1887750.
^ http://www.petmd.com/pet-medication/famotidine. Missing or empty |title= (help)
^ Fogg TB, Semple D (29 November 2007). "Combination therapy with H2 and H1 antihistamines in acute, non compromising allergic reactions". BestBets. Manchester, England: Manchester Royal Infirmary. Retrieved 26 April 2011.
^ Pepcid Complete
^ http://www.nlm.nih.gov/medlineplus/druginfo/meds/a687011.html. Missing or empty |title= (help)
^ "Pepcid Side Effects & Drug Interactions". RxList.com. 2008. Retrieved 2008-07-31.
^ US patent 4283408, HIRATA YASUFUMI; YANAGISAWA ISAO; ISHII YOSHIO; TSUKAMOTO SHINICHI; ITO NORIKI; ISOMURA YASUO; TAKEDA MASAAKI, "Guanidinothiazole compounds, process for preparation and gastric inhibiting compositions containing them", issued 1981-08-11
^ "Sankyo Pharma". Skyscape Mediwire. 2002. Retrieved 2009-10-30. ^{[dead link]}
^ Howard, JM; Chremos, AN; Collen, MJ; McArthur, KE; Cherner, JA; Maton, PN; Ciarleglio, CA; Cornelius, MJ; Gardner, JD; Jensen, RT (April 1985). "Famotidine, a new, potent, long-acting histamine H2-receptor antagonist: comparison with cimetidine and ranitidine in the treatment of Zollinger-Ellison syndrome.". Gastroenterology 88 (4): 1026–33. PMID 2857672.
^ http://www.medicines.org.uk/emc/medicine/20012. Retrieved 7 June 2015. Missing or empty |title= (help)
^ "Formulation and Evaluation of Gastroretentive Floating Tablets of Famotidine". Farmavita.Net. 2008. Retrieved 2009-01-30.
^ Meskanen, K; Ekelund, H; Laitinen, J; Neuvonen, PJ; Haukka, J; Panula, P; Ekelund, J (August 2013). "A randomized clinical trial of histamine 2 receptor antagonism in treatment-resistant schizophrenia.". Journal of Clinical Psychopharmacology 33 (4): 472–478. doi:10.1097/JCP.0b013e3182970490. PMID 23764683.

UpToDate Contents

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1. 抗潰瘍剤の薬理学 pharmacology of antiulcer medications
2. 血清クレアチニン濃度を上昇させる剤 drugs that elevate the serum creatinine concentration
3. 小児および思春期における胃食道逆流症のマネージメント management of gastroesophageal reflux disease in children and adolescents
4. 非ステロイド性抗炎症剤（NSAIDs）（アスピリンを含む）：胃十二指腸障害の二次予防 nsaids including aspirin secondary prevention of gastroduodenal toxicity
5. 集中治療室（ICU）におけるストレス潰瘍の予防 stress ulcer prophylaxis in the intensive care unit

English Journal

An Efficient Ion-Pair Liquid Chromatographic Method for the Determination of Some H2 Receptor Antagonists.

Elshaboury SR1, Mohamed NA1, Ahmed S2, Farrag S1.
Journal of chromatographic science.J Chromatogr Sci.2016 Mar;54(3):419-28. doi: 10.1093/chromsci/bmv159. Epub 2015 Nov 3.
A simple, efficient and reliable ion-pair chromatography (IPC) method was developed and validated for the determination of some H2 receptor antagonists including ranitidine (RAN), nizatidine (NIZ) and famotidine (FAM). The use of IPC separations provided improved peak resolution with good peak shape
PMID 26538490

Central histaminergic system interplay with suppressive effects of immune challenge on food intake in chicken.

Zendehdel M1, Baghbanzadeh A1, Aghelkohan P1, Hassanpour S2.
British poultry science.Br Poult Sci.2016 Feb 29. [Epub ahead of print]
1. The aim of the current study was to investigate the interaction of the lipopolysaccharide and histaminergic systems on appetite regulation in broilers. Effects of intracerebroventricular (ICV) injection of α-fluoromethylhistidine (α-FMH, histidine decarboxylase inhibitor), chlorpheniramine (his
PMID 26924422

Positive regulation of the enzymatic activity of gastric H+,K+-ATPase by sialylation of its β-subunit.

Fujii T1, Watanabe M1, Shimizu T1, Takeshima H2, Kushiro K3, Takai M3, Sakai H4.
Biochimica et biophysica acta.Biochim Biophys Acta.2016 Feb 26. pii: S0005-2736(16)30067-0. doi: 10.1016/j.bbamem.2016.02.029. [Epub ahead of print]
The gastric proton pump (H+,K+-ATPase) consists of a catalytic α-subunit (αHK) and a glycosylated β-subunit (βHK). βHK glycosylation is essential for the apical trafficking and stability of αHK in gastric parietal cells. Here, we report the properties of sialic acids at the termini of the olig
PMID 26922883

Related Pictures

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★リンクテーブル★

リンク元

「ファモチジン」

Famotidine
Systematic (IUPAC) name
	3-[({2-[(diaminomethylidene)amino]-1,3-thiazol-4-yl}methyl)sulfanyl]-N'-sulfamoylpropanimidamide
Clinical data
Trade names	Pepcid
AHFS/Drugs.com	monograph
MedlinePlus	a687011
Licence data	US FDA:link
Pregnancy; category	B1 (Au), B (U.S.);
Legal status	Pharmacist only S3/S4(AU), General Availability (OTC)(UK),; Over the Counter(US);
Routes of; administration	Oral (tablet form)
Pharmacokinetic data
Bioavailability	40-45% (Oral)
Protein binding	15-20%
Metabolism	hepatic
Biological half-life	2.5-3.5 hours
Excretion	Renal (25-30% unchanged [Oral])
Identifiers
CAS Registry Number	76824-35-6
ATC code	A02BA03
PubChem	CID: 3325
IUPHAR/BPS	7074
DrugBank	DB00927
ChemSpider	3208
UNII	5QZO15J2Z8
KEGG	D00318
ChEBI	CHEBI:4975
ChEMBL	CHEMBL902
Chemical data
Formula	C8H15N7O2S3
Molecular mass	337.449 g/mol
	SMILES O=S(=O)(N=C(N)CCSCc1nc(/N=C(/N)N)sc1)N ;
	InChI InChI=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) ; Key:XUFQPHANEAPEMJ-UHFFFAOYSA-N ;
(what is this?) (verify)

　　[★]

英: famotidine
商: ガスイサン、ガスセプト、ガスター、ガスドック、ガスペラジン、ガスポート、ガスメット、ガスリック、ガモファー、クリマーゲン、ストマルコン、チオスター、ファモガスト、ファモスタジン、ブロスター、モミアロン、Pepcid
関: ヒスタミン受容体、消化性潰瘍用剤

消化性潰瘍治療薬

攻撃因子抑制剤

H2ブロッカー = ヒスタミンH2受容体選択的阻害薬

持続時間が長い(1日2,3回でよい)
般試薬で10mg錠、臨床薬では20mg錠

用量調節

腎機能障害がある場合に血中未変化体濃度が上昇しうるため、用量の調節が必要である。

Ccr(mL/min)	投与方法
≧60	1日20mg 1日2回
60＞　＞30	1日20mg 1日1回
60＞　＞30	1日10mg 1日2回
30≧	2-3日20mg 1日1回
30≧	1日10mg 1日1回

副作用

無顆粒症、心室細動、不全収縮、間質性肺炎、腎炎

[DP-1] Truven Health Analytics, Inc. DRUGDEX® System (Internet) [cited 2013 Oct 10]. Greenwood Village, CO: Thomsen Healthcare; 2013.

[2] Humphries TJ, Merritt GJ (August 1999). "Review article: drug interactions with agents used to treat acid-related diseases" (PDF). Aliment. Pharmacol. Ther. 13 (Suppl 3): 18–26. doi:10.1046/j.1365-2036.1999.00021.x. PMID 10491725.

[3] Kanayama, S (January 1999). "[Proton-pump inhibitors versus H2-receptor antagonists in triple therapy for Helicobacter pylori eradication].". Nihon rinsho. Japanese journal of clinical medicine 57 (1): 153–6. PMID 10036954.

[4] Soga, T; Matsuura, M; Kodama, Y; Fujita, T; Sekimoto, I; Nishimura, K; Yoshida, S; Kutsumi, H; Fujimoto, S (August 1999). "Is a proton pump inhibitor necessary for the treatment of lower-grade reflux esophagitis?". Journal of gastroenterology 34 (4): 435–40. PMID 10452673.

[5] Borody, TJ; Andrews, P; Fracchia, G; Brandl, S; Shortis, NP; Bae, H (October 1995). "Omeprazole enhances efficacy of triple therapy in eradicating Helicobacter pylori.". Gut 37 (4): 477–81. PMID 7489931.

[6] Hu, FL; Jia, JC; Li, YL; Yang, GB (2003). "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 31 (6): 469–74. PMID 14708410.

[7] Kirika, NV; Bodrug, NI; Butorov, IV; Butorov, SI (2004). "[Efficacy of different schemes of anti-helicobacter therapy in duodenal ulcer].". Terapevticheskii arkhiv 76 (2): 18–22. PMID 15106408.

[8] Fujiwara, Y; Higuchi, K; Nebiki, H; Chono, S; Uno, H; Kitada, K; Satoh, H; Nakagawa, K; Kobayashi, K; Tominaga, K; Watanabe, T; Oshitani, N; Arakawa, T (June 2005). "Famotidine vs. omeprazole: a prospective randomized multicentre trial to determine efficacy in non-erosive gastro-oesophageal reflux disease.". Alimentary pharmacology & therapeutics. 21 Suppl 2: 10–8. PMID 15943841.

[9] La Corte, R; Caselli, M; Castellino, G; Bajocchi, G; Trotta, F (June 1999). "Prophylaxis and treatment of NSAID-induced gastroduodenal disorders.". Drug safety 20 (6): 527–43. PMID 10392669.

[10] Laine, L; Kivitz, AJ; Bello, AE; Grahn, AY; Schiff, MH; Taha, AS (March 2012). "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 107 (3): 379–86. doi:10.1038/ajg.2011.443. PMID 22186979.

[11] Escolano, F; Castaño, J; López, R; Bisbe, E; Alcón, A (October 1992). "Effects of omeprazole, ranitidine, famotidine and placebo on gastric secretion in patients undergoing elective surgery.". British journal of anaesthesia 69 (4): 404–6. PMID 1419452.

[12] Vila, P; Vallès, J; Canet, J; Melero, A; Vidal, F (November 1991). "Acid aspiration prophylaxis in morbidly obese patients: famotidine vs. ranitidine.". Anaesthesia 46 (11): 967–9. PMID 1750602.

[13] Jahr, JS; Burckart, G; Smith, SS; Shapiro, J; Cook, DR (July 1991). "Effects of famotidine on gastric pH and residual volume in pediatric surgery.". Acta anaesthesiologica Scandinavica 35 (5): 457–60. PMID 1887750.

[14] ttp://www.petmd.com/pet-medication/famotidine. Missing or empty |title= (help)

[15] Fogg TB, Semple D (29 November 2007). "Combination therapy with H2 and H1 antihistamines in acute, non compromising allergic reactions". BestBets. Manchester, England: Manchester Royal Infirmary. Retrieved 26 April 2011.

[16] Pepcid Complete

[17] ttp://www.nlm.nih.gov/medlineplus/druginfo/meds/a687011.html. Missing or empty |title= (help)

[18] "Pepcid Side Effects & Drug Interactions". RxList.com. 2008. Retrieved 2008-07-31.

[19] US patent 4283408, HIRATA YASUFUMI; YANAGISAWA ISAO; ISHII YOSHIO; TSUKAMOTO SHINICHI; ITO NORIKI; ISOMURA YASUO; TAKEDA MASAAKI, "Guanidinothiazole compounds, process for preparation and gastric inhibiting compositions containing them", issued 1981-08-11

[20] "Sankyo Pharma". Skyscape Mediwire. 2002. Retrieved 2009-10-30. ^{[dead link]}

[21] Howard, JM; Chremos, AN; Collen, MJ; McArthur, KE; Cherner, JA; Maton, PN; Ciarleglio, CA; Cornelius, MJ; Gardner, JD; Jensen, RT (April 1985). "Famotidine, a new, potent, long-acting histamine H2-receptor antagonist: comparison with cimetidine and ranitidine in the treatment of Zollinger-Ellison syndrome.". Gastroenterology 88 (4): 1026–33. PMID 2857672.

[22] ttp://www.medicines.org.uk/emc/medicine/20012. Retrieved 7 June 2015. Missing or empty |title= (help)

[23] "Formulation and Evaluation of Gastroretentive Floating Tablets of Famotidine". Farmavita.Net. 2008. Retrieved 2009-01-30.

[24] Meskanen, K; Ekelund, H; Laitinen, J; Neuvonen, PJ; Haukka, J; Panula, P; Ekelund, J (August 2013). "A randomized clinical trial of histamine 2 receptor antagonism in treatment-resistant schizophrenia.". Journal of Clinical Psychopharmacology 33 (4): 472–478. doi:10.1097/JCP.0b013e3182970490. PMID 23764683.

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