Wikipedia

Famotidine

"Cepal" redirects here. For the international organization, seeUnited Nations Economic Commission for Latin America and the Caribbean.

Famotidine,sold under the brand namePepcidamong others, is ahistamine H2receptor antagonistmedication that decreasesstomach acidproduction.[4]It is used to treatpeptic ulcer disease,gastroesophageal reflux disease,andZollinger-Ellison syndrome.[4]It is takenby mouthor byinjection into a vein.[4]It begins working within an hour.[4]

Famotidine
Clinical data
Pronunciation/fəˈmɒtɪdiːn/
Trade namesPepcid, Zantac 360, others
AHFS/DrugsMonograph
MedlinePlusa687011
License data
Pregnancy
category
Routes of
administration		By mouth,intravenous
ATC code
Legal status
Legal status
Pharmacokineticdata
Bioavailability40–45% (by mouth)[2]
Protein binding15–20%[2]
Eliminationhalf-life2.5–3.5 hours[2]
ExcretionKidney(25–30% unchanged [Oral])[2]
Identifiers
  • 3-[({2-[(diaminomethylidene)amino]-1,3-thiazol-4-yl}methyl)sulfanyl]-N-sulfamoylpropanimidamide
CAS Number
PubChemCID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
PDB ligand
CompTox Dashboard(EPA)
ECHA InfoCard100.116.793Edit this at Wikidata
Chemical and physical data
FormulaC8H15N7O2S3
Molar mass337.44g·mol−1
3D model (JSmol)
  • NS(=O)(=O)/N=C(\N)CCSCc1csc(n1)N=C(N)N
  • 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)checkY
  • Key:XUFQPHANEAPEMJ-UHFFFAOYSA-NcheckY
(verify)

Common side effects include headache, intestinal upset, and dizziness.[4]Serious side effects may includepneumoniaandseizures.[4][5]Use inpregnancyappears safe but has not been well studied, while use duringbreastfeedingis not recommended.[1]

Famotidine was patented in 1979 and came into medical use in 1985.[6]It is available as ageneric medication.[5]In 2022, it was the 49th most commonly prescribed medication in the United States, with more than 13million prescriptions.[7][8]

Medical uses

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Pharmacokinetics

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Famotidine has a delayed onset of action, beginning after 90 minutes. However, famotidine has a duration of effect of at least 540 minutes (9.0 h). At its peak effect, 210 minutes (3.5 h) after administration, famotidine reduces acid secretion by 7.3 mmol per 30 minutes.[20]

Side effects

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The most common side effects associated with famotidine use includeheadache,dizziness,andconstipationordiarrhea.[21][22]

Famotidine may contribute toQT prolongation,[23]particularly when used with other QT-elongating drugs, or in people with poorkidney function.[24]

Mechanism of action

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Activation of H2receptors located onparietal cellsstimulatesproton pumpsto secrete acid into the stomach lumen. Famotidine, anH2antagonist,blocks the action ofhistamineon the parietal cells, ultimately reducing acid secretion into the stomach.

Interactions

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Unlikecimetidine,the first H2antagonist, famotidine has a minimal effect on thecytochrome P450enzyme system, and does not appear to interact with as many drugs as other medications in its class. Some exceptions include antiretrovirals such as atazanavir, chemotherapeutics such as doxorubicin, and antifungal medications such as itraconazole.[25][26][27]

History

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Famotidine was developed byYamanouchi PharmaceuticalCo.[28]It was licensed in the mid-1980s byMerck & Co.[29]and is marketed by a joint venture between Merck and Johnson & Johnson. Theimidazolering of cimetidine was replaced with a 2-guanidinothiazole ring. Famotidine proved to be nine times more potent thanranitidine,and thirty-two times more potent thancimetidine.[30]

It was first marketed in 1981. Pepcid RPDorally disintegrating tabletswere 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 calledPepcid Complete,which combines famotidine with anantacidin a chewable tablet to quickly relieve the symptoms of excess stomach acid, is available. In the UK, this product was known as PepcidTwo until its discontinuation in April 2015.[31]

Famotidine has poorbioavailibility(50%) due to low gastroretention time. Famotidine is less soluble at higher pH, and when used in combination with antacids gastroretention time is increased. This promotes local delivery of these drugs to receptors in the parietal cell membrane and increases bioavailibility. Researchers are developing tablet formulations that rely on other gastroretentive drug delivery systems such as floating tablets to further increase bioavailibility.[32]

Society and culture

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Certain preparations of famotidine are availableover the counter(OTC) in various countries. In the United States and Canada, 10 mg and 20 mg tablets, sometimes in combination with anantacid,[33][34]are available OTC. Larger doses still require a prescription.

Formulations of famotidine in combination withibuprofenwere marketed byHorizon Pharmaunder the trade name Duexis.[35]

Research

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COVID-19

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At the start of theCOVID-19 pandemic,some doctors observed that anecdotally some hospitalized patients in China may have had better outcomes on famotidine than other patients that were not taking famotidine. This led to hypotheses about use of famotidine in treatment of COVID-19.[36][37]Famotidine was considered a possible treatment for COVID-19 due to its potential anti-inflammatory effects. It was thought that famotidine could modify lung inflammation caused by coronaviruses. However, studies have shown that famotidine is not effective in reducing mortality or improving recovery in COVID-19 patients.[38]Famotidine primarily works by blocking the effects of histamine and has some potential mechanisms of action that may contribute to its anti-inflammatory properties, including the inhibition of the production of certain pro-inflammatory cytokines such asTNF- AlphaandIL-6.[39][40]Another hypothesis was that famotidine might activate thevagus nerveinflammatory reflex to attenuate cytokine storm.[40]Yet another hypothesis was that famotidine can reduce the activation ofmast cellsand the subsequent release ofinflammatory mediators,therefore acting as amast cell stabilizer.[41][39]However, while famotidine may have some anti-inflammatory effects, there is currently insufficient evidence to support its use for treating inflammation associated with COVID-19.[38]Therefore, it is not recommended for this purpose.[42]

Other

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Small-scale studies have shown inconsistent and inconclusive evidence of efficacy in treatment-refractoryschizophrenia.[43]

Veterinary uses

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Famotidine is given to dogs and cats with acid reflux.[44]

References

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