|Systematic (IUPAC) name|
|Licence data||US FDA:|
|Oral (tablet form)|
|Biological half-life||2.5-3.5 hours|
|Excretion||Renal (25-30% unchanged [Oral])|
|Molecular mass||337.449 g/mol|
|(what is this?)|
Famotidine (//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.
- 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.
- Prevention of NSAID induced peptic ulcers.
- Given to surgery patients before operations to reduce the risk of aspiration pneumonitis.
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, are available OTC. Larger doses still require a medical prescription.
Famotidine was developed by Yamanouchi Pharmaceutical Co. It was licensed in the mid-80s by Merck & Co. 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.
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.
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.
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