76824-35-6NC(N)=Nc1nc(CSCCC(N)=NS(N)(=O)=O)cs1XUFQPHANEAPEMJ-UHFFFAOYSA-NFamotidine is a member of guanidines, a sulfonamide and a member of 1,3-thiazoles. It has a role as a H2-receptor antagonist, an anti-ulcer drug and a P450 inhibitor.
76824-35-6DTXSID5023039CHEBI:4975Pharmaceuticals -> Listed in ZINC15
Pharmaceuticals -> Gastric and Ulcer Drugs
Pharmaceuticals
-0.64
-0.56
174.3 Ų [M+Na]+ [CCS Type: DT; Buffer gas: N2; Ionization: ESI+; Dataset: TOXCAST; Source Identifier: DTXSID5023039]
171.05 Ų [M+Na]+ [CCS Type: TW; Method: calibrated with polyalanine and drug standards]
167.2 Ų [M+H]+ [CCS Type: TW; Method: calibrated with polyalanine and drug standards]
165.9 Ų [M+H]+ [CCS Type: TW; Method: Major Mix IMS/Tof Calibration Kit (Waters)]
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Famotidine decreases the production of gastric acid, suppresses acid concentration and pepsin content, and decreases the volume of gastric secretion. Famotidine inhibits both basal and nocturnal gastric acid secretion, as well as acid secretion stimulated by food, caffeine, insulin, and pentagastrin. Famotidine has a dose-dependent therapeutic action, with the highest dose having the most extended duration of action and the highest inhibitory effect on gastric acid secretion. Following oral administration, the onset of action is within one hour, and the peak effect is reached within 1-3 hours. The duration of effect is about 10-12 hours.
Histamine acts as a local hormone that stimulates the acid output by parietal cells via a paracrine mechanism. Neuroendocrine cells called enterochromaffin-like (ECL) cells lie close to the parietal cells and regulate the basal secretion of histamine. Histamine release is also promoted from stimulation by acetylcholine and gastrin, a peptide hormone. Gastrin (G) cells release gastrin, which works on CCK<sub>2</sub> receptors on ECL cells. This action promotes the release of histamine from ECL cells. Upon release, histamine acts on H<sub>2</sub> receptors expressed on the basolateral membrane of parietal cells, leading to increased intracellular cAMP levels and activated proton pumps on parietal cells. Proton pump releases more protons into the stomach, thereby increasing the secretion of acid. In conditions that are associated with acid hypersecretion such as ulcers, there is a loss of regulation of acid secretion. Famotidine works on H<sub>2</sub> receptors and blocks the actions of histamine.
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Following oral administration, the absorption of famotidine is dose-dependent and incomplete. The oral bioavailability ranges from 40-50%, and the Cmax is reached in 1-4 hours post-dosing. While the bioavailability can be slightly increased with the intake of food and decreased by antacids, there is no clinical significance.
About 65-70% of the total administered dose of famotidine undergoes renal elimination, and 30-35% of the dose is cleared by metabolism. Following intravenous administration, about 70% of the drug is eliminated in the urine as an unchanged drug.
The steady-state volume of distribution ranges from 1.0 to 1.3 L/kg. Famotidine is found in breast milk; however, it is found in breast milk at the lowest concentrations compared to other H<sub>2</sub> receptor antagonists.
Renal clearance is 250-450 mL/min, indicating some tubular excretion. Because the renal clearance rate exceeds the glomerular filtration rate, famotidine is thought to be mainly eliminated via both glomerular filtration and renal tubular secretion.
개요Famotidine is a competitive histamine H2-receptor antagonist, and the main pharmacodynamic effect of famotidine is to cause the inhibition of gastric secretion. Famotidine on decomposition releases toxic products such as carbon oxides (CO, CO2), nitrogen oxides (NO, NO2), and sulphur oxides (SO2, SO3). Famotidine is a medication that is available both in prescription and over-the-counter forms. It is used to treat conditions related to the oesophagus, stomach, and intestines. Some specific famotidine is used for the treatment of duodenal ulcers, gastric ulcers (stomach ulcers), gastroesophageal reflux disease (GERD), and pathological hypersecretory conditions that occur when stomach acid is secreted/ produced in very large quantities, an abnormal health condition called ‘Zollinger-Ellison syndrome’.
용도Contact dermatitis from famotidine, a H2 -receptor agonist, was described in a nurse. In industry, three cases were reported due to intermediates of synthesis, 2- diamino-ethylene-amino-thiazolyl-methylenethiourea-dichloride and 4-chloromethyl-2-guanidinothiazolenitrochloride.
일반 설명Famotidine is a histamine H2-receptor antagonist, which promotes the healing of erosive esophagitis, gastric and duodenal ulcers since it inhibits the gastric acid secretion in humans.Pharmaceutical secondary standards for application in quality control, provide pharma laboratories and manufacturers with a convenient and cost-effective alternative to the preparation of in-house working standards.