Famotidine

Histamine H2-receptor antagonist CAS# 76824-35-6

Famotidine

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Quality Control of Famotidine

Number of papers citing our products

Chemical structure

Famotidine

3D structure

Chemical Properties of Famotidine

Cas No. 76824-35-6 SDF Download SDF
PubChem ID 5702160 Appearance Powder
Formula C8H15N7O2S3 M.Wt 337.45
Type of Compound N/A Storage Desiccate at -20°C
Solubility DMSO : ≥ 100 mg/mL (296.34 mM)
H2O : < 0.1 mg/mL (insoluble)
*"≥" means soluble, but saturation unknown.
Chemical Name 3-[[2-(diaminomethylideneamino)-1,3-thiazol-4-yl]methylsulfanyl]-N'-sulfamoylpropanimidamide
SMILES NC(N)=Nc1scc(CSCCC(N)=N[S](N)(=O)=O)n1
Standard InChIKey XUFQPHANEAPEMJ-UHFFFAOYSA-N
Standard 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)
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of Famotidine

DescriptionFamotidine is a competitive histamine H2-receptor antagonist. Its main pharmacodynamic effect is the inhibition of gastric secretion. Target: Histamine H2 Receptor Famotidine is a histamine H2-receptor antagonist that inhibits stomach acid production, and it is commonly used in the treatment of peptic ulcer disease (PUD) and gastroesophageal reflux disease (GERD/GORD). Famotidine Group(2 mg/kg/day) were significantly lower than the equivalent parameters for the Control Group on both the third and seventh days post-surgery. famotidine exerts detrimental effects on the anastomotic bursting pressure and hydroxyproline content of perianastomotic tissues in the colon of rats [1]. famotidine increased the transgastric potential difference (PD) and promoted the recovery of decreased transgastric PD induced by acidified ethanol in rats. The preventive effect of famotidine on gastric lesions is attributable not only to suppression of acid secretion but to activation of the gastric mucosal defensive mechanisms [2].

References:
[1]. Inan, A., et al., Effects of the histamine H2 receptor antagonist famotidine on the healing of colonic anastomosis in rats. Clinics (Sao Paulo), 2009. 64(6): p. 567-70. [2]. Miyata, K., et al., Studies on the mechanism for the gastric mucosal protection by famotidine in rats. Jpn J Pharmacol, 1991. 55(2): p. 211-22.

Famotidine Dilution Calculator

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Famotidine Molarity Calculator

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Preparing Stock Solutions of Famotidine

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.9634 mL 14.817 mL 29.634 mL 59.268 mL 74.085 mL
5 mM 0.5927 mL 2.9634 mL 5.9268 mL 11.8536 mL 14.817 mL
10 mM 0.2963 mL 1.4817 mL 2.9634 mL 5.9268 mL 7.4085 mL
50 mM 0.0593 mL 0.2963 mL 0.5927 mL 1.1854 mL 1.4817 mL
100 mM 0.0296 mL 0.1482 mL 0.2963 mL 0.5927 mL 0.7409 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on Famotidine

Famotidine is a competitive histamine H2-receptor antagonist. Its main pharmacodynamic effect is the inhibition of gastric secretion.Famotidine is a histamine H2-receptor antagonist that inhibits stomach acid production, and it is commonly used in the tre

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References on Famotidine

Repeated Famotidine Administration Results in a Diminished Effect on Intragastric pH in Dogs.[Pubmed:27906465]

J Vet Intern Med. 2017 Jan;31(1):117-123.

BACKGROUND: Famotidine is an acid suppressant commonly administered to dogs. Prolonged Famotidine use in people results in decreased efficacy, but the effect in dogs is unknown. HYPOTHESIS/OBJECTIVES: To compare the effect of repeated oral administration of Famotidine or placebo on intragastric pH and serum gastrin in dogs. We hypothesized that Famotidine would have a diminished effect on intragastric pH on day 13 compared to day 1. ANIMALS: Six healthy adult colony Beagles. METHODS: Randomized, 2-factor repeated-measures crossover design. All dogs received oral placebo or 1.0 mg/kg Famotidine q12h for 14 consecutive days. Intragastric pH monitoring was used to continuously record intragastric pH on treatment days 1-2 and 12-13. Mean pH as well as mean percentage time (MPT) that intragastric pH was >/=3 or >/=4 were compared between and within groups by analysis of variance. Serum gastrin was measured on days 0, 3, and 12 for each treatment. RESULTS: Continued administration of Famotidine resulted in a significant decrease in mean pH, MPT >/=3, and MPT >/=4 (P < .0001) on day 12 and 13. This resulted in a mean decrease in pH by 1.63 on days 12 and 13 compared to days 1 and 2. Furthermore, a mean decrease of MPT >/=3 and MPT >/=4 by 33 and 45% was observed for the same time period, respectively. CONCLUSIONS AND CLINICAL IMPORTANCE: Continued administration of Famotidine results in a diminished effect on intragastric pH in dogs. Caution is advised when recommending long-term, daily oral administration of Famotidine to dogs.

Famotidine-induced reversal of meperidine-related serotonin syndrome: a case report.[Pubmed:28367296]

Korean J Anesthesiol. 2017 Apr;70(2):221-223.

Serotonin syndrome is an unexpected fatal adverse event related to serotonergic medication. This case report is the first report describing the possible treatment effect of Famotidine on serotonin syndrome. Furthermore, this is the first case report of serotonin syndrome induced by meperidine alone in a patient with no previous history suggesting a susceptibility to serotonin syndrome. A 70-year-old male with no recent history of serotonergic drug use presented with severe serotonin syndrome following ureteroscopy, possibly due to postoperative meperidine administration. The patient's symptoms included hypertension, tachycardia, tachypnea, hyperthermia, myoclonus, diaphoresis, retching, nausea, agitation, and semicoma mentality with no pupillary light reflex. Symptoms began to subside immediately after the administration of intravenous Famotidine for prevention of aspiration pneumonia, with mental and neurological symptoms showing improvement initially, followed by autonomic symptoms. This case report suggests that the histamine type 2 receptor antagonist Famotidine may be an effective emergency treatment for serotonin syndrome.

A Rare Case of Famotidine-Induced Delirium in a Peritoneal Dialysis Patient.[Pubmed:28153970]

Perit Dial Int. 2017 1-2;37(1):118-120.

H2 receptor antagonists are commonly employed to manage gastro-esophageal reflux and peptic ulcer diseases with a very low incidence of side effects. Herein, we report an extremely rare incidence of Famotidine-induced acute confusion in a patient with end-stage renal failure. We also discuss the pharmacokinetic properties of Famotidine and its interplay with compromised renal function to result in neuropsychiatric manifestations, highlighting the importance of dosage ad ustment in individuals with renal insufficiency.

Design of PEG-grafted-PLA nanoparticles as oral permeability enhancer for P-gp substrate drug model Famotidine.[Pubmed:28151040]

J Microencapsul. 2017 Feb;34(1):91-103.

Bioavailability of oral drugs can be limited by an intestinal excretion process mediated by P-glycoprotein (P-gp). Polyethylene glycol (PEG) is a known P-gp inhibitor. Dispersion of Famotidine (a P-gp substrate) within PEGylated nanoparticles (NPs) was used to improve its oral bioavailability. In this work, we evaluated the potential impact of NPs prepared from a grafted copolymer of polylactic acid and PEG on P-gp function by studying in vitro permeability of Famotidine across Caco-2 cells. Copolymers of PEG grafted on polylactic acid (PLA) backbone (PLA-g-PEG) were synthesised with 1 mol% and 5 mol% PEG vs. lactic acid monomer using PEG 750 and 2000 Da. The polymers were used to prepare Famotidine-loaded NPs and tested in vitro on Caco-2 cells. Significant decrease in basolateral-to-apical transport of Famotidine was observed when Famotidine was encapsulated in NPs prepared from PLA-g-PEG5%. NPs prepared from PLA-g-PEG5% are promising to improve oral bioavailability of P-gp substrates.

Description

Famotidine (MK-208) is a competitive histamine H2-receptor antagonist. Its main pharmacodynamic effect is the inhibition of gastric secretion.

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