Ranitidine bismuth citrate

Ranitidine bismuth citrate
Clinical data
Trade names	Tritec, Pylorid
Identifiers
	IUPAC name bismuth;(E)-1-N'-[2-[[5-[(dimethylamino)methyl]furan-2-yl]methylsulfanyl]ethyl]-1-N-methyl-2-nitroethene-1,1-diamine;2-hydroxypropane-1,2,3-tricarboxylate;
CAS Number	128345-62-0 ;
PubChem CID	3033887 ;
ChemSpider	2298462 ;
UNII	7AJ51I17KG ;
KEGG	D05699 ;
Chemical and physical data
Formula	C19H27BiN4O10S
Molar mass	712.48 g·mol−1
3D model (JSmol)	Interactive image ;
	SMILES CNC(=C[N+](=O)[O-])NCCSCC1=CC=C(O1)CN(C)C.C(C(=O)[O-])C(CC(=O)[O-])(C(=O)[O-])O.[Bi+3];
	InChI InChI=1S/C13H22N4O3S.C6H8O7.Bi/c1-14-13(9-17(18)19)15-6-7-21-10-12-5-4-11(20-12)8-16(2)3;7-3(8)1-6(13,5(11)12)2-4(9)10;/h4-5,9,14-15H,6-8,10H2,1-3H3;13H,1-2H2,(H,7,8)(H,9,10)(H,11,12);/q;;+3/p-3/b13-9+;;; Key:XAUTYMZTJWXZHZ-IGUOPLJTSA-K;

Last updated January 01, 2021

Ranitidine bismuth citrate - drug, which has antisecretory and bactericidal action.

Shape

Physical

Pills. The film-coated tablet contains ranitidine bismuth citrate 400 mg; in a blister 14 pcs., in a box 1, 2 or 4 blisters.

Chemical

N- / 2 - /// 5 - / (Dimethylamino) methyl / -2-furanyl / methyl / thio / ethyl / -N'-methyl-2-nitro-1,1-ethenediamine bismuth citrate.^{[ clarification needed ]}

Pharmacological properties

Antiulcer, which is mediated by two active ingredients. Ranitidine - a blocker of H₂-histamine receptors, suppresses basal and stimulated, day and night gastric acid secretion, reducing both the volume of its secretion and the concentration hydrochloric acid and pepsin are secreted. Bismuth citrate in vitro has a bactericidal effect on Helicobacter pylori, a protective effect on the gastric mucosa.

Indications

Stomach ulcer and duodenal ulcer, including those associated with Helicobacter pylori (in combination with amoxicillin or clarithromycin ohm).

Prospects for repurposing

Ranitidine bismuth citrate may also be effective against coronavirus and SARS-CoV-2, since it exhibits low cytotoxicity and is able to protect cells from infection with the SARS-CoV-2 virus, with a selectivity index of several times higher than that of remdesivir a. This is due to the fact that it inhibits the activity required for viral replication helicase Nsp13 SARS-CoV-2 due to irreversible displacement of zinc (II) ions from enzyme and bismuth ions ( III)^[1]

Contraindications

Hypersensitivity, acute porphyria, chronic renal failure (CC less than 25 ml / min), childhood (up to 14 years), pregnancy, lactation.

Side effects

From the digestive system: gastralgia, diarrhea or constipation, increased activity of "hepatic" transaminases, hepatitis (hepatocellular, cholestatic or mixed, with or without jaundice, usually reversible), acute pancreatitis. From the side of the cardiovascular system: decrease BP, bradycardia, AV block, chest pain, asystole (with injection). On the part of the hematopoietic organs: anemia, leukopenia, thrombocytopenia, agranulocytosis, pancytopenia, aplasia bone marrow. From the nervous system and sensory organs: headache, dizziness, depression, hallucinations, in severe and elderly patients - impaired visual perception (associated with a violation of accommodation); violation of taste; tremor, confusion. From the side of the musculoskeletal system: arthralgia, myalgia. Allergic reactions: pruritus, urticaria, angioedema, bronchospasm, anaphylactic shock, anaphylactoid reactions. Others: gynecomastia in men.

Overdose. Symptoms: neuro- and nephrotoxicity. Treatment: gastric lavage, symptomatic therapy. Ranitidine and bismuth can be removed from the bloodstream by hemodialysis a.

Method of administration and dosage

Inside, regardless of food intake, 2 times a day (morning and evening). In the treatment and prevention of benign gastric and duodenal ulcers, as well as for the eradication of Helicobacter pylori and the relief of concomitant symptoms of dyspepsia, the following combination therapy regimens are used. Within 7 days - 3 drugs: Scheme 1. 2 times a day - ranitidine bismuth citrate 400 mg, clarithromycin 500 mg, metronidazole 400 mg or amoxicillin 1 g. Scheme 2. 2 times a day - ranitidine bismuth citrate 400 mg, clarithromycin 250 mg, metronidazole 400 or 500 mg or tinidazole 500 mg. Scheme 3. Ranitidine bismuth citrate 400 mg 2 times a day, metronidazole 500 mg 3 times a day, tetracycline 500 mg 4 times a day. Scheme 4. 2 times a day - ranitidine bismuth citrate 400 mg, tinidazole 500 mg, amoxicillin 1 g. Within 14 days - 2 drugs: Scheme 5. Ranitidine bismuth citrate 400 mg 2 times a day and clarithromycin 500 mg 2 or 3 times a day. Scheme 6. Ranitidine bismuth citrate 400 mg 2 times a day and amoxicillin 500 mg 4 times a day. To stimulate regeneration processes in ulcerative diseases of the stomach and duodenal ulcer - 800 mg / day (for 2 doses) for 28 days. For the treatment of duodenal ulcers - 800 mg / day (for 2 doses) for 4 weeks (can be extended up to 8 weeks if necessary); with a stomach ulcer - 8 weeks.

Special instructions

Before starting therapy, the possibility of gastric ulcer malignancy is excluded, since ranitidine bismuth citrate can mask the symptoms of carcinoma of the stomach. Patients with mild or moderate renal impairment with CC of at least 50 ml / min do not require dose adjustment. In elderly patients with CC more than 25 ml / min, the dose is not changed. Dose changes in liver failure are not required, since ranitidine and bismuth are excreted mainly by the kidneys. H ₂ -histamine receptor blockers should be taken 2 hours after taking itraconazole a or ketoconazole a to avoid a significant decrease in their absorption. H ₂ -histamine receptor blockers can counteract the effects of pentagastrin a and histamine a on gastric acid-forming function, so use H _{2 blockers within 24 hours prior to the test} -histamine receptors are not recommended. H ₂ -histamine receptor blockers can suppress the cutaneous reaction to histamine, thus resulting in to false negative results (it is recommended to discontinue the use of H ₂ -histamine receptor blockers before performing diagnostic skin tests to detect an immediate allergic skin reaction). As with the use of other medicines containing bismuth, darkening of feces and blackening of the tongue are possible. The drug is taken with food or regardless of food intake.

Interaction

Clarithromycin increases the absorption of ranitidine. The concentration of clarithromycin in plasma does not change when combined with ranitidine bismuth citrate. With the simultaneous administration of ranitidine bismuth citrate with antacids, the absorption of bismuth does not change. Medicines that depress the bone marrow increase the risk of neutropenia. Reduces the absorption of itraconazole and ketoconazole due to an increase in pH in the gastrointestinal tract.

Notes

Related Research Articles

Peptic ulcer disease (PUD) is a break in the inner lining of the stomach, the first part of the small intestine, or sometimes the lower esophagus. An ulcer in the stomach is called a gastric ulcer, while one in the first part of the intestines is a duodenal ulcer. The most common symptoms of a duodenal ulcer are waking at night with upper abdominal pain and upper abdominal pain that improves with eating. With a gastric ulcer, the pain may worsen with eating. The pain is often described as a burning or dull ache. Other symptoms include belching, vomiting, weight loss, or poor appetite. About a third of older people have no symptoms. Complications may include bleeding, perforation, and blockage of the stomach. Bleeding occurs in as many as 15% of cases.

H₂ antagonists, sometimes referred to as H2RAs and also called H₂ blockers, are a class of medications that block the action of histamine at the histamine H₂ receptors of the parietal cells in the stomach. This decreases the production of stomach acid. H₂ antagonists can be used in the treatment of dyspepsia, peptic ulcers and gastroesophageal reflux disease. They have been surpassed by proton pump inhibitors (PPIs); the PPI omeprazole was found to be more effective at both healing and alleviating symptoms of ulcers and reflux oesophagitis than the H₂ blockers ranitidine and cimetidine.

Famotidine Medication that reduces stomach acid

Famotidine, sold under the brand name Pepcid among others, is an Histamine H₂ receptor antagonist medication that decreases stomach acid production. It is used to treat peptic ulcer disease, gastroesophageal reflux disease, and Zollinger-Ellison syndrome. It is taken by mouth or by injection into a vein. It begins working within an hour.

Esomeprazole, sold under the brand name Nexium among others, is a medication which reduces stomach acid. It is used to treat gastroesophageal reflux disease, peptic ulcer disease, and Zollinger–Ellison syndrome. Effectiveness is similar to other proton pump inhibitors (PPIs). It is taken by mouth or injection into a vein.

Gastritis is inflammation of the lining of the stomach. It may occur as a short episode or may be of a long duration. There may be no symptoms but, when symptoms are present, the most common is upper abdominal pain. Other possible symptoms include nausea and vomiting, bloating, loss of appetite and heartburn. Complications may include stomach bleeding, stomach ulcers, and stomach tumors. When due to autoimmune problems, low red blood cells due to not enough vitamin B12 may occur, a condition known as pernicious anemia.

Achlorhydria and hypochlorhydria refer to states where the production of hydrochloric acid in gastric secretions of the stomach and other digestive organs is absent or low, respectively. It is associated with various other medical problems.

Ranitidine Medication that decreases stomach acid

Ranitidine, sold under the brand name Zantac among others, is a medication that decreases stomach acid production. It is commonly used in treatment of peptic ulcer disease, gastroesophageal reflux disease, and Zollinger–Ellison syndrome. Tentative evidence shows it to be of benefit for hives. It can be given by mouth, injection into a muscle, or injection into a vein.

A vagotomy is a surgical procedure that involves removing part of the vagus nerve.

Timeline of peptic ulcer disease and <i>Helicobacter pylori</i>

This is a timeline of the events relating to the discovery that peptic ulcer disease and some cancers are caused by H. pylori. In 2005, Barry Marshall and Robin Warren were awarded the Nobel Prize in Physiology or Medicine for their discovery that peptic ulcer disease (PUD) was primarily caused by Helicobacter pylori, a bacterium with affinity for acidic environments, such as the stomach. As a result, PUD that is associated with H. pylori is currently treated with antibiotics used to eradicate the infection. For decades prior to their discovery, it was widely believed that PUD was caused by excess acid in the stomach. During this time, acid control was the primary method of treatment for PUD, to only partial success. Among other effects, it is now known that acid suppression alters the stomach milieu to make it less amenable to H. pylori infection.

Helicobacter pylori eradication protocols is a standard name for all treatment protocols for peptic ulcers and gastritis in the presence of Helicobacter pylori infection. The primary goal is not only temporary relief of symptoms but also total elimination of H. pylori infection. Patients with active duodenal or gastric ulcers and those with a prior ulcer history should be tested for H. pylori. Appropriate therapy should be given for eradication. Patients with MALT lymphoma should also be tested and treated for H. pylori since eradication of this infection can induce remission in many patients when the tumor is limited to the stomach. Several consensus conferences, including the Maastricht Consensus Report, recommend testing and treating several other groups of patients but there is limited evidence of benefit. This includes patients diagnosed with gastric adenocarcinoma, patients found to have atrophic gastritis or intestinal metaplasia, as well as first-degree relatives of patients with gastric adenocarcinoma since the relatives themselves are at increased risk of gastric cancer partly due to the intrafamilial transmission of H. pylori. To date, it remains controversial whether to test and treat all patients with functional dyspepsia, gastroesophageal reflux disease, or other non-GI disorders as well as asymptomatic individuals.

Lafutidine (INN) is a second generation histamine H₂ receptor antagonist having multimodal mechanism of action and used to treat gastrointestinal disorders. It is marketed in Japan and India.

Ebrotidine is an H₂ receptor antagonist with gastroprotective activity against ethanol-, aspirin- or stress-induced gastric mucosal damage. The antisecretory properties of ebrotidine are similar to those of ranitidine, and approximately 10-fold greater than those of cimetidine. Ebrotidine has anti-Helicobacter pylori activity via inhibition of the urease enzyme and the proteolytic and mucolytic activities of the bacterium. However, its activity is synergistic with a number of antibacterial agents. Ebrotidine counteracts the inhibitory effects of H. pylori lipopolysaccharides. Ebrotidine was withdrawn from the market due to risks of hepatotoxicity.

There are several classes of drugs for acid-related disorders, such as dyspepsia, peptic ulcer disease (PUD), gastroesophageal reflux disease (GORD/GERD), or laryngopharyngeal reflux.

Helicobacter felis is a bacterial species in the Helicobacteraceae family, Campylobacterales order, Helicobacter genus. This bacterium is Gram-negative, microaerophilic, urease-positive, and spiral-shaped. Its type strain is CS1T. It can be pathogenic.

Helicobacter salomonis is a species within the Helicobacter genus of Gram-negative bacteria. Helicobacter pylori is by far the best known Helicobacter species primarily because humans infected with it may develop gastrointestinal tract diseases such as stomach inflammation, stomach ulcers, duodenal ulcers, stomach cancers of the nonlymphoma type, and various subtypes of extranodal marginal zone lymphomass, e.g. those of the stomach, small intestines, large intestines, and rectumn. H. pylori is also associated with the development of bile duct cancer and has been associated with a wide range of other diseases, although its role in the development of many of these other diseases requires further study. Humans infected with H. salomonis may develop some of the same gastrointestinal diseases viz., stomach inflammation, stomach ulcers, duodenal ulcers, stomach cancers that are not lymphomas, and extranodal marginal B cell lymphomas of the stomach. Other non-H. pylori Helicobacter species that are known to be associated with these gastrointestinal diseases are Helicobacter bizzozeronii, Helicobacter suis, Helicobacter felis, and Helicobacter heilmannii s.s. Because of their disease associations, these four Helicobacter species plus H. salomonis are often group together and termed Helicobacter heilmannii sensu lato.

Bismuth subcitrate potassium is a bismuth salt used in combination with antibiotics and a proton pump inhibitor for the treatment of Helicobacter pylori infections.

Helicobacter heilmannii sensu lato refers to a group of bacterial species within the Helicobacter genus. The Helicobacter genus consists of at least 40 species of spiral-shaped flagellated, Gram-negative bacteria of which the by far most prominent and well-known species is Helicobacter pylori. H. pylori is associated with the development of gastrointestinal tract diseases such as stomach inflammation, stomach ulcers, duodenal ulcers, stomach cancers that are not lymphomas, and various subtypes of extranodal marginal zone lymphomass, e.g. those of the stomach, small intestines, large intestines, and rectumn. H. pylori has also been associated with the development of bile duct cancer and has been associated with a wide range of other diseases although its role in the development of many of these other diseases requires further study.

Helicobacter bizzozeronii is a species within the Helicobacter genus of Gram-negative bacteria. Helicobacter pylori is by far the best known Helicobacter species, primarily because humans infected with it may develop gastrointestinal tract diseases such as stomach inflammation, stomach ulcers, duodenal ulcers, stomach cancers of the nonlymphoma type, and various subtypes of extranodal marginal zone lymphomass, e.g. those of the stomach, small intestines, large intestines, and rectumn. H. pylori is also associated with the development of bile duct cancer and has been associated with a wide range of other diseases although its role in the development of many of these other diseases requires further study. Humans infected with H. bizzozeronii are prone to develop some of the same gastrointestinal diseases viz., stomach inflammation, stomach ulcers, duodenal ulcers, stomach cancers that are not lymphomas, and extranodal marginal B cell lymphomas of the stomach. Other non-H. pylori Helicobacter species that are known to be associated with these gastrointestinal diseases are Helicobacter felis, Helicobacter salomonis, Helicobacter suis, and Helicobacter heilmannii s.s. Because of their disease associations, these four Helicobacter species plus H. bizzozeronii are often grouped together and termed Helicobacter heilmannii sensu lato.

Helicobacter suis is a species within the Helicobacter genus of Gram-negative bacteria. Helicobacter pylori is by far the best known Helicobacter species, primarily because humans infected with it may develop gastrointestinal tract diseases such as stomach inflammation, stomach ulcers, duodenal ulcers, stomach cancers of the nonlymphoma type, and various subtypes of extranodal marginal zone lymphomass, e.g. those of the stomach, small intestines, large intestines, and rectumn. H. pylori is also associated with the development of bile duct cancer and has been associated with a wide range of other diseases although its role in the development of many of these other diseases requires further study. Humans infected with H. suis may develop some of the same gastrointestinal diseases - stomach inflammation, stomach ulcers, duodenal ulcers, stomach cancers that are not lymphomas, and extranodal marginal B cell lymphomas of the stomach. Other non-H. pylori Helicobacter species that are known to be associated with these gastrointestinal diseases are Helicobacter bizzozeronii, Helicobacter salomonis, Helicobacter felis, and Helicobacter heilmannii s.s. Because of their disease associations, these four Helicobacter species plus H. suis are often group together and termed Helicobacter heilmannii sensu lato.

Helicobacter heilmannii s.s. is a species within the Helicobacter genus of Gram negative bacteria. Helicobacter pylori is by far the best known Helicobacter species primarily because humans infected with it may develop gastrointestinal tract diseases such as stomach inflammation, stomach ulcers, duodenal ulcers, stomach cancers of the non-lymphoma type, and various subtypes of extranodal marginal zone lymphomass, e.g. those of the stomach, small intestines, large intestines, and rectumn. H. pylori is also associated with the development of bile duct cancer and has been associated with a wide range of other diseases although its role in the development of many of these other diseases requires further study. Humans infected with H. heilmannii s.s. may develop some of the same gastrointestinal diseases viz., stomach inflammation, stomach ulcers, duodenal ulcers, stomach cancers that are not lymphomas, and extranodal marginal B cell lymphomas of the stomach. Other non-H. pylori Helicobacter species that are known to be associated with these gastrointestinal diseases are Helicobacter bizzozeronii, Helicobacter suis, Helicobacter felis, and Helicobacter salomonis. Because of their disease associations, these four Helicobacter species plus H. heilmannii s.s. are often group together and termed Helicobacter heilmannii sensu lato.

References

↑ Yuan S, Wang R, Chan JF, Zhang AJ, Cheng T, Chik KK, et al. (November 2020). "Metallodrug ranitidine bismuth citrate suppresses SARS-CoV-2 replication and relieves virus-associated pneumonia in Syrian hamsters". Nature Microbiology. 5 (11): 1439–1448. doi: 10.1038/s41564-020-00802-x . PMID 33028965. S2CID 222216457.

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[pmid33028965-1] Yuan S, Wang R, Chan JF, Zhang AJ, Cheng T, Chik KK, et al. (November 2020). "Metallodrug ranitidine bismuth citrate suppresses SARS-CoV-2 replication and relieves virus-associated pneumonia in Syrian hamsters". Nature Microbiology. 5 (11): 1439–1448. doi: 10.1038/s41564-020-00802-x . PMID 33028965. S2CID 222216457.

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