| Candidate ID: | R0481 |
| Source ID: | DB01294 |
| Source Type: | approved; vet_approved |
| Compound Type: |
small molecule
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| Compound Name: |
Bismuth subsalicylate
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| Synonyms: |
2-Hydroxy-benzo[1,3,2]dioxabismin-4-one; Basic bismuth salicylate; Bismuth oxide salicylate; Bismuth oxysalicylate; Bismuth subsalicylate; Pink bismuth; Wismutsubsalicylat
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| Molecular Formula: |
C7H5BiO4
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| SMILES: |
O[Bi]1OC(=O)C2=CC=CC=C2O1
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| Structure: |
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| DrugBank Description: |
Bismuth subsalicylate is an antacid and anti-diarrheal agent. Exhibiting antibacterial and gastroprotective properties, bismuth subsalicylate is an insoluble salt of linked to trivalent . Each molecule of bismuth subsalicylate contains 58% bismuth and 42% salicylate by weight. Bismuth subsalicylate has been around for over 100 years: it was originally developed in 1901 for hygienic use and sanitation for cholera infection.
Bismuth subsalicylate was first approved by the FDA in 1939 and is now mainly used to relieve nausea, diarrhea, and gastrointestinal discomfort. It is an active ingredient found in Pepto-Bismol, a common over-the-counter medication that is used to temporarily treat discomforts of the stomach and gastrointestinal tract. Bismuth subsalicylate is a component of HELIDAC Therapy (bismuth subsalicylate, , and ), which is a treatment regimen indicated for the eradication of _H. pylori_ for treatment of patients with _H. pylori_ infection and duodenal ulcer disease.
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| CAS Number: |
14882-18-9
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| Molecular Weight: |
362.0926
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| DrugBank Indication: |
Bismuth subsalicylate is indicated to temporarily relieve diarrhea, travelers' diarrhea, and upset stomach due to overindulgence in food and drink, including heartburn, indigestion, nausea, gas, belching, and fullness.
Bismuth subsalicylate is a component of HELIDAC Therapy (bismuth subsalicylate, , and ), which is a treatment regimen indicated for the eradication of _H. pylori_ for treatment of patients with _H. pylori_ infection and duodenal ulcer disease.
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| DrugBank Pharmacology: |
Bismuth subsalicylate is an antacid and antimicrobial, gastroprotective, anti-secretory, and anti-inflammatory actions. It works to reduce the severity and incidence of flatulence and diarrhea, and consequently relieving gastrointestinal discomfort. In one study, bismuth subsalicylate was prevented traveler's diarrhea with a protection rate >60%.
Organobismuth compounds, formed by the breakdown of bismuth subsalicylate in the gastrointestinal tract, inhibit the growth of _Helicobacter pylori_ and other bacteria implicated in gastrointestinal disorders, and some fungi. In one study, bismuth subsalicylate was shown to eradicate up to 90% of _H. pylori_ infection when used as part of a quadruple therapy regimen containing a proton pump inhibitor, tetracycline, and metronidazole. Bismuth subsalicylate exhibited antimicrobial activity against _Clostridium difficile_, enterotoxigenic _Escherichia coli_ O157:H7, _norovirus_, and other common enteric pathogens such as _Salmonella_ and _Shigella_.
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| DrugBank MoA: |
The exact mechanism of bismuth subsalicylate is not fully understood. Bismuth subsalicylate is an insoluble complex that constitutes salicylic acid and trivalent bismuth. Once orally administered, bismuth subsalicylate hydrolyzes in the stomach into bismuth oxychloride, which is minimally absorbed into the bloodstream, and salicylic acid, which is almost completely absorbed. Bismuth interacts with other anions and compounds, such as hydrochloric acid, bicarbonate, phosphate, and hydrogen sulfide, in the gastrointestinal tract to form bismuth salts such as bismuth oxychloride, bismuth subcarbonate, bismuth phosphate, and bismuth sulfide. Bismuth salts possess bactericidal and antimicrobial activity, mainly by preventing bacteria from binding and growing on the mucosal cells of the stomach. It has no effects on normal gut flora. By preventing bacteria from binding to mucosal cells, bismuth subsalicylate prevents intestinal secretion and fluid loss, promotes fluid and electrolyte reabsorption, reduces gastrointestinal inflammation, and promotes the healing of pre-existing ulcer in the stomach. Salicylic acid from dissociated bismuth subsalicylate adds to the anti-inflammatory actions of bismuth salts by inhibiting the cyclooxygenase enzyme and limiting the formation of prostaglandin, a pro-inflammatory mediator. Bismuth subsalicylate exhibits cytoprotective and demulcent activity, which makes it an effective drug in peptic ulcer disease. It blocks the adhesion of H. pylori to the gastric epithelial cells and blocks the bacteria's enzyme activities, including phospholipase, protease, and urease.
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| Targets: |
--
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| Inclusion Criteria: |
Therapeutic strategy associated
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