Bismuth subnitrate
Identification
- Summary
Bismuth subnitrate is a medication used as an antacid.
- Generic Name
- Bismuth subnitrate
- DrugBank Accession Number
- DB13209
- Background
Bismuth subnitrate, also referred to as bismuth oxynitrate or bismuthyl nitrate, is a highly water-soluble crystalline compound that has been used as a treatment for duodenal ulcers and anti-diarrheic agent 1. The use of bismuth substrate as an active ingredient in over-the-counter antacids is approved by the FDA.
- Type
- Small Molecule
- Groups
- Approved
- Structure
- Weight
- Average: 1461.98
Monoisotopic: 1461.87284 - Chemical Formula
- Bi5H9N4O22
- Synonyms
- Bismuth hydroxide nitrate oxide
- Bismuth nitrate, basic
- Bismuth subnitrate
- Bismuthum subnitricum
- External IDs
- C.I. 77169
Pharmacology
- Indication
Indicated for over-the-counter use as an antacid.
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- Pharmacodynamics
Bismuth subnitrate acts as an antacid that exert protective effects on the gastric mucosa 1. In a double-blind endoscopically controlled study, bismuth substrate was demonstrated to be effective for symptomatic relief in duodenal ulcers 2. In the alcohol model of mucosal injury in the rat, bismuth substrate was shown to be cytoprotective 2. In a randomized clinical study consisting of patients with H. pylori-associated duodenal ulcer, adjunctive use of colloidal bismuth subnitrate in a short treatment regimen with omeprazole and clarithromycin resulted in improved eradication rate of H. pylori 3.
- Mechanism of action
Based on the findings of a clinical investigation in patients with duodenal ulcer disease and healthy volunteers receiving oral bismuth subnitrate tablets, the protective effects of bismuth subnitrate may be secondary to endogenous mucosal prostaglandin (PGE2) production, which is one of the deficient factors observed in peptic ulcer disease 2. Antacid neutralizing activity of bismuth subnitrate was demonstrated to have a significant postprandial effect on gastric pH 2.
- Absorption
Bismuth subnitrate may undergo minimal gastrointestinal absorption which may be potentiated with concomitant administration of sulfhydryl compounds 5 when dissolved in citrate buffer solution 1. Approximately 0.2% of orally administered bismuth is absorbed systematically from the gastrointestinal tract with the peak plasma concentration typically occurring within 1 hour 5.
- Volume of distribution
Bismuth has been shown to accumulate preferentially in the kidneys 1.
- Protein binding
Upon accumulation in the kidneys, bismuth may bind to a bismuth-metal binding protein in the kidney 4.
- Metabolism
No pharmacokinetic data available.
- Route of elimination
Bismuth may undergo both urinary and faecal excretion, however the exact proportion contributed by each route is still unknown 4.
- Half-life
The distribution half-life of bismuth is approximately 1 to 4 hours, and the elimination half-life is 5 to 11 days 5.
- Clearance
No pharmacokinetic data available.
- Adverse Effects
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- Toxicity
Reported oral dose range for moderate toxicity or possibly lethal toxicity in humans is 0.5-5 g/kg 5. Nephropathy, encephalopathy, osteoarthropathy, gingivitis, stomatitis and colitis have been attributed to bismuth toxicity in humans 4.
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your softwareAcetaminophen Bismuth subnitrate can cause a decrease in the absorption of Acetaminophen resulting in a reduced serum concentration and potentially a decrease in efficacy. Acetophenazine Bismuth subnitrate can cause a decrease in the absorption of Acetophenazine resulting in a reduced serum concentration and potentially a decrease in efficacy. Alendronic acid The serum concentration of Alendronic acid can be decreased when it is combined with Bismuth subnitrate. Alimemazine Bismuth subnitrate can cause a decrease in the absorption of Alimemazine resulting in a reduced serum concentration and potentially a decrease in efficacy. Allopurinol The therapeutic efficacy of Allopurinol can be decreased when used in combination with Bismuth subnitrate. Amisulpride Amisulpride may increase the neurotoxic activities of Bismuth subnitrate. Amitriptyline Amitriptyline may increase the neurotoxic activities of Bismuth subnitrate. Amitriptylinoxide Amitriptylinoxide may increase the neurotoxic activities of Bismuth subnitrate. Amoxapine Amoxapine may increase the neurotoxic activities of Bismuth subnitrate. Amphetamine The serum concentration of Amphetamine can be increased when it is combined with Bismuth subnitrate. Identify potential medication risksEasily compare up to 40 drugs with our drug interaction checker.Get severity rating, description, and management advice.Learn more - Food Interactions
- Not Available
Products
- Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.
- Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Hemorro-dol Sup Bismuth subnitrate (37.8 mg) + Balsam of Peru (22.6 mg) + Belladonna (11.25 mg) + Benzocaine (50 mg) + Bismuth subcarbonate (86.4 mg) + Boric acid (226.7 mg) + Ephedrine sulfate (2.5 mg) + Zinc oxide (226.7 mg) Suppository Rectal Produits Francais Labs Inc. 1981-12-31 1997-05-30 Canada อูลก๊าสตริน Bismuth subnitrate (150 MG) + Glycyrrhiza glabra (400 MG) + Sodium aluminosilicate (280 MG) Tablet บริษัท โรงงานเภสัชกรรม เกร๊ทเตอร์ฟาร์ม่า จำกัด จำกัด 1995-12-29 Not applicable Thailand
Categories
- ATC Codes
- A02BX12 — Bismuth subnitrate
- Drug Categories
- Alimentary Tract and Metabolism
- Antacids
- Bismuth containing drugs
- Drugs for Acid Related Disorders
- Drugs for Peptic Ulcer and Gastro-Oesophageal Reflux Disease (Gord)
- Elements
- Elements, Radioactive
- Gastric Acid Lowering Agents
- Gastrointestinal Agents
- Isotopes
- Metals
- Metals, Heavy
- Neurotoxic agents
- Radioisotopes
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of inorganic compounds known as post-transition metal nitrates. These are inorganic compounds in which the largest oxoanion is nitrate, and in which the heaviest atom not in an oxoanion is a post-transition metal.
- Kingdom
- Inorganic compounds
- Super Class
- Mixed metal/non-metal compounds
- Class
- Post-transition metal oxoanionic compounds
- Sub Class
- Post-transition metal nitrates
- Direct Parent
- Post-transition metal nitrates
- Alternative Parents
- Post-transition metal salts / Inorganic salts / Inorganic oxides / Inorganic hydrides
- Substituents
- Inorganic hydride / Inorganic oxide / Inorganic post-transition metal salt / Inorganic salt / Post-transition metal nitrate
- Molecular Framework
- Not Available
- External Descriptors
- Not Available
- Affected organisms
- Not Available
Chemical Identifiers
- UNII
- H19J064BA5
- CAS number
- 1304-85-4
- InChI Key
- QGWDKKHSDXWPET-UHFFFAOYSA-E
- InChI
- InChI=1S/5Bi.4NO3.9H2O.O/c;;;;;4*2-1(3)4;;;;;;;;;;/h;;;;;;;;;9*1H2;/q5*+3;4*-1;;;;;;;;;;-2/p-9
- IUPAC Name
- pentabismuth(3+) ion nonahydroxide tetranitrate oxidandiide
- SMILES
- [OH-].[OH-].[OH-].[OH-].[OH-].[OH-].[OH-].[OH-].[OH-].[O--].[Bi+3].[Bi+3].[Bi+3].[Bi+3].[Bi+3].[O-][N+]([O-])=O.[O-][N+]([O-])=O.[O-][N+]([O-])=O.[O-][N+]([O-])=O
References
- General References
- Kondo Y, Himeno S, Satoh M, Naganuma A, Nishimura T, Imura N: Citrate enhances the protective effect of orally administered bismuth subnitrate against the nephrotoxicity of cis-diamminedichloroplatinum. Cancer Chemother Pharmacol. 2004 Jan;53(1):33-8. doi: 10.1007/s00280-003-0706-9. Epub 2003 Oct 7. [Article]
- Pugh S, Lewin MR: Mechanism of action of Roter (bismuth subnitrate) in patients with duodenal ulcer disease and healthy volunteers. J Gastroenterol Hepatol. 1990 Jul-Aug;5(4):382-6. [Article]
- Forne M, Viver JM, Espinos JC, Coll I, Tresserra F, Garau J: Impact of colloidal bismuth subnitrate in the eradication rates of Helicobacter pylori infection-associated duodenal ulcer using a short treatment regimen with omeprazole and clarithromycin: a randomized study. Am J Gastroenterol. 1995 May;90(5):718-21. [Article]
- Slikkerveer A, de Wolff FA: Pharmacokinetics and toxicity of bismuth compounds. Med Toxicol Adverse Drug Exp. 1989 Sep-Oct;4(5):303-23. [Article]
- BISMUTH SUBNITRATE - National Library of Medicine HSDB Database - Toxnet [Link]
- External Links
Clinical Trials
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Suppository Rectal Tablet - Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) Decomposes at 260 MSDS boiling point (°C) Decomposes at 260 MSDS water solubility Insoluble MSDS - Predicted Properties
Property Value Source logP 0.84 Chemaxon pKa (Strongest Basic) -9.9 Chemaxon Physiological Charge -1 Chemaxon Hydrogen Acceptor Count 3 Chemaxon Hydrogen Donor Count 0 Chemaxon Polar Surface Area 66.2 Å2 Chemaxon Rotatable Bond Count 0 Chemaxon Refractivity 8.35 m3·mol-1 Chemaxon Polarizability 3.28 Å3 Chemaxon Number of Rings 0 Chemaxon Bioavailability 1 Chemaxon Rule of Five No Chemaxon Ghose Filter No Chemaxon Veber's Rule No Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
- Not Available
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS Not Available
Drug created at June 23, 2017 20:37 / Updated at February 21, 2021 18:54