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药品详细

Bismuth Subsalicylate(水杨酸铋)

化学结构式图
中文名
水杨酸铋
英文名
Bismuth Subsalicylate
分子式
C7H5BiO4
化学名
2-hydroxy-2H,4H-benzo[d]1,3-dioxa-2-bismacyclohexan-4-one
分子量
Average: 362.0926
Monoisotopic: 361.999166889
CAS号
14882-18-9
ATC分类
A02B 未知;A02B 未知;A02B 未知
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍

Bismuth subsalicylate is the active ingredient in the popular medication Pepto-Bismol that is used to treat nausea, heartburn, indigestion, upset stomach, diarrhea, and other temporary discomforts of the stomach and gastrointestinal tract. It is also the main ingredient of Kaopectate. It displays anti-inflammatory action (due to salicylic acid) and also acts as an antacid and mild antibiotic.

生产厂家
    封装厂家
    参考
    Synthesis Reference Not Available
    General Reference
    1. Goldenberg MM, Honkomp LJ, Burrous SE, Castellion AW: Protective effect of Pepto-Bismol liquid on the gastric mucosa of rats. Gastroenterology. 1975 Sep;69(3):636-40. Pubmed
    剂型
    规格
    化合物类型
    Type small molecule
    Classes
    • Benzoates
    • Salicylates and Derivatives
    Substructures
    • Benzyl Alcohols and Derivatives
    • Acetates
    • Benzoates
    • Salicylates and Derivatives
    • Phenols and Derivatives
    • Benzene and Derivatives
    • Heterocyclic compounds
    • Aromatic compounds
    • Benzoyl Derivatives
    • Phenyl Esters
    适应症
    药理
    Indication Used to treat nausea, heartburn, indigestion, upset stomach, diarrhea, and other temporary discomforts of the stomach and gastrointestinal tract.
    Pharmacodynamics Bismuth subsalicylate displays anti-inflammatory action (due to salicylic acid) and also acts as an antacid and mild antibiotic. It can also cause a black tongue and black stools in some users of the drug, when it combines with trace amounts of sulfur in their saliva and gastrointestinal tract. This discoloration is temporary and harmless.
    Mechanism of action As an antidiarrheal, the exact mechanism has not been determined. Bismuth subsalicylate may exert its antidiarrheal action not only by stimulating absorption of fluid and electrolytes across the intestinal wall (antisecretory action) but also, when hydrolyzed to salicylic acid, by inhibiting synthesis of a prostaglandin responsible for intestinal inflammation and hypermotility. In addition, bismuth subsalicylate binds toxins produced by Escherichia coli. Both bismuth subsalicylate and the intestinal reaction products, bismuth oxychloride and bismuth hydroxide, are believed to have bactericidal action. As an antacid, bismuth has weak antacid properties.
    Absorption Following oral administration, absorption of the salicylate component from the small intestine is generally rapid and complete (>90%).
    Volume of distribution Not Available
    Protein binding Not Available
    Metabolism
    Based on in vitro dissociation data and in vivo animal data, bismuth subsalicylate is believed to be largely hydrolyzed in the stomach to bismuth oxychloride and salicylic acid. In the small intestine, nondissociated bismuth subsalicylate reacts with other anions (bicarbonate and phosphate) to form insoluble bismuth salts. In the colon, nondissociated bismuth subsalicylate and other bismuth salts react with hydrogen sulfide to produce bismuth sulfide, a highly insoluble black salt responsible for the darkening of the stools.
    Route of elimination Not Available
    Half life Not Available
    Clearance Not Available
    Toxicity Not Available
    Affected organisms Not Available
    Pathways Not Available
    理化性质
    Properties
    State solid
    Experimental Properties Not Available
    Predicted Properties
    Property Value Source
    water solubility 5.97e+01 g/l ALOGPS
    logP 0.37 ALOGPS
    logP 1.11 ChemAxon
    logS -0.78 ALOGPS
    pKa (strongest acidic) 14.3 ChemAxon
    pKa (strongest basic) -3.1 ChemAxon
    physiological charge 0 ChemAxon
    hydrogen acceptor count 3 ChemAxon
    hydrogen donor count 1 ChemAxon
    polar surface area 55.76 ChemAxon
    rotatable bond count 0 ChemAxon
    refractivity 35.72 ChemAxon
    polarizability 15.67 ChemAxon
    药物相互作用
    Drug Interaction
    Acetazolamide The salicylate, bismuth subsalicylate, at high dose increases the effect of the carbonic anhydrase inhibitor, acetazolamide.
    Amprenavir The antiacid decreases the absorption of amprenavir
    Atazanavir This gastric pH modifier decreases the levels/effects of atazanavir
    Betamethasone The corticosteroid, betamethasone, may decrease the effect of the salicylate, bismuth subsalicylate.
    Fludrocortisone The corticosteroid, fludrocortisone, may decrease the effect of the salicylate, bismuth subsalicylate.
    Gliclazide The salicylate, bismuth subsalicylate, increases the effect of the sulfonylurea, gliclazide.
    Glyburide The salicylate, bismuth subsalicylate, increases the effect of the sulfonylurea, glibenclamide.
    Hydrocortisone The corticosteroid, hydrocortisone, may decrease the effect of the salicylate, bismuth subsalicylate.
    Methazolamide The salicylate, bismuth subsalicylate, at high dose increases the effect of the carbonic anhydrase inhibitor, methazolamide.
    Methotrexate The salicylate, bismuth subsalicylate, increases the effect and toxicity of methotrexate.
    Minocycline Formation of non-absorbable complexes
    Prednisolone The corticosteroid, prednisolone, may decrease the effect of the salicylate, bismuth subsalicylate.
    Prednisone The corticosteroid, prednisone, may decrease the effect of the salicylate, bismuth subsalicylate.
    Probenecid The salicylate, bismuth subsalicylate, decreases the uricosuric effect of probenecid.
    Tetracycline Formation of non-absorbable complexes
    Triamcinolone The corticosteroid, triamcinolone, may decrease the effect of the salicylate, bismuth subsalicylate.
    食物相互作用
    Not Available

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