Bismuth subcitrate

Tripotassium dicitratobismuthate [57644-54-9] (bismuth subcitrate), De-Nol is a buffered aqueous suspension of a poorly defined, water-insoluble bismuth compound. It is said to very effective for the treatment of gastric and duodenal ulcers (180,184). There have not yet been any reports of bismuth encephalopathy following the use of this dmg. 

Widespread medicinal use of colloidal bismuth subcitrate (CBS) has prompted extensive studies of bismuth compounds involving the citrate anion. Bismuth citrate is essentially insoluble in water, but a dramatic increase in solubility with increasing pH has been exploited as a bio-ready source of soluble bismuth, a material referred to as CBS. Formulation of these solutions is complicated by the variability of the bismuth anion stoichiometry, the presence of potassium and/ or ammonium cations, the susceptibility of bismuth to oxygenation to Bi=0, and the incorporation of water in isolated solids. Consequently, a variety of formulas are classified in the literature as CBS. Solids isolated from various, often ill-defined combinations of bismuth citrate, citric acid, potassium hydroxide, or ammonium hydroxide have been assigned formulas on the basis of elemental analysis data or by determination of water and ammonia content, but are of low significance in the absence of complementary data other than thermal analysis (163), infrared spectroscopy (163), or NMR spectroscopy (164). In this context, the Merck index lists the chemical formula of CBS as KgfNHJaBieOafOHMCeHsCbh in the 11th edition (165), but in the most recent edition provides a less precise name, tripotassium dicitrato bismuthate (166). 

X-Ray Crystallographic Data for Solids Described as Colloidal Bismuth Subcitrate (Hcit = [C02CH2C(0H)(C02)CH2C02]3-)... 

Bismuth compounds have been used for treating gastrointestinal disorders for more than two centuries (451). These include bicarbonate, nitrate and salicylate salts, and colloidal bismuth subcitrate. These are all Bi(III) compounds Bi(V) is usually a strong oxidant. Their structures are largely unknown and often contain a mixture of anionic ligands. This reflects the strong tendency of Bi(III) to hydrolyze and form stable hydroxo and oxo complexes. The first pKa of Bi(III) in water is ca. 1.5. Bismuth(III) has a variable coordination number, from 3 to 10. 

Magnesium Carbonate (Gaviscon Extra Strength, Liquid) Antidiarrheals Bismuth Subcitrate/... 

Two bismuth compounds are available bismuth subsalicylate, a nonprescription formulation containing bismuth and salicylate, and bismuth subcitrate potassium. In the USA, bismuth subcitrate is available only as a combination prescription product that also contains metronidazole and tetracycline for the treatment of H pylori. Bismuth subsalicylate undergoes rapid dissociation within the stomach, allowing absorption of salicylate. Over 99% of the bismuth appears in the stool. Although minimal (< 1%), bismuth is absorbed it is stored in many tissues and has slow renal excretion. Salicylate (like aspirin) is readily absorbed and excreted in the urine. 

Aluminum Hydroxide Magnesium Trisilicate (Gaviscon) Aluminum Hydroxide (Amphojel, ALtemaGEL) Aluminum Hydroxide + Magnesium Carbonate (Gaviscon Extra Strength, Liquid) Antidiarrheals Bismuth Subcitrate/ Metronidazole/ Tetracycline (Pylera) Bismuth Subsalicylate (Pepto-Bismol) Diphenoxylate w/ Atropine (Lomotil, Lonox)... 

F. Huwez, et al., Acute renal failure after overdose of colloidal bismuth subcitrate. Lancet 340 1298, 1992. 

CBS = colloidal bismuth subcitrate RBC = ranitidine bismuth citrate approximate formulas. 

Tripotassium dicitratobismuthate, bismuth subcitrate, (De-Nol) This substance was originally thought to act mainly by chelating with protein in the ulcer base to form a coating, which protects the ulcer from the adverse influences of acid, pepsin and bile. Subsequently, bismuth chelate was found to possess an additional valuable action, namely activity against Helicobacter pylori, especially when combined with an antimicrobial (see below). 

A 17-year-old girl took 25 tablets of bismuth subcitrate 300 mg (total 7.5 g) in a suicide attempt and developed severe renal insufficiency (34). Renal biopsy showed evidence of acute tubular necrosis, with epithelial flattening, lumen widening, and atrophic changes in the convoluted tubules and mononuclear cell infiltration and edema in the interstitium. She was managed with hemodialysis and recovered. 

Sarikaya M, Sevinc A, Ulu R, Ates F, Ari F. Bismuth subcitrate nephrotoxicity. A reversible cause of acute oliguric renal failure. Nephron 2002 90(4) 501-2. 

Hruz P, Mayr M, Low R, Drewe J, Huber G. Fanconi s syndrome, acute renal failure, and tonsil ulcerations after colloidal bismuth subcitrate intoxication. Am J Kidney Dis 2002 39(3) E18. 

A host of bismuth compounds has been used for studies involving antibacterial and antitumor activities and warfare agents. It should be noted that many of the compounds are no longer in use, because with the advent of other natural compounds these metallic species are used very little. The most common compounds used to date are bismuth subcitrate or bismuth subsalicylate as bacterial intestinal agents and for action against ulcers (Pepto-bismol Proctor and Gamble). In both cases these were provided as colloidal agents which had limited water solubility. 

Trade names Bismatrol Bismuth subcitrate Bismuth subgallate (colostomy deodorant) Bismuth subnitrate and Bismuth idoform paraffin paste (BIPP) Bismuth sucralfate Caved-S Colo-Fresh De-Nol Devrom Diotame Helidac (Prometheus) Pepto-Bismol (Procter Gamble) Pink Bismuth... 

Betasept chlorhexidine bismuth Bismatrol, Bismuth subcitrate, Bismuth subgallate,... 

Acetylcysteine Bismuth subcitrate Etamsylate Fluvastatine Pamindronic acid Quinine Tizanidine Tropisetron... 

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