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Bismuth Compounds

Bismuto, compuestos de.

Bismuth compounds have been used for their astringent and antidiarrhoeal properties in a variety of gastrointestinal disorders, and have been applied topically in skin disorders and anorectal disorders such as haemorrhoids. Certain salts are active against Helicobacter pylori and are used in the treatment of peptic ulcer disease.

Bismuth Aluminate

(US Adopted Name)

Drug Nomenclature

Synonyms: Aluminato de bismuto; Aluminum Bismuth Oxide
USAN: Bismuth Aluminate
Molecular formula: Bi2(Al2O4)3,10H2O =952.0
CAS: 12284-76-3 (anhydrous bismuth aluminate)

Pharmacopoeias. In China, and France.

Bismuth Citrate

Note. Do not confuse with bismuth subcitrate potassium or tripotassium dicitratobismuthate (colloidal bismuth subcitrate).

Pharmacopoeias. In US.

The United States Pharmacopeia 31, 2008 (Bismuth Citrate). A white, amorphous or crystalline powder. Insoluble in water and in alcohol soluble in dilute ammonia solution and in solutions of alkali citrates. Store in airtight containers. Protect from light. Prevent exposure to temperatures above 40°.

Bismuth Oxide

Drug Nomenclature

Synonyms: Óxido de bismuto; Bismuth Trioxide
Molecular formula: Bi2O3 =466.0
CAS: 1304-76-3

Bismuth Salicylate

Bismuth CompoundsDrug Nomenclature

Synonyms: Bázisos bizmut-szalicilát; Basic Bismuth Salicylate; Bismuth Oxysalicylate; Bismuthi Subsalicylas; Bismuto subsalicilatas; Salicilato de bismuto; Salicylan bismutitý zásaditý; Vismutsubsalicylat; Vismuttisubsalisylaatti
USAN: Bismuth Subsalicylate
Molecular formula: C7H5BiO4 =362.1
CAS: 14882-18-9

Pharmacopoeias. In Europe and US.

European Pharmacopoeia, 6th ed. (Bismuth Subsalicylate). A complex of bismuth and salicylic acid. It contains not less than 56% and not more than 59.4% of Bi, calculated with reference to the dried substance. A white or almost white powder. Practically insoluble in water and in alcohol dissolves in mineral acids with decomposition. Protect from light.

The United States Pharmacopeia 31, 2008 (Bismuth Subsalicylate). A basic salt corresponding to C7H5Bi04 and containing not less than 56.0% and not more than 59.4% of Bi and not less than 36.5% and not more than 39.3% of total salicylates. It is a fine, odourless, white to off-white micro-crystalline powder. Practically insoluble in water, in alcohol, and in ether. It reacts with alkalis and mineral acids. Store in airtight containers. Protect from light.

Bismuth Subcarbonate

(US Adopted Name)

Drug Nomenclature

Bismuth CompoundsSynonyms: Bázisos bizmutkarbonát; Basic Bismuth Carbonate; Basisches Wismutkarbonat; Bism. Carb.; Bismuth Carbonate; Bismuth Oxycarbonate; Bismuthi Subcarbonas; Bismuto subkarbonatas; Bismutylum Carbonicum; Carbonato de Bismutila; Subcarbonato de bismuto; Uhličitan bismutitý zásaditý; Vismutsubkarbonat; Vismuttisubkarbonaatti
USAN: Bismuth Subcarbonate
Molecular formula: CBi2O5 =510.0
CAS: 5892-10-4 (anhydrous bismuth subcarbonate); 5798-45-8 (bismuth subcarbonate hemihydrate)

Pharmacopoeias. In China, Europe, and US.

European Pharmacopoeia, 6th ed. (Bismuth Subcarbonate). A white or almost white powder. Practically insoluble in water and in alcohol. It dissolves in mineral acids with effervescence. Protect from light.

The United States Pharmacopeia 31, 2008 (Bismuth Subcarbonate). A white or almost white powder. Practically insoluble in water, in alcohol, and in ether dissolves in dilute acids with effervescence. Protect from light.

Bismuth Subcitrate Potassium

(US Adopted Name)

Note. Do not confuse with bismuth citrate or tripotassium dicitratobismuthate (colloidal bismuth subcitrate).

Bismuth Subgallate

(US Adopted Name)

Drug Nomenclature

Synonyms: Bázisos bizmut-gallát; Basic Bismuth Gallate; Basisches Wismutgallat; Bism. Subgall.; Bismuth Oxygallate; Bismuthi Subgallas; Bismuto subgalatas; Gallan bismutitý zásaditý; Subgalato de bismuto; Vismutsubgallat; Vismuttisubgallaatti
USAN: Bismuth Subgallate
Molecular formula: C7H5BiO6 =394.1
CAS: 99-26-3

Pharmacopoeias. In Europe, Japan, and US.

 

European Pharmacopoeia, 6th ed. (Bismuth Subgallate). A complex of bismuth and gallic acid. It contains not less than 48% and not more than 51 % of Bi, calculated with reference to the dried substance. A yellow powder. Practically insoluble in water and in alcohol dissolves in mineral acids with decomposition and in alkali hydroxides, producing a reddish-brown liquid. Protect from light.

The United States Pharmacopeia 31, 2008 (Bismuth Subgallate). A basic salt containing 52 to 57% of Bi203 when dried at 105° for 3 hours. It is an odourless amorphous bright yellow powder. Practically insoluble in water, in alcohol, in chloroform, and in ether insoluble in very dilute mineral acids dissolves readily with decomposition in warm, moderately dilute hydrochloric, nitric, or sulfuric acids readily dissolves in solutions of alkali hydroxides to form a clear yellow liquid which rapidly becomes deep red. Store in airtight containers. Protect from light.

Bismuth Subnitrate

Drug Nomenclature

Synonyms: Bázisos bizmut-nitrát; Basic Bismuth Nitrate; Basisches Wismutnitrat; Bism. Subnit.; Bismuth (Sous-Nitrate de) Lourd; Bismuth Hydroxide Nitrate Oxide; Bismuth Nitrate, Heavy; Bismuth Oxynitrate; Bismuthi Subnitras; Bismuthyl Nitrate; Bismuto subnitratas; Bismuto subnitratas sunkusis; Magistery of Bismuth; Nitrato de Bismutilo; Subazotato de Bismuto; Subnitrato de bismuto; Vismutsubnitrat; Vismuttisubnitraatti; White Bismuth
Molecular formula: Bi5O(OH)9(NO3)4 =1462.0
CAS: 1304-85-4
ATC code: A02BX12

Pharmacopoeias. In Europe, Japan, and US. France also includes Bismuth (Sous-Nitrate de) Leger (Bismuthi Subnitras Levis) which is described as a variable mixture of bismuth hydroxide, carbonate, and subnitrate.

European Pharmacopoeia, 6th ed. (Bismuth Subnitrate, Heavy). It contains not less than 71 % and not more than 74% of Bi, calculated with reference to the dried substance. A white or almost white powder. Practically insoluble in water and in alcohol dissolves in mineral acids with decomposition.

The United States Pharmacopeia 31, 2008 (Bismuth Subnitrate). A basic salt containing not less than 79% of Bi203 calculated on the dried basis. It is a white, slightly hygroscopic powder. Practically insoluble in water and in alcohol readily dissolves in nitric and hydrochloric acids.

Tripotassium Dicitratobismuthate

Drug Nomenclature

Synonyms: Colloidal Bismuth Subcitrate; Dicitratobismutato tripotásico
CAS: 57644-54-9
ATC code: A02BX05

Note. Do not confuse with bismuth citrate or bismuth subcitrate potassium.

Adverse Effects, Treatment, and Precautions

The bismuth compounds listed above are insoluble or very poorly soluble, and bismuth toxicity does not appear to be common if they are used for limited periods. However, excessive or prolonged dosage may produce symptoms of bismuth poisoning, and for this reason long-term systemic therapy is not recommended. Reversible encephalopathy (see below) was once a problem in some countries, notably France and Australia bone and joint toxicity had also occurred, sometimes associated with the encephalopathy. This led to restrictions on the use of bismuth salts and a virtual disappearance of these toxic effects. Nausea and vomiting have been reported. Darkening or blackening of the faeces and tongue may occur due to conversion to bismuth sulfide in the gastrointestinal tract.

The effects of acute bismuth intoxication include gastrointestinal disturbances, skin reactions, stomatitis, and discoloration of mucous membranes a characteristic blue line may appear on the gums. There may be renal failure and liver damage. Other adverse effects may not be related to the bismuth content. With bismuth subnitrate given orally there is a risk of the nitrate being reduced in the intestines to nitrite and the development of methaemoglobinaemia. Absorption of salicylate occurs from oral bismuth salicylate and therefore the adverse effects, treatment of adverse effects, and precautions of aspirin should be considered.

Gastric lavage should be considered in overdosage activated charcoal by mouth and the use of a chelating agent such as dimercaprol, succimer, or unithiol have been recommended (see also Overdosage, below). Renal function should be monitored for 10 days after acute overdosage.

Bismuth compounds should not be given to patients with moderate to severe renal impairment.

Encephalopathy. Reviews and reports of bismuth encephalopathy. Many of the original reports implicated bismuth subgallate or subnitrate, in most but not all cases at high doses or for prolonged periods toxicity has also occurred with other salts. Patients receiving the subcitrate (480 mg daily) or the subnitrate (1.8 g daily) for 8 weeks in the treatment of Helicobacter pylori infection, showed no evidence of neurological changes compared with a control group.

TOPICAL APPLICATION. Encephalopathy has been associated with the use of bismuth iodoform paraffin paste (BIPP) for the packing of wound cavities after surgery to the head and neck, although there is some debate as to whether the bismuth or the iodoform component is responsible.

Overdosage. Bismuth salicylate or tripotassium dicitratobismuthate in recommended doses are rarely associated with serious adverse effects but there are reports of renal failure, encephalopathy, and neurotoxicity in acute or chronic overdose. Bismuth has been detected in the blood, urine, stools, and kidneys of these patients a blood concentration of 1.6 micrograms/mL was found 4 hours after an oral dose of 9.6 g.

The optimal treatment of bismuth overdosage is unknown. Gastric lavage, purgation, and hydration should be considered, even if the patient presents late, as bismuth may be absorbed from the colon. Chelating agents may be effective unithiol has been reported to increase the renal clearance of bismuth with a reduction in the blood concentration. Haemodialysis may be necessary” but whether this hastens tissue clearance is uncertain. Haemodialysis plus unithiol treatment has been reported to successfully eliminate bismuth. Peritoneal dialysis has also been effectively used in a paediatric patient.

Prolonged ingestion of bismuth salicylate in excessive doses by an elderly diabetic was associated with hearing disturbances, vertigo, acid-base abnormalities and mild clotting disturbances. The toxicity was thought to be due to the salicylate component.

Toxicity from non-conventional use. The FDA has warned against use of an injectable product called bismacine or chromacine, which contains large amounts of bismuth. There are reports of death or serious adverse effects associated with its use. Although unlicensed for any use, bismacine has apparently been used in alternative medicine to treat Lyme disease.

 

Interactions

Bismuth salts given orally reduce the absorption of tetracyclines, possibly by chelation or by reducing tetracycline solubility as a result of increasing the gastric pH. This interaction can be minimised by separating doses of the two drugs by a couple of hours. The clinical significance of this interaction to the use of bismuth salts for peptic ulcer disease is unclear tripotassium dicitratobismuthate or bismuth salicylate have been given at the same time as tetracycline as part of triple therapy for the eradication of Helicobacterpylori.

Antisecretory drugs. Pretreatment with omeprazole resulted in about a threefold increase in absorption of bismuth from tripotassium dicitratobismuthate in 6 healthy subjects. The mean peak plasma concentration of bismuth after a single dose of 240 mg of tripotassium dicitratobismuthate was increased from 36.7 to 86.7 nanograms/mL after omeprazole suggesting an increased risk of toxicity from combined therapy. The mechanism was thought to be the increase in gastric pH produced by the antisecretory drug as similar results had been reported with ranitidine However, the clinical significance of these interactions to the use of antisecretory drugs with bismuth compounds for eradication of Helicobacter pylori is unclear bismuth compounds have been combined with proton pump inhibitors or H2 antagonists in short-term regimens as part of triple or quadruple therapy.

Pharmacokinetics

Poorly soluble bismuth compounds are largely converted to insoluble bismuth oxide, hydroxide, and oxychloride in the acidic environment of the stomach. Most of the bismuth compounds included in this monograph are thus only slightly absorbed. Increased gastric pH may increase bismuth absorption — see Antisecretory Drugs, above. Unabsorbed bismuth is excreted in the faeces. Absorbed bismuth is distributed throughout body tissues, including bone, and is slowly excreted in the urine and bile. It has a plasma half-life of about 5 days and continues to be excreted for about 12 weeks after stopping therapy.

Uses and Administration

Some insoluble salts of bismuth are given orally for their supposed antacid action and for their mildly astringent action in various gastrointestinal disorders, including diarrhoea and dyspepsia. Such salts include the aluminate, salicylate, subcarbonate, and subnitrate. Bismuth salicylate, which is given as an antidiarrhoeal and weak antacid in doses up to about 4 g daily in divided doses, possesses in addition the properties of the salicylates.

Tripotassium dicitratobismuthate is active against Helicobacter pylori and has been used as triple therapy (with metronidazole and either tetracycline or amoxicillin) to eradicate this organism and thereby prevent relapse of duodenal ulcer. It is also used as a mucosal protectant for the treatment of peptic ulcer disease. Bismuth subcitrate potassium and bismuth salicylate are also active against H. pylori and have been used similarly in eradication regimens.

The usual oral dose of tripotassium dicitratobismuthate in benign gastric and duodenal ulceration is 240 mg twice daily, or 120 mg four times daily before food. Treatment is for a period of 4 weeks, extended to 8 weeks if necessary. Maintenance therapy with tripotassium dicitratobismuthate is not recommended although treatment may be repeated after a drug-free interval of one month. When used as part of triple therapy the usual dose of tripotassium dicitratobismuthate has been 120 mg four times daily for 2 weeks. The usual dose of bismuth salicylate as part of triple therapy is 525 mg four times daily for 2 weeks. Appropriate antisecretory treatment with a histamine H2-antagonist or a proton pump inhibitor is usually added to these regimens.

A complex of bismuth citrate with ranitidine, ranitidine bismuth citrate, is also used in the treatment of peptic ulcer disease.

Some insoluble salts of bismuth have been used topically in the treatment of skin disorders, wounds, and burns. Some have been used as ingredients of ointments or suppositories (sometimes containing more than one bismuth salt) in the treatment of haemorrhoids and other anorectal disorders. Bismuth compounds that have been used topically and/or rectally include the oxide, subgallate, and subnitrate bismuth re-sorcinol compounds have also been used. For the use of bismuth subnitrate and iodoform paste as a wound dressing, see Iodoform.

Numerous other salts and compounds of bismuth have been promoted for various therapeutic purposes. Gly-cobiarsol was formerly given orally as an amoebicide.

Homoeopathy. Bismuth has been used in homoeopathic medicines under the following names: Bismuth-um Bismutum metallicum.

Bismuth oxide has been used in homoeopathic medicines under the following names: Bismuthum oxydatum; Bis. ox.

Bismuth subnitrate has been used in homoeopathic medicines under the following names: Heavy bismuth subnitrate; Bismuthi subnitras ponderosus; Bismutum subnitricum; Bism. sub.

Preparations

BPC 1954: Bismuth Subnitrate and Iodoform Paste

The United States Pharmacopeia 31, 2008: Bismuth Subsalicylate Magma Bismuth Subsalicylate Oral Suspension Bismuth Subsalicylate Tablets Compound Resorcinol Ointment Milk of Bismuth.

Proprietary Preparations

Argentina: Re-Dux Sesamoil

Brazil: Pepto-Bismol Peptosan Peptulan Senophile

Canada: Bismed Maalox Multi-action Neo-Laryngobis Pepto-Bismol Personnel

Czech Republic: De-Nol Jatrox

France: Amygdorectol

Germany: Angass S Dermatol Haemo-Exhirud Bufexamac Katuldn-R Stryphnasal N Telen

Greece: De-Nol

Hong Kong: De-Nol

Hungary: De-Nol

India: Trymo

Indonesia: Scantoma

Ireland: De-Noltab

Israel: Kalbeten Pink Bismuth

Italy: De-Nol

Mexico: Biselicf Bismed Bismofarma Bisval Facidmol Itamol Pepto-Bismol Siparox Sucrato

The Netherlands: De-Nol

New Zealand: De-Nol

Portugal: De-Nol

Russia: De-Nol

South Africa: De-Nol

Singapore De-Nol

Spain: Gastrodenol Rectamigdol

Switzerland: Amygdorectol

Thailand: Gastro-Bismol

Turkey: De-Nol Dermatol

UK: De-Noltab Pepto-Bismol

USA: Bismatrol Children’s Kaopectate Devrom K-Pek Kao-Tin Kaopectate Kapectolin Maalox Total Stomach Relief Peptic Relief Pepto-Bismol

 

Multi-ingredient

Argentina: Anusol Anusol Duo S Benitol Bismuto con Pectina Colistop Colistoral Crema De Bismuto Cutidermin Gastop Gastranil Gastricur Histidanol Lemil Mabis

Belgium: Gastrofilm Procto-Synalar Rectovasol

Brazil: Aftine Anusol-HC Bismu-Jet Bisuisanf Claudemor Colutoide Cutisanol Magnesia Bisurada Neoseptil Salicilato de Bismuto Composto Senophile

Canada: Bismutal Onrectal Pepto-Bismol Thunas Pile

Czech Republic: Carbocit Mastu S Sagittaproct Spofax Suspensio Visnevski cum Pice Liquida Herbacos

Finland: Tannopon

France: Anoreine Anusol Cutiphile Paps Pholcones Bismuth

Germany: Angass Anisan Bismolan H Corti Bismolan N Bismolan Combustin Heilsalbe Duoventrin Eulatin N Eulatin NN Faktu akut Friosmin N Hamo-ratiopharm N Hamoagil plus Mastu S Nervogastrol N Pascomag Spasmo-Nervogastrol Tamposit N Ventricon N Wismut comp

Hong Kong: Anusol Anusol-HC Haemoral Mastu S Rowatanal

Hungary: Bolus Adstringens Dermaforine Mastu S Nilacid

Indonesia: Anusol Anusol-HC

Ireland: Anugesic-HC Anusol Anusol-HC Rowatanal

Italy: Antiemorroidali Anusol

Malaysia: Rowatanal

Mexico: Estomacurol Heliton

The Netherlands: Anaesthetica Roteroblong Maagtabletten Theranal

Poland: Gastro Hemo rectal

Portugal: Claudemor Servetinal Synalar Rectal

Russia: Anaesthesol Anusol Neo-Anusol Proctosan Simetrid

South Africa: Anugesic Anusol Arola Rosebalm Biskapect Bisma Rex Chloropect Enterodyne Kantrexil Sentinel Ulcer Mixture

Singapore: Rowatanal

Spain: Grietalgen Grietalgen Hidrocort Hemodren Compuesto Nasopomada Pomada Infantil Vera Sabanotropico Synalar Rectal

Switzerland: Bismorectal Cicafissan Euproctol N Fissan Furodermal Haemocortin Haemolan La pommade du Dr Brand Leucen Magenpulver Hafter Magentabletten Hafter Rectoseptal-Neo bismuthe

Turkey: Dermikolin Hemoralgine Kortos Metamorfoz

UK: Anugesic-HC Anusol Anusol-HC, Plus HC Bisma-Rex Hemocane Moorland OxBipp Stomach Mixture

USA: Anumed Anumed HC BFI Calmol Helidac Hem-Prep Hemril K-C Kao-Paverin Kaodene Non-Narcotic Mammol Fylera Rectagene Medicated Rectal Balm

Venezuela: Claudemorf Klincosal Polantac.

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