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PubMedDate not supplied

Uptake of bismuth in motor neurons of mice after single oral doses of bismuth compounds.

Bismuth, a component of many gastrointestinal medications, is a heavy metal little studied as regards nervous system uptake. We were interested to see if low doses of intragastric bismuth entered the nervous system, and if dietary selenium influenced the amount of bismuth detected. Mice were given 40 to 1200 mg/kg of bismuth subnitrate (BSN), bismuth subsalicylate (BSS), colloidal bismuth subcitrate (CBS), or ranitidine bismuth citrate (RBC) intragastrically. Mice on low- or high-selenium diets were given 4 to 32 mg/kg of bismuth from RBC. One week later, sections of nervous tissue were stained with autometallography to detect bismuth grains (Bi(AMG)). Bismuth was found in neurons with axons outside of the nervous system, in particular motor neurons, and in cells outside the blood-brain barrier. The lowest bismuth dose which resulted in Bi(AMG) in motor neurons was 696 mg/kg from BSN, 57 mg/kg from BSS, 29 mg/kg from CBS, and 26 mg/kg from RBC. No bismuth was seen in motor neurons of mice on the low-selenium diet. Intragastric doses of bismuth therefore enter mouse motor neurons, and the amount detectable varies with dietary selenium.

Administration, Oral↗
PubMedDate not supplied

Pharmacokinetics and toxicity of bismuth compounds.

Inorganic bismuth salts are poorly soluble in water: solubility is influenced by the acidity of the medium and the presence of certain compounds with (hydr)oxy or sulfhydryl groups. The analysis of bismuth in biological material is not standardised and is subject to large variation; it is difficult to compare data from different studies, and older data should be approached with caution. The normal concentration of bismuth in blood is between 1 and 15 micrograms/L, but absorption from oral preparations produces a significant rise. Distribution of bismuth in the organs is largely independent of the compound administered or the route of administration: the concentration in kidney is always highest and the substance is also retained there for a long time. It is bound to a bismuth-metal binding protein in the kidney, the synthesis of which can be induced by the metal itself. Elimination from the body takes place by the urinary and faecal routes, but the exact proportion contributed by each route is still unknown. Elimination from blood displays multicompartment pharmacokinetics, the shortest half-life described in humans being 3.5 minutes, and the longest 17 to 22 years. A number of toxic effects have been attributed to bismuth compounds in humans: nephropathy, encephalopathy, osteoarthropathy, gingivitis, stomatitis and colitis. Whether hepatitis is a side effect, however, is open to dispute. Each of these adverse effects is associated with certain bismuth compounds. Bismuth encephalopathy occurred in France as an epidemic of toxicity and was associated with the intake of inorganic salts including bismuth subnitrate, subcarbonate and subgallate. In the prodromal phase patients developed problems in walking, standing or writing, deterioration of memory, changes in behaviour, insomnia and muscle cramps, together with several psychiatric symptoms. The manifest phase started abruptly and was characterised by changes in awareness, myoclonia, astasia and/or abasia and dysarthria. Patients recovered spontaneously after discontinuation of bismuth. Intestinal lavage, forced diuresis and haemodialysis have been tried without positive effects on the clinical condition of the patient or on blood bismuth concentration, and the use of dimercaprol as an antidote has produced reports of both positive and negative findings. To confirm the diagnosis of bismuth encephalopathy, it is essential to find elevated bismuth concentrations in blood, plasma, serum or CSF. A safety level of 50 micrograms/L and an alarm level of 100 micrograms/L have been suggested in the past, but no proof is available to support the choice of these levels.(ABSTRACT TRUNCATED AT 400 WORDS)

Animals↗
PubMedDate not supplied

In vitro and in vivo effects of three bismuth compounds on fermentation by colonic bacteria.

Three bismuth compounds (tripotassium dicitrate bismuthate, bismuth subsalicylate, and bismuth subnitrate) were tested in vitro and in vivo for their effect on fermentation by colonic bacteria. The studies in vitro were done with use of a technique designed to determine the effect of each one of the bismuth compounds on the fermentation of several stool samples that had been mixed with lactose as additional fermentable substrate (fermentation of lactose-enriched stools, FLES). The three bismuth compounds reduced FLES significantly in 47 (81%) of 58 of the stool samples used to test their effect. Bismuth subsalicylate, which reduced FLES in 10 of 10 stool samples, showed the greatest reduction (mean reduction, 74%; P less than .0001). The in vivo studies, done in six flatulent patients, showed significant reduction (P less than .01) of colonic fermentation of ingested raffinose by oral bismuth subnitrate given for 8 days.

Adolescent↗
PubMedDate not supplied

Pharmacology of bismuth-containing compounds.

Bismuth compounds have been used for more than two centuries. A review of the modes of action, pharmacokinetics, and toxicity of two commonly used compounds, colloidal bismuth subcitrate and bismuth subsalicylate, is presented. In humans bismuth toxicity is unlikely when therapeutic doses of these compounds are administered for the appropriate duration. The recent use of bismuth compounds to eradicate infection with Helicobacter pylori and to prevent travelers' diarrhea has resulted in scientific reevaluation of these agents.

Anti-Ulcer Agents↗
PubMed1997

Novel bismuth compounds have in vitro activity against Helicobacter pylori.

The increasing antimicrobial resistance in Helicobacter pylori has led to the search for new therapeutic agents. In this in vitro study, novel compounds combining bismuth with sialic acid inhibitors were investigated for bactericidal activity using time-kill methodology. The activity of these compounds was compared to bismuth subcitrate against a type strain and a clinical isolate of H. pylori. The compounds tested showed cidal activity which was related to the bismuth component of each drug. These compounds may offer a potential advantage over current bismuth preparations with the sialic acid inhibitor moiety interfering with adhesion of H. pylori to gastric epithelium.

Bacterial Adhesion↗
PubMed2006

Effect of oral administration of bismuth compounds on Campylobacter colonization in broilers.

Bismuth compounds have been used since the 18th century to treat gastrointestinal ailments in man. Colloidal bismuth subcitrate (De-Nol) is currently used in combination with antibiotics to reduce enteric Helicobacter pylori colonization as a treatment of stomach ulcers. We investigated whether bismuth citrate or its parent compound, colloidal bismuth subcitrate, would reduce colonization of the closely related foodborne pathogen, Campylobacter jejuni in chickens. In 2 studies, birds were either fed 0, 50, or 200 ppm bismuth citrate or bismuth subcitrate (De-Nol) for 10 or 21 d and were orally challenged with 7 combined strains of C. jejuni (n = 6 birds/treatment). For both treatment groups, cecal Campylobacter colonization was reduced when birds were fed 200 ppm for 10 d but not 21 d. For the 50 ppm treatment group, only birds dosed with bismuth citrate for 21 d demonstrated any reduction in cecal Campylobacter concentrations when compared with controls. These data suggest that bismuth citrate and colloidal bismuth subcitrate may reduce cecal colonization by Campylobacter in broilers, but these effects are inconsistent.

Administration, Oral↗
PubMed1998

Chemical structure of bismuth compounds determines their gastric ulcer healing efficacy and anti-Helicobacter pylori activity.

The recognition of the role of Helicobacter pylori in the pathogenesis of peptic ulcer disease has led to renewed interest in bismuth pharmacology since bismuth compounds have both anti-Helicobacter pylori and ulcer healing properties. The precise chemical structure of current bismuth compounds is not known. This has hindered the development of new and potentially more efficacious formulations. We have created two new compounds, 2-chloro-1,3-dithia-2-bismolane (CDTB) and 1,2-[bis(1,3-dithia-2-bismolane)thio]ethane (BTBT), with known structure. In a rat model of gastric ulceration, BTBT was comparable to, and CDTB was significantly less effective than colloidal bismuth subcitrate in healing cryoprobe-induced ulcers. However, both BTBT and CDTB inhibited H. pylori growth in vitro at concentrations <1/10 that of colloidal bismuth subcitrate. The effects on ulcer healing are not mediated by suppression of acid secretion, pepsin inhibition, or prostaglandin production. Since all treated animals received the same amount of elemental bismuth, it appears that the efficacy of bismuth compounds varies with compound structure and is not simply dependent on the delivery of bismuth ion. Because the structure of the novel compounds is known, our understanding of the relationship of bismuth compound structure and to biologic activity will increase. In the future it may be possible to design other novel bismuth compounds with more potent anti-H. pylori and ulcer healing effects.

Animals↗
PubMed2002

Antimony and bismuth compounds in oncology.

The main group elements antimony and bismuth are used clinically, primarily for the treatment of Leishmaniasis (antimony) and ulcers (bismuth). Despite their medicinal efficacy, the exploration of the anti-cancer potential of antimony and bismuth compounds is not as well developed as for other metal-containing species. The results of cytotoxicity and anti-tumour screening for antimony(III), antimony(V) and bismuth(III) compounds are summarised in this review. While this is a relatively undeveloped field of research endeavour, promising anti-tumour activity has been reported, in particular for bismuth compounds.

Animals↗
PubMed1995

Influence of hydroxycarboxylic acids on the water solubility of various bismuth compounds.

In an equilibrium dialysis assay (bismuth being determined by atomic absorption spectrometry) a constant amount of bismuth (Bi, CAS 7440-69-9) (final maximum conc. 50 mumol Bi/l) was dialyzed against solutions with increasing concentrations of the chelators (0-25 mmol/l). At pH 5, 50% of Bi(III) nitrate was soluble in solutions with 0.3, 6.3, 13.4 and 14.6 mmol/l of edetic acid (EDTA), citric, tartaric and malic acid, respectively. At the highest concentration applied, lactic acid kept 7% of bismuth in solution. Without any chelator, bismuth was found to be essentially insoluble (limit of detection: approx. 4 nmol Bi/l). A concentration-dependent increase in solubility was found also for the other bismuth compounds; the sequence of the solubilizing capacity of the chelators was the same as for Bi(III) nitrate. Lowering the pH to 3 generally increased and raising the pH to 7, decreased the solubility of bismuth.

Bismuth↗
PubMed1999

Antimicrobial activities of synthetic bismuth compounds against Clostridium difficile.

Clostridium difficile is a major nosocomial pathogen responsible for pseudomembranous colitis and many cases of antibiotic-associated diarrhea. Because of potential relapse of disease with current antimicrobial therapy protocols, there is a need for additional and/or alternative antimicrobial agents for the treatment of disease caused by C. difficile. We have synthesized a systematic series of 14 structurally simple bismuth compounds and assessed their biological activities against C. difficile and four other gastrointestinal species, including Helicobacter pylori. Here, we report on the activities of six compounds that exhibit antibacterial activities against C. difficile, and some of the compounds have MICs of less than 1 microgram/ml. Also tested, for comparison, were the activities of bismuth subcitrate and ranitidine bismuth citrate obtained from commercial sources. C. difficile and H. pylori were more sensitive both to the synthetic bismuth compounds and to the commercial products than were Escherichia coli, Pseudomonas aeruginosa, and Proteus mirabilis, and the last three species were markedly resistant to the commercial bismuth salts. Testing with human foreskin fibroblast cells revealed that some of the synthetic compounds were more cytotoxic than others. Killing curves for C. difficile treated with the more active compounds revealed rapid death, and electron microscopy showed that the bismuth of these compounds was rapidly incorporated by C. difficile. Energy dispersive spectroscopy X-ray microanalysis of C. difficile cells containing electron-dense material confirmed the presence of internalized bismuth. Internalized bismuth was not observed in C. difficile treated with synthetic bismuth compounds that lacked antimicrobial activity, which suggests that the uptake of the metal is required for killing activity. The nature of the carrier would seem to determine whether bismuth is transported into susceptible bacteria like C. difficile.

Anti-Bacterial Agents↗
PubMed1988

Biological activity of organometallic bismuth compounds.

The chemical aspects of organometallic bismuth(III) compounds are discussed with respect to the stability of the metal-carbon sigma bond, their low dipole moments, and the limited solubility of these complexes in hydrophilic solvents. A new Bi heterocycle, which is of potential interest in terms of stability and solution behaviour, was shown to exist as an intermediate under the conditions in the mass spectrometer. Although generally bismuth organic compounds are extremely toxic, in the 1970s they became important as biocides and this is still being investigated. They have also been discussed as irritation causing chemical warfare agents. While their application in chemotherapy never became very widespread because antibiotics were discovered, in the last few years the antitumor activity of some derivatives has been reported.

Animals↗
PubMed1992

Comparison of one-day oral dosing with three bismuth compounds for the suppression of Helicobacter pylori assessed by the 13C-urea breath test.

Assessment of intragastric urease activity by the 13C-urea breath test was performed before and after one day of dosing with either De-Noltabs (tripotassium dicitrato bismuthate, one tablet 1 q.d.s.), Pepto-Bismol liquid (bismuth salicylate 30 ml q.d.s.), or Roter tablets (bismuth subnitrate, one tablet q.d.s.) in twelve Helicobacter pylori-positive patient volunteers. There was a significant decrease in the excess of 13CO2 after one day of dosing with each of the three bismuth compounds, but analysis of variance could detect no difference between the effects of the three compounds. Systemic absorption of bismuth following oral dosing with either Pepto-Bismol or Roter is minimal, yet both compounds have a suppressive effect on H. pylori similar to that of De-Noltab. This study suggests that the action of all three bismuth compounds is within the gastric lumen, and that systemic absorption of bismuth is not necessary for activity against H. pylori.

Adult↗
PubMed1992

Bismuth absorption from 205Bi-labelled pharmaceutical bismuth compounds used in the treatment of peptic ulcer disease.

The absorption of bismuth from five 205Bi-labelled pharmaceutically used bismuth compounds was studied in man. From single oral doses of all compounds under investigation only less than 0.1% bismuth was absorbed and excreted with the urine. A significantly higher absorption was observed from the colloidal bismuth subcitrate (0.042% of the dose) and the basic bismuth gallate (0.038%) than from the basic bismuth salicylate, nitrate, and aluminate (0.005-0.002%). No retention of bismuth in the whole body was found from the single dose experiment. The biologic fast-term half-lives of absorbed bismuth were calculated to be 0.12 and 1.5 days.

Adult↗
PubMed2002

Radiopacity in bone cements using an organo-bismuth compound.

In a joint replacement surgery it is vital for bone cement to be radiologically detectable. Consequently, heavy metal salts of barium and zirconia are incorporated as a contrast medium for this purpose. The addition of such particulate additives, however, can be detrimental to some of the physical, mechanical and biological properties. The present study reports the feasibility of using an organo-bismuth compound, namely. triphenyl bismuth (TPB) as a radiopaque agent for orthopaedic bone cements. TPB was incorporated in the bone cement matrix by two methods, (i) blending: TPB was added to the polymer phase of the bone cement and (ii) dissolution: by dissolving TPB in the monomer phase methylmethacrylate. The results showed that the inclusion of TPB at concentrations of 15% and 25% by weight of the polymer, in the bone cement matrix did not affect the polymerisation exotherm temperature and setting time. Furthermore, the addition of TPB via the dissolution method provided a statistically significant increase in the strain to failure in comparison to commercial acrylic cements containing barium sulphate, thus reducing the brittleness of the cement. The detrimental effects on the mechanical properties post conditioning in water, was also much less pronounced in the homogeneous TPB cements in comparison to barium sulphate containing cements. These observations can be attributed to the formation of a homogeneous and continuous matrix of the resultant bone cement with a much lower porosity.

Bismuth↗
PubMed1991

The effect of GR122311X, a bismuth compound with H2-antagonist activity, on 24-hour intragastric acidity.

GR122311X (ranitidine bismuth citrate Glaxo Group Research Ltd) is a bismuth compound with histamine H2-receptor antagonist activity. The gastric acid antisecretory activity of three oral dosage regimens of GR122311X was compared with placebo and 150 mg ranitidine b.d. The median 24-h integrated intragastric acidity was 38, 26 and 18% of the median placebo value during dosing with GR122311X 196, 391 and 782 mg b.d., respectively. The 24-h acid suppression with GR122311X 391 mg b.d. was not significantly different to that produced by 150 mg ranitidine b.d. (24% of placebo acidity). The median 24-h urinary bismuth excretion increased with rising dosage of GR122311X from 19.2 micrograms with 196 mg b.d., to 36.4 micrograms with 391 mg b.d., to 68.7 micrograms with 782 mg b.d. In conclusion, GR122311X is an effective antisecretory agent with modest systemic bismuth absorption.

Adolescent↗
PubMed2000

Therapeutic role for bismuth compounds in TNBS-induced colitis in the rat.

The 2,4,6-trinitrobenzene sulfonic acid (TNBS) -induced model of chronic inflammation of the rat colon was used to determine the efficacy of bismuth subsalicylate (BSS), bismuth subcitrate (CBS), and 5-aminosalicylic acid (5-ASA) administered in enema form. A novel bismuth compound 1, 2-bis[2-(1,3-dithiobismolane)thio]ethane [Bi2(EDT)3] was also tested. On day 1 colitis was induced with 50 mg TNBS/50% ethanol in female Sprague-Dawley rats, while controls received a saline enema. On day 3, twice-daily treatment with enemas of either saline, BSS, CBS, Bi2(EDT)3, or 5-ASA were initiated in the colitis and control rats. All rats were killed on day 14, and the colons excised, weighed, rated macroscopically, and then fixed for hematoxylin and eosin staining. Blinded microscopic scoring was used to determine injury and healing in all groups. Colon mass and macroscopic scores were increased (P < 0.05) in the group of rats treated with TNBS (N = 16) compared to saline controls (N = 12). Colon mass and macroscopic scores in controls treated with BSS (N = 4), CBS (N = 4), Bi2(EDT)3 (N = 4), and 5-ASA (N = 4) alone did not differ from saline control animals. Macroscopic scoring showed a decrease (P < 0.05) in the degree of damage in the group of rats treated with TNBS plus BSS (N = 15), TNBS plus Bi2(EDT)3 (N = 10) and TNBS plus CBS (N = 4) compared to the group of rats treated with TNBS plus saline (N = 16). A decrease (P < 0.05) in injury and an increase (P < 0.05, Kruskal-Wallis) in healing was observed in the groups of rats treated with TNBS plus BSS, TNBS plus CBS, and TNBS plus 5-ASA compared to the group of rats treated with TNBS plus saline. It appeared that Bi2(EDT)3 was not protective against injury at the microscopic level but that the novel Bi2(EDT)3 has an effective healing capacity at the macroscopic level. We conclude that BSS and CBS decrease injury and/or promote healing as effectively as 5-ASA in this model.

Animals↗