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PubMed1993

Bismuth in human serum: reference interval and concentrations after intake of a therapeutic dose of colloidal bismuth subcitrate.

A sensitive method for the determination of the bismuth concentration in human serum is described. Analyses were carried out by inductively coupled plasma-mass spectrometry (ICP-MS), after a simple dilution of the samples with nitric acid. The detection limit of the applied method is 0.007 microgram/l whereas relative standard deviations varied from 5.7 to 13.6%. Determination of reference values in human serum of healthy adults gave a range from < 0.007 to 0.067 microgram/l (19 persons). Bismuth concentrations in serum were also measured before, during and after the intake of therapeutic doses of colloidal bismuth subcitrate (CBS). About 1.5-2 h after the intake of one tablet of CBS, the bismuth concentration in serum was found to have increased 51-1483 times (two apparently healthy volunteers and six hospitalized patients), showing that the serum bismuth concentrations can increase by several orders of magnitude during the intake of CBS. During the intake of four tablets of CBS per day by two apparently healthy volunteers, bismuth concentrations in serum after an overnight fast were found to be, respectively, 5.56 and 8.1 micrograms/l on day 15 and 4.28 and 13.6 micrograms/l on day 29. After stopping the therapy, the concentration of bismuth in serum slowly returned towards normal over a period of months.

Adult↗
PubMed1999

Bismuth-mediated disruption of the glycocalyx-cell wall of Helicobacter pylori: ultrastructural evidence for a mechanism of action for bismuth salts.

The mechanism of bismuth's bactericidal activity against Helicobacter pylori was investigated using transmission electron microscopy (TEM) and analytical electron microscopy (AEM); time-kill kinetic methods evaluated the effect of excess divalent cations. TEM analysis of untreated H. pylori revealed a normal morphology. In contrast, H. pylori exposed to bismuth salts had swollen, distorted cells with membrane-cell wall blebbing and a cytoplasm containing electron-dense, sometimes crystalline aggregates. By AEM, swollen cells contained bismuth at the cell periphery, whereas bacillary forms contained cytoplasmic bismuth localizations. Time-kill studies showed that the bactericidal activity of bismuth could be prevented by pretreatment with divalent cations. The effects of bismuth salts on the glycocalyces-cell walls of H. pylori with reversal of bactericidal activity by divalent cations are identical to those produced by other polycationic agents on various gram-negative bacilli. We conclude that disruption of the glycocalyces-cell walls of H. pylori is one mechanism of action for bismuth salts.

Anti-Bacterial Agents↗
PubMed1990

The absorption of bismuth and salicylate from oral doses of Pepto-Bismol (bismuth salicylate).

Plasma bismuth and plasma salicylate concentrations were measured before and after three 30-ml oral doses of bismuth salicylate (Pepto-Bismol liquid) in 10 fasting healthy subjects. From 0 to 120 min following the first dose of bismuth salicylate, the plasma bismuth concentration was less than 1 ng/ml. The peak median plasma bismuth concentration was at +240 min (1.7 ng/ml; range 0.8-5.3 ng/ml). Salicylate appeared in the plasma of all subjects at +30 min, and it reached a peak at +120 min (median 61 mg/L; range 46-104 mg/L). The study demonstrates that, despite rapid and substantial absorption of salicylate, there is negligible absorption of bismuth into the bloodstream from standard oral doses of bismuth salicylate.

Adult↗
PubMedDate not supplied

Absorption of bismuth from two bismuth compounds before and after healing of peptic ulcers.

BACKGROUND/AIMS: Previous reports state that there is absorption of bismuth through active peptic ulcers. It was therefore of interest to investigate the extent of absorption in patients at the ulcer and post-ulcer stages. METHODOLOGY: Twenty H. pylori-positive patients with gastroscopically verified gastric or duodenal ulcers were randomly allocated to ingest 3000 mg bismuth subnitrate (BSN) (10 patients) or 480 mg colloidal bismuth subcitrate (CBS) (10 patients). Bismuth serum concentration in 12 samples drawn during the first 4 hours after drug intake was analyzed and the area under the curve (Bi-AUC) was calculated. Anti-H. pylori therapy with amoxicillin and lanzoprazole eradicated H. pylori in 10 patients and healed the ulcers in all patients 4 weeks after therapy ended, then the bismuth absorption test was repeated. RESULTS: There was no significant difference between ulcer- and post-ulcer Bi-AUC for patients receiving BSN or for patients receiving CBS. On a molar basis, CBS gave a 17.4-fold greater absorption of bismuth compared to BSN. CONCLUSIONS: The presence of an active ulcer does not significantly influence the absorption of bismuth from CBS or BSN.

Administration, Oral↗
PubMed1985

Brain and blood levels of bismuth after oral or parenteral administration of tripotassium-dicitrato bismuthate to rats.

Bismuth levels in blood and brain of rats have been measured following acute or subchronic administration of tri-potassium-dicitrato bismuthate (TDB) by intraperitoneal injection or by gavage. After parenteral administration, the presence of bismuth in blood was associated with appreciable bismuth concentrations in brain of treated animals (approximately equal to 10-30% of blood levels). In contrast, following oral treatment, no bismuth was detected in brain of animals, even at doses of TDB able to produce blood bismuth concentrations comparable with those obtained after intraperitoneal administration. The formation of different bismuth species in blood of treated animals depending upon the route of administration of TDB is suggested.

Administration, Oral↗
PubMedDate not supplied

Histochemical tracing of bismuth in testis from rats exposed intraperitoneally to bismuth subnitrate.

The histochemical silver amplification technique autometallography (AMG), was used to trace bismuth in the testis of Wistar rats injected intraperitoneally with bismuth subnitrate. In the seminiferous tubules, bismuth was located in lysosomes of Sertoli cells closely associated with heads of spermatids in the late stages of the spermatogenesis, i.e. shortly before the release of Step 19 spermatids in Stage XIII. No bismuth-specific AMG silver grains were detected in the spermatogenic cell line. However, tails of free sperm cells located in the tubular lumen showed autometallographic grains in close contact to the nine outer microtubule doublets in the axonema. Leydig cells concentrated huge amounts of AMG-bismuth in their lysosomes. Furthermore, parallel exposure to selenium significantly increased the amount of histochemically traceable bismuth in the rat testis.

Animals↗
PubMed1990

D-penicillamine does not increase urinary bismuth excretion in patients treated with tripotassium dicitrato bismuthate.

Twenty-four urinary bismuth excretion was measured in five patients who had been treated with tripotassium dicitrato bismuthate, before and after single 1 g oral dose of D-penicillamine. Before dosing with D-penicillamine, the median 24 h urinary bismuth output was 55 micrograms 24 h-1 (range 17-156 micrograms 24 h-1) and following dosing with D-penicillamine the median 24 h urinary bismuth output was 53 micrograms 24 h-1 (range 12-156 micrograms 24 h-1). D-penicillamine does not facilitate the urinary excretion of bismuth, hence it is unsuitable for use as an oral chelator in patients with bismuth intoxication.

Aged↗
PubMed1990

Bismuth induced encephalopathy caused by tri potassium dicitrato bismuthate in a patient with chronic renal failure.

A 68 year old man with a creatinine clearance rate of only 15 ml/min took twice the recommended dose of tripotassium dicitrato bismuthate (TDB) as DeNol liquid; 10 ml qds; a total of 864 mg bismuth daily for two months. Whole blood bismuth concentrations rose to 880 micrograms/l and he developed global cerebral dysfunction with hallucinations, ataxia, and an abnormal EEG. Renal clearance of bismuth rose from 0.24 to 2.4 ml/min when the heavy metal chelator 2-3 dimercapto-1 propane sulphonic acid (DMPS) was given by mouth. Bismuth was measured by a novel method involving inductively coupled plasma source mass spectrometry. Fifty days after stopping TDB, whole blood bismuth concentrations fell to 46 micrograms/l and the patient's EEG returned to normal. His mental function also recovered completely. The case serves as a timely reminder that TDB should not be administered to patients with renal disorders, as stated in the data sheet.

Aged↗
PubMed1991

A study relating to bioavailability and renal elimination of bismuth after oral administration of basic bismuth nitrate.

The extent to which bismuth is absorbed following single and multiple oral administration of basic bismuth nitrate was investigated in healthy male subjects. The blood concentration of bismuth and the amounts excreted in urine and feces were determined. The results show that only a small fraction of the administered bismuth dose given in this form is absorbed. Existing differences in the absorption kinetics between this relatively insoluble bismuth salt and colloidal bismuth citrate are discussed.

Administration, Oral↗
PubMed1977

[Bismuth treatment and blood bismuth levels].

The authors report the results of bismuth blood levels in 41 patients treated by oral route with bismuth salts used in gastro-enterology according to the Bensaude rule (10 to 20 g/day, 20 days/month). Median bismuth blood level during the period of treatment amounts to 13 microgram/l. It decreases to 7 microgram/l during the period of therapeutic withdrawal. In patients with bismuth encephalopathies (63 cases recorded in the literature) median values range from 680 to 700 microgram/l. The authors recommend the determination of bismuth blood levels as a monitoring method in bismuth treatment and propose the following values:--normal level during treatment : less than 50 microgram/l (in Bi metal);--alarm level : 50 to 100 microgram/l : (patients to be monitored);--toxicity level less than 100 microgram/l : (treatment to be interrupted).

Bismuth↗
PubMed1999

Colloidal bismuth pectin: an alternative to bismuth subcitrate for the treatment of Helicobacter pylori--positive duodenal ulcer.

BACKGROUND: Bismuth triple therapy provides consistently good results in Helicobacter pylori eradication worldwide, whereas quadruple therapy using a combination of omeprazole and bismuth triple regimen has produced cure rates in excess of 90%. The prevalence of metronidazole-resistant strains was 26.8% in our area. Colloidal bismuth pectin (CBP) is a new, lower-priced bismuth salt made in China. The purpose of this study was to investigate the efficacy and safety of CBP triple and quadruple regimens in the treatment of H. pylori-positive duodenal ulcer. MATERIALS AND METHODS: In this prospective trial, 205 patients with H. pylori-positive duodenal ulcer were allocated randomly to receive one of four regimens: metronidazole, 200 mg; amoxicillin, 250 mg; and colloidal bismuth subcitrate (CBS), 120 mg (group 1), or CBP, 100 mg qid (group 2) for 2 weeks, then continued CBS, 240 mg, or CBP, 200 mg bid for a further 2 weeks. A quadruple regimen using a combination of omeprazole, 20 mg bid, and CBS triple therapy (group 3) or CBP triple therapy (group 4), respectively, was given to patients for 1 week, followed by omeprazole, 20 mg once daily for a further 3 weeks. Further endoscopy was performed at least 4 weeks after cessation of the treatment. H. pylori status was determined by histology, a 14C urea breath test, and a urease test. RESULTS: The per-protocol H. pylori cure rates were 85% (22 of 26 patients), 90% (35 of 39), 96% (46 of 48), and 95% (75 of 79) for groups 1 through 4. In the intention-to-treat analysis, cure rates were 79% (22 of 28), 83% (35 of 42), 90% (46 of 51), and 89% (75 of 84), respectively. The cure rates of quadruple therapy were higher than those of triple therapy; an 8.2% difference was not statistically significant (95% confidence interval [CI], 2.3-18.7%). The ulcer-healing rates were 88%, 87%, 98%, and 97%, respectively, for groups 1 through 4. The ulcer pain was relieved more rapidly in quadruple- than in triple-therapy regimens. Two patients discontinued treatment prematurely owing to drug-related side effects. CONCLUSION: One-week quadruple therapy is highly effective and safe in H. pylori eradication in Chinese patients. CBP is as effective as CBS.

Adolescent↗
PubMed2004

Bismuth uptake in rat testicular macrophages: a follow-up observation suggesting that bismuth alters interactions between testicular macrophages and Leydig cells.

Recent studies suggest that bismuth accumulates in Leydig cells. In addition, a reduced level of serum testosterone and a statistically significant reduction of Leydig cells have been observed. It was therefore hypothesized that Bi has a direct toxic effect on rat Leydig cells. We have now developed a method for double labeling of bismuth and ED-2 (a marker for testicular macrophages). The present data demonstrate that the heavily bismuth-loaded cells in rat testis, originally interpreted as being Leydig cells, are bismuth-loaded macrophages. Consequently, our data suggest a modified hypothesis regarding bismuth-induced interactions between testicular macrophages and Leydig cells.

Animals↗
PubMed1979

Double-blind controlled trial with colloidal bismuth subcitrate in the treatment of symptomatic duodenal ulcers with special references to blood and urine bismuth levels.

To test the efficacy and toxicity of colloidal bismuth subcitrate (CBS) in a double-blind trial, forty-six consecutive outpatients with active duodenal ulceration were randomly allocated either to treatment with CBS or to a placebo for a period of four weeks. Symptomatic assessment was based on frequency and severity of pain. The ulcer size was measured endoscopically before and at the end of the trial. During the trial blood and urinary bismuth concentrations were measured. The symptomatic assessment of the patients receiving CBS or placebo showed that the reduction in pain was highly significant in both groups, but there was statistically significant difference in the degree of reduction of duodenal ulcer size in favour of the colloidal bismuth subcitrate-treated group (p less than 0.025). Although a marked increase in urinary bismuth concentration was noted, the blood bismuth levels remained within the acceptable levels.

Adult↗
PubMed1989

Absorption and elimination of bismuth from oral doses of tripotassium dicitrato bismuthate.

The pharmacokinetics of bismuth subcitrate were studied in plasma and urine under conditions of single and multiple dosing (28-56 days) using atomic absorption technique. Single dose plasma pharmacokinetics showed peak concentrations of 5.5-57.5 micrograms.l-1 (mean = 24.7 micrograms.l-1), reached between 30 and 60 min post dosing with an apparent biphasic elimination pattern. Multiple dose studies showed a continuing rise in plasma concentration and urine excretion rate reaching apparent steady-state levels over 7-29 days (mean = 18 days). Washout studies in 6 individuals reciprocated accumulation. Maximum equilibrated plasma levels of 7.6-58.3 micrograms.l-1 (mean = 38.3 micrograms.l-1) were well below those associated with encephalopathy. The half-life of bismuth elimination was 20.7 days. Present patterns of intermittent dosing with bismuth are unlikely to be associated with bismuth accumulation despite slow accumulation and elimination.

Adult↗
PubMed2006

Inhibition of urease by bismuth(III): implications for the mechanism of action of bismuth drugs.

Bismuth compounds are widely used for the treatment of peptic ulcers and Helicobacter pylori infections. It has been suggested that enzyme inhibition plays an important role in the antibacterial activity of bismuth towards this bacterium. Urease, an enzyme that converts urea into ammonia and carbonic acid, is crucial for colonization of the acidic environment of the stomach by H. pylori. Here, we show that three bismuth complexes exhibit distinct mechanisms of urease inhibition, with some differences dependent on the source of the enzyme. Bi(EDTA) and Bi(Cys)(3) are competitive inhibitors of jack bean urease with K(i) values of 1.74 +/- 0.14 and 1.84 +/- 0.15 mM, while the anti-ulcer drug, ranitidine bismuth citrate (RBC) is a non-competitive inhibitor with a K (i) value of 1.17 +/- 0.09 mM. A (13)C NMR study showed that Bi(Cys)(3) reacts with jack bean urease during a 30 min incubation, releasing free cysteines from the metal complex. Upon incubation with Bi(EDTA) and RBC, the number of accessible cysteine residues in the homohexameric plant enzyme decreased by 5.80 +/- 0.17 and 11.94 +/- 0.13, respectively, after 3 h of reaction with dithiobis(2-nitrobenzoic acid). Kinetic analysis showed that Bi(EDTA) is both a competitive inhibitor and a time-dependent inactivator of the recombinant Klebsiella aerogenes urease. The active C319A mutant of the bacterial enzyme displays a significantly reduced sensitivity toward inactivation by Bi(EDTA) compared with the wild-type enzyme, consistent with binding of Bi(3+) to the active site cysteine (Cys(319)) as the mechanism of enzyme inactivation.

Amino Acid Sequence↗
PubMedDate not supplied

In vitro antimicrobial activity of bismuth subsalicylate and other bismuth salts.

This report demonstrates that bismuth subsalicylate (BSS) effectively inhibits growth of a number of bacterial strains known to cause diarrhea, including Escherichia coli, Salmonella, Shigella, and Campylobacter. Other bismuth salts and sodium salicylate, a hydrolysis product of BSS in the gut, also were examined and were shown to have various degrees of activity. Growth of the organisms was monitored in vitro by inoculating culture fluid that contained one of the compounds to be tested and determining the concentration of viable organisms over a 24-hour period. Control cultures of each organism were grown in the absence of bismuth subsalicylate. BSS inhibited growth of all organisms examined in a dose-dependent fashion. Reductions of 2-6 logs, as compared with controls, were observed in cultures grown in the presence of 10-50 mM BSS. Other bismuth salts displayed various degrees of inhibition. These results suggest that the efficacy of BSS as an antidiarrheal agent may be related to an antimicrobial mechanism of action.

Bacteria↗
PubMed1999

One-week ranitidine bismuth citrate versus colloidal bismuth subcitrate-based anti-Helicobacter triple therapy: a prospective randomized controlled trial.

OBJECTIVE: The efficacy of 1 wk bismuth triple therapy is adversely influenced by the presence of metronidazole resistance. In vitro studies suggest that ranitidine bismuth citrate (RBC) plus metronidazole exhibit synergistic activity against metronidazole resistant strains of Helicobacter pylori (H. pylori). Whether this confers a superior clinical efficacy remains unproven. This study compared the efficacy of RBC-based triple therapy with bismuth triple therapy in eradication of H. pylori. METHODS: Patients with H. pylori-related ulcer disease or gastritis were randomized to receive either 400/mg of RBC twice daily plus 400/mg of metronidazole and 500/mg of tetracycline four times daily for 1 wk (RMT) or 120/mg of colloidal bismuth subcitrate, 400/mg of metronidazole, and 500/mg of tetracycline, all given four times daily for 1 wk (BMT). Metronidazole susceptibility was determined by the E-test and pretreatment resistance was defined as minimum inhibitory concentration > or = 32/mg/L. RESULTS: Of 100 consecutive patients randomized, two patients were lost to follow-up in each group. Forty-three of 85 (51%) H. pylori isolates were metronidazole resistant. Per-protocol cure rate for RMT and BMT was 40 of 41 (98%) and 37 of 44 (84%), respectively (p = 0.058). Intent-to-treat cure rate for RMT and BMT was 46 of 50 and 41 of 50, respectively (92% vs 82%, p = 0.23). A significantly higher eradication of metronidazole resistant H. pylori was observed in the RMT group (25 of 25, 100%) than in the BMT group (12 of 16, 75%), (p = 0.018). Side effects observed in the two treatment groups were comparable. CONCLUSIONS: One week of RBC triple therapy with metronidazole and tetracycline is an effective anti-Helicobacter therapy. This regimen is more appropriate in areas of high prevalence of metronidazole resistance.

Adolescent↗
PubMed1996

Gastroprotective effect of ranitidine bismuth citrate is associated with increased mucus bismuth concentration in rats.

BACKGROUND: Antisecretory and bismuth compounds protect the gastric mucosa from injury resulting from non-steroidal anti-inflammatory drugs. AIM: To study the mechanism underlying the gastroprotective effects of ranitidine bismuth citrate (GG311) in rats. METHODS: Indomethacin rat injury model and in vivo microscopy in which acid output, surface cell intracellular pH (pHi), gastric mucus gel thickness, and mucosal blood flow were measured simultaneously. RESULTS: In injury studies, GG311 dose dependently protected against severe injury induced by indomethacin (60 mg/kg subcutaneously). In in vivo microscopic studies, indomethacin significantly decreased mucus gel thickness and increased the initial rate of acidification of gastric surface cells when the superfusate pH was lowered from 7.4 to 1.0, and impaired pHi during acid exposure. Indomethacin had no effect on mucosal blood flow or acid output. GG311 alone had no effect on gel thickness, blood flow, or pHi homeostasis during acid exposure, but improved the initial acidification rate and pHi during superfusion with pH 1.0 solutions in the presence of indomethacin. In separate experiments, indomethacin pretreatment considerably increased gastric mucus bismuth concentrations in rats given GG311. CONCLUSIONS: The gastroprotective effect of GG311 against indomethacin induced gastric injury is associated with high and prolonged gastric mucus bismuth concentrations, which may impair proton permeation across the mucus gel.

Analysis of Variance↗