Abstract
Inorganic bismuth derivatives have good antibacterial properties and are considered to be only slightly toxic to humans because of their low uptake into human cells. Compounds containing bismuth are therefore widely used in medical applications. Bismuth-containing pharmaceuticals, partially in synergy with antibiotics, are already used or are being considered in the treatment of infections caused by certain bacteria, especially to eradicate Helicobacter pylori, Pseudomonas aeruginosa, Burkholderia multivorans and B. cenocepacia. However, careless use of bismuth containing pharmaceuticals can result in encephalopathy, renal failure and other adverse effects. Microbial methylation of bismuth by the human gut microbiota has recently been reported. As the lipophilicity and thus the membrane permeability of bismuth are increased by these methylation processes, the toxic effects on human cells and on members of the beneficial “physiological” gut microbiota must be considered in medical application of bismuth-containing drugs.
Highlights
SummaryInorganic bismuth derivatives have good antibacterial properties and are considered to be only slightly toxic to humans because of their low uptake into human cells
Bismuth is a heavy metal and was regarded until recently to be the heaviest stable element
The current concepts in the management of Helicobacter pylori infections recommend a triple therapy using a proton-pump inhibitor (PPI) or ranitidine bismuth citrate (RBC) with the antibiotics clarithromycin (500 mg twice a day) and amoxicillin (1000 mg twice a day) or metronidazole (500 mg twice a day) as first-line treatment, and a quadruple therapy consisting of PPI, bismuth subsalicylate (BSS) or subcitrate (120 mg four times a day) in combination with the antibiotics metronidazole (500 mg three times a day) and tetracycline (500 mg four times a day) for at least one week as second-line therapy [6]
Summary
Inorganic bismuth derivatives have good antibacterial properties and are considered to be only slightly toxic to humans because of their low uptake into human cells. Compounds containing bismuth are widely used in medical applications. Bismuth-containing pharmaceuticals, partially in synergy with antibiotics, are already used or are being considered in the treatment of infections caused by certain bacteria, especially to eradicate Helicobacter pylori, Pseudomonas aeruginosa, Burkholderia multivorans and B. cenocepacia. Careless use of bismuth containing pharmaceuticals can result in encephalopathy, renal failure and other adverse effects. Microbial methylation of bismuth by the human gut microbiota has recently been reported. As the lipophilicity and the membrane permeability of bismuth are increased by these methylation processes, the toxic effects on human cells and on members of the beneficial “physiological” gut microbiota must be considered in medical application of bismuth-containing drugs
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