Antisecretory Drugs for Eradication of &lt;i&gt;Helicobacter pylori&lt;/i&gt;: Antibacterial Activity and Synergism with Antimicrobial Agents

Scarpignato, Carmelo; Pelosini, Iva

doi:10.1159/000061964

Cited by 14 publications

(19 citation statements)

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“…In contrast to metronidazole, no strain tested exhibited primary resistance. Furthermore, the activity of rifaximin was only slightly affected by lowering the pH of the medium, conversely from what is currently observed with other antibiotics [14]. The lack of antagonism towards amoxicillin and CBS suggested that a combination of this rifamycin together with these antimicrobials could be used in vivo.…”

Section: In Vitro Activity Of Rifaximin Against Helicobacter Pylorimentioning

confidence: 72%

“…Furthermore, the gastric lumen is a hostile environment for antimicrobials because the drugs must penetrate thick mucus and may need to be active at low pH values [14]. Successful therapy requires a combination of drugs that prevent the emergence of resistance and reach the bacteria within its various niches.…”

Section: Therapy Of Helicobacter Pylori Infectionmentioning

confidence: 99%

“…The organism is able to survive over a wide pH range. It is found within the gastric mucus layer, deep within the mucus-secreting glands of the antrum, attached to cells, and even within cells [14]. The organism must be eradicated from each of these potential niches and this is a daunting task for any single antibiotic.…”

Section: Introductionmentioning

confidence: 99%

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Eradication of <i>Helicobacter pylori</i>: Are Rifaximin-Based Regimens Effective?

Gasbarrini

Pelosini

et al. 2006

Digestion

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Rifaximin is a non-absorbed semisynthetic rifamycin derivative with a broad spectrum of antibacterial activity including Gram-positive and Gram-negative bacteria, both aerobes and anaerobes. Although originally developed for the treatment of infectious diarrhea, the appreciation of the pathogenic role of gut bacteria in several organic and functional gastrointestinal diseases has increasingly broadened its clinical use. Being the antibiotic active against Helicobacter pylori, even towards clarithromycin-resistant strain, and being the primary resistance very rare, several investigations explored its potential use for eradication of the microorganism. Rifaximin alone proved to be effective, but even the highest dose (1,200 mg daily) gave a cure rate of only 30%. Dual and triple therapies were also studied, with the better results obtained with rifaximin-clarithromycin and rifaximin-clarithromycin-esomeprazole combinations. However, the eradication rates (60–70%) obtained with these regimens were still below the standard set by the Maastricht Consensus guidelines. Although rifaximin-based eradication therapies are promising, new antimicrobial combinations (with and without proton pump inhibitors) need to be explored in well-designed clinical trials including a large cohort of H. pylori-infected patients. The remarkable safety of rifaximin will allow high-dose regimens of longer duration (e.g. 10 or 14 days) to be tested with confidence in the hope of achieving better eradication rates. A drawback of rifaximin could be its inability to reach sufficiently high concentrations in the gastric mucus layer under and within which H. pylori is commonly located and this would likely affect eradication rate. Taking these considerations into account, bioadhesive rifaximin formulations able to better and persistently cover gastric mucosa, or combination with mucolytic agents, such as pronase or acetylcysteine, need to be evaluated in order to better define the place of this antibiotic in our therapeutic armamentarium.

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Section: In Vitro Activity Of Rifaximin Against Helicobacter Pylorimentioning

confidence: 72%

Section: Therapy Of Helicobacter Pylori Infectionmentioning

confidence: 99%

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Eradication of <i>Helicobacter pylori</i>: Are Rifaximin-Based Regimens Effective?

Gasbarrini

Pelosini

et al. 2006

Digestion

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“…In contrast to metronidazole, no strain tested exhibited primary resistance [52,53]. Furthermore, the activity of rifaximin was only slightly affected by lowering the pH of the medium, conversely from what is currently observed with other antibiotics [56]. Last but not least, rifaximin was shown to be active against clarithromycin-resistant strains [54].…”

Section: In Vitro Activitymentioning

confidence: 99%

“…The organism is able to survive over a wide pH spectrum. It is found within the gastric mucus layer, deep within the mucus-secreting glands of the antrum, attached to cells, and even within cells [56]. The organism must be eradicated from each of these potential niches and this is a daunting task for any single antibiotic.…”

Section: Bowel Preparation For Colorectal Surgerymentioning

confidence: 99%

Rifaximin, a Poorly Absorbed Antibiotic: Pharmacology and Clinical Potential

2005

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Rifaximin (4-deoxy-4′-methylpyrido[1′,2′-1,2]imidazo- [5,4-c]-rifamycin SV) is a synthetic antibiotic designed to modify the parent compound, rifamycin, in order to achieve low gastrointestinal (GI) absorption while retaining good antibacterial activity. Both experimental and clinical pharmacology clearly show that this compound is a nonsystemic antibiotic with a broad spectrum of antibacterial action covering Gram-positive and Gram-negative organisms, both aerobes and anaerobes. Being virtually nonabsorbed, its bioavailability within the GI tract is rather high with intraluminal and fecal drug concentrations that largely exceed the minimal inhibitory concentration values observed in vitro against a wide range of pathogenic organisms. The GI tract represents, therefore, the primary therapeutic target and GI infections the main indication. The appreciation of the pathogenic role of gut bacteria in several organic and functional GI diseases has increasingly broadened its clinical use, which is now extended to hepatic encephalopathy, small intestine bacterial overgrowth, inflammatory bowel disease and colonic diverticular disease. Potential indications include the irritable bowel syndrome and chronic constipation, Clostridium difficile infection and bowel preparation before colorectal surgery. Because of its antibacterial activity against the microorganism and the lack of strains with primary resistance, some preliminary studies have explored the rifaximin potential for Helicobacter pylori eradication. Oral administration of this drug, by getting rid of enteric bacteria, could also be employed to achieve selective bowel decontamination in acute pancreatitis, liver cirrhosis (thus preventing spontaneous bacterial peritonitis) and nonsteroidal anti-inflammatory drug (NSAID) use (lessening in that way NSAID enteropathy). This antibiotic has, therefore, little value outside the enteric area and this will minimize both antimicrobial resistance and systemic adverse events. Indeed, the drug proved to be safe in all patient populations, including young children. Although rifaximin has stood the test of time, it still attracts the attention of both basic scientists and clinicians. As a matter of fact, with the advancement of the knowledge on microbial-gut interactions in health and disease novel indications and new drug regimens are being explored. Besides widening the clinical use, the research on rifaximin is also focused on the synthesis of new derivatives and on the development of original formulations designed to expand the spectrum of its clinical use.

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New drugs to suppress acid secretion: current and future developments

Scarpignato

2007

Drug Discovery Today: Therapeutic Strategies

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Antisecretory Drugs for Eradication of <i>Helicobacter pylori</i>: Antibacterial Activity and Synergism with Antimicrobial Agents

Cited by 14 publications

References 0 publications

Eradication of <i>Helicobacter pylori</i>: Are Rifaximin-Based Regimens Effective?

Eradication of <i>Helicobacter pylori</i>: Are Rifaximin-Based Regimens Effective?

Rifaximin, a Poorly Absorbed Antibiotic: Pharmacology and Clinical Potential

New drugs to suppress acid secretion: current and future developments

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