|Trade names||Xifaxan, Xifaxanta, Normix, other|
|Elimination half-life||6 hours|
|Chemical and physical data|
|Molar mass||785.879 g/mol|
|3D model (JSmol)|
|(what is this?)|
Rifaximin, sold under the trade name Xifaxan among others, is an antibiotic used to treat traveler's diarrhea, irritable bowel syndrome, and hepatic encephalopathy. It has poor absorption when taken by mouth.
It is based on rifamycin. Rifaximin was approved for medical use in the United States in 2004. In the United States it costs 62.13 USD per day for 1100 mg of rifaximin (1,864.00 USD per month) as of January 2017. In Russia as of 2016 a similar dose costs 231.25 RUB (approximately 4 USD).
Irritable bowel syndrome
Rifaximin possesses anti-inflammatory and antibacterial properties and additionally, it is a nonabsorbable antibiotic that acts locally in the gut. These properties make it efficacious in relieving chronic functional symptoms of non-constipation type irritable bowel syndrome (IBS). It appears to retain its therapeutic properties for this indication, even after repeated courses. Rifaximin is particularly indicated where small intestine bacterial overgrowth is suspected of involvement in a person’s IBS. Symptom relief or improvement can be obtained for abdominal pain, bloating, and stool consistency. A drawback is that repeated courses may be necessary for relapse of symptoms.
C. difficile infection
Rifaximin may also be a useful addition to vancomycin when treating patients with relapsing C. difficile infection. However the quality of evidence of these studies was judged to be low. Although exposure to rifamycins in the past may increase risk for resistance, so rifaximin should be avoided in such cases.
In the United States, rifaximin has orphan drug status for the treatment of hepatic encephalopathy. Although high-quality evidence is still lacking, rifaximin appears to be as effective as or more effective than other available treatments for hepatic encephalopathy (such as lactulose), is better tolerated, and may work faster. Rifaximin is taken by mouth. It has minimal side effects, prevents reoccurring encephalopathy, and is associated with high patient satisfaction. People are more compliant and satisfied to take this medication than any other due to minimal side effects, prolonged remission, and overall cost. The drawbacks to rifaximin are increased cost and lack of robust clinical trials for HE without combination lactulose therapy.
Rifaximin has few side effects. Side effects are generally mild and uncommon; this is largely because very little of the drug is absorbed from the gut meaning systemic side effects are absent. Clostridium difficile infection does not typically result from rifaximin therapy unless risk factors such as immunosuppression and hospitalisation are present. Rifaximin is active against Clostridium difficile.
Rifaximin is not significantly absorbed from the gut and therefore does not have significant interactions with other drugs in people with normal liver function.
Mechanism of action
Rifaximin interferes with transcription by binding to the β-subunit of bacterial RNA polymerase. This results in the blockage of the translocation step that normally follows the formation of the first phosphodiester bond, which occurs in the transcription process.
Rifaximin has a very low bioavailability due to it is poorly absorbed after oral administration. Because rifaximin is absorbed poorly, most of the drug taken orally stays in the gastrointestinal tract where the infection takes place. Because of this local action within the gut and the lack of horizontal transfer of resistant genes the development of bacterial resistance is rare.
Rifaximin is a low cost drug. In the United States, Salix Pharmaceuticals holds a US Patent for rifaximin and markets the drug under the name Xifaxan. In addition to receiving FDA approval for traveler’s diarrhea and (marketing approved for) hepatic encephalopathy, rifaximin received FDA approval for IBS in May 2015. No generic formulation is available in the US and none has appeared due to the fact that the FDA approval process was ongoing. If rifaximin receives full FDA approval for hepatic encephalopathy it is likely that Salix will maintain marketing exclusivity and be protected from generic formulations until March 24, 2017.
Rifaximin is approved in 33 countries for GI disorders. On August 13, 2013, Health Canada issued a Notice of Compliance to Salix Pharmaceuticals Inc. for the drug product Zaxine. In India it is available under the brand names Ciboz and Xifapill. In Russia and Ukraine the drug is sold under the name Alfa Normix (Альфа Нормикс), produced by Alfa Wassermann S.p.A (Italy).
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