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Rifaximin

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AHFS/Drugs.com
  
Monograph

Routes of administration
  
by mouth

Molar mass
  
785.879 g/mol

MedlinePlus
  
a604027

CAS ID
  
80621-81-4

Rifaximin

Trade names
  
Xifaxan, Xifaxanta, Normix, other

Pregnancy category
  
US: C (Risk not ruled out)

ATC code
  
A07AA11 (WHO) D06AX11 (WHO) QG51AA06 (WHO) QJ51XX01 (WHO)

Rifaximin is an antibiotic used to treat traveler's diarrhea, irritable bowel syndrome, and hepatic encephalopathy. It has poor absorption when taken by mouth.

Contents

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 as of 2016 exchange rate).

Medical uses

Rifaximin may be used to treat and prevent traveler's diarrhea.

Irritable bowel syndrome

It may be efficacious in relieving chronic functional symptoms of bloating and flatulence that are common in irritable bowel syndrome (IBS),

C. difficile infection

Rifaximin may also be a useful addition to vancomycin when treating patients with relapsing C. difficile infections. Although exposure to rifamycins in the past may increase risk for resistance, so rifaximin should be avoided in such cases.

Hepatic encephalopathy

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. Patients are more compliant and satisfied to take this medication than any other due to minimal side effects, prolong remission, and overall cost. The drawbacks to rifaximin are increased cost and lack of robust clinical trials for HE without combination lactulose therapy.

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.

Availability

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).

References

Rifaximin Wikipedia