Rifaximin

Rifaximin Uses, Dosage, Side Effects, Food Interaction and all others data.

Rifaximin is a non-aminoglycoside semi-synthetic antibacterial derived from rifamycin SV. It inhibits bacterial RNA synthesis by binding to the bacterial DNA-dependent RNA polymerase and has antibacterial activity against Escherichia coli (E. coli).

Rifaximin is a structural analog of rifampin and a non-systemic, gastrointestinal site-specific antibiotic. This non-systemic property of the drug is due to the addition of a pyridoimidazole ring, which renders it non-absorbable. Rifaximin acts by inhibiting bacterial ribonucleic acid (RNA) synthesis and contributes to restore intestinal microflora imbalance. Other studies have also shown rifaximin to be an pregnane X receptor (PXR) activator. As PXR is responsible for inhibiting the proinflammatory transcription factor NF-kappa B (NF-κB) and is inhibited in inflammatory bowel disease (IBD), rifaximin was proven to be effective for the treatment of IBS-D.

Trade Name Rifaximin
Availability Prescription only
Generic Rifaximin
Rifaximin Other Names Rifaxidin, Rifaximin, Rifaximina, Rifaximine, Rifaximinun
Related Drugs ciprofloxacin, dicyclomine, sulfamethoxazole / trimethoprim, Bactrim, loperamide, lactulose, Bentyl, hyoscyamine, Xifaxan, Imodium
Weight 200mg, 550mg
Type Tablet, Oral Tablet
Formula C43H51N3O11
Weight Average: 785.8785
Monoisotopic: 785.352359489
Groups Approved, Investigational
Therapeutic Class Miscellaneous Antibiotics
Manufacturer Nexeum Pharmaceuticals
Available Country India, United States
Last Updated: September 19, 2023 at 7:00 am
Rifaximin
Rifaximin

Uses

Acute infectious diarrhoea including travelers diarrhoea, Diarrhoea predominant Irritable Bowel Syndrome (IBS-D), Hepatic Encephalopathy (H.E.)

Rifaximin is also used to associated treatment for these conditions: Bacterial Infections, Clostridium difficile infection recurrence, Hepatic Encephalopathy (HE), Irritable Bowel Syndrome (IBS), Traveler's Diarrhea

How Rifaximin works

Rifaximin acts by inhibiting RNA synthesis in susceptible bacteria by binding to the beta-subunit of bacterial deoxyribonucleic acid (DNA)-dependent ribonucleic acid (RNA) polymerase enzyme. This binding blocks translocation, which stops transcription.

Dosage

Rifaximin dosage

Acute Infectious Diarrhoea including Travelers’ Diarrhoea: 200 mg three times daily for 3 days.

Diarrhoea predominant Irritable Bowel Syndrome (IBS-D): 550 mg three times daily for 14 days.

Hepatic Encephalopathy (H.E.): 550 mg twice daily

Side Effects

Common side effects are nausea, vomiting, abdominal pain, flatulence, headache and dizziness.

Toxicity

LD50 > 2 g/kg (orally, in rats)

Precaution

Pregnancy and lactation. Caution in severe hepatic impairment (Child-Pugh class C). Not effective against diarrhoea caused by pathogen other than E. coli ; or diarrhoea complicated by fever and/or blood in the stool. Prolonged use may result in Clotridum difficile-associated diarrhoea. Severe hepatic impairment (Child-pugh class C).

Interaction

Although In vitro studies demonstrated the potential of Rifaximin to interact with cytochrome P450 (CYP3A4), a clinical drug-drug interaction study demonstrated that Rifaximin did not significantly affect the pharmacokinetics of midazolam. An additional clinical drug-drug interaction study showed no effect of Rifaximin on the presystemic metabolism of an oral contraceptive containing ethinyl estradiol and norgestimate. Therefore, clinical interactions with drugs metabolized by human cytochrome P450 isozymes are not expected.

Food Interaction

  • Take with or without food. Fatty meals may increase the systemic AUC of rifaximin, but do not impact Cmax. Rifaximin is an antibacterial used for local action in the gastrointestinal tract; therefore, changes in systemic exposure may not significantly impact efficacy.

Elimination Route

Low absorption in both the fasting state and when administered within 30 minutes of a high-fat breakfast.

Half Life

Approximately 6 hours.

Elimination Route

In a mass balance study, after administration of 400 mg 14C-rifaximin orally to healthy volunteers, of the 96.94% total recovery, 96.62% of the administered radioactivity was recovered in feces almost exclusively as the unchanged drug and 0.32% was recovered in urine mostly as metabolites with 0.03% as the unchanged drug.Rifaximin accounted for 18% of radioactivity in plasma. This suggests that the absorbed rifaximin undergoes metabolism with minimal renal excretion of the unchanged drug

Pregnancy & Breastfeeding use

Pregnancy Category C. There are no adequate and well-controlled studies in pregnant women. Rifaximin should be used during pregnancy only if the potential benefit outweighs the potential risk to the fetus.

Use in Lactation: It is not known whether Rifaximin is excreted in human milk. Because many drugs are excreted in human milk and because of the potential for adverse reactions in nursing infants from Rifaximin, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.

Contraindication

Rifaximin is contraindicated in patients with a hypersensitivity to Rifaximin, or any of the Rifamycin antimicrobial agents, or any of the components of Rifaximin.

Special Warning

Use in Children: The safety and effectiveness of Rifaximin 200 mg in pediatric patients with travelers’ diarrhoea less than 12 years of age have not established.The safety and effectiveness of Rifaximin 550 mg for hepatic encephalopathy have not been established in patients <18 years of age.

Use in geriatric patients: Clinical studies of Rifaximin tablets did not include sufficient numbers of subjects aged 65 and over to determine whether they respond differently than younger subjects.

Use in Renal Insufficient Patients:The pharmacokinetics of Rifaximin in patients with impaired renal function has not been studied.

Use in Hepatic Insufficient Patients:No dosage adjustment with Rifaximin is necessary due to its limited systemic absorption. Nonetheless, caution should be exercised when Rifaximin is administered to patients with severe hepatic impairment.

Acute Overdose

No specific information is available on the treatment of over dosage with Rifaximin. In case of over dosage, discontinue Rifaximin, treat symptomatically and institute supportive measures as required.

Storage Condition

Store at 20-25° C; excursions permitted to 15-30° C.

Innovators Monograph

You find simplified version here Rifaximin

Rifaximin contains Rifaximin see full prescribing information from innovator Rifaximin Monograph, Rifaximin MSDS, Rifaximin FDA label

FAQ

What is Rifaximin used for?

Rifaximin is used to treat traveler's diarrhea that is caused by a bacteria called Escherichia coli. It is also used to prevent hepatic encephalopathy, which is a condition that occurs when your liver does not work normally.Rifaximin is also used to treat irritable bowel syndrome with diarrhea.

How safe is Rifaximin?

Rifaximin is safe and well tolerated for long-term maintenance of remission from overt hepatic encephalopathy.

How does Rifaximin work?

Rifaximin treats traveler's diarrhea and irritable bowel syndrome by stopping the growth of the bacteria that cause diarrhea. Rifaximin treats hepatic encephalopathy by stopping the growth of bacteria that produce toxins and that may worsen liver disease.

What are the common side effects of Rifaximin?

Common side effects of Rifaximin are include:

  • Gas (flatulence)
  • Headache
  • Feeling as if your bowels are not completely emptied
  • Feeling you need to urgently empty your bowels
  • Abdominal or stomach pain
  • Nausea
  • Constipation
  • Fever
  • Vomiting
  • Bloating
  • Dizziness
  • Tired feeling
  • Swelling in your hands, feet, or torso

Is Rifaximin safe during pregnancy?

There are no adequate and well controlled studies in pregnant women.Rifaximin tablets should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Is Rifaximin safe during breastfeeding?

Rifaximin is poorly absorbed orally and used only for gastrointestinal infections. It is not likely to reach the breastmilk or bloodstream of the infant or cause any adverse effects in breastfed infants after maternal use.

When Is the best taken of Rifaximin?

Rifaximin usually 2 times a day (every 12 hours).Take this medication at the same time(s) every day.

Can I take Rifaximin on an empty stomach?

Rifaximin should be taken on an empty stomach.

Should Rifaximin be taken with food?

You may take this medicine with or without food.

Is Rifaximin strong antibiotic?

Rifaximin is a gastrointestinal-selective antibiotic with a broad spectrum of antimicrobial activity, an excellent safety profile, minimal drug interactions, and negligible impact on the intestinal microbiome.

How fast does Rifaximin work?

After just two weeks of treatment, relief lasted for up to 6 months.

Who should not take Rifaximin?

You should not take Rifaximin if you are allergic to Rifaximin. Tell your doctor if you have ever had.Tell your doctor if you are pregnant or breastfeeding.Rifaximin should not be given to a child younger than 12 years old.

Is Rifaximin safe for liver?

Rifaximin could theoretically prevent SBP in patients with liver cirrhosis by reducing gut bacteria.

Can Rifaximin help constipation?

The antibiotic Rifaximin is used to treat non-constipated irritable bowel syndrome (IBS).

How long can I take Rifaximin?

You may take Rifaximin with or without food. For travelers' diarrhea, Rifaximin is usually taken for only 3 days.

Is Rifaximin safe for kidneys?

While the effects of Rifaximin have been shown to be protective against acute kidney injury  and hepatorenal syndrome in alcohol-induced cirrhosis, its long-term effects on the renal function of other cirrhotic patients are unknown.

What happens if I miss a dose of Rifaximin?

Take Rifaximin as soon as you can, but skip the missed dose if it is almost time for your next dose. Do not take two doses at one time.

What should I avoid while taking Rifaximin?

Antibiotic medicines can cause diarrhea, which may be a sign of a new infection. If you have diarrhea that is watery or bloody, call your doctor before using anti-diarrhea medicine.

How many Rifaximin can Rifaximin take in a day?

Adults and children 12 years of age and older 200 milligrams (mg) three times a day for 3 days. Children younger than 12 years of age.Use and dose must be determined by your doctor.

*** Taking medicines without doctor's advice can cause long-term problems.
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