Rifagrap
Rifagrap Uses, Dosage, Side Effects, Food Interaction and all others data.
Rifagrap 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).
Rifagrap 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. Rifagrap 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 | Rifagrap |
| 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 |
| Type | Tablet |
| Formula | C43H51N3O11 |
| Weight | Average: 785.8785 Monoisotopic: 785.352359489 |
| Groups | Approved, Investigational |
| Therapeutic Class | Miscellaneous Antibiotics |
| Manufacturer | Grapple Life Sciences Private Limited |
| Available Country | India |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Acute infectious diarrhoea including travelers diarrhoea, Diarrhoea predominant Irritable Bowel Syndrome (IBS-D), Hepatic Encephalopathy (H.E.)
Rifagrap 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 Rifagrap works
Rifagrap 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
Rifagrap 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 Rifagrap to interact with cytochrome P450 (CYP3A4), a clinical drug-drug interaction study demonstrated that Rifagrap did not significantly affect the pharmacokinetics of midazolam. An additional clinical drug-drug interaction study showed no effect of Rifagrap 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. Rifagrap is an antibacterial used for local action in the gastrointestinal tract; therefore, changes in systemic exposure may not significantly impact efficacy.
Rifagrap Drug Interaction
Unknown: aspirin, lorazepam, amoxicillin / clavulanate, diphenhydramine, duloxetine, metronidazole, furosemide, pregabalin, polyethylene glycol 3350, esomeprazole, acetaminophen, pantoprazole, acetaminophen, cyanocobalamin, ascorbic acid, cholecalciferol, alprazolam, ondansetron, sertraline, cetirizine
Rifagrap Disease Interaction
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.Rifagrap 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. Rifagrap 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 Rifagrap 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 Rifagrap, 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
Rifagrap is contraindicated in patients with a hypersensitivity to Rifagrap, or any of the Rifamycin antimicrobial agents, or any of the components of Rifagrap.
Special Warning
Use in Children: The safety and effectiveness of Rifagrap 200 mg in pediatric patients with travelers’ diarrhoea less than 12 years of age have not established.The safety and effectiveness of Rifagrap 550 mg for hepatic encephalopathy have not been established in patients <18 years of age.
Use in geriatric patients: Clinical studies of Rifagrap 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 Rifagrap in patients with impaired renal function has not been studied.
Use in Hepatic Insufficient Patients:No dosage adjustment with Rifagrap is necessary due to its limited systemic absorption. Nonetheless, caution should be exercised when Rifagrap is administered to patients with severe hepatic impairment.
Acute Overdose
No specific information is available on the treatment of over dosage with Rifagrap. In case of over dosage, discontinue Rifagrap, 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 Rifagrap
Rifagrap contains Rifaximin see full prescribing information from innovator Rifagrap Monograph, Rifagrap MSDS, Rifagrap FDA label
FAQ
What is Rifagrap used for?
Rifagrap 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.Rifagrap is also used to treat irritable bowel syndrome with diarrhea.
How safe is Rifagrap?
Rifagrap is safe and well tolerated for long-term maintenance of remission from overt hepatic encephalopathy.
How does Rifagrap work?
Rifagrap treats traveler's diarrhea and irritable bowel syndrome by stopping the growth of the bacteria that cause diarrhea. Rifagrap 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 Rifagrap?
Common side effects of Rifagrap 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 Rifagrap safe during pregnancy?
There are no adequate and well controlled studies in pregnant women.Rifagrap tablets should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
Is Rifagrap safe during breastfeeding?
Rifagrap 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 Rifagrap?
Rifagrap usually 2 times a day (every 12 hours).Take this medication at the same time(s) every day.
Can I take Rifagrap on an empty stomach?
Rifagrap should be taken on an empty stomach.
Should Rifagrap be taken with food?
You may take this medicine with or without food.
Is Rifagrap strong antibiotic?
Rifagrap 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 Rifagrap work?
After just two weeks of treatment, relief lasted for up to 6 months.
Who should not take Rifagrap?
You should not take Rifagrap if you are allergic to Rifagrap. Tell your doctor if you have ever had.Tell your doctor if you are pregnant or breastfeeding.Rifagrap should not be given to a child younger than 12 years old.
Is Rifagrap safe for liver?
Rifagrap could theoretically prevent SBP in patients with liver cirrhosis by reducing gut bacteria.
Can Rifagrap help constipation?
The antibiotic Rifagrap is used to treat non-constipated irritable bowel syndrome (IBS).
How long can I take Rifagrap?
You may take Rifagrap with or without food. For travelers' diarrhea, Rifagrap is usually taken for only 3 days.
Is Rifagrap safe for kidneys?
While the effects of Rifagrap 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 Rifagrap?
Take Rifagrap 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 Rifagrap?
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 Rifagrap can Rifagrap 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.
