Peringatan Keamanan

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

Rifaximin

DB01220

small molecule approved investigational

Deskripsi

Rifaximin is a semisynthetic, rifamycin-based non-systemic antibiotic, meaning that the drug will not pass the gastrointestinal wall into the circulation as is common for other types of orally administered antibiotics. It has multiple indications and is used in treatment of traveller's diarrhea caused by E. coli; reduction in risk of overt hepatic encephalopathy recurrence; as well as diarrhea-predominant irritable bowel syndrome (IBS-D) in adult women and men. It is marketed under the brand name Xifaxan by Salix Pharmaceuticals.

Struktur Molekul 2D

Berat 785.8785
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) Approximately 6 hours.
Volume Distribusi -
Klirens (Clearance) -

Absorpsi

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

Metabolisme

In vitro drug interactions studies have shown that rifaximin, at concentrations ranging from 2 to 200 ng/mL, did not inhibit human hepatic cytochrome P450 isoenzymes: 1A2, 2A6, 2B6, 2C9, 2C19, 2D6, 2E1, and 3A4. In an in vitro hepa-tocyte induction model, rifaximin was shown to induce cytochrome P450 3A4 (CYP3A4), an isoenzyme which rifampin is known to induce.

Rute Eliminasi

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

Interaksi Makanan

1 Data
  • 1. 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.

Interaksi Obat

255 Data
Cyclosporine The serum concentration of Rifaximin can be increased when it is combined with Cyclosporine.
Aripiprazole The metabolism of Aripiprazole can be increased when combined with Rifaximin.
Aripiprazole lauroxil The metabolism of Aripiprazole lauroxil can be increased when combined with Rifaximin.
Fluconazole The serum concentration of Rifaximin can be increased when it is combined with Fluconazole.
Erythromycin The serum concentration of Rifaximin can be increased when it is combined with Erythromycin.
Sildenafil The serum concentration of Rifaximin can be increased when it is combined with Sildenafil.
Reserpine The serum concentration of Rifaximin can be increased when it is combined with Reserpine.
Sorafenib The serum concentration of Rifaximin can be increased when it is combined with Sorafenib.
Loxapine The serum concentration of Rifaximin can be increased when it is combined with Loxapine.
Quinine The serum concentration of Rifaximin can be increased when it is combined with Quinine.
Ritonavir The serum concentration of Rifaximin can be increased when it is combined with Ritonavir.
Toremifene The serum concentration of Rifaximin can be increased when it is combined with Toremifene.
Simvastatin The serum concentration of Rifaximin can be increased when it is combined with Simvastatin.
Verapamil The serum concentration of Rifaximin can be increased when it is combined with Verapamil.
Tamoxifen The serum concentration of Rifaximin can be increased when it is combined with Tamoxifen.
Mifepristone The serum concentration of Rifaximin can be increased when it is combined with Mifepristone.
Vardenafil The serum concentration of Rifaximin can be increased when it is combined with Vardenafil.
Tacrolimus The serum concentration of Rifaximin can be increased when it is combined with Tacrolimus.
Conivaptan The serum concentration of Rifaximin can be increased when it is combined with Conivaptan.
Quinidine The serum concentration of Rifaximin can be increased when it is combined with Quinidine.
Zonisamide The serum concentration of Rifaximin can be increased when it is combined with Zonisamide.
Tipranavir The serum concentration of Rifaximin can be increased when it is combined with Tipranavir.
Ketoconazole The serum concentration of Rifaximin can be increased when it is combined with Ketoconazole.
Amiodarone The serum concentration of Rifaximin can be increased when it is combined with Amiodarone.
Carvedilol The serum concentration of Rifaximin can be increased when it is combined with Carvedilol.
Itraconazole The serum concentration of Rifaximin can be increased when it is combined with Itraconazole.
Propafenone The serum concentration of Rifaximin can be increased when it is combined with Propafenone.
Clarithromycin The serum concentration of Rifaximin can be increased when it is combined with Clarithromycin.
Saquinavir The serum concentration of Rifaximin can be increased when it is combined with Saquinavir.
Lapatinib The serum concentration of Rifaximin can be increased when it is combined with Lapatinib.
Paliperidone The serum concentration of Rifaximin can be increased when it is combined with Paliperidone.
Mibefradil The serum concentration of Rifaximin can be increased when it is combined with Mibefradil.
Lopinavir The serum concentration of Rifaximin can be increased when it is combined with Lopinavir.
Biricodar The serum concentration of Rifaximin can be increased when it is combined with Biricodar.
Nilotinib The serum concentration of Rifaximin can be increased when it is combined with Nilotinib.
Elacridar The serum concentration of Rifaximin can be increased when it is combined with Elacridar.
Flibanserin The serum concentration of Rifaximin can be increased when it is combined with Flibanserin.
Vandetanib The serum concentration of Rifaximin can be increased when it is combined with Vandetanib.
Telaprevir The serum concentration of Rifaximin can be increased when it is combined with Telaprevir.
Zosuquidar The serum concentration of Rifaximin can be increased when it is combined with Zosuquidar.
Tariquidar The serum concentration of Rifaximin can be increased when it is combined with Tariquidar.
Temsirolimus The serum concentration of Rifaximin can be increased when it is combined with Temsirolimus.
Simeprevir The serum concentration of Rifaximin can be increased when it is combined with Simeprevir.
Isavuconazonium The serum concentration of Rifaximin can be increased when it is combined with Isavuconazonium.
Brefeldin A The serum concentration of Rifaximin can be increased when it is combined with Brefeldin A.
Ticagrelor The serum concentration of Rifaximin can be increased when it is combined with Ticagrelor.
Lomitapide The serum concentration of Rifaximin can be increased when it is combined with Lomitapide.
Crizotinib The serum concentration of Rifaximin can be increased when it is combined with Crizotinib.
Vemurafenib The serum concentration of Rifaximin can be increased when it is combined with Vemurafenib.
Linagliptin The serum concentration of Rifaximin can be increased when it is combined with Linagliptin.
Mirabegron The serum concentration of Rifaximin can be increased when it is combined with Mirabegron.
Regorafenib The serum concentration of Rifaximin can be increased when it is combined with Regorafenib.
Enzalutamide The serum concentration of Enzalutamide can be decreased when it is combined with Rifaximin.
Ponatinib The serum concentration of Rifaximin can be increased when it is combined with Ponatinib.
Canagliflozin The serum concentration of Rifaximin can be increased when it is combined with Canagliflozin.
Afatinib The serum concentration of Rifaximin can be increased when it is combined with Afatinib.
Ledipasvir The serum concentration of Rifaximin can be increased when it is combined with Ledipasvir.
Vorapaxar The serum concentration of Rifaximin can be increased when it is combined with Vorapaxar.
Suvorexant The serum concentration of Rifaximin can be increased when it is combined with Suvorexant.
Netupitant The serum concentration of Rifaximin can be increased when it is combined with Netupitant.
Cobicistat The serum concentration of Rifaximin can be increased when it is combined with Cobicistat.
Palbociclib The serum concentration of Rifaximin can be increased when it is combined with Palbociclib.
Daclatasvir The serum concentration of Rifaximin can be increased when it is combined with Daclatasvir.
Niguldipine The serum concentration of Rifaximin can be increased when it is combined with Niguldipine.
Lumacaftor The serum concentration of Rifaximin can be increased when it is combined with Lumacaftor.
Rolapitant The serum concentration of Rifaximin can be increased when it is combined with Rolapitant.
Venetoclax The serum concentration of Rifaximin can be increased when it is combined with Venetoclax.
Asunaprevir The serum concentration of Rifaximin can be increased when it is combined with Asunaprevir.
Velpatasvir The serum concentration of Rifaximin can be increased when it is combined with Velpatasvir.
Isavuconazole The serum concentration of Rifaximin can be increased when it is combined with Isavuconazole.
Neratinib The serum concentration of Rifaximin can be increased when it is combined with Neratinib.
Valspodar The serum concentration of Rifaximin can be increased when it is combined with Valspodar.
Dacomitinib The serum concentration of Rifaximin can be increased when it is combined with Dacomitinib.
Glasdegib The serum concentration of Rifaximin can be increased when it is combined with Glasdegib.
Voxilaprevir The serum concentration of Rifaximin can be increased when it is combined with Voxilaprevir.
Sarecycline The serum concentration of Rifaximin can be increased when it is combined with Sarecycline.
Erdafitinib The serum concentration of Rifaximin can be increased when it is combined with Erdafitinib.
Laniquidar The serum concentration of Rifaximin can be increased when it is combined with Laniquidar.
Enasidenib The serum concentration of Rifaximin can be increased when it is combined with Enasidenib.
Pibrentasvir The serum concentration of Rifaximin can be increased when it is combined with Pibrentasvir.
Glecaprevir The serum concentration of Rifaximin can be increased when it is combined with Glecaprevir.
Dexniguldipine The serum concentration of Rifaximin can be increased when it is combined with Dexniguldipine.
ONT-093 The serum concentration of Rifaximin can be increased when it is combined with ONT-093.
Elagolix The serum concentration of Rifaximin can be increased when it is combined with Elagolix.
Fedratinib The serum concentration of Rifaximin can be increased when it is combined with Fedratinib.
Istradefylline The serum concentration of Rifaximin can be increased when it is combined with Istradefylline.
Lasmiditan The serum concentration of Rifaximin can be increased when it is combined with Lasmiditan.
Norgestimate The serum concentration of Rifaximin can be increased when it is combined with Norgestimate.
Carfilzomib The serum concentration of Rifaximin can be increased when it is combined with Carfilzomib.
Favipiravir The serum concentration of Rifaximin can be increased when it is combined with Favipiravir.
Methylene blue The serum concentration of Rifaximin can be increased when it is combined with Methylene blue.
Pralsetinib The serum concentration of Rifaximin can be increased when it is combined with Pralsetinib.
Clofazimine The serum concentration of Rifaximin can be increased when it is combined with Clofazimine.
Lonafarnib The serum concentration of Rifaximin can be increased when it is combined with Lonafarnib.
Arsenic trioxide The serum concentration of Rifaximin can be increased when it is combined with Arsenic trioxide.
Mefloquine The serum concentration of Rifaximin can be increased when it is combined with Mefloquine.
Cethromycin The serum concentration of Rifaximin can be increased when it is combined with Cethromycin.
Eliglustat The serum concentration of Rifaximin can be increased when it is combined with Eliglustat.
Umbralisib The serum concentration of Rifaximin can be increased when it is combined with Umbralisib.
Diosmin The serum concentration of Rifaximin can be increased when it is combined with Diosmin.

Target Protein

DNA-directed RNA polymerase subunit beta rpoB
Nuclear receptor subfamily 1 group I member 2 NR1I2

Referensi & Sumber

Synthesis reference: Giuseppe Viscomi, Manuela Campana, Dario Braga, Donatella Confortini, Vincenzo Cannata, Paolo Righi, Goffredo Rosini, "Polymorphic forms of rifaximin, processes for their production and uses thereof." U.S. Patent US20050272754, issued December 08, 2005.
Artikel (PubMed)
  • PMID: 20586560
    Cottreau J, Baker SF, DuPont HL, Garey KW: Rifaximin: a nonsystemic rifamycin antibiotic for gastrointestinal infections. Expert Rev Anti Infect Ther. 2010 Jul;8(7):747-60. doi: 10.1586/eri.10.58.
  • PMID: 15976747
    Williams R, Bass N: Rifaximin, a nonabsorbed oral antibiotic, in the treatment of hepatic encephalopathy: antimicrobial activity, efficacy, and safety. Rev Gastroenterol Disord. 2005;5 Suppl 1:S10-8.
  • PMID: 19881343
    Koo HL, DuPont HL: Rifaximin: a unique gastrointestinal-selective antibiotic for enteric diseases. Curr Opin Gastroenterol. 2010 Jan;26(1):17-25. doi: 10.1097/MOG.0b013e328333dc8d.
  • PMID: 15598963
    Pakyz AL: Rifaximin: a new treatment for travelers' diarrhea. Ann Pharmacother. 2005 Feb;39(2):284-9. Epub 2004 Dec 14.
  • PMID: 20561708
    Jalan R: Rifaximin in hepatic encephalopathy: more than just a non-absorbable antibiotic? J Hepatol. 2010 Sep;53(3):580-2. doi: 10.1016/j.jhep.2010.05.002. Epub 2010 May 31.
  • PMID: 18657018
    Lawrence KR, Klee JA: Rifaximin for the treatment of hepatic encephalopathy. Pharmacotherapy. 2008 Aug;28(8):1019-32. doi: 10.1592/phco.28.8.1019.
  • PMID: 20331580
    Layer P, Andresen V: Review article: rifaximin, a minimally absorbed oral antibacterial, for the treatment of travellers' diarrhoea. Aliment Pharmacol Ther. 2010 Jun;31(11):1155-64. doi: 10.1111/j.1365-2036.2010.04296.x. Epub 2010 Mar 11.
  • PMID: 19442033
    Ojetti V, Lauritano EC, Barbaro F, Migneco A, Ainora ME, Fontana L, Gabrielli M, Gasbarrini A: Rifaximin pharmacology and clinical implications. Expert Opin Drug Metab Toxicol. 2009 Jun;5(6):675-82. doi: 10.1517/17425250902973695.
Menampilkan 8 dari 15 artikel.

Contoh Produk & Brand

Produk: 12 • International brands: 3
Produk
  • Xifaxan
    Tablet • 200 mg/1 • Oral • US • Approved
  • Xifaxan
    Tablet • 550 mg/1 • Oral • US • Approved
  • Xifaxan
    Tablet • 200 mg/1 • Oral • US • Approved
  • Xifaxan
    Tablet • 200 mg/1 • Oral • US • Approved
  • Xifaxan
    Tablet • 200 mg/1 • Oral • US • Approved
  • Xifaxan
    Tablet • 550 mg/1 • Oral • US • Approved
  • Xifaxan
    Tablet • 550 mg/1 • Oral • US • Approved
  • Xifaxan
    Tablet • 200 mg/1 • Oral • US • Approved
Menampilkan 8 dari 12 produk.
International Brands
  • Normix
  • Rifacol
  • Xifaxsan

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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