Drug intelligence / Profile preview

rifaximin + loperamide

Development stage
Phase 4
Lead developer
Salix Pharmaceuticals
Modality
Small Molecules
Administration
Oral
01

Overview

Rifaximin + loperamide is a combination therapy used primarily for the treatment of traveler's diarrhea. Rifaximin is a non-systemic, gut-selective antibiotic that inhibits bacterial RNA synthesis by binding to the beta-subunit of bacterial DNA-dependent RNA polymerase, thereby blocking transcription in susceptible bacteria. Loperamide is an antimotility agent that acts as a peripheral mu-opioid receptor agonist in the gastrointestinal tract to reduce intestinal motility and fluid secretion. The combination provides more rapid symptom relief and higher rates of clinical cure compared to either agent alone, with fewer stools passed in the first 24 hours and reduced abdominal cramps. This regimen has been shown to be well tolerated and may represent an improved standard of care for traveler's diarrhea[1][2][4][5][6].

Other names
rifaximin and loperamide combination
02

Targets

rpoB (DNA-directed RNA polymerase subunit beta)MOR (Mu opioid receptor)

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