Comparative Pharmacology
Head-to-head clinical analysis: RIFAXIMIN versus SEPTRA.
Peer-Reviewed Evidence
Head-to-head clinical analysis: RIFAXIMIN versus SEPTRA.
RIFAXIMIN vs SEPTRA
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Rifaximin is a non-aminoglycoside, semi-synthetic antibiotic derived from rifamycin that inhibits bacterial RNA synthesis by binding to the beta-subunit of bacterial DNA-dependent RNA polymerase, thereby blocking transcription.
SEPTRA (trimethoprim/sulfamethoxazole) is a combination of two antifolate agents: sulfamethoxazole inhibits dihydropteroate synthase, blocking the conversion of PABA to dihydrofolic acid; trimethoprim inhibits dihydrofolate reductase, preventing the reduction of dihydrofolic acid to tetrahydrofolic acid. This sequential blockade disrupts bacterial folate synthesis and nucleic acid production.
550 mg orally three times daily for 14 days for travelers' diarrhea; 200 mg orally three times daily for 3 days for irritable bowel syndrome with diarrhea; 400 mg orally three times daily for 7 days for hepatic encephalopathy.
Trimethoprim-sulfamethoxazole (TMP-SMX) 160 mg/800 mg (double strength) orally every 12 hours; for severe infections, intravenous dosing: 8-10 mg/kg/day (TMP component) divided every 6, 8, or 12 hours.
None Documented
None Documented
Clinical Note
moderateRifaximin + Digoxin
"The serum concentration of Digoxin can be increased when it is combined with Rifaximin."
Clinical Note
moderateRifaximin + Levofloxacin
"The serum concentration of Levofloxacin can be increased when it is combined with Rifaximin."
Clinical Note
moderateRifaximin + Estrone sulfate
"The serum concentration of Estrone sulfate can be decreased when it is combined with Rifaximin."
Clinical Note
moderateRifaximin + Tranilast
The terminal elimination half-life is approximately 1.8 to 2.5 hours in patients with normal hepatic function. Due to negligible systemic absorption, the half-life has limited clinical relevance; drug action is largely confined to the gastrointestinal tract.
Sulfamethoxazole: 9-12 hours (normal renal function); Trimethoprim: 8-11 hours (normal renal function). In severe renal impairment (CrCl <15 mL/min), half-life prolongs significantly (up to 24-30 hours for sulfamethoxazole, 20-30 hours for trimethoprim).
Rifaximin is primarily eliminated in feces as unchanged drug (>96% of an oral dose). Renal excretion is negligible (<0.4%). Biliary excretion is minimal due to poor systemic absorption.
Renal excretion of unchanged sulfamethoxazole (~20%) and trimethoprim (~50-60%) with additional hepatic metabolism (acetylation, glucuronidation) of sulfamethoxazole; total renal elimination accounts for ~80-90% of the dose (sulfamethoxazole 30% parent, 40% metabolites; trimethoprim 60-80% parent, remainder as metabolites). Biliary/fecal <5%.
Category A/B
Category C
Antibiotic
Antibiotic
"The serum concentration of Tranilast can be decreased when it is combined with Rifaximin."