Comparative Pharmacology
Head-to-head clinical analysis: SEPTRA versus TRIMETHOPRIM SULFATE AND POLYMYXIN B SULFATE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: SEPTRA versus TRIMETHOPRIM SULFATE AND POLYMYXIN B SULFATE.
SEPTRA vs TRIMETHOPRIM SULFATE AND POLYMYXIN B SULFATE
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
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.
Trimethoprim inhibits bacterial dihydrofolate reductase, blocking tetrahydrofolate synthesis and thereby inhibiting thymidine synthesis. Polymyxin B disrupts bacterial cell membrane integrity by binding to lipopolysaccharides in Gram-negative bacteria.
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.
One drop in each affected eye every 2 to 4 hours for 7 to 10 days.
None Documented
None Documented
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).
Trimethoprim: 8-10 hours (normal renal function); Polymyxin B: 6 hours (prolonged in renal impairment).
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%.
Trimethoprim: renal (80-90% unchanged, 10-20% metabolites); Polymyxin B: renal (60% unchanged, 40% nonrenal).
Category C
Category D/X
Antibiotic
Antibiotic