Comparative Pharmacology
Head-to-head clinical analysis: SEPTRA GRAPE versus TRIMETHOPRIM.
Peer-Reviewed Evidence
Head-to-head clinical analysis: SEPTRA GRAPE versus TRIMETHOPRIM.
SEPTRA GRAPE vs TRIMETHOPRIM
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Septra Grape (trimethoprim/sulfamethoxazole) inhibits bacterial folic acid synthesis via sequential blockade: sulfamethoxazole inhibits dihydropteroate synthase, and trimethoprim inhibits dihydrofolate reductase, leading to bactericidal activity.
Trimethoprim inhibits bacterial dihydrofolate reductase (DHFR), preventing the reduction of dihydrofolate to tetrahydrofolate, thereby inhibiting thymidine synthesis and bacterial DNA replication. It has bacteriostatic activity against susceptible organisms.
160 mg trimethoprim / 800 mg sulfamethoxazole (1 double-strength tablet) orally every 12 hours.
Adult: 100 mg orally twice daily or 200 mg once daily for uncomplicated UTI; for severe infections, up to 20 mg/kg/day in divided doses. IV: 10-20 mg/kg/day divided every 6-12 hours.
None Documented
None Documented
Clinical Note
moderateTrimethoprim + Teriflunomide
"The metabolism of Teriflunomide can be decreased when combined with Trimethoprim."
Clinical Note
moderateTrimethoprim + Sulfisoxazole
"The metabolism of Sulfisoxazole can be decreased when combined with Trimethoprim."
Clinical Note
moderateTrimethoprim + Cyclosporine
"The metabolism of Cyclosporine can be decreased when combined with Trimethoprim."
Clinical Note
moderateTrimethoprim + Fluconazole
Trimethoprim: 8-10 hours (renal impairment >24h). Sulfamethoxazole: 10-13 hours (acetylation phenotype; prolonged in renal impairment). Clinical: Dosing interval generally 12h; adjust CrCl <30 mL/min.
Terminal elimination half-life is 8-12 hours in adults with normal renal function; prolonged to 20-40 hours in severe renal impairment (CrCl <15 mL/min).
Renal: 50-70% unchanged (trimethoprim), 30-50% as N-acetyl metabolite; sulfamethoxazole: 70-80% as metabolites, 20-30% unchanged; biliary excretion minimal (<5% total).
Renal excretion: approximately 50-60% of the dose is excreted unchanged in urine via glomerular filtration and tubular secretion; about 10-20% as metabolites (conjugated and oxidized forms); biliary/fecal excretion accounts for less than 10%.
Category C
Category D/X
Antibiotic
Antibiotic
"The metabolism of Fluconazole can be decreased when combined with Trimethoprim."