Comparative Pharmacology
Head-to-head clinical analysis: GANTRISIN versus SULFATRIM DS.
Peer-Reviewed Evidence
Head-to-head clinical analysis: GANTRISIN versus SULFATRIM DS.
GANTRISIN vs SULFATRIM-DS
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Competitive inhibitor of dihydropteroate synthase, blocking para-aminobenzoic acid (PABA) incorporation into dihydropteroic acid, thereby inhibiting bacterial folate synthesis and nucleic acid production.
Sulfamethoxazole inhibits bacterial dihydropteroate synthase, blocking folate synthesis. Trimethoprim inhibits bacterial dihydrofolate reductase, inhibiting reduction of dihydrofolate to tetrahydrofolate. Sequential blockade of folate metabolism exerts bactericidal effect.
2-4 g orally initially, then 4-8 g daily in 3-6 divided doses
One double-strength tablet (160 mg trimethoprim/800 mg sulfamethoxazole) orally every 12 hours.
None Documented
None Documented
7-12 hours (mean 10 hours); prolonged to 20-50 hours in renal impairment (CrCl <30 mL/min)
SMX: 9-11 hours (terminal); TMP: 8-10 hours; prolonged in renal impairment (creatinine clearance <30 mL/min: up to 20-30 hours for both).
Renal: 70% as unchanged drug; hepatic metabolism: 30% as acetylated metabolites; biliary: <3%
Renal: 50-70% of total sulfamethoxazole (SMX) and 30% of trimethoprim (TMP) as unchanged drug via glomerular filtration and tubular secretion; 20-40% of SMX as N4-acetylated metabolite; biliary excretion accounts for <5%.
Category C
Category C
Sulfonamide Antibiotic
Sulfonamide Antibiotic