Comparative Pharmacology
Head-to-head clinical analysis: GANTRISIN versus SULFATRIM.
Head-to-head clinical analysis: GANTRISIN versus SULFATRIM.
GANTRISIN vs SULFATRIM
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.
Sulfatrim is a combination of sulfamethoxazole, a dihydropteroate synthase inhibitor that blocks folate synthesis, and trimethoprim, a dihydrofolate reductase inhibitor that blocks reduction of dihydrofolate to tetrahydrofolate, resulting in sequential inhibition of bacterial folate metabolism.
2-4 g orally initially, then 4-8 g daily in 3-6 divided doses
160 mg trimethoprim / 800 mg sulfamethoxazole (1 DS tablet) orally every 12 hours for 10-14 days.
None Documented
None Documented
7-12 hours (mean 10 hours); prolonged to 20-50 hours in renal impairment (CrCl <30 mL/min)
Sulfamethoxazole: 9-11 hours (prolonged in renal impairment, e.g., up to 30 hours in severe renal failure). Trimethoprim: 8-10 hours (prolonged in hepatic impairment).
Renal: 70% as unchanged drug; hepatic metabolism: 30% as acetylated metabolites; biliary: <3%
Renal (70-80% as unchanged sulfamethoxazole and N4-acetylated metabolite; 30-40% as unchanged trimethoprim), biliary/fecal (20-30% sulfamethoxazole; 10-20% trimethoprim)
Category C
Category C
Sulfonamide Antibiotic
Sulfonamide Antibiotic