Comparative Pharmacology
Head-to-head clinical analysis: GANTRISIN versus SULFATRIM SS.
Head-to-head clinical analysis: GANTRISIN versus SULFATRIM SS.
GANTRISIN vs SULFATRIM-SS
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, blocking reduction of dihydrofolate to tetrahydrofolate. Sequential blockade produces bactericidal synergy.
2-4 g orally initially, then 4-8 g daily in 3-6 divided doses
1 double-strength tablet (160 mg trimethoprim / 800 mg sulfamethoxazole) 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)
SMX: 9-12 hours (increased in renal impairment); TMP: 8-11 hours (increased in renal impairment); both prolonged in elderly.
Renal: 70% as unchanged drug; hepatic metabolism: 30% as acetylated metabolites; biliary: <3%
Renal excretion of unchanged sulfamethoxazole (SMX) approximately 20%, trimethoprim (TMP) approximately 60%; biliary/fecal elimination minor (SMX <5%, TMP <10%).
Category C
Category C
Sulfonamide Antibiotic
Sulfonamide Antibiotic