Comparative Pharmacology
Head-to-head clinical analysis: GANTRISIN versus SULFAMETHOPRIM.
Head-to-head clinical analysis: GANTRISIN versus SULFAMETHOPRIM.
GANTRISIN vs SULFAMETHOPRIM
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.
Sulfamethoprim is a combination of sulfamethoxazole and trimethoprim. Sulfamethoxazole inhibits bacterial dihydropteroate synthase, blocking folic acid synthesis; trimethoprim inhibits bacterial dihydrofolate reductase, also blocking folic acid synthesis. This sequential blockade produces bactericidal effects.
2-4 g orally initially, then 4-8 g daily in 3-6 divided doses
Oral or intravenous: 800 mg sulfamethoxazole / 160 mg trimethoprim 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)
Terminal elimination half-life: 8-12 hours in adults with normal renal function. Prolonged in renal impairment (up to 24-48 hours).
Renal: 70% as unchanged drug; hepatic metabolism: 30% as acetylated metabolites; biliary: <3%
Renal: 60-80% as unchanged drug via glomerular filtration and tubular secretion; biliary: 5-10%; fecal: <5%.
Category C
Category C
Sulfonamide Antibiotic
Sulfonamide Antibiotic