Comparative Pharmacology
Head-to-head clinical analysis: SULFAMETHOPRIM versus TRIMETH SULFA.
Peer-Reviewed Evidence
Head-to-head clinical analysis: SULFAMETHOPRIM versus TRIMETH SULFA.
SULFAMETHOPRIM vs TRIMETH/SULFA
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
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.
Trimethoprim inhibits bacterial dihydrofolate reductase (DHFR), blocking conversion of dihydrofolate to tetrahydrofolate; sulfamethoxazole inhibits bacterial dihydropteroate synthase, blocking incorporation of para-aminobenzoic acid into folic acid. Sequential blockade of folate synthesis produces synergistic bactericidal effect.
Oral or intravenous: 800 mg sulfamethoxazole / 160 mg trimethoprim every 12 hours.
1 double-strength tablet (160 mg trimethoprim / 800 mg sulfamethoxazole) orally every 12 hours for 14 days.
None Documented
None Documented
Terminal elimination half-life: 8-12 hours in adults with normal renal function. Prolonged in renal impairment (up to 24-48 hours).
Trimethoprim: 8-11 hours; Sulfamethoxazole: 9-11 hours. Prolonged in renal impairment (up to 24-30 hours for both). Clinical context: Dosing interval is typically 12 hours in normal renal function; adjust in CrCl <15-30 mL/min.
Renal: 60-80% as unchanged drug via glomerular filtration and tubular secretion; biliary: 5-10%; fecal: <5%.
Trimethoprim: 50-60% unchanged in urine; Sulfamethoxazole: 15-30% unchanged in urine, with acetylation and glucuronidation metabolites. Approximately 80-90% of dose recovered in urine within 72 hours; remainder via feces.
Category C
Category C
Sulfonamide Antibiotic
Sulfonamide Antibiotic