Comparative Pharmacology
Head-to-head clinical analysis: TRIMETHOPRIM versus ZOSYN IN PLASTIC CONTAINER.
Head-to-head clinical analysis: TRIMETHOPRIM versus ZOSYN IN PLASTIC CONTAINER.
TRIMETHOPRIM vs ZOSYN IN PLASTIC CONTAINER
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Trimethoprim inhibits bacterial dihydrofolate reductase (DHFR), preventing the reduction of dihydrofolate to tetrahydrofolate, thereby inhibiting thymidine synthesis and bacterial DNA replication. It has bacteriostatic activity against susceptible organisms.
Piperacillin, a ureidopenicillin, inhibits bacterial cell wall synthesis by binding to penicillin-binding proteins (PBPs), inhibiting transpeptidation and autolysin inhibitors. Tazobactam, a beta-lactamase inhibitor, irreversibly inactivates beta-lactamases, preventing hydrolysis of piperacillin.
Adult: 100 mg orally twice daily or 200 mg once daily for uncomplicated UTI; for severe infections, up to 20 mg/kg/day in divided doses. IV: 10-20 mg/kg/day divided every 6-12 hours.
3.375 g (piperacillin 3 g + tazobactam 0.375 g) intravenously every 6 hours over 30 minutes. For nosocomial pneumonia, 4.5 g every 6 hours.
None Documented
None Documented
Clinical Note
moderateTrimethoprim + Teriflunomide
"The metabolism of Teriflunomide can be decreased when combined with Trimethoprim."
Clinical Note
moderateTrimethoprim + Sulfisoxazole
"The metabolism of Sulfisoxazole can be decreased when combined with Trimethoprim."
Clinical Note
moderateTrimethoprim + Cyclosporine
"The metabolism of Cyclosporine can be decreased when combined with Trimethoprim."
Clinical Note
moderateTrimethoprim + Fluconazole
Terminal elimination half-life is 8-12 hours in adults with normal renal function; prolonged to 20-40 hours in severe renal impairment (CrCl <15 mL/min).
Piperacillin: 0.7-1.2 hours (normal renal function). Tazobactam: 0.7-0.9 hours. Clinically, half-life extends to 2-6 hours in renal impairment (CrCl <20 mL/min); requires dose adjustment.
Renal excretion: approximately 50-60% of the dose is excreted unchanged in urine via glomerular filtration and tubular secretion; about 10-20% as metabolites (conjugated and oxidized forms); biliary/fecal excretion accounts for less than 10%.
Piperacillin: ~68% renal (glomerular filtration and tubular secretion), 9-17% biliary. Tazobactam: ~80% renal (unchanged and inactive metabolite). Mean cumulative urinary recovery: piperacillin 68%, tazobactam 80%; fecal recovery: piperacillin ~11%, tazobactam <1%.
Category D/X
Category C
Antibiotic
Antibiotic
"The metabolism of Fluconazole can be decreased when combined with Trimethoprim."