Comparative Pharmacology
Head-to-head clinical analysis: AUGMENTIN 400 versus BICILLIN L A.
Peer-Reviewed Evidence
Head-to-head clinical analysis: AUGMENTIN 400 versus BICILLIN L A.
AUGMENTIN '400' vs BICILLIN L-A
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Augmentin '400' is a combination of amoxicillin (a beta-lactam antibiotic) and clavulanate (a beta-lactamase inhibitor). Amoxicillin inhibits bacterial cell wall synthesis by binding to penicillin-binding proteins (PBPs), while clavulanate irreversibly inhibits beta-lactamase enzymes, preventing inactivation of amoxicillin.
Penicillin G benzathine is a slow-release formulation that provides prolonged tissue concentrations. It inhibits bacterial cell wall synthesis by binding to penicillin-binding proteins (PBPs), inhibiting transpeptidation, and activating autolytic enzymes, leading to cell lysis.
500 mg (amoxicillin 400 mg / clavulanate 57 mg) orally every 12 hours or 875 mg (amoxicillin 700 mg / clavulanate 100 mg) orally every 12 hours; usual duration 5-10 days.
1.2 million units intramuscularly as a single dose for treatment of streptococcal pharyngitis; for syphilis, 2.4 million units intramuscularly weekly for 1-3 weeks depending on stage.
None Documented
None Documented
Amoxicillin: 1-1.3 hours (prolonged to ~7 hours in renal impairment, e.g., CrCl <10 mL/min). Clavulanate: 1-1.2 hours (prolonged in renal impairment). Clinical context: Dosing interval adjustment required for CrCl <30 mL/min.
Terminal half-life: 30-60 hours (prolonged due to slow absorption from IM depot; clinically allows single-dose regimen for syphilis)
Amoxicillin: ~50-70% renal (tubular secretion and glomerular filtration) as unchanged drug, remainder metabolized to penicilloic acid. Clavulanate: ~30-50% renal as unchanged drug, remainder metabolized and excreted via bile/feces. Total renal clearance accounts for ~60-80% of elimination for both components.
Renal: 60-90% unchanged; biliary/fecal: minor (<10%)
Category C
Category C
Penicillin Antibiotic
Penicillin Antibiotic