Comparative Pharmacology
Head-to-head clinical analysis: AUGMENTIN 400 versus BICILLIN C R.
Peer-Reviewed Evidence
Head-to-head clinical analysis: AUGMENTIN 400 versus BICILLIN C R.
AUGMENTIN '400' vs BICILLIN C-R
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.
Benzathine penicillin G and procaine penicillin G are beta-lactam antibiotics that inhibit bacterial cell wall synthesis by binding to penicillin-binding proteins (PBPs), inhibiting transpeptidase activity, 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 (600,000 units procaine penicillin G and 600,000 units benzathine penicillin G) for moderate to severe infections; for mild infections, 600,000 units intramuscularly as a single dose.
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.
Penicillin G: 0.5-1 hour in normal renal function; prolonged to 7-10 hours in anuria. Benzathine component sustains low levels for days; effective half-life of benzathine penicillin G is 3-5 days due to slow release.
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 excretion primarily via glomerular filtration and tubular secretion; approximately 60-70% of penicillin G is excreted unchanged in urine within 6 hours; benzathine and procaine components are metabolized and excreted renally as well; small amounts in bile and feces.
Category C
Category C
Penicillin Antibiotic
Penicillin Antibiotic