Comparative Pharmacology
Head-to-head clinical analysis: AUGMENTIN 500 versus BICILLIN C R.
Peer-Reviewed Evidence
Head-to-head clinical analysis: AUGMENTIN 500 versus BICILLIN C R.
AUGMENTIN '500' vs BICILLIN C-R
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Amoxicillin is a semisynthetic aminopenicillin that inhibits bacterial cell wall synthesis by binding to penicillin-binding proteins (PBPs), inhibiting transpeptidation and disrupting cell wall integrity, leading to bacteriolysis. Clavulanate is a beta-lactamase inhibitor that irreversibly binds to and inactivates a broad range of beta-lactamases, preventing degradation of amoxicillin and extending its spectrum to include beta-lactamase-producing bacteria.
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.
1 tablet (amoxicillin 500 mg / clavulanate 125 mg) orally every 8 hours or 1 tablet (amoxicillin 875 mg / clavulanate 125 mg) orally every 12 hours for mild to moderate infections. For severe infections, use 875 mg/125 mg every 12 hours.
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; clavulanate: 1 hour. In renal impairment (CrCl <30 mL/min): amoxicillin 7-20 hours, clavulanate 4-6 hours. Extends dosing interval.
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.
Renal excretion 50-70% (amoxicillin) and 40-60% (clavulanate) as unchanged drug; tubular secretion and glomerular filtration. Fecal elimination <10%.
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