Clavulanic acid, the first β-lactamase inhibitor, was isolated from Streptomyces clavuligerus and is commonly used alongside antibiotics like amoxicillin or ticarcillin. It acts as a "suicide inhibitor," permanently inactivating β-lactamase enzymes that degrade β-lactam antibiotics. This combination restores the effectiveness of antibiotics against resistant bacteria. While clavulanic acid lacks significant antimicrobial activity alone, its synergistic use is critical for treating β-lactamase-producing pathogens. Clavulanic acid demonstrates variable pharmacokinetics in both adults and children, influenced by factors like age, route of administration, and disease state. It is rapidly absorbed after oral ingestion, with bioavailability around 60%, reaching peak concentrations within 0.7–2.0 hours. Metabolism involves hepatic pathways with partial renal clearance, and plasma protein binding is about 30%. However, variability in elimination rates highlights the need for clavulanic acid-specific dosing strategies, especially in pediatrics.
Keij, F. M., Tramper-Stranders, G. A., Koch, B. C. P., Reiss, I. K. M., Muller, A. E., Kornelisse, R. F., & Allegaert, K. (2022). Pharmacokinetics of clavulanic acid in the pediatric population: A systematic literature review. Clinical Pharmacokinetics.
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Keij, F. M., Tramper-Stranders, G. A., Koch, B. C. P., Reiss, I. K. M., Muller, A. E., Kornelisse, R. F., & Allegaert, K. (2022). Pharmacokinetics of clavulanic acid in the pediatric population: A systematic literature review. Clinical Pharmacokinetics.
Keij, F. M., Tramper-Stranders, G. A., Koch, B. C. P., Reiss, I. K. M., Muller, A. E., Kornelisse, R. F., & Allegaert, K. (2022). Pharmacokinetics of clavulanic acid in the pediatric population: A systematic literature review. Clinical Pharmacokinetics.
Keij, F. M., Tramper-Stranders, G. A., Koch, B. C. P., Reiss, I. K. M., Muller, A. E., Kornelisse, R. F., & Allegaert, K. (2022). Pharmacokinetics of clavulanic acid in the pediatric population: A systematic literature review. Clinical Pharmacokinetics.