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Clavulanic acid

Clavulanic acid

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Substance Overview and History

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.

References:

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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FAQ
What is clavulanic acid and how does it work?
Clavulanic acid is a β-lactamase inhibitor used alongside antibiotics like amoxicillin or ticarcillin. It inactivates β-lactamase enzymes that degrade β-lactam antibiotics, restoring their effectiveness against resistant bacteria.
References:

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.

Why is clavulanic acid used in combination with other antibiotics?
While clavulanic acid has little antimicrobial activity on its own, it is crucial in combination with antibiotics like amoxicillin to treat β-lactamase-producing pathogens, which are resistant to standard antibiotics.
References:

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.

What factors influence the pharmacokinetics of clavulanic acid?
The pharmacokinetics of clavulanic acid are influenced by factors such as age, route of administration, disease state, and whether the individual is an adult or a child.
References:

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.