Powered by OpenAIRE graph
Found an issue? Give us feedback
addClaim

Pharmacokinetic properties of beta-lactamase inhibitors.

Authors: A, de la Pena; H, Derendorf;

Pharmacokinetic properties of beta-lactamase inhibitors.

Abstract

In recent years, the use of combinations of beta-lactam-antibiotics with beta-lactamase inhibitors has been proven to be a useful and effective strategy to improve upon the therapeutic value of beta-lactam antibiotics. The objective of this article is to evaluate the pharmacokinetic properties of three commercially available beta-lactamase inhibitors.Based on published articles in the literature, the pharmacokinetic properties of the beta-lactamase inhibitors clavulanic acid, sulbactam and tazobactam are reviewed and compared.There are some considerable differences between these three compounds: Only clavulanic acid is orally bioavailable. Tazobactam and sulbactam are eliminated renally to a larger extent than clavulanic acid. Tazobactam's total body clearance is almost twice that of sulbactam, and the two drugs differ significantly in their degree of protein-binding. Furthermore, sulbactam has a larger volume of distribution than tazobactam.When choosing combinations of a beta-lactam antibiotic with a beta-lactamase inhibitor, it is important to make sure that the pharmacokinetic properties of drug and inhibitor are similar and remain similar under changing pathophysiological conditions. Hence, beta-lactam inhibitors should not be freely interchanged, but for each beta-lactam antibiotic the best partner needs to be identified. If this is done properly, fixed combinations of beta-lactam-antibiotic and beta-lactamase inhibitor are appropriate and convenient. This situation may represent one of the few cases in pharmacotherapy, where fixed combinations of two drugs are beneficial.

Related Organizations
Keywords

Aging, Tazobactam, Biological Availability, Penicillanic Acid, Drug Synergism, Absorption, Anti-Bacterial Agents, Sulbactam, Humans, Kidney Diseases, Enzyme Inhibitors, beta-Lactamase Inhibitors, Clavulanic Acid, Half-Life

  • BIP!
    Impact byBIP!
    selected citations
    These citations are derived from selected sources.
    This is an alternative to the "Influence" indicator, which also reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).
    15
    popularity
    This indicator reflects the "current" impact/attention (the "hype") of an article in the research community at large, based on the underlying citation network.
    Average
    influence
    This indicator reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).
    Top 10%
    impulse
    This indicator reflects the initial momentum of an article directly after its publication, based on the underlying citation network.
    Average
Powered by OpenAIRE graph
Found an issue? Give us feedback
selected citations
These citations are derived from selected sources.
This is an alternative to the "Influence" indicator, which also reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).
BIP!Citations provided by BIP!
popularity
This indicator reflects the "current" impact/attention (the "hype") of an article in the research community at large, based on the underlying citation network.
BIP!Popularity provided by BIP!
influence
This indicator reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).
BIP!Influence provided by BIP!
impulse
This indicator reflects the initial momentum of an article directly after its publication, based on the underlying citation network.
BIP!Impulse provided by BIP!
15
Average
Top 10%
Average
Upload OA version
Are you the author of this publication? Upload your Open Access version to Zenodo!
It’s fast and easy, just two clicks!