
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.
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
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
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