Pharmacokinetics and pharmacogenetics of macrolides (literature review)

Skryabina A.A., Nikiforov V.V., Shakhmardanov M.Z., Zastrozhin M.S., Sychev D.A.

Pirogov Russian National Research Medical University, Moscow
Moscow Research and Practical Centre on Addictions, Moscow
Russian Medical Academy of Continuous Professional Education, Moscow

The aim of this research is to systematize scientific data on the pharmacokinetics and pharmacogenetics of macrolides. Macrolides are a class of broad-spectrum antibiotics used to treat a wide range of both topical and systemic infectious diseases. Despite the fact that macrolide use is generally considered to be safe, in a number of patients it can be associated with dose-dependent adverse drug reactions (ADRs), reducing the safety of therapy in these patients. Knowledge of the peculiarities of pharmacokinetics, pharmacodynamics and pharmacogenetics of macrolides is necessary to assess the effect of genetically determined activity of cytochrome isoenzymes of the P450 system on plasma concentration, efficacy and safety of antibiotics from this group. This will make it possible to develop approaches to personalizing the selection of an effective and safe dose of macrolides based on the clinical and biological parameters of the patient.
Results: it was found that genotypic variability affects both the transport of macrolides and their metabolism. It has been shown that polymorphism of a number of candidate genes can affect the pharmacokinetics and pharmacodynamics of macrolides, which may explain the differences in the efficacy and safety of therapy in different patients.