HMG-CoA reductase inhibitors are among the most proscribed drugs in the world. The main effect is their reduction of LDL cholesterol, which is why they are used in primary and secondary prevention of many cardiovascular diseases. The goal of the study was to review statin pharmacokinetics and pharmacodynamics, focusing on the biotransformation of the four statins registered on the Croatian market, and their paths of entry and exit from the cell. The research for the study has been conducted through academic research papers published in scientific journals and available for the review through the following databases: PubMed, Mendeley, textbooks and other literature. The results show that the statins are highly heterogeneous group considering the origin of each statin, their structural and physico-chemical properties, and their clinical effects that result from these properties. When including statins into therapy, it is important to consider the various enzymes involved in their metabolism and pharmacogenomic characteristics of the patient to avoid interaction and toxicity of statins and to maximize the therapeutic effect.