Local anesthetics are chemical substances, whose mechanism of action is based on reversible blockage of sodium voltage channels, lead to the inhibition neural impulse transduction. In order to acces their binding site, localized on the inner side of the nerve cell memmbrane, they need to cross lipoprotein matrix, which is enabled by their liposolubility, constant of dissociation and low molecular mass. Local anesthetics can be divided into two groups: aminoesters, such as cocaine, procaine, 2-chloroprocaine, tetracaine, and aminoamids, such as lidocaine, prilocaine, mepivacaine, bupivacaine, etidocaine, ropivacaine and levobupivacaine. The main distinctions between the groups are the instability of the aminoesteric chemical bound, their allergic potential and metabolic differences. This explains why the aminoesters are more rarely used in the clinical practice and are substituted by aminoamides. Furthermore, this review includes a systematic overview of the most important local anesthetics in clinical practice. They are broadly used in surgery for infiltration anesthesia, topical, spinal and epidural, as such as peripheral nerve blocks. They are also used for postoperative analgesia which improves patient recovery and decreeses systemic stress response. Systemic administration of lidocaine for ventricular arrythmia treatment following myocardial ishemia. Adverse effects are the following: allergic reaction (rarely) and systemic toxicity due to accidental intravascular administration. The choice of local anesthetics depends on the clinical state of the individual, onset velocity of anesthesia needed , anesthetic duration and physical-chemical properties of the medication.