Farmakokinetické aspekty léčby dlouhodobě působícími antipsychotiky a specifika preparátů 1. generace // SOLEN

Psychiatria pre prax 1/2026

Pharmacokinetic aspects of the treatment with long-acting injectable antipsychotics and specific features of the first generation preparations

Long acting injectable antipsychotics overcome few troubles related to long term treatment of patients with schizophrenia, especially the frequent non-adherence. They are used in the treatment of schizophrenia for almost 60 years. Compared to per os drug forms, the principles of pharmacokinetics are different. Its dynamics is led by the amount of a drug released from the site of application. Using the simple conversion of equivalent dose is burdened with a risk of plasma level decline and resulting increased risk of relapse; to overcome this, using of per os supplementation or loading patterns is recommended. The use of TDM is advantageous during switch and a dose titration. In the Czech Republic, four drugs are available from the group of first generation antipsychotics in the form of long acting injections. Individual drugs differ in their pharmacokinetic parameters and the recommended patterns of supplementation or loading.

Keywords: antipsychotics, long acting injections, pharmacokinetics, schizophrenia, titration, plasma levels