Antipsychotic drugs are a class of psychiatric medication worldwide used to treat psychotic symptoms principally in bipolar disorder, schizophrenia and other psycho-organic disorders. The traditional sample preparation techniques such as liquid-liquid extraction (LLE) or solid phase extraction (SPE), which were widely used, tend to have many drawbacks because they include complicated, time-consuming steps and they require large sample size as well large amounts of organic solvent. Therefore, due to the modern analytical requirements, such as miniaturization, automation and reduction of solvent volume and time, many microextraction procedures have been developed. In this review we aim to present an overview of those techniques which are used prior to liquid chromatography analyses both for forensic toxicology in different biological matrices as well as for therapeutic drug monitoring.