Therapeutic drug monitoring (TDM), as part of clinical process of medical treatments, is commonly used to maintain ‘therapeutic’ drug concentrations. TDM is useful to identify the causes of unwanted or unexpected responses, to prevent unnecessary diagnostic testing, to improve clinical outcomes, and even to save lives. The determination of drug concentration in blood samples requires an excellent sample preparation procedure. Recent trends in sample preparation include miniaturization, automation, high-throughput performance, on-line coupling with analytical instruments and low-cost operation through extremely low or no solvent consumption. Microextraction techniques, such as liquid- and solid-phase microextraction, have these advantages over the traditional techniques. This paper reviews the recent developments in microextraction techniques used for drug monitoring in serum, plasma or blood samples. Copyright © 2012 John Wiley & Sons, Ltd.