Contrary to the situation in "classical" clinical pharmacology, non-steady state phenomena play a fundamental role for clinical pharmacology in anesthesia. Their understanding is of tantamount importance for the safe and efficient application of drugs relevant to anesthesia. Concepts like optimised target-controlled infusion (TCI), effect compartment targeting and the small margin of error tolerable during maintained spontaneous ventilation, force the anesthesiologist to acquire a firm understanding of the difference between the concentration time course at the effect side vs. time course of the plasma concentration. The underlying concepts, their application for the rational use of muscle relaxants, propofol with TCI systems, volatile anaesthetics and opioids will be discussed.