Since the first report of alpha2-adrenoceptor agonists, the list of clinical indications for this class of drugs continues to expand. Alpha2-adrenoceptor agonists have several beneficial actions during the perioperative period. They exert a central sympatholytic action, thus improving haemodynamic stability in response to endotracheal intubation and surgical stress, reducing anaesthetic and opioid requirements, and causing sedation, anxiolysis and analgesia. Furthermore, alpha2-adrenoceptor agonists may offer benefits in the prophylaxis and treatment of perioperative myocardial ischaemia and their role in pain management and regional anaesthesia is increasing. The development of new, highly selective compounds which not only reduce anaesthetic requirements but induce anaesthesia by themselves may provide a new concept for the administration of anaesthesia.