Background: Premedication is an integral part of any anaesthetic protocol and the drugs chosen for premedication will determine the characteristics of the ensuing anaesthetic. Choosing appropriate premedicant drugs for the individual patient is vital to ensure a smooth and stress‐free anaesthetic. Normally, a balanced premedication protocol involving both a sedative and a hypnotic is advocated. This allows the two key aims of premedication – sedation and analgesia – to be met. Synergistic sedation between most sedatives and opioids also means that combining these drugs allows lower doses of each individual agent to be used.Aim of the article: This article discusses how it is important to know the clinical pharmacology of the different drugs used for premedication in order to make a rational decision about premedicant selection. One way to think about premedicant selection is based on the American Society of Anaesthesiologists (ASA) physical status classification system of the cat or dog, whereby the health status of the individual is used to inform about suitable premedication protocols.