Many factors may influence the actions and fates of anesthetic and anesthetic-related agents in ruminant animals. These considerations need to be taken into account when these drugs are employed clinically. Some of the major principles governing the disposition of CNS-active drugs are reviewed, with special emphasis on the uniqueness of ruminant animals. General pharmacokinetic considerations are also covered as a preamble to a commentary on the kinetic characteristics of anesthetic and anesthetic-related agents that are commonly used in domesticated ruminants.