The use of pharmacological agents as rehabilitative tools following brain injury remains to some degree both a science and an art. Recent work in the area of the neural sciences has shed new light on the workings of basic CNS neurochemical systems and the use of pharmacologic agents in altering central neurophysiologic processes. The major central neurochemical systems are reviewed both anatomically and physiologically. An overview is provided of basic neuropharmacologic agents by class. Lastly, some of the newer neuropharmacological options for treatment of post-acute brain injury deficits are examined.