Veterinary behavioral medicine remains an under-supported, under-appreciated, and under-taught specialty within veterinary medicine. Neuropsychopharmacology is the aspect that has provided the field with the most scientific legitimacy, but is also one of the most hotly debated. Paradigms for use of pharmacologic intervention include firstly ruling out any underlying medical cause. If a behavioral diagnosis can be made, treatment with psychotropic medication may be considered, although their use is most effective as part of an integrated treatment program that includes behavior modification. Used without an understanding of the mechanism of action, pharmacologic intervention may only blunt or mask behavior without altering processes or environments that produced the behavior. This paper reviews specific drugs, mechanism of action of those drugs, and relevant uses are reviewed for cats. Future advances in treatment in veterinary behavioral medicine will be pharmacological and neurophysiological. As the field of veterinary behavioral medicine expands, its paradigm will enlarge to include routine combination therapy and the implementation of neuropharmacological intervention as a diagnostic tool.