Lack of approved pharmaceutical agents and/or pharmacokinetic data in the literature for exotic, wildlife, and zoo species is a major issue for veterinarians. These practitioners must take approved agents (veterinary or human) and extrapolate their use to non-approved species with little or no scientific basis to support this decision. There is little information concerning pharmacokinetic parameters for drugs in non-domestic species. Zoo veterinarians often have to formulate the medication(s) into a meal, hoping that the animal will ingest it. Due to lack of patient compliance, the veterinarian may have to resort to other means of drug administration. Additionally, due to the value of these animals, the traditional method of 'trial and error' for treatment selection and resulting compliance is often inappropriate, and lends itself to a mentality where no zoo veterinarian wants to be the first to administer an agent/formulation in an untested species. This review intends to present the current state of zoological pharmacology and the direction it may be heading.