Study of the clinical pharmacology of SCI has revealed population-specific patterns of drug metabolism and disposition. PD/PK profiles reflect the changed physiology associated with SCI and correlate well with the neurologic or anatomic level and the magnitude and completeness of the injury. The greatest value of SCI PK/PD profiles lies in their use in developing criteria and strategies for the optimal prescribing of drugs and in therapeutic drug monitoring. Patients with SCI, acute or long-standing, comprise a therapeutically unique and distinct population. Rational, efficacious, and cost-effective approaches to drug development and pharmacotherapy in spinal cord-injured patients can only come about when population-specific PK/PD behavior is incorporated early into the drug development process and used to develop safe, effective therapeutic guidelines.