Advances in neurobiology over the past several decades have revolutionized psychiatry and the related discipline of psychopharmacology. While once predominantly psychoanalytical, modern psychiatry embraced the neurobiological-altering power of psychopharmacology. With this embrace came a seemingly daunting obsession with efficacies, toxicities, indications, contraindications, drug-to-drug interactions, and ever-refined clinical studies. Although our knowledge of psychopharmacology has inevitably widened, there are many fundamental properties of pharmacology that can be used to prescribe psychotropic agents more accurately and effectively. All clinicians who are exposed to patients with mental illness will benefit from a basic understanding of the kinetics and dynamics of pharmacology, as well as the uses and considerations of common agents. This chapter details some of the overarching principles of psychopharmacology in an attempt to lay the groundwork for many of the specific details regarding psychotropic classes. When prescribing psychotropic agents, details can be recalled through an understanding of a drug’s inherent properties, what it works on, and what the body does to the drug. Rather than memorizing every detail of a drug’s side effects, it is manageable to recall the neurotransmitter systems impacted, and how this interaction can lead to side effects. This chapter also focuses briefly on the process of drug development and marketing. Awareness of an agent’s conception to widespread use will answer some of the hesitations physicians may have such when encountering psychotropics with black box warnings or prescribing an agent during pregnancy. Finally, some of the most common side effects and lab monitoring considerations that neurologists will likely encounter are reviewed.