The Ups and Downs of Novel Antiemetic Drugs, Part 1: Substance P, 5-HT, and the Neuropharmacology of Vomiting

Article Abstract

Neuropharmacology of the peptide neurotransmitter substance P is just now being unraveled. An interesting and somewhat surprising therapeutic application, namely prevention of cancer chemotherapy-induced nausea and vomiting (CINV), has recently been approved for aprepitant (Emend), an agent that blocks the receptors for substance P, known as neurokinin-1, or NK1, receptors. Someday, NK1 antagonists may also become novel psychotherapeutic agents for depression and other stress-related conditions. For now, an understanding of these agents may be enhanced by a review of the neuropharmacology of emesis, including how substance P helps to regulate this reflex within the central nervous system (CNS) via NK1 receptors in the brainstem vomiting center.