The Pharmacology and Use of H1-Receptor-Antagonist Drugs

Abstract

The H₁-receptor antagonists are among the most widely used medications in the world. We review here the molecular basis of their action and their clinical pharmacology, efficacy in allergic disorders, and adverse effects. Although we will discuss the first-generation, relatively sedating H₁-receptor antagonists briefly, we will emphasize the role of the second-generation, relatively nonsedating H₁ antagonists (Figure 1) and will identify future directions for research of these agents.Molecular Basis of ActionHistamine mediates a variety of physiologic and pathologic responses in different tissues and cells and is an important chemical mediator of inflammation in . . .