A Receptor Pharmacokinetic View for Antileukotriene Agents

Abstract

Antileukotriene agents montelucast and pranlukast commonly used to treat allergic rhinitis are classified into chemical mediator receptor antagonists and antihistamine agents, and their intensity and onset different widely. Clinical experience suggests that antileukotriene agents have a slower onset and weaker efficacy than antihistamine agents. Such characteristics of anti-leukotriene agents are argued from the standpoint of receptor pharmacokinetics.
The dissociation constant kd of antileukotriene agents are similar to Kd of leukotrienes and the concentration of antileukotriene agents in nasal mucosa insufficient to inhibit leukotriene brinding to receptors. Despite these features, antileukotriene agents are expected to be very effective against nasal symptoms such as allergenic inflammation.