Safety of antileukotriene agents in asthma management

Objective: This article presents information on the safety of zafirlulast, montelukast, and zileuton, three antileukotrienes (anti-LTs) approved in th e United States for the prophylaxis and treatment of asthma. After reading this article, readers should have an understanding both of the general safe ty of anti-LTs and their specific adverse effects. Data Sources: Relevant and appropriate controlled clinical studies on the s afety of anti-LTs in asthma were used. Only literature in the English langu age was reviewed. Study Selection: Material was taken from academic/scholarly journals and ap propriate reviews. Results: Antiasthma agents, including corticosteroids, beta (2)-agonists, a nd methylxanthines, may be categorized into two classes: those used for the long-term control and prevention of persistent asthma and those used for t he prompt relief of acute symptoms and exacerbations of the disease. Althou gh most agents are safe and well tolerated when used properly, adverse effe cts may occur with use at higher dose levels. The anti-LTs, including zafir lukast, montelukast, and zileuton, are the first new pharmacologic class in the therapeutic armamentarium for asthma management to be approved in the United States in the past 20 years. Both zafirlukast and montelukast carry pregnancy category B classification whereas zileuton carries pregnancy cate gory C classification. The most common adverse effects observed in clinical trials were headache, pharyngitis, abdominal pain, dyspepsia, and cough. Conclusions: The results of clinical trials and real-world experience indic ate that these agents are generally safe and well tolerated, with an incide nce of adverse effects comparable with placebo.