Zileuton

• Zileuton is an oral medication used for the chronic treatment and prevention of asthma symptoms.
• Its primary mechanism of action involves inhibiting the enzyme 5-lipoxygenase, which reduces the production of inflammatory leukotrienes.
• It is not intended for the relief of acute asthma attacks but rather for long-term control.
• Potential side effects include headache, nausea, and, importantly, elevated liver enzymes, requiring regular monitoring.
• Comprehensive drug information highlights its role in asthma management, contraindications, and potential drug interactions.

What is Zileuton?

Zileuton is an orally administered medication classified as a leukotriene synthesis inhibitor. It is specifically designed for the prophylaxis and chronic treatment of asthma in adults and children 12 years of age and older. Unlike bronchodilators that provide immediate relief, Zileuton works to prevent asthma symptoms by addressing the underlying inflammatory processes in the airways. It is crucial to understand that Zileuton is not a rescue medication for acute asthma attacks and should not be used to treat sudden breathing difficulties.

Zileuton Uses and Mechanism of Action

Zileuton is primarily indicated for the long-term control of asthma. It helps reduce the frequency and severity of asthma symptoms, such as wheezing, shortness of breath, chest tightness, and coughing, by decreasing inflammation and bronchoconstriction in the airways. The medication is typically prescribed when other standard asthma treatments are insufficient or when a patient experiences persistent asthma symptoms.

The zileuton mechanism of action involves selectively inhibiting the enzyme 5-lipoxygenase. This enzyme is critical in the arachidonic acid pathway, where it catalyzes the formation of leukotrienes. Leukotrienes, particularly leukotriene B4 and the cysteinyl leukotrienes (C4, D4, E4), are potent inflammatory mediators released by various cells in the airways, including mast cells, eosinophils, and macrophages. These substances contribute significantly to the pathophysiology of asthma by:

• Causing bronchoconstriction (narrowing of the airways).
• Increasing vascular permeability, leading to airway edema.
• Promoting mucus secretion.
• Recruiting inflammatory cells to the airways.

By inhibiting 5-lipoxygenase, Zileuton effectively blocks the synthesis of these inflammatory leukotrienes, thereby reducing airway inflammation and improving lung function over time. This targeted approach helps patients manage their asthma more effectively, leading to fewer exacerbations and an improved quality of life.

Zileuton Side Effects and Drug Information

Like all medications, Zileuton can cause zileuton side effects, which range from mild to severe. Common side effects often include headache, nausea, abdominal pain, and general weakness. More serious, though less common, side effects can involve the liver. Zileuton has been associated with elevated liver enzymes, and in rare cases, severe liver injury. For this reason, regular monitoring of liver function tests (LFTs) is essential before starting treatment and periodically throughout therapy, especially during the first year. Patients should be advised to report any symptoms of liver dysfunction, such as persistent nausea, vomiting, dark urine, yellowing of the skin or eyes (jaundice), or unusual fatigue, to their healthcare provider immediately.

Comprehensive zileuton drug information highlights several important considerations for its safe and effective use. Zileuton is contraindicated in patients with active liver disease or persistently elevated liver enzymes. It is available in immediate-release and extended-release formulations, with specific dosing regimens that must be followed as prescribed. Zileuton can interact with other medications, potentially altering their effects or increasing the risk of side effects. Notable drug interactions include warfarin, which may lead to an increased risk of bleeding, and theophylline, which may result in increased theophylline levels. Patients should always inform their healthcare provider about all medications, supplements, and herbal products they are taking to avoid potential interactions. Adherence to the prescribed dosage and regular follow-up with a healthcare professional are crucial for optimizing treatment outcomes and managing potential risks.