Antileukotrienes – Effects, Uses and Side Effects
Antileukotrienes are medications that block the effects of leukotrienes and are primarily used to treat asthma and allergic rhinitis.
Things worth knowing about "Antileukotrienes"
Antileukotrienes are medications that block the effects of leukotrienes and are primarily used to treat asthma and allergic rhinitis.
What Are Antileukotrienes?
Antileukotrienes (also known as leukotriene receptor antagonists or leukotriene inhibitors) are a class of drugs that interfere with the inflammatory process by blocking the action of leukotrienes. Leukotrienes are naturally occurring signaling molecules (inflammatory mediators) released during allergic and inflammatory reactions. They cause airway narrowing, increased mucus production, and inflammation.
Mechanism of Action
Leukotrienes are produced from arachidonic acid via the enzyme 5-lipoxygenase. They bind to specific receptors (primarily CysLT1 receptors) on airway cells, triggering inflammation, bronchoconstriction (narrowing of the airways), and excess mucus secretion.
Antileukotrienes work through two main mechanisms:
- Leukotriene receptor antagonists (LTRAs): These drugs block CysLT1 receptors, preventing leukotrienes from exerting their effects. The most well-known agent in this class is montelukast.
- 5-Lipoxygenase inhibitors: These inhibit the enzyme 5-lipoxygenase, reducing leukotriene production overall. An example is zileuton, which is approved in the United States but not in all European countries.
Indications
Antileukotrienes are primarily used for the following conditions:
- Bronchial asthma: As long-term preventive therapy, particularly for mild to moderate asthma, exercise-induced asthma, and aspirin-exacerbated respiratory disease
- Allergic rhinitis: For the management of seasonal and perennial allergic rhinitis (hay fever)
- Urticaria: As an add-on therapy in some cases of chronic hives
Key Active Substances
- Montelukast (e.g., Singulair): The most widely used LTRA; approved for adults and children as young as 6 months
- Zafirlukast: Approved in some countries, less commonly used in Europe
- Zileuton: A 5-lipoxygenase inhibitor approved in the United States
Dosage and Administration
Antileukotrienes are typically taken once daily by mouth as a tablet, chewable tablet, or granule formulation. The appropriate dosage depends on the patient's age and the condition being treated and should always follow the prescribing physician's instructions. In asthma management, they are often used as add-on therapy alongside inhaled corticosteroids but do not replace them entirely.
Side Effects
Antileukotrienes are generally well tolerated. Possible side effects include:
- Headache
- Gastrointestinal complaints (e.g., abdominal pain, nausea)
- Elevated liver enzymes (rare)
- Neuropsychiatric effects: Sleep disturbances, nightmares, irritability, depression, anxiety, and in rare cases suicidal thoughts (particularly associated with montelukast; flagged by the EMA and FDA)
Due to neuropsychiatric risks, the European Medicines Agency (EMA) has recommended that montelukast should only be used when other treatments are inadequate or not tolerated.
Contraindications and Interactions
Antileukotrienes should not be used in patients with known hypersensitivity to the active substance. Clinically relevant drug interactions include:
- Drugs metabolized via the hepatic CYP enzyme system (e.g., certain antiepileptics and antibiotics)
- Phenobarbital and rifampicin may accelerate the metabolism of montelukast, reducing its efficacy
References
- Global Initiative for Asthma (GINA): Global Strategy for Asthma Management and Prevention, 2023. Available at: https://ginasthma.org
- European Medicines Agency (EMA): Montelukast - neuropsychiatric reactions, EMA/CHMP Review, 2020. Available at: https://www.ema.europa.eu
- Barnes PJ: Pathophysiology of allergic inflammation. Immunological Reviews, 2011; 242(1): 31-50. PubMed PMID: 21429319.
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