Leukotrienes (LTs) are a family of inflammatory mediators including
LTA4,
LTB4,
LTC4,
LTD4, and
LTE4. By competitive binding to the cysteinyl LT1 (
CysLT1) receptor, LT receptor antagonist drugs, such as
montelukast,
zafirlukast, and
pranlukast, block the effects of CysLTs, improving the symptoms of some chronic
respiratory diseases, particularly
bronchial asthma and
allergic rhinitis. We reviewed the efficacy of antileukotrienes in upper airway inflammatory diseases. An update on the use of antileukotrienes in upper airway diseases in children and adults is presented with a detailed literature survey. Data on LTs, antileukotrienes, and antileukotrienes in chronic
rhinosinusitis and
nasal polyps,
asthma, and
allergic rhinitis are presented. Antileukotriene drugs are classified into two groups: CysLT receptor antagonists (
zafirlukast,
pranlukast, and
montelukast) and LT synthesis inhibitors (
5-lipoxygenase inhibitors such as
zileuton, ZD2138,
Bay X 1005, and
MK-0591). CysLTs have important proinflammatory and profibrotic effects that contribute to the extensive hyperplastic
rhinosinusitis and nasal polyposis (NP) that characterise these disorders. Patients who receive
zafirlukast or
zileuton tend to show objective improvements in, or at least stabilisation of, NP.
Montelukast treatment may lead to clinical subjective improvement in NP.
Montelukast treatment after sinus surgery can lead to a significant reduction in eosinophilic cationic
protein levels in serum, with a beneficial effect on nasal and pulmonary symptoms and less impact in NP. Combined inhaled
corticosteroids and long-acting β-agonists treatments are most effective for preventing exacerbations among paediatric
asthma patients. Treatments with medium- or high-dose inhaled
corticosteroids, combined inhaled
corticosteroids and LT receptor antagonists, and low-dose inhaled
corticosteroids have been reported to be equally effective. Antileukotrienes have also been reported to be effective for
allergic rhinitis.