Table 1.

Main pharmacological characteristics of antileukotrienes (reproduced with permission from reference [2]).

Drug	Mechanism of action	Indication	Benefits	Side effects	Dose	Comments
Montelukast	CysLT1 receptor antagonism	asthma, allergic rhinitis	as monotherapy in children with mild persistent asthma; particularly effective in exercise-induced asthma, ASA, allergen-induced asthma; as add-on therapy with ICS	headache, abdominal pain; possible association with Churg-Strauss syndrome	adults: 10 mg o.d. children 6 to 14 years of age: 5 mg o.d. children 2 to 5 years of age: 4 mg o.d.	most widely prescribed CysLT1 receptor antagonist
Pranlukast	CysLT1 receptor antagonism	asthma, allergic rhinitis	particularly effective in exercise-induced asthma, ASA, allergen-induced asthma; as add-on therapy with ICS	abdominal pain, liver enzymes elevations; possible association with Churg-Strauss syndrome	adults: 225 mg b.i.d.	only marketed in Asia
Zafirlukast	CysLT1 receptor antagonism	asthma	particularly effective in exercise-induced asthma, ASA, allergen-induced asthma; as add-on therapy with ICS	headache, abdominal pain, liver enzymes elevations; possible association with Churg-Strauss syndrome	children ≥ 12 years of age and adults: 20 mg b.i.d. children 5 to 11 years of age: 10 mg b.i.d.	first CysLT1 receptor antagonist to be approved; food and drug interactions
Zileuton	5-LO inhibition	asthma	particularly effective in exercise-induced asthma and ASA	headache, abdominal pain; liver enzymes elevations (5%)	adults and children 12 years of age and older: 600 mg q.i.d.	virtually abandoned because of poor compliance and hepatic toxicity

Abbreviations: ASA = aspirin-sensitive asthma; CysLT = cysteinyl-leukotrienes; ICS = inhaled corticosteroids.