Masilukast

Masilukast

Masilukast is a leukotriene receptor antagonist (LTRA) used in the management of asthma and allergic rhinitis. It functions by blocking the action of leukotrienes, which are inflammatory chemicals the body releases after coming in contact with an allergen or irritant. By inhibiting these chemicals, masilukast helps to reduce inflammation, bronchoconstriction, and mucus production in the airways.

Pharmacology

Masilukast is a selective and competitive antagonist of the cysteinyl leukotriene receptor 1 (CysLT1). Leukotrienes are produced by the action of the enzyme 5-lipoxygenase on arachidonic acid, and they play a key role in the pathophysiology of asthma and allergic rhinitis. By blocking the CysLT1 receptor, masilukast prevents leukotrienes from exerting their effects on the respiratory tract, thereby reducing symptoms such as wheezing, shortness of breath, and nasal congestion.

Clinical Use

Masilukast is primarily indicated for the prophylaxis and chronic treatment of asthma in adults and children. It is also used to relieve symptoms of seasonal and perennial allergic rhinitis. Unlike beta-agonists, masilukast is not used for the relief of acute asthma attacks.

Dosage and Administration

Masilukast is typically administered orally, with the dosage varying based on age and the specific condition being treated. It is often taken once daily in the evening, as leukotriene levels are higher at night.

Side Effects

Common side effects of masilukast include headache, dizziness, abdominal pain, and fatigue. Rare but serious side effects may include mood changes, suicidal thoughts, and liver dysfunction. Patients are advised to report any unusual psychological symptoms to their healthcare provider.

Mechanism of Action

Masilukast works by binding to the CysLT1 receptor on target cells in the lungs and nasal passages, thereby preventing leukotrienes from binding to these receptors. This action reduces the inflammatory response and helps to keep the airways open.

Research and Development

Masilukast was developed as part of a class of drugs aimed at providing an alternative to corticosteroids for the management of asthma and allergies. Ongoing research is exploring its potential use in other inflammatory conditions and its long-term safety profile.

Also see

• Leukotriene receptor antagonist
• Asthma management
• Allergic rhinitis
• Cysteinyl leukotriene receptor

{{Drugbox | verifiedfields = changed | verifiedrevid = 477002123 | IUPAC_name = (E)-1-[[3-[2-(7-chloroquinolin-2-yl)ethenyl]phenyl]methyl]piperidine | image = Masilukast_structure.png | width = 200 | tradename = Masilukast | legal_status = Rx-only | routes_of_administration = Oral | bioavailability = 64% | protein_bound = 99% | metabolism = Hepatic | elimination_half-life = 2.7–5.5 hours | excretion = Fecal (86%), renal (10%) }}