Introduction
Montelukast Sodium is a highly selective, orally active cysteinyl leukotriene receptor antagonist (LTRA) and a non-steroidal anti-inflammatory pharmaceutical agent, specifically targeting the cysteinyl leukotriene 1 (CysLT1) receptor. It is a core clinical drug for the long-term management of asthma and allergic rhinitis in children, adolescents and adults, with the unique advantage of no glucocorticoid-related adverse effects and simple once-daily administration. Its chemical formula is C₃₅H₃₅ClNNaO₃S, and it is formulated into a variety of age-adapted oral preparations—oral granules (for infants ≥6 months), chewable tablets (for children 2–14 years old), and conventional tablets (for adolescents ≥15 years old and adults)—to meet the clinical needs of different populations. Characterized by good oral bioavailability (~64% for adults), rapid absorption (unaffected by food intake), a moderate elimination half-life (2.7–5.5 hours in adults, longer in children), and extensive tissue distribution, it exerts sustained anti-inflammatory and bronchodilatory effects with bedtime administration. With excellent tolerability and a low incidence of adverse reactions, it is widely used in pediatrics, pulmonology, otorhinolaryngology and general medicine, and is a first-line choice for the long-term control of mild to moderate asthma and symptomatic relief of allergic rhinitis, especially for patients who cannot tolerate inhaled glucocorticoids or prefer oral medication.
Core Pharmacological Mechanism (to support its therapeutic uses)
Montelukast Sodium exerts its therapeutic effects by potently and selectively competing with endogenous cysteinyl leukotrienes (CysLTs) for binding to the CysLT1 receptor expressed on the surface of airway smooth muscle cells, nasal mucosal vascular endothelial cells, bronchial epithelial cells and inflammatory cells (eosinophils, mast cells). CysLTs (mainly LTC4, LTD4 and LTE4) are key pro-inflammatory mediators produced and released by mast cells, eosinophils and other immune cells in response to allergen stimulation, respiratory tract irritation or inflammation; they are the core pathological mediators of asthma and allergic rhinitis, responsible for triggering a series of pathological reactions in the respiratory tract.
By blocking the CysLT1 receptor, montelukast sodium reverses and inhibits all CysLTs-induced pathological effects, achieving three core therapeutic actions:
Bronchorelaxation and anti-asthmatic effect: It directly relaxes CysLTs-contracted airway smooth muscle, reduces airway hyperresponsiveness (AHR)—a hallmark of asthma—and prevents airway spasm induced by allergens, cold air, exercise or irritants.
Anti-inflammatory effect on the respiratory tract: It inhibits the infiltration and activation of inflammatory cells (eosinophils, mast cells) in the bronchial and nasal mucosa, reduces the secretion of airway mucus and the permeability of nasal mucosal blood vessels, and alleviates mucosal edema and congestion, thereby reducing the underlying inflammation of asthma and allergic rhinitis.
Symptomatic relief of allergic rhinitis: It inhibits CysLTs-induced nasal mucosal vasodilation, edema and hypersecretion, rapidly relieving core allergic rhinitis symptoms such as nasal congestion, rhinorrhea, sneezing and pruritus, with a synergistic effect on both upper and lower respiratory tract symptoms (the "unified airway" effect).
Notably, montelukast sodium is a prophylactic and long-term control drug, not a rescue medication for acute attacks: it does not have a rapid bronchodilatory effect and cannot relieve acute asthma exacerbations or severe allergic rhinitis symptoms, as it targets the underlying inflammatory mechanism rather than directly relaxing acutely contracted airways or blocking immediate allergic reactions. In addition, it has no affinity for other receptors (e.g., adrenergic, cholinergic, histamine H1 receptors), which eliminates off-target adverse reactions and ensures high pharmacological specificity.
Primary Therapeutic Uses
Montelukast Sodium is clinically indicated for the long-term prophylaxis and control of asthma and the symptomatic relief of allergic rhinitis in infants, children, adolescents and adults. It is also the first-line drug for the prevention of exercise-induced bronchoconstriction (EIB) and is effective for patients with comorbid asthma and allergic rhinitis (the most common clinical comorbidity), exerting a unified therapeutic effect on the upper and lower respiratory tracts. Its specific clinical applications are as follows:
1. Long-term Control and Prophylaxis of Asthma
It is a first-line oral agent for the long-term control of mild to moderate persistent asthma in patients aged ≥6 months (infants, children, adolescents and adults), and can be used as an adjuvant drug for moderate to severe persistent asthma in combination with inhaled glucocorticoids (ICS) to reduce the ICS dose and minimize steroid-related adverse effects. It effectively prevents asthma attacks induced by allergens, cold air, smoke, dust or exercise, reduces the frequency and severity of asthma symptoms (cough, wheezing, shortness of breath, chest tightness), improves lung function (forced expiratory volume in 1 second, FEV1) and exercise tolerance, and decreases the need for short-acting beta2-agonists (SABA) as rescue medication. It is particularly suitable for asthma patients who cannot tolerate or are non-adherent to inhaled medication (a common issue in children and elderly patients), and for patients with mild asthma who prefer oral monotherapy.
2. Prevention of Exercise-Induced Bronchoconstriction (EIB)
It is a first-line prophylactic drug for EIB in patients aged ≥6 years old (children, adolescents and adults)—a common condition characterized by acute airway spasm, wheezing and shortness of breath within 15–30 minutes after strenuous exercise. Administered 1–2 hours before exercise, montelukast sodium effectively prevents EIB for up to 24 hours, with no need for additional pre-exercise medication for a single daily dose. It is a preferred alternative for patients who cannot tolerate inhaled beta2-agonists (the traditional EIB prophylaxis) or have adverse reactions to them, and for pediatric patients who have difficulty using inhalers.
3. Symptomatic Relief of Allergic Rhinitis (Seasonal and Perennial)
It is used for the symptomatic treatment of seasonal allergic rhinitis (SAR) (caused by pollen, mold spores) and perennial allergic rhinitis (PAR) (caused by dust mites, pet dander, indoor mold) in patients aged ≥2 years old (children, adolescents and adults). It effectively relieves all core nasal symptoms (nasal congestion, rhinorrhea, sneezing, nasal pruritus) and associated ocular symptoms (ocular pruritus, tearing, conjunctival congestion), with a therapeutic effect onset within 24 hours of the first dose and sustained relief with once-daily administration. It can be used as monotherapy for mild to moderate allergic rhinitis or as an adjuvant drug for severe allergic rhinitis in combination with intranasal glucocorticoids or oral antihistamines, and is particularly effective for nasal congestion—a symptom that is often poorly controlled by antihistamines alone.
4. Treatment of Comorbid Asthma and Allergic Rhinitis
It is the first-line choice for patients with concurrent asthma and allergic rhinitis (a clinical comorbidity with an incidence of >70% in asthmatics), as it exerts a unified airway anti-inflammatory effect on both the upper (nasal mucosa) and lower (bronchial mucosa) respiratory tracts. By targeting the common inflammatory mediator (CysLTs) of both diseases, it simultaneously controls asthma symptoms and relieves allergic rhinitis symptoms, reducing the mutual triggering of the two conditions (e.g., nasal congestion-induced mouth breathing exacerbating asthma, asthma inflammation worsening nasal symptoms) and improving the overall clinical outcome of patients.
5. Pediatric Asthma and Allergic Rhinitis (Special Populations)
Formulated as oral granules (for ≥6 months) and chewable tablets (for 2–14 years), it is the most widely used oral anti-asthma and anti-allergic drug in pediatrics. It is the first-line prophylactic drug for mild persistent asthma in infants and young children (≥6 months), a population with limited treatment options (few inhaled drugs are approved for this age group), and effectively relieves allergic rhinitis symptoms in children ≥2 years old with good compliance and tolerability. The age-adapted formulations avoid the difficulty of inhaler use in young children, making it a core drug for pediatric respiratory allergy management.
Clinical Application Key Points
Montelukast Sodium features simple administration, age-adapted formulations and excellent tolerability, but its clinical use requires clear differentiation between prophylactic/long-term control and acute rescue treatment, with individualized dosing based on age and indication. Key application points are as follows:
1. Administration and Dosage
Oral administration, once daily at bedtime (the optimal time for asthma and allergic rhinitis management, as symptoms often worsen at night or in the early morning); can be taken with or without food (food has no effect on absorption or efficacy). Granules can be mixed with a small amount of cold or room-temperature food (e.g., applesauce, milk) or water (avoid hot liquids, which may destroy the drug) for infants and young children who cannot swallow tablets. Chewable tablets should be chewed thoroughly before swallowing; conventional tablets are swallowed whole with water. Fixed age-based dosing (no weight adjustment required for most age groups) for asthma, allergic rhinitis and EIB prevention:
Infants (6–23 months): 4 mg once daily (granules), for asthma prophylaxis only;
Children (2–5 years): 4 mg once daily (granules/chewable tablets), for asthma prophylaxis and allergic rhinitis;
Children (6–14 years): 5 mg once daily (chewable tablets), for asthma prophylaxis, allergic rhinitis and EIB prevention;
Adolescents (≥15 years) and Adults: 10 mg once daily (conventional tablets), for all indications (asthma, allergic rhinitis, EIB prevention).
For EIB prevention only: a single dose is taken 1–2 hours before exercise; if a daily bedtime dose is already used, no additional dose is needed for pre-exercise prophylaxis (the daily dose provides sustained EIB protection).
2. Main Adverse Reactions
Montelukast Sodium has an excellent safety profile with mild, transient and rare adverse reactions (overall incidence <5%), most of which resolve spontaneously with continued treatment or drug withdrawal, and no need for dose reduction in most cases. Adverse reactions are similar across all age groups, with no significant difference between children and adults:
Most common (incidence <2%): Mild gastrointestinal symptoms (abdominal pain, diarrhea, nausea, vomiting), headache, fatigue, and upper respiratory tract infection-like symptoms (sore throat, runny nose)—mostly mild and non-specific;
Less common (incidence <1%): Dizziness, insomnia, irritability, dry mouth, rash, and pruritus; in children, occasional transient behavioral changes (hyperactivity, tantrums) which resolve with drug withdrawal;
Rare severe adverse reactions (extremely rare): Severe allergic reactions (angioedema, anaphylaxis, urticaria), elevated hepatic transaminases (reversible after withdrawal), psychiatric symptoms (depression, suicidal ideation—reported in rare cases, mostly in adolescents and adults with a history of mental illness), and arthralgia/myalgia. Severe adverse reactions require immediate drug discontinuation and medical intervention.
Notably, the incidence of adverse reactions is not dose-related, and long-term use (≥12 months) has no cumulative toxic effects, making it suitable for chronic long-term treatment.
3. Contraindications
Montelukast Sodium is contraindicated only in patients with hypersensitivity to montelukast sodium, any component of the pharmaceutical preparation, or other leukotriene receptor antagonists. There are no other absolute contraindications, and it is well-tolerated in most special populations (excluding severe hepatic/renal insufficiency, for which limited data exist).
4. Key Precautions
Not for acute asthma attacks: It is a long-term control/prophylactic drug and has no rapid bronchodilatory effect; it cannot be used to relieve acute asthma exacerbations (wheezing, severe shortness of breath, chest tightness), for which short-acting beta2-agonists (SABA) and systemic glucocorticoids are the first-line rescue medications. Discontinuation of the drug in asthmatics may lead to asthma exacerbation, so gradual withdrawal is recommended if needed.
Psychiatric symptom monitoring: Rare cases of psychiatric symptoms (depression, anxiety, suicidal ideation, abnormal behavior) have been reported in adolescents and adults; closely monitor mood and behavior changes in patients with a history of mental illness, and discontinue the drug immediately if such symptoms occur.
Hepatic function monitoring: Routine liver function monitoring is not required for normal patients; if jaundice, persistent fatigue or abdominal pain occurs, check hepatic transaminases (ALT/AST), and discontinue the drug if transaminases are elevated to >3 times the upper limit of normal (extremely rare).
Pregnancy and lactation: Use only when the therapeutic benefit outweighs the potential fetal/infant risk (limited human safety data; animal studies show no teratogenic effects). The drug is excreted in breast milk in small amounts, so breastfeeding is recommended only if necessary, with close monitoring of the infant for adverse reactions.
Hepatic/renal insufficiency: No dose adjustment is required for patients with mild to moderate hepatic or renal insufficiency (the drug is mainly metabolized by the liver and excreted in bile, with minimal renal excretion); limited data exist for severe hepatic/renal insufficiency, so use with caution.
Driving and operating machinery: May cause mild dizziness or fatigue in rare cases; avoid high-risk activities if such symptoms occur, as they are transient and resolve spontaneously.
Abrupt withdrawal: No severe withdrawal symptoms; gradual discontinuation is recommended for asthmatics to avoid transient asthma symptom worsening (no need for gradual withdrawal for allergic rhinitis alone).
5. Drug Interactions
Montelukast Sodium has an extremely low risk of clinically significant drug interactions due to its high receptor selectivity, minimal metabolism by hepatic cytochrome P450 (CYP450) enzymes (no induction or inhibition of CYP450 isoenzymes), and lack of binding to plasma proteins (low protein binding rate). It can be safely combined with most commonly used respiratory, anti-allergic and cardiovascular drugs, with no significant interactions reported. Key minor interactions are as follows:
Inhaled glucocorticoids (ICS) and short-acting beta2-agonists (SABA): No interaction; safe for combination use in moderate to severe asthma, with synergistic anti-asthmatic effects (montelukast for anti-inflammation, SABA for acute rescue, ICS for strong local anti-inflammation).
Oral antihistamines and intranasal glucocorticoids: No interaction; safe for combination use in severe allergic rhinitis, with synergistic symptomatic relief (montelukast for nasal congestion, antihistamines for sneezing/rhinorrhea, intranasal ICS for severe mucosal inflammation).
Warfarin: A minor increase in international normalized ratio (INR) may occur in a small number of patients on long-term warfarin therapy; monitor INR once after initiating montelukast, with no need for routine monitoring or dose adjustment (the effect is mild and non-clinically significant).
Phenobarbital and other CYP450 inducers: Slight acceleration of montelukast metabolism (no significant reduction in plasma concentration or therapeutic effect); no dose adjustment is required for clinical use.
Antifungal drugs and macrolide antibiotics: No inhibition of montelukast metabolism; safe for combination use in patients with asthma/allergic rhinitis complicated by bacterial/fungal infections.
Over-the-counter (OTC) drugs: No interaction with antipyretics (acetaminophen, ibuprofen), cough suppressants or cold preparations; can be safely used together.
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