Singulair: Targeted Leukotriene Inhibition for Asthma & Allergy Control
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Synonyms
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Singulair (montelukast sodium) is a leukotriene receptor antagonist (LTRA) prescription medication indicated for the prophylactic and chronic treatment of asthma, the relief of symptoms of seasonal allergic rhinitis (hay fever), and the prevention of exercise-induced bronchoconstriction (EIB). It functions by selectively blocking the action of cysteinyl leukotrienes, potent inflammatory mediators involved in the underlying pathophysiology of allergic inflammation and bronchoconstriction. This targeted mechanism offers a non-steroidal approach to managing chronic inflammatory conditions of the airways.
Features
- Active Ingredient: Montelukast sodium.
- Drug Class: Selective and orally active leukotriene receptor antagonist.
- Available Formulations: Film-coated tablets (4mg, 5mg, 10mg), chewable tablets (4mg, 5mg), and oral granules (4mg packet).
- Dosing Regimen: Once-daily administration, typically in the evening.
- Mechanism of Action: Binds with high affinity and selectivity to the CysLT1 receptor, inhibiting the action of leukotrienes LTC4, LTD4, and LTE4.
Benefits
- Provides sustained, 24-hour control of underlying airway inflammation, reducing the frequency and severity of asthma exacerbations.
- Improves overall asthma control as measured by reduced daytime symptoms, less nocturnal awakening, and decreased need for rescue short-acting beta-agonists (SABAs).
- Offers effective relief from the nasal and ocular symptoms of seasonal allergic rhinitis, such as sneezing, rhinorrhea, nasal congestion, and itchy/watery eyes.
- Delivers prophylactic protection against exercise-induced bronchoconstriction when taken at least 2 hours prior to physical activity.
- Serves as a convenient add-on therapy for patients whose asthma is not adequately controlled on inhaled corticosteroids, potentially allowing for corticosteroid dose reduction.
- Presents an oral alternative for patients, particularly pediatric populations, who have difficulty with or are non-adherent to inhaled delivery systems.
Common use
Singulair is commonly prescribed for the chronic management of mild to moderate persistent asthma in adults and pediatric patients 12 months of age and older. It is used to prevent symptoms and improve overall control. It is also indicated for the relief of symptoms of seasonal allergic rhinitis in adults and children ages 2 years and older, and for the prevention of exercise-induced bronchoconstriction in patients 6 years of age and older. It is not indicated for the reversal of acute asthma attacks.
Dosage and direction
Dosage is based on the indication and the age of the patient. Administration is once daily, with or without food. For asthma and allergic rhinitis, the dose is typically taken in the evening. For exercise-induced bronchoconstriction, it should be taken at least 2 hours before exercise and not more than once in a 24-hour period.
- Asthma & Perennial Allergic Rhinitis (15 years and older): 10 mg tablet daily.
- Asthma & Perennial Allergic Rhinitis (6 to 14 years): 5 mg chewable tablet daily.
- Asthma (2 to 5 years): 4 mg chewable tablet or one 4 mg oral granule packet daily.
- Asthma (12 to 23 months): One 4 mg oral granule packet daily.
- Exercise-Induced Bronchoconstriction (6 years and older): One tablet (appropriate strength) at least 2 hours before exercise. The oral granules can be administered directly in the mouth, dissolved in 5mL of cold or room temperature baby formula or breast milk, or mixed with a spoonful of one of the following soft foods: applesauce, mashed carrots, rice, or ice cream. The entire dose must be administered within 15 minutes of preparation.
Precautions
Patients should be advised that Singulair is not a bronchodilator and should not be used to treat acute episodes of asthma. Acute asthma exacerbations require an inhaled short-acting beta-agonist. Patients should be instructed not to decrease the dose or stop taking any other anti-asthma medications unless instructed by a physician. Systemic eosinophilia, sometimes presenting with clinical features of vasculitis consistent with Churg-Strauss syndrome, has been reported rarely. This has been associated with the reduction of oral corticosteroid therapy. Healthcare providers should be alert to eosinophilia, vasculitic rash, worsening pulmonary symptoms, cardiac complications, and/or neuropathy in their patients. Patients with phenylketonuria (PKU) should be informed that the 4mg and 5mg chewable tablets contain aspartame, a source of phenylalanine.
Contraindications
Singulair is contraindicated in patients with known hypersensitivity to montelukast or any other component of the formulation. Hypersensitivity reactions have included anaphylaxis, angioedema, rash, and urticaria.
Possible side effect
The most common adverse reactions in clinical trials (incidence ≥1% and greater than placebo) included:
- Upper respiratory infection
- Fever
- Headache
- Pharyngitis
- Cough
- Nasal congestion
- Abdominal pain
- Diarrhea
- Influenza
- Rhinorrhea
- Sinusitis
- Otitis media Serious side effects, though rare, have been reported and include:
- Neuropsychiatric events (e.g., agitation, aggressive behavior, sleep disturbances, depression, suicidal thoughts and behavior)
- Severe allergic reactions (e.g., swelling of the face, lips, tongue, and/or throat, hives, itching, rash)
- Eosinophilic conditions
- Increased bleeding tendency
Drug interaction
Formal drug interaction studies have shown Singulair does not have clinically important effects on the pharmacokinetics of several drugs, including theophylline, prednisone, prednisolone, oral contraceptives, terfenadine, digoxin, and warfarin. However, phenobarbital, which induces hepatic metabolism, decreased the AUC of montelukast approximately 40%. The clinical relevance of this effect is not known. Caution is advised when co-prescribing with strong CYP450 enzyme inducers like rifampin.
Missed dose
Patients should be instructed to take the next dose at the regular time. They should not take a double dose to make up for the missed one.
Overdose
Experience in marketed use is limited. In chronic asthma studies, montelukast has been administered at doses up to 200 mg per day to patients for 22 weeks with no clinically important adverse experiences. In the event of an overdose, the patient should be treated supportively, and the symptoms should be managed. It is not known if montelukast is removed by peritoneal dialysis or hemodialysis.
Storage
Store at 20°C to 25°C (68°F to 77°F); excursions permitted between 15°C and 30°C (59°F and 86°F). Store in the original container and protect from moisture and light. Keep the bottle tightly closed. Discard any unused granules 6 months after opening the aluminum foil pouch.
Disclaimer
This information is for educational purposes only and is not a substitute for professional medical advice, diagnosis, or treatment. Always seek the advice of your physician or other qualified health provider with any questions you may have regarding a medical condition or medication. Never disregard professional medical advice or delay in seeking it because of something you have read here.
Reviews
“After struggling with nighttime coughing from mild persistent asthma, Singulair has been a game-changer. My sleep quality has improved dramatically, and my reliance on my albuterol inhaler has decreased significantly. It’s a simple, once-daily pill that fits easily into my routine.” - M.B., 42 “As a pediatrician, I find Singulair to be a valuable tool for managing asthma in young children who cannot effectively use inhalers. The granule formulation allows for easy administration. We’ve seen a notable reduction in exacerbations requiring oral steroids in our compliant patients.” - Dr. A. Evans, MD “I was prescribed Singulair for my seasonal allergies after antihistamines made me too drowsy. It effectively controls my sneezing and itchy eyes throughout the worst of the pollen season without any sedative effects.” - J.K., 31 “It is crucial for prescribers and parents to remain vigilant for any behavioral changes in children taking montelukast. While it is effective for many, we must balance the benefits with the potential, though rare, risk of neuropsychiatric events.” - Pediatric Pulmonologist