Medication: Montelukast | Medication Information and Guidelines |
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Recommended Dose and Dosage Regimen | The recommended dose of montelukast varies depending on the age of the patient and the condition being treated. For the treatment of asthma in adults and adolescents 15 years of age and older, the typical dose is 10 mg orally once daily in the evening. For children 6 to 14 years of age, the recommended dose is 5 mg orally once daily in the evening. For the prevention of exercise-induced bronchoconstriction, a single dose of 10 mg should be taken at least 2 hours before exercise. Montelukast should be taken regularly as prescribed, even when symptoms are controlled, to achieve optimal therapeutic benefit. Follow your healthcare provider’s instructions regarding dosing and administration. |
Frequency of Administration | Montelukast is typically administered orally once daily, preferably in the evening, with or without food. For the prevention of exercise-induced bronchoconstriction, a single dose should be taken at least 2 hours before engaging in physical activity. |
Route of Administration | Montelukast is available for oral administration as tablets, chewable tablets, and oral granules. The tablets and chewable tablets should be swallowed whole with a glass of water, while the oral granules can be administered directly into the mouth or mixed with a spoonful of soft food (e.g., applesauce, yogurt). |
Mechanism of Action (MOA) | Montelukast is a leukotriene receptor antagonist that selectively inhibits the actions of leukotriene D4 (LTD4) at the cysteinyl leukotriene receptor CysLT1 in the airways and other tissues. By blocking the binding of LTD4 to its receptor, montelukast prevents the bronchoconstrictor, proinflammatory, and edema-promoting effects mediated by leukotrienes in asthma and allergic rhinitis. Montelukast also inhibits the influx of inflammatory cells, eosinophils, and other leukocytes into the airways, and reduces mucus secretion and airway hyperresponsiveness. |
Pharmacokinetics (PK) | Montelukast is well absorbed after oral administration, with peak plasma concentrations achieved within 3-4 hours. Food does not significantly affect the extent of absorption but may delay the time to peak concentration. Montelukast undergoes extensive hepatic metabolism via cytochrome P450 enzymes, primarily CYP2C8 and CYP3A4, to form pharmacologically inactive metabolites. The elimination half-life of montelukast is approximately 2.7 to 5.5 hours in adults and longer in pediatric patients. The majority of the dose is excreted in the feces as metabolites, with minimal renal elimination. Dosage adjustments are not necessary based on renal function. |
Pharmacodynamics (PD) | Montelukast exerts its pharmacodynamic effects by selectively antagonizing the actions of leukotriene D4 (LTD4) at the cysteinyl leukotriene receptor CysLT1 in the airways and other tissues. By inhibiting the binding of LTD4 to its receptor, montelukast blocks the bronchoconstrictor, proinflammatory, and edema-promoting effects mediated by leukotrienes in asthma and allergic rhinitis. Montelukast also attenuates airway inflammation, mucus secretion, smooth muscle contraction, and airway hyperresponsiveness associated with asthma and allergic conditions. |
Pathophysiology | Montelukast is indicated for the prophylaxis and chronic treatment of asthma in adults and pediatric patients, and for the relief of symptoms of allergic rhinitis in adults and pediatric patients 2 years of age and older. Asthma is a chronic inflammatory disorder characterized by reversible airflow obstruction, airway hyperresponsiveness, and respiratory symptoms such as wheezing, dyspnea, coughing, and chest tightness. Allergic rhinitis is an inflammatory condition of the nasal mucosa triggered by exposure to allergens, leading to symptoms such as nasal congestion, sneezing, rhinorrhea, and itching. |
Primary Indications | Prophylaxis and chronic treatment of asthma in adults and pediatric patients, relief of symptoms of allergic rhinitis in adults and pediatric patients 2 years of age and older. |
Contraindications | Contraindications to montelukast use include hypersensitivity to montelukast or any component of the formulation. Montelukast should not be used to treat acute asthma attacks or status asthmaticus, and is not recommended for patients with severe hepatic impairment. Montelukast should be used with caution in patients with a history of psychiatric disorders or neuropsychiatric events, as well as in pediatric patients with a history of seizures. |
Purpose of Taking Medication | The purpose of montelukast therapy is to provide long-term control and management of asthma and allergic rhinitis by reducing airway inflammation, bronchoconstriction, and symptoms associated with these conditions. Montelukast is used as part of a comprehensive treatment regimen, including inhaled corticosteroids, bronchodilators, and other medications, to achieve and maintain asthma control and improve quality of life in affected patients. |
Usage Instructions | Take montelukast orally as directed by your healthcare provider, usually once daily in the evening with or without food. Swallow the tablets whole or chew the chewable tablets thoroughly before swallowing. For oral granules, administer the contents of the packet directly into the mouth and swallow without chewing, or mix with a spoonful of soft food (e.g., applesauce, yogurt) and consume immediately. Do not mix oral granules with any liquid other than baby formula or breast milk. |
Precautions and Care | Patients taking montelukast should be monitored for signs of neuropsychiatric events, including agitation, aggression, anxiety, depression, insomnia, irritability, suicidal ideation, and hallucinations. Discontinue montelukast and seek medical attention if neuropsychiatric symptoms occur or worsen during treatment. Use caution when driving or operating machinery until the effects of montelukast are known, as it may cause dizziness, drowsiness, or changes in mental alertness. |
Dietary Considerations | There are no specific dietary restrictions associated with montelukast use. Maintain a balanced diet and adequate hydration to support overall health and well-being. Avoid excessive consumption of alcohol or other substances that may exacerbate adverse effects or interact with montelukast. |
Missed Dose | If a dose of montelukast is missed, take it as soon as remembered, unless it is almost time for the next scheduled dose. Do not double the dose to make up for a missed one. Resume the regular dosing schedule and continue taking montelukast as prescribed by your healthcare provider. |
Possible Side Effects | Common side effects of montelukast may include headache, abdominal pain, nausea, diarrhea, upper respiratory infection, cough, and fever. Less common side effects may include dizziness, fatigue, rash, sleep disturbances, and behavioral changes. Rare but serious adverse effects may include neuropsychiatric events, allergic reactions, eosinophilia, and hepatotoxicity. Contact your healthcare provider if you experience severe or persistent side effects while taking montelukast. |
Storage and Disposal | Store montelukast tablets and chewable tablets at room temperature away from moisture, heat, and light. Keep the medication out of reach of children and pets. Unused or expired medication should be disposed of properly according to local regulations or guidelines for pharmaceutical waste disposal. Oral granules should be stored in the original foil packet at room temperature and used within 15 minutes of opening. |
Overdose or Emergency | In case of montelukast overdose or emergency, seek immediate medical attention or contact a poison control center. Overdose may lead to excessive systemic effects such as dizziness, drowsiness, headache, abdominal pain, and nausea. Treatment of montelukast overdose is supportive and symptomatic, with monitoring of vital signs and appropriate management of adverse effects as needed. |
Monitoring and Laboratory Tests | Patients receiving montelukast therapy require regular monitoring of clinical symptoms, treatment response, and adverse effects throughout the course of treatment. Monitor for signs of asthma exacerbations, allergic rhinitis symptoms, and neuropsychiatric events, particularly during the initiation of therapy or dosage adjustments. Additional monitoring may include pulmonary function tests, allergy testing, and laboratory assessments as clinically indicated. |
Important Note: Always consult with a healthcare professional for personalized medical advice and guidance regarding the use of montelukast, especially regarding dosing, administration, and potential side effects. Your healthcare provider can provide tailored recommendations based on your individual medical history, current medications, and specific treatment needs. Never self-adjust your montelukast regimen or discontinue treatment without first consulting your healthcare provider. If you have any questions or concerns about montelukast or its use, talk to your doctor or pharmacist for further information and assistance.