Montelukast 4mg Oral Granules
WARNING: For all uses of this drug:Severe mental health problems have happened with this drug or after it has been stopped. These problems include depression or suicidal thoughts or actions. These problems can happen in people with and without a history of mental or mood problems. Watch people who take this drug closely. Call the doctor right away if any changes in mood or behavior that are new or worse occur. This includes signs like depression; thoughts or actions of suicide; not able to focus; bad or strange dreams; anxiety; hallucinations (seeing or hearing things that are not there); memory problems; sleep walking; stuttering; shakiness; trouble sleeping; trouble controlling body movements; or feeling agitated, confused, irritable, or restless. Talk with the doctor to be sure that the benefits of this drug are more than the risks.For allergic reasons:This drug must only be used when other drugs cannot be used or have not worked. If you have questions, talk with the doctor. @ COMMON USES: It is used to prevent breathing problems that happen with exercise.It is used to treat or prevent asthma.It is used to ease allergy signs.It may be given to you for other reasons. Talk with the doctor.For breathing problems:Do not use this drug to treat intense flare-ups of shortness of breath. Use a rescue inhaler. If you have questions, talk with the doctor.
Drug Class
Antiasthmatic, Antiallergic
Pharmacologic Class
Leukotriene Receptor Antagonist (LTRA)
Pregnancy Category
B
FDA Approved
Feb 1998
DEA Schedule
Not Controlled
Overview
What is this medicine?
Montelukast is a medicine that helps prevent and treat asthma symptoms like wheezing and shortness of breath, and also helps with allergy symptoms like sneezing and runny nose. It works by blocking natural substances in your body called leukotrienes, which can cause inflammation and tightening of airways.
How to Use This Medicine
Taking Your Medication Correctly
To ensure you get the most benefit from your medication, follow these steps:
Take your medication exactly as directed by your doctor and read all the information provided.
You can take your medication with or without food.
If you are taking the granule form, you can place it directly in your mouth or mix it with cold or room temperature applesauce, baby formula, breast milk, mashed carrots, rice, or ice cream. However, do not mix the granules with any other liquids.
Only open the packet when you are ready to take a dose, and take it within 15 minutes of opening. Do not store opened packets for future use.
Continuing Your Medication Regimen
Continue taking your medication even when you are not experiencing symptoms.
If you are taking this medication to prevent breathing problems that occur with exercise, take it at least 2 hours before exercising.
If you are taking this medication for asthma, take it in the evening as directed.
Storing and Disposing of Your Medication
Store your medication at room temperature, protected from light and moisture.
Keep it in a dry place, away from the bathroom, and store it in its original container.
Missing a Dose
If you miss a dose, skip it and return to your regular dosing schedule.
* Do not take two doses at the same time or take extra doses to make up for a missed dose.
To ensure you get the most benefit from your medication, follow these steps:
Take your medication exactly as directed by your doctor and read all the information provided.
You can take your medication with or without food.
If you are taking the granule form, you can place it directly in your mouth or mix it with cold or room temperature applesauce, baby formula, breast milk, mashed carrots, rice, or ice cream. However, do not mix the granules with any other liquids.
Only open the packet when you are ready to take a dose, and take it within 15 minutes of opening. Do not store opened packets for future use.
Continuing Your Medication Regimen
Continue taking your medication even when you are not experiencing symptoms.
If you are taking this medication to prevent breathing problems that occur with exercise, take it at least 2 hours before exercising.
If you are taking this medication for asthma, take it in the evening as directed.
Storing and Disposing of Your Medication
Store your medication at room temperature, protected from light and moisture.
Keep it in a dry place, away from the bathroom, and store it in its original container.
Missing a Dose
If you miss a dose, skip it and return to your regular dosing schedule.
* Do not take two doses at the same time or take extra doses to make up for a missed dose.
Lifestyle & Tips
- Take montelukast once daily in the evening, even if you feel well. It is a preventive medicine, not a rescue medicine for sudden asthma attacks.
- Do not stop taking other asthma medications unless directed by your doctor.
- For oral granules: Administer directly into the mouth, or mix with a spoonful of soft food (e.g., applesauce, carrots, rice, ice cream) or in 5 mL of breast milk or formula. Consume within 15 minutes of opening the packet. Do NOT mix with other liquids besides breast milk or formula.
- Keep all doctor appointments and follow-up visits to monitor your condition and medication effectiveness.
- Avoid known asthma and allergy triggers (e.g., pollen, dust mites, pet dander, smoke).
Available Forms & Alternatives
Dosing & Administration
Adult Dosing
Standard Dose:
Not indicated for 4mg oral granules. Adult dose for asthma/allergies is typically 10mg once daily.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established for infants under 6 months. For 6-23 months (asthma/perennial allergic rhinitis): 4mg oral granules once daily in the evening.
Child:
For 2-5 years (asthma/allergic rhinitis): 4mg oral granules once daily in the evening. For 6-14 years (asthma/allergic rhinitis): 5mg chewable tablet once daily in the evening.
Adolescent:
Not indicated for 4mg oral granules. Adolescent dose (15 years and older) for asthma/allergies is typically 10mg once daily.
Dose Adjustments
Renal Impairment:
Mild:
No adjustment needed
Moderate:
No adjustment needed
Severe:
No adjustment needed
Dialysis:
No adjustment needed; Montelukast is highly protein-bound and not significantly removed by dialysis.
Hepatic Impairment:
Mild:
No adjustment needed
Moderate:
No adjustment needed
Severe:
Use with caution; specific recommendations not available. Montelukast is extensively metabolized by the liver.
Pharmacology
Mechanism of Action
Montelukast is a selective and orally active leukotriene receptor antagonist that specifically inhibits the cysteinyl leukotriene CysLT1 receptor. Cysteinyl leukotrienes (LTC4, LTD4, LTE4) are potent inflammatory eicosanoids released from various cells, including mast cells and eosinophils. These leukotrienes bind to CysLT1 receptors in the airways and on other pro-inflammatory cells, causing bronchoconstriction, mucus secretion, vascular permeability, and eosinophil recruitment. By blocking the CysLT1 receptor, montelukast inhibits these actions, leading to bronchodilation and reduction of inflammatory processes associated with asthma and allergic rhinitis.
Pharmacokinetics
Absorption:
Bioavailability:
64% (10mg tablet, oral)
Tmax:
2-4 hours (oral granules in children)
FoodEffect:
Food does not significantly affect the bioavailability of montelukast oral granules when administered with a meal. However, for optimal absorption, it is often recommended to administer granules directly into the mouth or mixed with a spoonful of soft food (e.g., applesauce, carrots, rice, ice cream) or in 5 mL of breast milk or formula, and consumed within 15 minutes.
Distribution:
Vd:
8-11 liters
ProteinBinding:
Greater than 99%
CnssPenetration:
Limited
Elimination:
HalfLife:
2.7-5.5 hours (adults)
Clearance:
Not available
ExcretionRoute:
Primarily bile/feces (approximately 86%), less than 0.2% in urine
Unchanged:
Less than 0.2% (in urine)
Pharmacodynamics
OnsetOfAction:
Within 1 day (for clinical improvement in asthma symptoms)
PeakEffect:
Not directly applicable as it's a prophylactic medication; sustained effect with daily dosing.
DurationOfAction:
24 hours (allows for once-daily dosing)
Safety & Warnings
BLACK BOX WARNING
Serious neuropsychiatric events have been reported with the use of montelukast. These include, but are not limited to, agitation, aggression, depression, sleep disturbances, tremor, suicidal thoughts and behavior. Because of the risk of neuropsychiatric events, montelukast should be used for allergic rhinitis only when other therapies have not been effective or are not tolerated. For asthma, montelukast should be used only when other therapies have not been effective or are not tolerated, or as an add-on therapy for patients whose asthma is not adequately controlled on other medications.
Side Effects
Urgent Side Effects: Seek Medical Attention Immediately
Although rare, some individuals may experience severe and potentially life-threatening side effects while taking this medication. If you exhibit any of the following symptoms, contact your doctor or seek medical help right away:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin (with or without fever)
+ Wheezing
+ Tightness in the chest or throat
+ Difficulty breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Signs of a severe skin reaction (Stevens-Johnson syndrome/toxic epidermal necrolysis), including:
+ Red, swollen, blistered, or peeling skin (with or without fever)
+ Red or irritated eyes
+ Sores in the mouth, throat, nose, or eyes
New or worsening trouble breathing
Fever
Flu-like symptoms
Sinus pain
Abnormal burning, numbness, or tingling sensations
Ear pain
Other Possible Side Effects
As with all medications, side effects can occur. Many people may not experience any side effects or may only have mild ones. If you are bothered by any of the following side effects or if they do not go away, contact your doctor or seek medical help:
Headache
Stomach pain or diarrhea
Signs of a common cold
Cough
This is not an exhaustive list of all possible side effects. If you have questions or concerns about side effects, consult your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Although rare, some individuals may experience severe and potentially life-threatening side effects while taking this medication. If you exhibit any of the following symptoms, contact your doctor or seek medical help right away:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin (with or without fever)
+ Wheezing
+ Tightness in the chest or throat
+ Difficulty breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Signs of a severe skin reaction (Stevens-Johnson syndrome/toxic epidermal necrolysis), including:
+ Red, swollen, blistered, or peeling skin (with or without fever)
+ Red or irritated eyes
+ Sores in the mouth, throat, nose, or eyes
New or worsening trouble breathing
Fever
Flu-like symptoms
Sinus pain
Abnormal burning, numbness, or tingling sensations
Ear pain
Other Possible Side Effects
As with all medications, side effects can occur. Many people may not experience any side effects or may only have mild ones. If you are bothered by any of the following side effects or if they do not go away, contact your doctor or seek medical help:
Headache
Stomach pain or diarrhea
Signs of a common cold
Cough
This is not an exhaustive list of all possible side effects. If you have questions or concerns about side effects, consult your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Seek Immediate Medical Attention If You Experience:
- Worsening asthma or allergy symptoms
- Signs of an allergic reaction (e.g., rash, hives, swelling of face/lips/tongue, difficulty breathing)
- New or worsening mood changes (e.g., feeling sad, anxious, irritable)
- Behavioral changes (e.g., agitation, aggression, restlessness)
- Sleep problems (e.g., nightmares, trouble sleeping)
- Thoughts of harming yourself or others
- Tremor or shaking
- Hallucinations (seeing or hearing things that are not there)
- Numbness or tingling in arms or legs
- Swelling of the face, lips, tongue, and/or throat (angioedema)
Before Using This Medicine
Before Taking This Medication: Important Information to Share with Your Doctor
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the allergic reaction you experienced, including any symptoms that occurred.
All medications you are currently taking, including prescription and over-the-counter (OTC) drugs, natural products, and vitamins. This information will help your doctor and pharmacist identify potential interactions between this medication and other substances you are taking.
* Any existing health problems, as this medication may interact with certain conditions or exacerbate underlying health issues.
To ensure your safety, it is crucial to verify that it is safe to take this medication with all your current medications and health conditions. Never start, stop, or adjust the dose of any medication without first consulting your doctor.
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the allergic reaction you experienced, including any symptoms that occurred.
All medications you are currently taking, including prescription and over-the-counter (OTC) drugs, natural products, and vitamins. This information will help your doctor and pharmacist identify potential interactions between this medication and other substances you are taking.
* Any existing health problems, as this medication may interact with certain conditions or exacerbate underlying health issues.
To ensure your safety, it is crucial to verify that it is safe to take this medication with all your current medications and health conditions. Never start, stop, or adjust the dose of any medication without first consulting your doctor.
Precautions & Cautions
Important Information to Share with Your Healthcare Team
It is crucial that you inform all of your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication. This will help ensure that you receive the best possible care.
Pregnancy and Breastfeeding
If you are pregnant, planning to become pregnant, or are breastfeeding, you must discuss the benefits and risks of this medication with your doctor. This will help you and your doctor make an informed decision about your treatment.
Managing Breathing Problems
If you are taking this medication for breathing problems, it is essential to monitor your condition closely. Contact your doctor immediately if:
Your breathing problems worsen
Your rescue inhaler is not effective
* You need to use your rescue inhaler more frequently than usual
Special Considerations for Asthma and Allergy Sufferers
If you are taking this medication for asthma or allergies, do not take an additional dose to prevent exercise-induced breathing problems.
Interactions with Other Medications
If you have asthma and experience worsening symptoms when taking aspirin, you should avoid taking aspirin and other nonsteroidal anti-inflammatory drugs (NSAIDs), such as ibuprofen and naproxen, while taking this medication.
Switching from a Steroid Medication
If you are switching to this medication from a steroid, do not stop taking the steroid suddenly. Instead, your doctor may need to gradually reduce the steroid dose to minimize the risk of side effects. Be sure to discuss this with your doctor to ensure a safe transition.
It is crucial that you inform all of your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication. This will help ensure that you receive the best possible care.
Pregnancy and Breastfeeding
If you are pregnant, planning to become pregnant, or are breastfeeding, you must discuss the benefits and risks of this medication with your doctor. This will help you and your doctor make an informed decision about your treatment.
Managing Breathing Problems
If you are taking this medication for breathing problems, it is essential to monitor your condition closely. Contact your doctor immediately if:
Your breathing problems worsen
Your rescue inhaler is not effective
* You need to use your rescue inhaler more frequently than usual
Special Considerations for Asthma and Allergy Sufferers
If you are taking this medication for asthma or allergies, do not take an additional dose to prevent exercise-induced breathing problems.
Interactions with Other Medications
If you have asthma and experience worsening symptoms when taking aspirin, you should avoid taking aspirin and other nonsteroidal anti-inflammatory drugs (NSAIDs), such as ibuprofen and naproxen, while taking this medication.
Switching from a Steroid Medication
If you are switching to this medication from a steroid, do not stop taking the steroid suddenly. Instead, your doctor may need to gradually reduce the steroid dose to minimize the risk of side effects. Be sure to discuss this with your doctor to ensure a safe transition.
Overdose Information
Overdose Symptoms:
- Abdominal pain
- Sleepiness
- Thirst
- Headache
- Vomiting
- Hyperactivity
What to Do:
Seek immediate medical attention or call 911. Contact a poison control center at 1-800-222-1222. Treatment is symptomatic and supportive. There is no specific antidote.
Drug Interactions
Moderate Interactions
- Phenobarbital
- Rifampin
- Phenytoin
Monitoring
Baseline Monitoring
Asthma/Allergy symptom severity
Rationale: To establish baseline disease control and assess treatment efficacy.
Timing: Prior to initiation of therapy
Neuropsychiatric history (e.g., depression, anxiety, behavioral changes)
Rationale: Montelukast has been associated with neuropsychiatric events. Baseline assessment helps identify risk factors and monitor for new or worsening symptoms.
Timing: Prior to initiation of therapy
Routine Monitoring
Asthma/Allergy symptom control
Frequency: Regularly (e.g., monthly initially, then every 3-6 months or as clinically indicated)
Target: Improved symptom control, reduced need for rescue medication, improved quality of life
Action Threshold: Worsening symptoms, increased rescue inhaler use, or lack of expected improvement
Neuropsychiatric symptoms (e.g., agitation, aggression, depression, sleep disturbances, suicidal thoughts)
Frequency: Ongoing, at each clinical visit and through caregiver report
Target: Absence of new or worsening symptoms
Action Threshold: Any new or worsening neuropsychiatric symptoms; consider discontinuation and alternative therapy.
Symptom Monitoring
- Worsening asthma symptoms (e.g., increased wheezing, shortness of breath, cough)
- Increased use of rescue inhaler
- Signs of allergic reaction (e.g., rash, hives, swelling, difficulty breathing)
- Behavioral changes (e.g., agitation, aggression, irritability)
- Mood changes (e.g., depression, anxiety)
- Sleep disturbances (e.g., nightmares, insomnia)
- Suicidal thoughts or behavior
- Tremor
- Hallucinations
Special Patient Groups
Pregnancy
Montelukast is Pregnancy Category B. Studies in animals have not shown harm to the fetus, but there are no adequate and well-controlled studies in pregnant women. Use during pregnancy only if clearly needed and the potential benefit outweighs the potential risk to the fetus.
Trimester-Specific Risks:
First Trimester:
No increased risk of major birth defects observed in human studies, but data are limited.
Second Trimester:
No specific risks identified.
Third Trimester:
No specific risks identified.
Lactation
Montelukast is excreted into human milk. The amount is very low, and adverse effects in breastfed infants are not expected. However, monitor the infant for potential adverse effects (e.g., irritability, sleep disturbances). The developmental and health benefits of breastfeeding should be considered along with the mother's clinical need for montelukast and any potential adverse effects on the breastfed infant from montelukast or from the underlying maternal condition.
Infant Risk:
L3 (Moderately Safe - Limited controlled studies show no increase in adverse effects for the infant. Risk of adverse effects is possible but unlikely.)
Pediatric Use
Montelukast 4mg oral granules are specifically indicated for pediatric patients aged 6 months to 5 years for asthma and perennial allergic rhinitis, and for patients aged 2 to 5 years for seasonal allergic rhinitis. Safety and efficacy in infants younger than 6 months have not been established. Close monitoring for neuropsychiatric events is crucial in all pediatric patients.
Geriatric Use
Clinical studies of montelukast did not include sufficient numbers of subjects aged 65 and over to determine whether they respond differently from younger subjects. However, no overall differences in safety or effectiveness were observed between elderly and younger subjects. Dosage adjustment is generally not required based on age alone.
Clinical Information
Clinical Pearls
- Montelukast is a once-daily medication, typically taken in the evening for asthma and allergic rhinitis.
- It is a controller medication, not a rescue inhaler for acute asthma attacks.
- Counsel patients and caregivers about the potential for neuropsychiatric side effects, including mood changes, behavioral disturbances, and suicidal thoughts. Advise them to report any such symptoms immediately.
- Oral granules can be given directly in the mouth or mixed with a small amount of soft food or breast milk/formula and must be consumed within 15 minutes.
- Montelukast can be used in conjunction with inhaled corticosteroids and other asthma therapies.
- Consider discontinuing montelukast if neuropsychiatric symptoms develop and persist, and explore alternative therapies.
Alternative Therapies
- Inhaled corticosteroids (e.g., fluticasone, budesonide)
- Long-acting beta-agonists (LABAs) (often in combination with ICS)
- Short-acting beta-agonists (SABAs) (for rescue)
- Cromolyn sodium (mast cell stabilizer)
- Omalizumab (anti-IgE monoclonal antibody, for severe allergic asthma)
- Mepolizumab, Reslizumab, Benralizumab (anti-IL-5 monoclonal antibodies, for severe eosinophilic asthma)
- Oral antihistamines (for allergic rhinitis)
- Nasal corticosteroids (for allergic rhinitis)
Cost & Coverage
Average Cost:
Varies widely, typically $30-$100+ per 30 packets
Generic Available:
Yes
Insurance Coverage:
Tier 1 or 2 (generic), Tier 3 or 4 (brand)
General Drug Facts
If your symptoms or health issues persist or worsen, it's essential to contact your doctor for further guidance. To ensure your safety, never share your medication with others or take someone else's medication.
This medication is accompanied by a Medication Guide, which provides crucial information about its use. Please read this guide carefully and review it again whenever you receive a refill. If you have any questions or concerns about this medication, don't hesitate to discuss them with your doctor, pharmacist, or other healthcare provider.
In the event of a suspected overdose, immediately call your local poison control center or seek emergency medical attention. Be prepared to provide detailed information about the overdose, including the medication taken, the quantity, and the time it occurred.
This medication is accompanied by a Medication Guide, which provides crucial information about its use. Please read this guide carefully and review it again whenever you receive a refill. If you have any questions or concerns about this medication, don't hesitate to discuss them with your doctor, pharmacist, or other healthcare provider.
In the event of a suspected overdose, immediately call your local poison control center or seek emergency medical attention. Be prepared to provide detailed information about the overdose, including the medication taken, the quantity, and the time it occurred.