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Top 3 Leukotriene Modifiers for Asthma and Nasal Allergies

Written by Andrew Le, MD

UpdatedMarch 12, 2024

Leukotriene modifiers, available in the late '90s, transformed global asthma treatment. Researchers in the late '70s and early '80s understood leukotriene structures and their role in asthma inflammation. These meds have proven effective since then.

Given their success in asthma, researchers hypothesized similar potential benefits in allergic rhinitis treatment, supported by recoverable leukotrienes in bronchoalveolar and nasal lavage fluids.

This article explores the Leukotriene Modifiers, examining their role in allergy and asthma management. It outlines administration guidelines, explores potential side effects, and highlights the top 3 modifiers for asthma and nasal allergies.

What Are Leukotriene Modifiers?

Leukotriene modifiers, categorized as leukotriene receptor antagonists, make up a medication class integral to the management of conditions such as:

Among the prominent members of this class are montelukast (Singulair), zafirlukast (Accolate), and zileuton (Zyflo). These medications play a pivotal role in modulating the inflammatory response triggered by leukotrienes, which are chemical compounds released by the body in response to exposure to allergens.

By targeting leukotrienes, these drugs aim to alleviate symptoms associated with allergic reactions, offering relief to individuals grappling with respiratory and nasal symptoms.

Role in Allergy Management

Leukotriene modifiers exert their therapeutic effects by interfering with the activity of leukotrienes, which are pivotal contributors to the inflammatory cascade responsible for symptoms like:

  • Nasal congestion
  • Sneezing
  • Itching associated with allergies

The process begins when the body encounters allergens, prompting the release of leukotrienes. These compounds, in turn, induce the characteristic symptoms of allergies.

Leukotriene modifiers disrupt this chain of events by blocking the action of leukotrienes, providing a targeted approach to managing allergic responses.

Role In Asthma Management

While not intended to relieve acute asthma attacks immediately, leukotriene modifiers are crucial in preventing and managing asthma symptoms. Leukotrienes contribute significantly to airway narrowing, a hallmark feature of asthma exacerbations.

By inhibiting the production or activity of leukotrienes, these medications aid in maintaining open airways, facilitating smoother breathing.

🩺 Doctor’s Note

It's important to emphasize that leukotriene modifiers are typically used in a comprehensive asthma management strategy and should not be relied upon as standalone treatments for acute attacks.

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Administration and Dosage Guidelines

Leukotriene modifiers, such as Montelukast, are prescribed to address allergy symptoms and assist with asthma management.

For individuals aged 2 and above, the recommended dosage varies. Children between the ages of 2 and 5 typically take one 4 mg chewable tablet daily. Those aged 6 to 14 are advised to take one 5 mg tablet per day, while individuals aged 15 and older are prescribed a daily 10 mg tablet.

Additionally, Montelukast is used for preventing exercise-induced asthma, with a dosage of 5 mg for ages 6 to 14 and 10 mg for those 15 and older, taken two hours before physical activity. To relieve allergic rhinitis symptoms, the dosage ranges from one 4 mg chewable tablet daily for ages 2 to 5 to one 10 mg tablet for individuals aged 15 and older.

Zafirlukast, marketed as Accolate, is another leukotriene modifier used to prevent and treat asthma in individuals aged 5 and above. The recommended dosage involves a 10 mg tablet twice daily for children aged 5 to 11, while those aged 12 and older should take a 20 mg tablet twice daily.

Zileuton, available as Zyflo CR, is a leukotriene modifier used to prevent and treat asthma for individuals aged 12 and older. The standard dosage involves two 600 mg tablets twice daily within one hour of meals.

🩺 Doctor’s Note

Dosages serve as general guidelines, and individuals should adhere to the specific instructions provided by their healthcare providers and outlined in the medication's prescribing information. Adjustments may be necessary based on individual health conditions and responses to the treatment.

Potential Side Effects

As with any medication, leukotriene modifiers come with potential side effects that individuals should be aware of. Common side effects may include:

Notably, montelukast, in particular, has been associated with severe mental health side effects, including thoughts of suicide. Individuals must be vigilant for any concerning symptoms and promptly report them to their healthcare providers.

This underscores the importance of regular monitoring and open communication between patients and healthcare professionals to ensure the timely identification and management of potential side effects.

Top 3 Leukotriene Modifiers for Asthma and Nasal Allergies

We understand the importance of addressing asthma and nasal allergies and recognizing the challenges of finding the right solution. To simplify this process, we've conducted thorough research about the Leukotriene Modifiers that effectively manage symptoms associated with asthma and nasal allergies.

Whether you seek a solution to initiate symptom control or maintain long-term relief, our carefully curated list of the top 3 Leukotriene Modifiers should help guide you.

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Zafirlukast is a leukotriene receptor antagonist prescribed to control and prevent symptoms such as wheezing and shortness of breath caused by asthma.

Accolate, the brand name for Zafirlukast, is available in oral tablet form. The cost for 60 tablets of the 10 mg strength is approximately $249, making it a moderately priced option for individuals seeking effective asthma management.


  • Effectively controls asthma symptoms by blocking leukotrienes.
  • Can be taken without regard to meals, enhancing convenience.
  • Suitable for long-term use, providing consistent symptom relief.


  • Requires regular, ongoing use, even during symptom-free periods.
  • Possible side effects include cold symptoms, diarrhea, and fatigue.
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Montelukast is another member of the leukotriene modifiers class, prescribed to control and prevent symptoms associated with asthma, including wheezing and shortness of breath. Additionally, it is effective in managing hay fever and allergic rhinitis.

Singulair, the brand name for Montelukast, is available in various forms, including oral and chewable tablets. The cost for 30 tablets of the 10 mg strength is approximately $286, positioning it as a moderately priced option.


  • Is indicated for asthma and allergy management.
  • Offers flexibility in dosing times, making it adaptable to individual schedules.
  • Can be used prophylactically before exercise to prevent asthma symptoms


  • May cause side effects such as headache, heartburn, and fatigue.
  • Requires consistent daily use for optimal effectiveness.
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Zileuton is a leukotriene modifier that controls and prevents asthma symptoms, including wheezing and shortness of breath. It is available in an extended-release tablet form, Zyflo CR, designed for twice-daily dosing.

Zyflo CR, the brand name for Zileuton, is available in 600 mg extended-release tablets. The cost for 120 tablets is approximately $3,968, positioning it as a higher-cost option compared to some alternatives.


  • Controls and prevents asthma symptoms through the inhibition of leukotriene synthesis.
  • Extended-release formulation allows for twice-daily dosing, promoting consistent coverage.
  • Suitable for long-term use, providing sustained symptom relief.


  • Not recommended for children under 12 due to potential liver problems.
  • Higher cost compared to some alternatives.

Wrap Up

The top Leukotriene Modifiers for managing asthma and allergies are montelukast (Singulair), zafirlukast (Accolate), and zileuton (Zyflo CR).

Montelukast and zafirlukast are more affordable options for controlling symptoms through leukotriene inhibition. Zileuton provides sustained relief with twice-daily dosing but at a higher cost.

These medications can effectively treat wheezing, congestion, and other allergy symptoms by blocking leukotrienes, key inflammatory mediators. Individuals should discuss these options with their doctor to determine if a Leukotriene Modifier is appropriate for their needs.

FAQs on Leukotriene Modifiers

What are leukotriene drugs for asthma?

Leukotriene drugs, such as montelukast and zafirlukast, are cysteinyl leukotriene receptor antagonists used to prevent and treat chronic asthma. They work by inhibiting the action of leukotrienes, eicosanoid inflammatory mediators derived from arachidonic acid. It's important to note that neither montelukast nor zafirlukast is suitable as a rescue medication during an acute asthmatic attack.

What is the function of leukotrienes?

Leukotrienes (LTs) are lipid mediators crucial in acute and chronic inflammation and allergic diseases. They exert their effects by binding to specific G-protein-coupled receptors.

Is Montelukast safe for asthma?

While considered generally safe, montelukast raises concerns about adverse drug reactions, including the rare incidence of Churg-Strauss syndrome. Additionally, despite limited data, there is a potential risk of neuropsychiatric events such as anxiety, depression, sleep disturbance, and suicidality.

Is Montelukast an asthma reliever?

Montelukast helps prevent airway narrowing caused by inflammation. It makes breathing easier and reduces the likelihood of asthma attacks. It's typically taken once a day in the evening, even when symptoms are absent. It is not used as a rescue medication for asthma exacerbation.

Why do you take montelukast at night?

Montelukast has a short half-life and peaks in the bloodstream 3-4 hours after a dose. It is advisable to take it at night to align peak drug levels,with the onset of symptoms, as recommended by healthcare providers and prescribing information.

How are leukotriene modifiers used in the treatment of asthma?

Leukotriene modifiers are used in combination with other asthma medications to improve long-term baseline lung function and decrease bronchial hyperresponsiveness that occurs in asthma.

Illustration of a healthcare provider asking questions on a smart phone.
Allergy treatment - Online visit
Get virtual care from a licensed clinician—no appointment needed
Illustration of a healthcare provider asking questions on a smart phone.
  • $29 one-time assessment
  • No video call or appointment necessary
  • Personalized treatment plan prescribed for your condition