Leukotriene modifiers: Uses, common brands, and safety info

If you have breathing problems due to a medical condition such as allergies, asthma, or chronic obstructive pulmonary disease (COPD), you may have heard of a type of drug called a leukotriene modifier. 

Leukotriene modifiers are also known as leukotriene receptor antagonists, or leukotriene antagonists. Leukotriene modifiers are a class of prescription drugs, and each drug in the class is approved by the U.S. Food and Drug Administration (FDA). Leukotriene receptor antagonists can be used to prevent breathing problems due to allergies, asthma, and COPD. Continue reading to learn more about leukotriene receptor antagonists.

What are leukotriene modifiers?

Leukotrienes are chemicals in the body. They are released after allergen exposure and can cause symptoms such as coughing, mucus, chest tightness, wheezing, difficulty breathing, and/or swelling of the airway. 

Leukotriene modifiers are medications that help improve breathing and asthma symptoms by blocking the effect of leukotrienes or by stopping your body from making leukotrienes. 

Leukotriene modifiers are often used as part of a treatment regimen that includes other medications, depending on the diagnosis. For example, an asthmatic patient may use other asthma medications such as a daily inhaler that is a combination of an inhaled corticosteroid and long-acting beta agonist, and a rescue inhaler as needed.

How do leukotriene modifiers work?

Leukotriene modifiers help relieve symptoms by decreasing leukotriene activity in the smooth muscles of the airway. They can do this in one of two ways, depending on what type of leukotriene modifier the drug is. 

Types of leukotriene modifiers

There are two types of leukotriene modifiers. 

Leukotriene receptor antagonists

Accolate (zafirlukast) and Singulair (montelukast) are leukotriene receptor antagonists. They work by binding to a receptor and blocking the effects of leukotriene.

Leukotriene synthesis inhibitor

Zyflo (zileuton) is a leukotriene synthesis inhibitor. It works by stopping an enzyme called 5-lipoxygenase from making leukotriene. It is also known as a 5-lipoxygenase inhibitor.

What are leukotriene modifiers used for?

All 3 leukotriene modifiers can be used for the prevention and chronic treatment of asthma in adults. They can also be used in pediatric patients, depending on their age.

• Accolate can be used in children 5 years and older.

• Singulair can be used in children 12 months and older.

• Zyflo can be used in children 12 years and older.

Additionally, Singulair is FDA approved for:

• Acute prevention of exercise-induced bronchoconstriction (EIB) in adults and children 6 years and older. Singulair is taken at least two hours before exercise. Patients who take Singulair for another indication, such as chronic asthma, should not take an additional dose to prevent EIB.

• Symptom relief of seasonal allergic rhinitis in adults and children 2 years and older when other medications do not work or cannot be tolerated.

• Symptom relief of perennial allergic rhinitis in adults and children 6 months and older when other medications do not work or cannot be tolerated.

Leukotriene modifiers do not treat acute asthma attacks or bronchospasm.

Who can take leukotriene modifiers?

Leukotriene modifiers are not appropriate for everyone. Before taking a leukotriene modifier, talk to your doctor about your medical history and conditions. Tell your doctor about all of the medications you take, including Rx and OTC drugs, and vitamins and supplements. This information will help the doctor ensure that a leukotriene modifier is prescribed safely and appropriately.

Men

Men can take a leukotriene modifier when appropriate for their medical condition(s), as long as the use is not contraindicated for any reason. 

Women

Women who are not pregnant or breastfeeding can take a leukotriene modifier when appropriate for their medical condition(s), as long as the use is not contraindicated for any reason.

Women who are pregnant or breastfeeding

Consult your doctor if you are pregnant, planning to become pregnant, or breastfeeding. 

There is limited human data on Accolate and Singulair in pregnancy. 

Zyflo should not be used in pregnancy. Based on animal data, Zyflo can harm the unborn baby. 

Children

Children, depending on age, can take a leukotriene modifier when appropriate for their medical condition(s), as long as the use is not contraindicated for any reason. 

• Accolate is approved for use in children 5 years and older.

• Singulair is approved for use in children 12 months and older for asthma, 6 years and older for EIB, 2 years and older for seasonal allergies, or 6 months and older for perennial allergies.

• Zyflo is approved for use in children 12 years and older.

Adults 65 years and older

• Singulair prescribing information warns that “greater sensitivity of some older individuals cannot be ruled out” although clinical trials showed similar safety and efficacy in older and younger adults. However, a dosage adjustment is not required in adults 65 years and older. 

• Accolate’s prescribing information states that older adults tend to clear the drug from the body slower. In some studies, adults aged 65 years and older had an increased frequency of infections compared to placebo (an inactive pill). However, the infections were not severe and did not require patients to stop taking Accolate. Another study showed that older adults had more adverse effects such as headache, diarrhea, nausea, and the common cold, although, in this study, they had fewer infections. 

• Zyflo’s prescribing information states that women over age 65 are at a higher risk for increased ALT levels (liver function tests). 

Are leukotriene modifiers safe?

Recalls

• Singulair recall (September 2018)

Restrictions

• Leukotriene modifiers are not safe for everyone. There are some cases where this type of drug should not be used. This includes people who are allergic to the individual drug or another leukotriene modifier. Also, a leukotriene modifier is not to be used to treat an acute asthma attack. 

• Accolate and Zyflo should not be used in people with liver problems.

There are also other precautions and warnings to note about leukotriene modifiers. Some of these precautions are:

• Leukotriene modifiers do not treat acute asthma attacks, including status asthmaticus. Always have rescue medication available (usually a short-acting beta agonist like albuterol). Although you can continue to take a leukotriene modifier during an acute asthma exacerbation, the leukotriene modifier does not treat the acute attack. 

• Accolate and Singulair can cause blood vessel inflammation. Notify your doctor immediately if you have numbness or tingling in your arms and legs, flulike symptoms, sinus pain, or a skin rash.

• Zyflo may cause liver problems. Call your doctor right away if you have nausea, stomach pain, itching, appetite loss, dark urine, clay-colored stools, or yellowing of the skin and whites of the eyes. Avoid alcohol while taking Zyflo.

Other Singulair warnings:

Singulair has a black box warning. This is the strongest warning required by the FDA. The warning states that serious neuropsychiatric events have been reported in people who take Singulair. Before taking Singulair, patients should discuss the benefits and risks with their doctor. While taking Singulair, patients should be closely monitored for symptoms. Symptoms may include:

• Abnormal dreams

• Agitation

• Aggressive behavior 

• Anxiety

• Depression

• Difficulty concentrating

• Disorientation 

• Hallucinations 

• Insomnia (trouble sleeping)

• Irritability 

• Memory problems

• Obsessive-compulsive symptoms

• Restlessness 

• Sleepwalking 

• Stuttering 

• Suicidal thoughts and behavior

• Tic 

• Tremor 

If any of these symptoms occur, stop taking Singulair and call your doctor right away or get emergency medical attention. 

Because each drug in the leukotriene modifier class is different, there are some other differences between the drugs. Before taking a leukotriene modifier, read the patient information leaflet and ask your doctor if you have any questions or concerns. 

Are leukotriene modifiers controlled substances?

No, leukotriene modifiers are not controlled substances.

Common leukotriene modifiers side effects

The most common side effects of leukotriene modifiers include:

• Headache

• Common cold symptoms

• Flulike symptoms such as fever

• Stomach problems: stomach pain, diarrhea, nausea, indigestion

• Cough 

• Ear infection 

• Rash/hives

• Sleep problems

• Anxiety/irritability 

• Restlessness  

• Tremor 

• Stomach virus (in children)

Allergic reactions are rare. If you experience symptoms of an allergic reaction, such as hives, difficulty breathing, or swelling of the face, lips, throat, or tongue, get emergency medical help right away. 

This is not a full list of side effects. Consult your healthcare provider for a full list of side effects. 

How much do leukotriene modifiers cost?

The price for a leukotriene modifier will vary based on the drug, quantity, and dose, as well as your insurance company benefits. Contact your insurance provider for the most up-to-date coverage information. All three leukotriene modifiers are available in generic form, making them less expensive than their brand-name counterparts. 

Singulair is inexpensive, while Accolate is more moderately priced, and Zyflo is the most expensive of the three drugs in the class. 

You can always use a free SingleCare card to save money on your prescriptions. Our customers find that they can save up to 80% on prescriptions. For example, the most common prescription for Singulair in adults is for generic montelukast, 30 tablets of 10 mg. With a SingleCare card, you can pay as little as about $8 for a one-month supply, or you can use our home delivery partner GeniusRx to have this prescription delivered to your door for about $6.