Mast cell stabilizers: Uses, common brands, and safety info

Allergic conditions can be unpleasant or even unbearable for many people. Allergies commonly manifest as head symptoms such as red, itchy eyes, headaches, or a runny nose. Other times, allergic conditions can be more serious. For example, asthma and allergies are closely related, and asthma symptoms can be worsened by allergens. For people with a rare condition called mastocytosis, allergens can cause significant symptoms including life-threatening allergic reactions. 

Many types of allergic conditions can be treated with a class of drugs called mast cell stabilizers. In this article, we will list the different brand and generic names, provide information on their cost, outline how the drugs work, and cover their uses and safety considerations.

Other mast cell stabilizers

•  Opticrom (Cromolyn eye drops)

•  Crolom (Cromolyn eye drops)

•  Alamast (pemirolast)

What are mast cell stabilizers?

Mast cell stabilizers are anti-inflammatory drugs used to alleviate asthma and several allergic conditions. They come in various forms such as inhalers, oral solutions, and eye drops. Most drugs in this class are available by prescription only. Examples include cromolyn eye drops and oral solution (Opticrom, Crolom, and Gastrocrom), pemirolast eye drops (Alamast), nedocromil eye drops (Alocril), and lodoxamide eye drops (Alomide). However, there is one mast cell stabilizer that is available over-the-counter: Nasalcrom nasal solution. Mast cell stabilizers are typically combined with other allergy medications such as antihistamines. In fact, many over-the-counter (OTC) eye drops contain antihistamines that also double as mast cell stabilizers, such as ketotifen, olopatadine, azelastine, bepotastine, and alcaftadine.

How do mast cell stabilizers work?

Mast cells are immune cells located throughout the body’s connective tissues. Examples of areas where mast cells are abundant include under the skin, near blood vessels and lymph vessels, inside nerves, and throughout the lungs and intestines. They release histamine and other immune mediators in response to triggers such as allergens or other immune events. 

Histamine, cytokines, prostaglandin, and other molecules are stored in structures inside mast cells called granules. These granules can travel to the cell membrane and fuse with it, which allows the contents to exit the cell (called ‘mast cell degranulation’). When the contents of mast cells are released, it causes typical allergic symptoms such as inflammation, swelling, tightness in the chest, and increased mucus production. Mast cell stabilizers prevent the release of histamine and other contents from mast cells. A signal that triggers mast cells to release the contents of their granules is dependent upon calcium ions (Ca2+). Mast cell stabilizers block calcium channels on mast cells and thus prevent mast cells from responding to this signal.

What are mast cell stabilizers used for?

•  Mastocytosis

•  Allergic conjunctivitis

•  Asthma

•  Seasonal allergic rhinitis

•  Perennial allergic conjunctivitis

•  Vernal keratoconjunctivitis (VKC)

•  Food allergies (off-label)

•  Inflammatory bowel disease (off-label)

Who can take mast cell stabilizers?

Infants and children

Cromolyn inhalation is approved for children ages 2 years and older for the preventative management of bronchial asthma and prevention of exercise-induced bronchospasm, and the nasal spray form is approved in children 2 years and older for allergic rhinitis. Oral cromolyn (Gastrocrom) is FDA approved for mastocytosis in children two years and older. Using Gastrocrom in infants and children under two years old is considered off-label, although some clinical data suggests doses under 40 mg/kg/day is sage in children 6 months and older, and doses under 20 mg/kg/day are safe in children under 6 months.

Nedocromil inhalation is approved for children 12 years and older. However, it is sometimes used off-label in patients younger than 12 years, and multiple studies suggest that Nedocromil is safe and effective for asthma in children younger than 12 years old. Alocril (nedocromil eye drops) are FDA approved for seasonal allergic conjunctivitis in children 3 years and older. Alomide (lodoxamide eye drops) are FDA approved for vernal keratoconjunctivitis (VKC) in children 2 years and older. Alamast (pemirolast eye drops) are FDA approved for allergic conjunctivitis in children 3 years and older.

Adults

Mast cell stabilizers are generally considered safe and effective for use in adults. The most common side effects are minor and may include brief discomfort at the administration site (nasal spray and eye drops), blurry vision, headaches, rash, or gastrointestinal discomfort (oral solution). Some patients may experience less tolerable side effects. It is important to consult a healthcare provider about troublesome side effects so that treatment can be adjusted accordingly.

Can you take mast cell stabilizers while pregnant or breastfeeding?

Mast cell stabilizers are relatively safe to use while pregnant or breastfeeding. Always consult a healthcare provider about the risks versus benefits when using any medication during pregnancy or while breastfeeding. Cromolyn sodium has low systemic absorption from all administration routes (oral, nasal, ophthalmic, and inhaled). Cromolyn is a preferred therapy over inhaled corticosteroids for asthma during pregnancy and lactation. There is limited data on the safety of nedocromil during pregnancy, although animal studies suggest that it does not cause fetal harm. Very small amounts of nedocromil are absorbed into the bloodstream after administration to the eye, so it is unlikely that infants would be exposed to harmful amounts of nedocromil through breast milk. Alomide (lodoxamide) is also minimally absorbed after administration to the eye and would not be expected to cause significant exposure to the fetus during pregnancy or to an infant through breast milk. Alamast (pemirolast eye drops) pose a greater risk than the previous agents. It is labeled with a pregnancy category ‘C’ by the FDA. Animal studies using very high doses showed an increase in birth defects in rats. Alamast should only be used during pregnancy if the benefits outweigh the risks. It is not known whether Alamast is excreted in breast milk, so women who are breastfeeding should use Alamast eye drops cautiously.

Seniors

Mast cell stabilizers are a safe and effective option for seniors. No differences in safety or effectiveness have been observed between young and elderly adults using mast cell stabilizers. However, general drug safety considerations still apply. For example, mast cell stabilizers are cleared from the body through the kidneys and liver, and age-related deterioration of kidney and liver function often require doses to be decreased for older patients to avoid increased side effects. Furthermore, older patients are more likely to have comorbid conditions and a higher number of total medications that may interact with mast cell stabilizers or make side effects less tolerable. Dose selection for seniors should start at the low end of the dosing range.

Are mast cell stabilizers safe?

Mast cell stabilizers are a relatively safe class of medications. No drugs in this class carry a black box warning on the package labeling. A black box warning is an FDA-issued statement that draws attention to serious side effects of medication. Mast cell stabilizers have been on the market for decades and no serious side effects have been demonstrated with their use. With any drug, certain precautions must be taken for patients who have hypersensitivities to drug components, patients who may eliminate drugs slowly due to kidney or liver impairment, and women who are pregnant or breastfeeding.

Recalls

There have been no recent recalls of mast cell stabilizers.

Restrictions

Do not use a mast cell stabilizer drug if you have a hypersensitivity to the active ingredient or any other component of the product.

Mast cell stabilizers are eliminated from the body through the liver or kidneys. Alocril, Alomide, and Alamast are primarily eliminated through the kidneys. Alamast is broken down chemically by the liver before it is eliminated through the kidneys. Cromolyn is eliminated primarily through the liver. Patients who have poor liver or kidney function require decreases in dosages to avoid drug accumulation and worsened side effects. Currently, drug manufacturers have not defined amounts that doses should be decreased for patients with renal or hepatic impairment.

Are mast cell stabilizers controlled substances?

No, mast cell stabilizers are not controlled substances.

Common mast cell stabilizers side effects

The following are common side effects that may occur while taking mast cell stabilizers. This is not an exhaustive list. Additional adverse effects may be common to individual drugs within this class. If you are experiencing worrisome or intolerable side effects, consult a doctor or pharmacist for further information and advice.

Oral solution:

• Nausea

• Vomiting

• Diarrhea

• Abdominal pain

• Constipation

• Erythema

• Photosensitivity

• Urticaria

Nasal spray:

• Headaches

• Brief stinging or sneezing after use

Eye drops:

• Burning of the eye upon administration

• Eye dryness

• Eye puffiness

• Eye irritation

• Itchiness

• Rash

• Stye

• Blurred vision

How much do mast cell stabilizers cost?

The retail price for brand-name mast cell stabilizer eye drops ranges from around $40 to $300. Cromolyn eye drops (Opticrom, Crolom) are significantly less expensive than Alocril and Alomide eye drops, which are only available as brand-name drugs. A SingleCare coupon can lower the cost of a 10 mL bottle of Alomide to less than $180 and can also lower the price of Alocril to approximately $233.

Gastrocrom can cost more than $1,400 for a 480 mL bottle, but it is available generically (cromolyn oral solution) for less than $600. Thankfully, a SingleCare can lower the price even more to under $100 with a generic Gastrocrom coupon. 

Nasalcrom nasal spray is the least expensive mast cell stabilizer and is available over-the-counter for around $13. It can be purchased for as little as $6.43 with a SingleCare coupon.

Resources for mast cell stabilizers dosages:

• Alamast

• Alocril

• Alocril package insert

• Alomide

• Cromolyn ophthalmic

• Cromolyn sodium ophthalmic solution package insert

• Cromolyn Drug Summary

• Gastrocrom

• When to ‘prescribe’ an OTC allergy drop