Mast Cell Stabilizer – Effects and Uses
Mast cell stabilizers are substances that prevent the release of inflammatory mediators from mast cells, thereby reducing allergic reactions.
Things worth knowing about "Mast Cell Stabilizer"
Mast cell stabilizers are substances that prevent the release of inflammatory mediators from mast cells, thereby reducing allergic reactions.
What Is a Mast Cell Stabilizer?
A mast cell stabilizer is a type of medication that prevents the activation of mast cells -- specialized immune cells found throughout the body, particularly in the skin, airways, and gastrointestinal tract. When exposed to an allergen, mast cells can become activated and release inflammatory substances such as histamine, leukotrienes, and prostaglandins. These mediators trigger the classic symptoms of an allergic reaction, including itching, swelling, runny nose, and difficulty breathing. Mast cell stabilizers block this release, acting as a preventive measure against allergic responses.
Mechanism of Action
Mast cell stabilizers work by inhibiting the process of degranulation -- the opening of storage vesicles (granules) inside mast cells that contain inflammatory mediators. While the precise molecular mechanism is not fully understood, it is believed that these agents inhibit the influx of calcium ions into the mast cell, which is required to trigger degranulation. By blocking this calcium entry, the granules remain intact and the release of inflammatory substances is prevented.
Indications and Uses
Mast cell stabilizers are primarily used for the prophylaxis (prevention) of allergic and inflammatory conditions. They do not provide immediate relief from an ongoing allergic reaction but must be used regularly to build up their protective effect. Common indications include:
- Allergic conjunctivitis (allergic inflammation of the eye): Eye drops containing cromoglicate
- Allergic rhinitis (hay fever): Nasal sprays for preventive use
- Allergic asthma: Inhaled formulations for attack prevention
- Mastocytosis: A condition involving an abnormal accumulation of mast cells in the body
- Food allergies and irritable bowel syndrome: Oral formulations (e.g., oral cromoglicate)
Key Active Substances
The most commonly used mast cell stabilizers include:
- Cromoglicic acid (sodium cromoglicate): The most widely used agent in this class. Available as eye drops, nasal spray, inhalation solution, and oral capsules.
- Nedocromil: Similar to cromoglicate, primarily used as an inhaler and eye drops.
- Ketotifen: Acts as both a mast cell stabilizer and an antihistamine; available as eye drops and oral tablets.
- Lodoxamide: Used as eye drops for the treatment of allergic conjunctivitis.
Dosage and Application
The appropriate dosage of a mast cell stabilizer depends on the specific substance, its formulation, and the condition being treated. It is important that these medications are used consistently and regularly, as they do not produce an immediate effect. Full protective benefit may take several days to weeks of regular use to develop. Eye drops are typically applied several times daily. For seasonal allergies, treatment should ideally begin a few weeks before the expected allergen exposure, such as before pollen season starts.
Side Effects
Mast cell stabilizers are generally very well tolerated because they are minimally absorbed into the bloodstream (low systemic bioavailability). Possible local side effects include:
- Burning or stinging sensation after applying eye drops
- Temporary cough with inhaled formulations
- Mild irritation of the nasal mucosa with nasal sprays
- Occasional nausea or stomach discomfort with oral use
Serious adverse effects are very rare. Mast cell stabilizers are generally considered safe for use in children and during pregnancy, though use should always be discussed with a qualified healthcare professional.
Comparison with Other Allergy Medications
Unlike antihistamines, which block the effects of already-released histamine, mast cell stabilizers work preventively by stopping histamine and other mediators from being released in the first place. Corticosteroids have a broader anti-inflammatory effect and are used for more severe allergic conditions. Mast cell stabilizers are particularly suitable for patients who require long-term, low-risk prophylactic therapy.
References
- Galli, S. J., Tsai, M. - IgE and mast cells in allergic disease. Nature Medicine, 18(5):693-704, 2012. PubMed PMID: 22561833.
- Rang, H. P. et al. - Rang and Dale's Pharmacology. 8th Edition. Elsevier, Edinburgh, 2016.
- World Allergy Organization (WAO) - White Book on Allergy. Milwaukee, WI: World Allergy Organization, 2011. Available at: www.worldallergy.org
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