Ketotifen: Comprehensive Overview

Mast cells, integral to the immune system and dispersed throughout the body, play a crucial role in protecting against infection through the inflammatory process. They are also involved in allergic and inflammatory responses. When triggered by allergens, medications, or specific ingredients, mast cells release inflammatory mediators like histamine causing immediate allergic reactions. Individuals with mast cell diseases or severe allergies may experience serious symptoms due to excessive mast cell mediator release and the accumulation of mast cells in major organ systems.

Mast Cell Activation Syndrome (MCAS) arises from the inappropriate release of inflammatory mediators, leading to persistent allergic-type symptoms across multiple organs. Symptoms can manifest in various ways, including itching, hives, abdominal discomfort, blood pressure fluctuations, respiratory issues, cognitive problems, and even anaphylactic reactions.

Mast Cell Stabilizers have proven beneficial in managing symptoms associated with MCAS, addressing stomach and bone pain, flushing, headaches, and cognitive functioning when administered orally. Topically, they can alleviate itching and hives. Compounded Ketotifen, not commercially available as capsules or cream in the U.S., stands out as a unique drug due to its dual function as a mast cell stabilizer and an antihistamine (H1).

Ketotifen is a medication primarily known for its role in treating allergic conditions. It is an antihistamine and mast cell stabilizer that has been used for decades to manage various allergic symptoms. Commercially available Ketotifen is widely employed in the U.S. as an ophthalmic solution to alleviate symptoms associated with allergic conjunctivitis, including redness, itching, and tearing.

Mechanism of Action:

Primarily acting as a mast cell stabilizer, it prevents degranulation triggered by allergens, medications, or stimuli, leading to reduced release of inflammatory mediators such as histamine, prostaglandins, leukotrienes, and tryptase. In addition, its antihistamine activity involves acting as an H1 receptor antagonist, blocking histamine binding and suppressing associated effects like itching, vasodilation, and bronchoconstriction. Furthermore, ketotifen is suggested to have long-term effects, preventing mast cell accumulation in major organ systems, making it a versatile therapeutic option for conditions including asthma, allergic rhinitis, chronic urticaria, and Mast Cell Activation Syndrome (MCAS).

Side Effect Profile:

Common side effects may include skin rash, drowsiness, weight gain, abdominal pain, and dry mouth while serious side effects are rare but may include allergic reaction to the medication or severe dizziness.

Patient Use:

Patients typically use ketotifen as a preventive measure to manage chronic allergy symptoms. It is often prescribed for individuals who experience seasonal allergies or have a history of asthma exacerbated by allergic triggers. Regular use is recommended for optimal effectiveness.

Compounded Ketotifen

Ketotifen capsules and tablets are available in other countries, such as Canada and Mexico, however it is not available in local pharmacies in the U.S. as a commercially approved drug. Despite oral Ketotifen's absence in the U.S. market, it can be compounded, typically in 0.25 mg, 0.5 mg, 1 mg, 2 mg, and 3 mg capsules or tablets with a prescription. Ketotifen capsules or tablets are available through compounding pharmacies with a valid prescription across the U.S. Ketotifen finds application in treating conditions such as asthma, food allergies, allergic rhinitis, chronic urticaria, and MCAS. While it is officially sanctioned for ophthalmic use in the U.S., oral forms continue to be frequently prescribed, particularly in cases related to chronic inflammatory response syndrome (CIRS). Numerous studies have demonstrated the safety, efficacy, and superiority of oral ketotifen over other antihistamines for treating CIRS and MCAS. Ketotifen is a versatile medication with a well-established role in managing allergic conditions. The option for compounding ensures that individuals with specific needs can still benefit from this medication in a tailored and patient-friendly manner.

References

• https://online-lexi-com.proxy.libraries.rutgers.edu/lco/action/doc/retrieve/docid/patch_f/3501743?cesid=2Y2U3IVR3TG&searchUrl=%2Flco%2Faction%2Fsearch%3Fq%3Dketotifen%26t%3Dname%26acs%3Dtrue%26acq%3Dketotif#
• https://www.drugs.com/cons/ketotifen-oral.html
• https://www.medicinenet.com/ketotifen-oral_tablet/article.htm
• https://go.drugbank.com/drugs/DB00920
• https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4309375/
• https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8177879/
• https://www.oanp.org/news/614122/Ketotifen-How-it-Works-and-Its-Uses-in-Your-Practice.htm
• https://www.mastcellhope.org/education/common-treatments/
• https://www.mayoclinic.org/drugs-supplements/ketotifen-oral-route/side-effects/drg-20064435?p=1
• https://forterx.com/ketotifen-capsule/