The Sound of Evolution
Ketotifen
Mechanism of action:
Ketotifen is a second-generation H₁ receptor antagonist and also functions as a mast cell stabilizer. It antagonizes H₁ receptors and prevents histamine from binding to them, thereby reducing symptoms caused by histamine release such as nasal itching, rhinorrhea, conjunctival redness and swelling, itching, and bronchoconstriction. Ketotifen can also inhibit degranulation of mast cells and basophils, reducing the release of multiple allergic mediators.
Reference(s):
1. Hawes EM et al. (1998). N⁺-glucuronidation, a common pathway in human metabolism of drugs with a tertiary amine group. Drug Metab Dispos.
2. Kato Y et al. (2013). Human UDP-glucuronosyltransferase (UGT) 2B10 in drug N-glucuronidation: substrate screening and comparison with UGT1A3 and UGT1A4. Drug Metab Dispos.
3. Sokol KC et al. (2013). Ketotifen in the management of chronic urticaria: resurrection of an old drug. Ann Allergy Asthma Immunol.